Rheological Investigation of Thermoresponsive Alginate-Methylcellulose Gels for Epidermal Growth Factor Formulation - MDPI
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cosmetics Article Rheological Investigation of Thermoresponsive Alginate-Methylcellulose Gels for Epidermal Growth Factor Formulation Olivia Eskens , Gianna Villani and Samiul Amin * Laboratory of Cosmetics and Pharmaceuticals, Department of Chemical Engineering, Manhattan College, Riverdale, New York, NY 10471, USA; oeskens01@manhattan.edu (O.E.); gvillani01@manhattan.edu (G.V.) * Correspondence: samin01@manhattan.edu Abstract: Epidermal growth factors (EGF) serve as promising candidates for skin regeneration and rejuvenation products, but their instability hinders them from widespread use. Protective immobilization and directed release can be achieved through implementing a hydrogel delivery system. Alginate and methylcellulose are both natural polymers offering biocompatibility and environmental sensitivity. This blended gel system was investigated rheologically to understand its performance in topical applications. Alginate and methylcellulose were found to form a synergistic gel system that resulted in superior viscosity and thermoresponsiveness compared to the individual components. Increasing methylcellulose concentration directly enhanced gel elasticity, and higher viscosities provided better thermal protection of EGF. The addition of EGF at 3.33 mg/mL resulted in a decrease of viscosity but an increase in viscoelastic modulus. EGF concentration also played a large role in shear viscosity and thermoresponsiveness of the ternary system. An alginate-methylcellulose system presents promising rheological tunability, which may provide EGF thermal protection in a topical delivery format. Keywords: epidermal growth factor; rheology; thermal response; smart polymers; skin regeneration; Citation: Eskens, O.; Villani, G.; topical delivery; hydrogel; alginate; methylcellulose Amin, S. Rheological Investigation of Thermoresponsive Alginate- Methylcellulose Gels for Epidermal Growth Factor Formulation. 1. Introduction Cosmetics 2021, 8, 3. https://doi.org/ The epidermal growth factor (EGF) is one of the earliest known polypeptide growth 10.3390/cosmetics8010003 factors and the originator of the EGF-like protein family. This class of peptides has highly similar structural and functional characteristics, promotes mitogenic activity, and typically Received: 7 December 2020 Accepted: 27 December 2020 uses the same receptors for response triggering [1]. EGF directly affects collagen, elastin, Published: 30 December 2020 and extracellular matrix biosynthesis, making it a prime candidate for skin regeneration and rejuvenation. These peptides also have characteristically short half-lives and low Publisher’s Note: MDPI stays neu- intercellular diffusion rates, allowing them to operate locally in the body but making them tral with regard to jurisdictional clai- challenging to formulate with. EGF possesses a variety of functional groups and a three- ms in published maps and institutio- dimensional conformation allowing degradation via chemical and physical pathways such nal affiliations. as protein denaturation, aggregation, hydrolysis of peptide bonds, or oxidation of amino acid side chains [2]. The integrity of growth factors is easily compromised, especially in prolonged storage conditions, by fluctuations in pH, temperature, or complex electrostatic and hydrophobic interactions [3]. EGF has an optimal pH stability range from 6.0 to 8.0 Copyright: © 2020 by the authors. Li- with an isoelectric point at 4.6, and an unfolding onset around 40 ◦ C with a transition censee MDPI, Basel, Switzerland. midpoint at 55.5 ◦ C [4,5]. Implementing delivery systems for EGF formulation has the This article is an open access article potential to reduce the peptide’s instability through diffusion-limiting immobilization and distributed under the terms and con- protective encasing [6]. ditions of the Creative Commons At- tribution (CC BY) license (https:// Polymeric biomatrix characteristics such as water content or crosslink density can creativecommons.org/licenses/by/ be tailored to optimize the diffusion-controlled EGF retention and release mechanisms. 4.0/). The physicochemical crosslinking of polymers also leaves them especially responsive to Cosmetics 2021, 8, 3. https://doi.org/10.3390/cosmetics8010003 https://www.mdpi.com/journal/cosmetics
Cosmetics 2021, 8, x FOR PEER REVIEW Cosmetics 2021, 8, 3 physicochemical crosslinking of polymers also leaves them especially2responsive of 11 to ronmental changes. In this study, we attempt to tune a hydrogel delivery vehicl thermoresponsiveness for EGF formulation. The target of the gel system is to effe immobilize EGF at storage conditions and evenly distribute EGF through therm environmental shear-induced changes. In thisgelstudy, we attempt degradation to tune upon a hydrogel topical delivery application. vehicle with Hydrogels provide ex thermoresponsiveness for EGF formulation. The target of the gel system is to effectively flexibility and hydration for skin compatibility, while extracellular matrix-inspired immobilize EGF at storage conditions and evenly distribute EGF through thermal and ery materials utilize the natural growth factor affinity and attachment techniques to shear-induced gel degradation upon topical application. Hydrogels provide excellent dermal release. For this reason, alginate is one of the components of the polymer flexibility and hydration for skin compatibility, while extracellular matrix-inspired delivery work. Additionally, alginate has previously shown an increase in EGF encapsulatio materials utilize the natural growth factor affinity and attachment techniques to mimic ciency as well as inherent regenerative properties [7]. Alginates transform to mat dermal release. For this reason, alginate is one of the components of the polymeric network. functions of skin cells and organs, which eventually leads to healing of the affecte Additionally, alginate has previously shown an increase in EGF encapsulation efficiency as on the body [8]. Sodium alginate is an anionic, hydrophilic polysaccharide that is ext well as inherent regenerative properties [7]. Alginates transform to match the functions from the cell walls of brown algae and various strains of bacteria. The molecular str of skin cells and organs, which eventually leads to healing of the affected area on the of sodium alginate is a linear alginic acid copolymer with linked 1-4 glucosidic body [8]. Sodium alginate is an anionic, hydrophilic polysaccharide that is extracted from These glucosidic bonds are formed by the homopolymeric blocks of ߚ-D-mannuron the cell walls of brown algae and various strains of bacteria. The molecular structure of sodium alginate is aߙ-L-guluronic and linear alginic acid, outlined inwith acid copolymer Figure 1. Alginate linked that contains 1-4 glucosidic bonds.a These high level of G glucosidic bonds are formed by the homopolymeric blocks of β-D-mannuronic acidwhile content results in stiff and brittle gels that tend to be more stable, and high M content leads to soft, elastic gels with high water adsorption α-L-guluronic acid, outlined in Figure 1. Alginate that contains a high level of G-block and ion exchange [8]. due to the attractive preferential forces of ions to the extended content results in stiff and brittle gels that tend to be more stable, while high M-block G-block residues content leads tothe alginate soft, elasticstructure. gels with [9] The high properties water of alginate adsorption and iongels can be[8]. exchange adjusted This iswith mol due to the attractive preferential forces of ions to the extended G-block residues withinconstituent weight, concentration, G-block distribution, cation availability, and the in tions [8]. alginate structure [9]. The properties of alginate gels can be adjusted with molecular weight, concentration, G-block distribution, cation availability, and constituent interactions [8]. M-block G-block (1-4)-linked β-D-mannuronate (1-4)-linked α-L-guluronate Figure 1. The chemical structure Figureof1.alginate. The chemical structure of alginate. Methylcellulose is the other component selected for the interpenetrated polymer Methylcellulose is the other component selected for the interpenetrated polym network due to its thermoresponsive behavior. Methylcellulose is a natural, heterogeneous work due to its thermoresponsive behavior. Methylcellulose is a natural, heteroge polymer that forms reversible gels upon heating, and its chemical structure is outlined in polymer that forms reversible gels upon heating, and its chemical structure is outli Figure 2. The highly substituted hydrophobic groups within methylcellulose form attractive Figure 2. The highly substituted hydrophobic groups within methylcellulose form complexes at increased temperatures, causing gelation [10]. At semi-dilute conditions, as tive complexes at increased temperatures, causing gelation [10]. At semi-dilute cond seen in our system, the viscosity of methylcellulose solutions decreases up to a critical as seen in our system, the viscosity of methylcellulose solutions decreases up to a c value then increases as a turbid gel develops [10,11]. Mixing alginate with methylcellulose value then increases as a turbid gel develops [10,11]. Mixing alginate with methylce creates a complex gel system where hydrophobic interaction, hydrogen bond formation creates a complex gel system where hydrophobic interaction, hydrogen bond form between carboxyl and hydroxy groups, and ionic crosslinking are synchronous [12]. The betweenof mild gelling conditions carboxyl and hydroxy both polymers, groups, along with and their ionic crosslinking immunogenic nature, are makesynchronous them [12 ideal candidatesmild gelling for the conditions preservation of both polymers, of sensitive along with their active pharmaceutical immunogenic components [8,12]. nature, This study aims to characterize the thermo-rheological behavior of the fluid gel system and comp them ideal candidates for the preservation of sensitive active pharmaceutical [8,12]. the effect of EGF whenThis study aims introduced into to thecharacterize the thermo-rheological behavior of the flu polymeric network. system and the effect of EGF when introduced into the polymeric network.
Cosmetics 2021, 8, 3 3 of 11 Cosmetics 2021, 8, x FOR PEER REVIEW 3 of 12 Figure 2. The chemical structure of methylcellulose. Figure 2. The chemical structure of methylcellulose. 2. Materials and Methods 2. Materials and Methods Alginic acid sodium salt from brown algae with medium viscosity was obtained from Alginic acid Sigma-AldrichsodiumInc. salt(St. from brown Louis, algae MO, withMethylcellulose USA). medium viscosity wasAlfa from obtained Aesarfrom(Ward Hill, Sigma-Aldrich MA, USA) with a defined 2% aqueous solution viscosity of 400 cP at 20 ◦Hill, Inc. (St. Louis, MO, USA). Methylcellulose from Alfa Aesar (Ward C was used. MA, USA) with a and Alginate defined 2% aqueous were methylcellulose solution viscosity of 400 simultaneously cP atinto stirred 20 °C was used.ofAl- a solution deionized ginate and methylcellulose were simultaneously stirred into a solution water at room temperature. To investigate composition-dependent gel properties, of deionized waterfirst, the at room alginate temperature. To investigate concentration composition-dependent was held constant at 1% w/v while gel properties, first, theconcentration methylcellulose algi- nate concentration varied between was held1%,constant 1.5%, and at 1% 2%w/v w/v.while methylcellulose Epidermal concentration growth factor var- from was obtained ied between Skin1%, 1.5%,Scientific. Actives and 2% w/v. TheEpidermal peptide gels growth were factor was formulated originally obtained from Skinmg/mL at 3.33 Ac- and tives Scientific. The peptide incorporated prior togels were originally polymeric formulated dissolving. After the at 3.33 initialmg/mL and incorpo- investigation, the alginate rated prior to polymeric concentration dissolving. was varied whileAftermethylcellulose the initial investigation, and peptidethe alginate concentra- concentrations were held tion wasconstant varied while methylcellulose and peptide concentrations were at 2% w/v and 3.33 mg/mL, respectively. Finally, the peptide concentration held constant at was 2% w/v and 3.33inmg/mL, varied the 1% respectively. Finally, the peptide alginate–2% methylcellulose concentration gel system was varied with additional in the concentrations of 1% alginate–2% 1.67 andmethylcellulose 6.67 mg/mL. All gelsolutions system with additional maintained concentrations a near-neutral pH.ofThe 1.67viscosity, and 6.67complex mg/mL. moduli, All solutions maintained a near-neutral and thermoresponsiveness of thepH. The viscosity, resulting gel systemscomplex were moduli, and investigated. thermoresponsiveness The Discovery of theHybrid resulting gel systems Rheometer were investigated. (DHR-3) from TA Instruments was employed to Thedetermine Discoverythe Hybrid Rheometer rheological (DHR-3) properties of thefrom TA Instruments wassystems alginate-methylcellulose employed bothtowith and determine without EGF. A stainless the rheological steel, of properties 40 mm cone plate with a 2-degreesystems the alginate-methylcellulose angle was bothusedwithto conduct all rheological and without experiments EGF. A stainless steel, on 40 the mmtemperature-controlled cone plate with a 2-degree Peltier plate. angle wasFlowusedsweeps to were conduct carried out between all rheological the shearonrate experiments therange of 0.1 to 5000 s−1 . Peltier temperature-controlled This encompasses plate. Flow storage, spreading, sweeps were carriedpumping, out between andtherubbing processes shear rate range during of 0.1 toproduct 5000 s-1. utilization. This encompasses An amplitude sweep was carried out over 0.01% to 50% oscillation storage, spreading, pumping, and rubbing processes during product utilization. An am- strain with a constant angular fre- quency of 10 rad s −1 on each gel system to define their individual linear viscoelastic regions. plitude sweep was carried out over 0.01% to 50% oscillation strain with a constant angular frequency Frequency of 10 rads sweeps were gel -1 on each conducted system within to definethetheir established individuallinear viscoelastic linear region with viscoelastic − 1 regions. angular Frequency frequency sweepsranging from 0.1 towithin were conducted 100 radthes established . All of these outlined linear experiments viscoelastic re- were gion with performed isothermally angular frequency at 25 ◦from ranging C, and0.1measurements to 100 rads-1.were taken All of these under steady-state outlined experi- sensing ments wereconditions. performed Temperature isothermally sweeps at 25 evaluated the thermosensitivity °C, and measurements were taken as under the gels approach and steady- surpasses the skin’s surface temperature of 37.5 ◦ C. A constant shear rate of 10 s−1 was state sensing conditions. Temperature sweeps evaluated the thermosensitivity as the gels approach applied to the sample, and surpasses the skin’sand the temperature surface temperaturewas increased of 37.5 by 1◦ C per °C. A constant shearminute rate ofbetween 25 ◦ C and 50 ◦ C. All experiments were run a minimum of twice to ensure reproducibility. 10 s-1 was applied to the sample, and the temperature was increased by 1°C per minute betweenThe 25 °Cdataand presented 50 °C. Allinexperiments this article are therun were mean values of of a minimum each sample’s twice to ensurevarious repro-trials, and across ducibility. The all data experiment presented and sample in this articletypes, are thea relative mean valuesstandard deviation of each sample’s of 10% or less was various trials, and across all experiment and sample types, a relative standard deviation of 10% or for the observed. Error bars for individual values were excluded in the following graphs less was sake of clarity. observed. Error bars for individual values were excluded in the following graphs for the sake of clarity. 3. Results and Discussion 3. Results andThe deformation and flow behavior of the fluid gel system is important to characterize Discussion the storage and release mechanisms of the EGF-loaded product when temperature and Theshear deformation stressorsand areflow behavior applied. of thesolutions Peptide fluid gel are system oftenis important to character- stored at cool temperatures to ize the storage prolong and releaselife, product mechanisms and a thickof the EGF-loaded product interpenetrated polymerwhen temperature network and limit should further shear stressors are applied. Peptide solutions are often stored at cool temperatures EGF deactivation. As the product is topically applied, temperature increases to match to pro- long product life, and the body, andahigh thickshear interpenetrated stresses arepolymer imposed, network resultingshould further limit in structural EGF breakdown and deactivation. As the product is topically applied, temperature increases to match pseudoplastic behavior. We aimed to introduce the impact of gel composition on the the body, and highstructure-property shear stresses are imposed, resulting relationship in structural of the ternary breakdown and pseudoplastic system. behavior. We aimed to introduce the impact of gel composition on the structure-property relationship of the ternary system.
Cosmetics Cosmetics 8,8, 2021, 2021, 3 x FOR PEER REVIEW 4 of 4 of 1211 3.1. Dynamic Viscosity 3.1.The viscosity Dynamic profile of the fluid gel is linked to the polymeric network and strength Viscosity of constituent interactions. The viscosity profile of Figure 3 explores the fluid the influence gel is linked of methylcellulose to the polymeric network andconcentra- strength of tion on the shear viscosity. The flow behavior of sodium alginate-methylcellulose constituent interactions. Figure 3 explores the influence of methylcellulose concentration systems has been previously characterized best by the non-Newtonian Hershel–Buckley on the shear viscosity. The flow behavior of sodium alginate-methylcellulose systems fluid model [13]. previously has been The dominant solution interactions characterized best by the of alginate are charge non-Newtonian repulsions between Hershel–Buckley fluid dissociated model [13]. carboxyl groups solution The dominant and the formation interactions of of hydrogen alginatebonds between are charge carboxylic repulsions ac- between ids and ionized dissociated carboxyl carboxyl groups. groups andMethylcellulose the formationsolution interactions of hydrogen bonds rely heavily between on hy- carboxylic drophobic acids andchain grouping. ionized carboxyl Both alginate groups. and methylcellulose Methylcellulose solutionsolutions haverely interactions a distinctive heavily on pseudoplastic hydrophobic chain grouping. Both alginate and methylcellulose solutions havein behavior at neutral pH. Some hydrophobic sections appear alginate a distinctive chains upon protonation pseudoplastic behavior atof neutral dissociated carboxyl pH. Some groups [13]. hydrophobic This gives sections appear rise into an increase alginate chains inupon hydrophobic protonationassociation between of dissociated alginategroups carboxyl and methylcellulose [13]. This gives in rise the interpenetrated to an increase in polymer network. hydrophobic The resultbetween association is a synergistic alginatecombination that has a in and methylcellulose higher viscosity than the interpenetrated either individual polymer network.component The result while shear-thinning is a synergistic is preserved, combination that and has athis trendviscosity higher is also seen than ineither individual component while an alginate-methylcellulose mixtureshear-thinning is preserved, and studied by Mehmandoost et this trendThis al. [13]. is also seen is not in an alginate-methylcellulose uncommon as enhanced stabilitymixture studied of physical andby Mehmandoost mechanical et al. [13]. properties This is not of biopolymer uncommon blends has been as appreciably enhanced stability reported of[14–18]. physical and mechanical properties of biopolymer blends has been appreciably reported [14–18]. Figure 3. The viscosity vs. shear rate behavior of alginate (blue), methylcellulose (yellow), and Figure 3. The viscosity vs. shear rate behavior of alginate (blue), methylcellulose (yellow), and mixtures of the two (green) with varying methylcellulose concentration (%w/v). The circular symbols mixtures of the two (green) with varying methylcellulose concentration (%w/v). The circular sym- appearing bols appearingin in thethe plots plotsrepresent representthe themean-values mean-values of discrete measurements of discrete measurementsevenly evenlyacquired acquiredatat logarithmicintervals logarithmic intervalsunder understeady-state steady-stateconditions, conditions,while whilethe thecontinuous continuous lines lines are are guides guides for for the the eye. MC: eye. methylcellulose; MC: methylcellulose; Alg: alginate. Alg: alginate. Theimpact The impactofofEGF EGFaddition additionononthe theshear shearviscosity viscosityofofthe themixtures mixtureswith withvarying varying methylcellulose concentration can be observed in Figure 4. When methylcellulose concentration can be observed in Figure 4. When EGF was introducedEGF was introduced into into the the system, system, therewas there was a marginalviscosity a marginal viscositydrop dropacross acrossallallsamples. samples.The Thelow low molecular molecular weight polypeptide may disrupt the polymer structural entanglement weight polypeptide may disrupt the polymer structural entanglement slightly, but slightly, butthe the synergistic and pseudoplastic nature of the fluid gel was still retained. It synergistic and pseudoplastic nature of the fluid gel was still retained. It is expected that is expected that the hightheviscosity high viscosity immobilizes immobilizes EGFtopical EGF while while application topical application begins tobegins to breakdown breakdown the gel the gel structure. At neutral pH, EGF carries a negative charge and structure. At neutral pH, EGF carries a negative charge and may demonstrate repulsivemay demonstrate repulsive interactions with the anionic alginate chain. EGF is also minorly composed of interactions with the anionic alginate chain. EGF is also minorly composed of hydropho- hydrophobic residues, which possibly complicates the hydrophobic relationship between bic residues, which possibly complicates the hydrophobic relationship between the long- the long-chain polymers. chain polymers.
Cosmetics 2021, 8, 3 5 of 11 Cosmetics 2021, 8, x FOR PEER REVIEW 5 of 12 5000 1.0% Alg – 1.0% MC 1.0% Alg – 1.5% MC Viscosity (cP) 1.0% Alg – 2.0% MC 500 1.0% Alg – 1.0% MC + EGF 1.0% Alg – 1.5% MC + EGF 1.0% Alg – 2.0% MC + EGF 50 1 10 100 1000 Shear Rate (1/s) FigureFigure 4. Shear 4. Shear viscosity viscosity behavior behavior of alginate-methylcellulose of alginate-methylcellulose mixtures(green) mixtures (green)with withvarying varying methylcellulose methylcellulose concentra- concentrations (%w/v)tions and(%w/v) and epidermal epidermal growth growth factor (EGF) factor (EGF) addition addition at 3.33 at 3.33 mg/mL(red). mg/mL (red). The Thecircular circularsymbols appearing symbols in theinplots appearing the plots represent the mean-values of discrete measurements evenly acquired at logarithmic intervals under steady-state condi- represent the mean-values of discrete measurements evenly acquired at logarithmic intervals under steady-state conditions, tions, while the continuous lines are guides for the eye. while the continuous lines are guides for the eye. 3.2. Viscoelastic Modulus The dynamic modulus further explores the system interactions and performance by 3.2. Viscoelastic Modulus evaluating gel stiffness. The storage modulus (G’) of pure alginate is consistently lower The than dynamic the modulus loss modulus further (G”) under explores a variety theconditions, of gel system interactions and the same and performance by development evaluating is seen ingel stiffness. Figure 5 [19].The storage While modulus the viscous (G’) of property of pure alginate alginate remainsis consistently dominant, thelower dif- than theference loss modulus between(G”) under the two a variety moduli of gelatconditions, decreased higher angularandfrequencies the same development revealing a de-is seen in Figure crease in5 [19]. phaseWhile the viscous angle and property a fluid-like of alginate viscoelastic behavior.remains On thedominant, other hand,the difference methyl- cellulose between theviscoelastic two moduli behavior resembled decreased moreangular at higher of an elastic gel system frequencies where G’aisdecrease revealing typi- in cally greater than G”, and the change in phase angle is smaller over phase angle and a fluid-like viscoelastic behavior. On the other hand, methylcellulosethe range of angular frequency.behavior viscoelastic The viscoelastic transition resembled moreofofthe analginate-methylcellulose elastic gel system where systems G’ isistypically better vis- greater ualized in Figure 5c. The G’/G” crossover took place at higher angular than G”, and the change in phase angle is smaller over the range of angular frequency. frequencies as methylcellulose concentration increased. The elastic component of the system took The viscoelastic transition of the alginate-methylcellulose systems is better visualized in stronger dominance as methylcellulose concentration increased, and gel stiffness was en- Figure 5c. The G’/G” crossover took place at higher angular frequencies as methylcellulose hanced. While the variance of total gel concentration between samples generates some concentration inconclusively,increased. this outcomeTheiselastic component similarly embodied by ofanthe system took stronger dominance alginate-carboxymethylcellulose as system, methylcellulose concentration as studied by Zheng et al. [19]. increased, and gel stiffness was enhanced. While the variance of total gel concentration between samples generates some inconclusively, this outcome is similarly embodied by an alginate-carboxymethylcellulose system, as studied by Zheng et al. [19]. Recalling that EGF caused a slight decrease in shear viscosity behavior, the impact on dynamic modulus should give more insight into the molecular interactions happening in the system. The influence of EGF addition on each gel system with varying methylcellulose concentration is explored in Figure 6. The strength of the gel does not appear to be jeopardized, suggesting a more complex interrelationship. It was observed that the change in phase angle decreases with increasing methylcellulose concentration, but the viscoelastic transition is not as dependent on methylcellulose concentration when EGF is in the system. In every instance measured, EGF increased gel stiffness signifying that the loss in viscosity is not necessarily due to a loss of structure. This is conversely related to the impact of silicone in a silicated hydroxypropylmethylcellulose-alginate gel network that hindered effective alginate chain interactions and ultimately reduced gel stiffness [18]. Although elastic modulus increases with the addition of EGF, the relaxation times shift to higher frequencies meaning shorter relaxation times. This may signal a new network structure forming between EGF and methylcellulose due to hydrophobic interaction. The complexity of the ternary interdependence needs to be more substantially defined in order to fully interpret viscoelastic properties.
Cosmetics 2021, 8, 3 6 of 11 Cosmetics 2021, 8, x FOR PEER REVIEW 6 of 12 100 10 Complex Modulus (Pa) 1 1% Alginate G' 1% Alginate G" 0.1 1% Methyl Cellulose G' 1% Methyl Cellulose G" 0.01 1% Alg – 1% MC G' 1% Alg – 1% MC G" 0.001 0.0001 0.1 1 10 100 Angular Frequency (rad/s) (a) 100 10 Complex Modulus (Pa) 1 1% Alginate G' 1% Alginate G" 0.1 2% Methyl Cellulose G' 2% Methyl Cellulose G" 0.01 1% Alg – 2% MC G' 1% Alg – 2% MC G" 0.001 0.0001 0.1 1 10 100 Angular Frequency (rad/s) Cosmetics 2021, 8, x FOR PEER REVIEW 7 of 12 (b) 100 10 Complex Modulus (Pa) 1% Alg – 1% MC G' 1 1% Alg – 1% MC G" 1% Alg – 1.5% MC G' 0.1 1% Alg – 1.5% MC G" 1% Alg – 2% MC G' 0.01 1% Alg – 2% MC G" 0.001 0.1 1 10 100 Angular Frequency (rad/s) (c) Figure 5. Viscoelastic moduli G’ () and G” () of the resulting gel systems: (a) 1% w/v alginate (blue), 1% w/v methyl- Figure 5. Viscoelastic moduli G’ (•) and G” (N) of the resulting gel systems: (a) 1% w/v alginate (blue), 1% w/v methylcellulose cellulose (yellow), and the mixture of the two (green); (b) 1% w/v alginate (blue), 2% w/v methylcellulose (yellow), and the (yellow), and the mixture mixture of the twoof(green); the two (c) (green); (b) 1% w/v alginate Alginate-methylcellulose mixtures (blue), 2% w/v with varying methylcellulose methylcellulose (yellow), concentration (w/v).and The the mixture circular and of the two (green); (c) triangular symbols appearing inmixtures Alginate-methylcellulose the plots represent the mean-values with varying of discrete measurements methylcellulose concentration evenly ac- The circular (w/v). quired at logarithmic intervals under steady-state conditions, while the continuous lines are guides for the eye. G: storage and triangular symbols modulus; appearing G”: loss modulus. in the plots represent the mean-values of discrete measurements evenly acquired at logarithmic intervals under steady-state conditions, while the continuous lines are guides for the eye. G: storage modulus; G”: loss modulus. Recalling that EGF caused a slight decrease in shear viscosity behavior, the impact on dynamic modulus should give more insight into the molecular interactions happening in the system. The influence of EGF addition on each gel system with varying methyl- cellulose concentration is explored in Figure 6. The strength of the gel does not appear to be jeopardized, suggesting a more complex interrelationship. It was observed that the
Cosmetics 2021, 8, 3 7 of 11 Cosmetics 2021, 8, x FOR PEER REVIEW 8 of 12 1% Alg – 1% MC G' 1% Alg – 1% MC G" 1% Alg – 1% MC + EGF G' 1% Alg – 1% MC + EGF G" 100 Complex Modulus (Pa) 10 1 0.1 0.01 0.001 0.1 1 10 100 Angular Frequency (rad/s) (a) 1% Alg – 1.5% MC G' 1% Alg – 1.5% MC G" 1% Alg – 1.5% MC + EGF G' 1% Alg – 1.5% MC + EGF G" 100 Complex Modulus (Pa) 10 1 0.1 0.1 1 10 100 Angular Frequency (rad/s) (b) 1% Alg – 2% MC G' 1% Alg – 2% MC G" 1% Alg – 2% MC + EGF G' 1% Alg – 2% MC + EGF G" 100 Complex Modulus (Pa) 10 1 0.1 0.1 1 10 100 Angular Frequency (rad/s) (c) Figure 6. The impactFigure of 3.336.mg/mL The impact of 3.33 mg/mL epidermal growth epidermal growth factor addition factor (red) on addition (red) onmoduli the viscoelastic the viscoelastic G’ (•) and G” (N) of moduli G’ () and G” () of various alginate-methylcellulose mixtures (green) with increasing various alginate-methylcellulose mixtures (green) with increasing methylcellulose concentration (w/v): (a) 1% alginate–1% methylcellulose concentration (w/v): (a) 1% alginate–1% methylcellulose; (b) 1% alginate–1.5% methylcellulose; (b) 1% alginate–1.5% methylcellulose; (c) 1% alginate–2% methylcellulose. The circular and triangular symbols appearing in the plots represent the mean-values of discrete measurements evenly acquired at logarithmic intervals under steady-state conditions, while the continuous lines are guides for the eye.
Cosmetics 2021, 8, x FOR PEER REVIEW 9 of 12 methylcellulose; (c) 1% alginate–2% methylcellulose. The circular and triangular symbols appear- ing in the plots represent the mean-values of discrete measurements evenly acquired at logarith- mic intervals under steady-state conditions, while the continuous lines are guides for the eye. Cosmetics 2021, 8, 3 8 of 11 3.3. Thermoresponsivity It is known that composition affects the initial thermal transitions and gelling tem- 3.3. Thermoresponsivity peratures of compound gel systems [20]. Figure 7a shows the impact of polymer blending and methylcellulose It is known that concentration composition affectson thermoresponsiveness. As expected, the initial thermal transitions pure alginate and gelling temper- showed atures ofa compound negligible reaction to increased gel systems [20]. Figuretemperature, 7a shows while methylcellulose the impact of polymerdecreased blending in andviscosity until a critical methylcellulose temperature concentration is met. The critical temperature on thermoresponsiveness. As expected, of pure alginate methyl- cellulose showed awas not significantly negligible reaction toinfluenced by the concentration increased temperature, range studied.decreased while methylcellulose As the pol-in ymers viscositywere mixed until together, a critical thermoresponsiveness temperature is met. The criticalwas enhanced.ofThe temperature purehydrophobic gel- methylcellulose ling was mechanism of methylcellulose not significantly influenced by the is suspected of intensifying concentration with As range studied. increasing concentra- the polymers were tion, mixed and hydrophobic together, interactions from was thermoresponsiveness alginate enhanceThe enhanced. thehydrophobic thermal transition. The gelling ther- mecha- nismreduction mal of methylcellulose of viscosityisreveals suspected of intensifying breakdown a dual-mechanistic with increasing concentration, of the prepared gel andnet- hydrophobic work during interactions from alginate topical application. Whenenhance EGF was theintroduced thermal transition. to theseThe thermal systems, new reduc- gel tion of viscositywere characteristics reveals a dual-mechanistic observed. Figure 7b shows breakdown of the a stronger prepared decrease gel network in viscosity during before the topical gelling critical application. When EGF temperature waswas met.introduced This may to bethese systems, attributed newthermal to EGF gel characteristics instability were observed. Figure 7b shows a stronger decrease in viscosity before and the consequential structural changes impacting the polymeric network. Introduction the critical gelling temperature was met. This may be attributed to EGF thermal instability of EGF generally increased the critical temperature in the mixtures studied and proposes and the consequen- tial structural that the largelychanges hydrophilicimpacting theof structure polymeric network. EGF somewhat Introduction obstructs of EGF generally the hydrophobic gelling increased the critical temperature in the mixtures studied and proposes that the largely procedure. hydrophilic structure of EGF somewhat obstructs the hydrophobic gelling procedure. 1% Alg – 1% MC 1% Alg – 1.5% MC 1% Alginate 1% Methylcellulose 1% Alg – 2% MC 1% Alg – 1% MC + EGF 2% Methylcellulose 1% Alg – 1% MC 1% Alg – 1.5% MC + EGF 1% Alg – 2% MC + EGF 1% Alg – 1.5% MC 1% Alg – 2% MC 1600 1600 1400 1400 1200 1200 Viscosity (cP) Viscosity (cP) 1000 1000 800 800 600 600 400 400 200 0 200 20 25 30 35 40 45 20 25 30 35 40 45 Temperature (°C ) Temperature (°C) (a) (b) Figure 7. The Figure 7. The response of gel response of gel systems systems with with varying varying methylcellulose methylcellulose concentration concentration (w/v) (w/v) as as temperature temperature increased increased by by 11 ◦°C C per minute: (a) Alginate (blue), methylcellulose (yellow), and the resulting mixtures of the two (green); (b) The impact per minute: (a) Alginate (blue), methylcellulose (yellow), and the resulting mixtures of the two (green); (b) The impact of of 3.33 mg/mL epidermal growth factor addition (red) on alginate-methylcellulose mixtures (green). Viscosity values were 3.33 mg/mL epidermal growth factor addition (red) on alginate-methylcellulose mixtures (green). Viscosity values were continuously acquired as a function of increasing temperature. continuously acquired as a function of increasing temperature. The The influence influence of of alginate alginate on on the the mixture mixture was was investigated investigated with with viscosity viscosity versus versus tem- tem- perature perature tests visualized in Figure 8a. The shear viscosity of the mixture seemed to tests visualized in Figure 8a. The shear viscosity of the mixture seemed be to be more strongly dependent on the alginate content. This could be due to the amplification more strongly dependent on the alginate content. This could be due to the amplification of of supportive supportive electrostatic electrostatic interactions interactions but but also also increased increased entanglement entanglement from from the larger the larger overall polymer content. An effective thermal decrease in viscosity is observed overall polymer content. An effective thermal decrease in viscosity is observed in these in these samples, but a critical temperature is not met in the testing range. The ratio of the samples, but a critical temperature is not met in the testing range. The ratio of the compo-compo- nents nents manipulates manipulates the onset of the onset of hydrophobic hydrophobic complexation. complexation. The The pH-dependent, pH-dependent, anionic anionic nature of alginate makes a good delivery system for cationic drugs through electrostatic interactions [21]. Sodium alginate interacted with lactoferrin through electrostatic attrac- tion and increased the heat stability of the protein [22]. It is important to consider the lactoferrin isoelectric point of 8.8, giving it a net positive charge in the neutral alginate
Cosmetics 2021, 8, x FOR PEER REVIEW 10 of 12 nature of alginate makes a good delivery system for cationic drugs through electrostatic interactions [21]. Sodium alginate interacted with lactoferrin through electrostatic attrac- tion and increased the heat stability of the protein [22]. It is important to consider the Cosmetics 2021, 8, 3 9 of 11 lactoferrin isoelectric point of 8.8, giving it a net positive charge in the neutral alginate gel, whereas EGF has an acidic isoelectric point. Interestingly, vascular endothelial growth factor encapsulation and release behavior were not affected by alginate concentration or G-block gel, content evenEGF whereas though has it analso hasisoelectric acidic a basic isoelectric point of 8.5vascular point. Interestingly, [23]. Bovine serum growth endothelial albuminfactor encapsulation has a similar andpoint isoelectric release behavior to EGF, were and its not affected release by alginatehydrogel from a comparable concentration or networkG-block at a pH content even of 7.4 was thoughdependent strongly it also has ona basic isoelectric alginate point of[12]. concentration 8.5 [23]. Bovine serum Addition- ally, electrostatic behavior within alginate is not influenced by heat treatment [22]. In Fig-hydrogel albumin has a similar isoelectric point to EGF, and its release from a comparable ure 8b, itnetwork can be at a pH of clearly 7.4 that seen was strongly dependent the critical on alginate temperature concentration is increased [12]. Additionally, with higher net- polymerelectrostatic and alginate behavior within alginate concentrations. There isis not lessinfluenced irregularity by as heat thetreatment viscosity[22]. In Figure 8b, of these EGF-loadedit cangels be minimizes, clearly seenindicating that the critical bettertemperature is increased protective capability. with The higherenhance- viscosity net-polymer and ment may alginate provideconcentrations. There isstructure, a more immobilized less irregularity as the viscosity and alginate of these electrostatic EGF-loaded behavior and gels minimizes, indicating better protective capability. The viscosity hydrogen bonding could increase the EGF affinity to the gel analogous to findings with enhancement may provide a more immobilized structure, and alginate electrostatic behavior and hydrogen bonding other proteins could increase the EGF affinity to the gel analogous to findings with other proteins Figure 8. The response of gel systems with varying alginate concentration (w/v) as temperature increased by 1 ◦ C per minute: (a) Alginate (blue), methylcellulose (yellow), and the resulting mixtures of the two (green); (b) The impact of 3.33 mg/mL epidermal growth factor addition (red) on alginate- methylcellulose mixtures (green). Viscosity values were continuously acquired as a function of increasing temperature.
Cosmetics 2021, 8, x FOR PEER REVIEW 11 of 12 Figure 8. The response of gel systems with varying alginate concentration (w/v) as temperature increased by 1 °C per minute: (a) Alginate (blue), methylcellulose (yellow), and the resulting mix- tures of the two (green); (b) The impact of 3.33 mg/mL epidermal growth factor addition (red) on Cosmetics 2021, 8, 3 alginate-methylcellulose mixtures (green). Viscosity values were continuously acquired as a func- 10 of 11 tion of increasing temperature. Lastly, the impact of EGF concentration on thermoresponsiveness was studied from Lastly, the impact of EGF concentration on thermoresponsiveness was studied from Figure 9 for the 1% alginate–2% methylcellulose system. As EGF concentration increased, Figure 9 for the 1% alginate–2% methylcellulose system. As EGF concentration increased, the critical temperature of the system decreased, signaling greater thermal instabilities. the critical temperature of the system decreased, signaling greater thermal instabilities. Similarly, higher higher Similarly, concentrations of growth concentrations factors factors of growth lead tolead lowerto encapsulation yields in lower encapsulation yields in other alginate delivery systems [8]. It is suspected that at higher EGF concentrations, other alginate delivery systems [8]. It is suspected that at higher EGF concentrations, the the protective capability of the gel network is insufficient. With this comes an implied pivotal protective capability of the gel network is insufficient. With this comes an implied pivotal ratio between EGF and ratio between EGFpolymer contentcontent and polymer where instabilities are effectively where instabilities minimized. are effectively The The minimized. samplesample containing the lowest amount of protein demonstrated additional synergy containing the lowest amount of protein demonstrated additional synergy as the as the shear viscosity surpassed that of the original alginate-methylcellulose system. shear viscosity surpassed that of the original alginate-methylcellulose system. 1% Alg – 2% MC 1% Alg – 2% MC + EGF (1.67 ug/mL) 1% Alg – 2% MC + EGF (3.33 ug/mL) 1% Alg – 2% MC + EGF (6.67 ug/mL) 3200 2700 2200 Viscosity (cP) 1700 1200 700 200 20 25 30 35 40 45 Temperature (°C) Figure 9. The effect of epidermal growth factor concentration (red) on the viscosity of 1% w/v alginate–2% w/v methylcellulose ◦ Figure 9. The effect of epidermal growthgel mixture factor (green) when concentration temperature (red) increased on the viscosity byw/v of 1% 1 C per minute. algi- nate–2%Viscosity values were gel w/v methylcellulose continuously acquired mixture (green) as atemperature when function of increased increasingbytemperature. 1 °C per minute. Viscosity values were continuously acquired as a function of increasing temperature. 4. Conclusions 4. ConclusionsThere is a wide range of prospective research to further define the structure-property There is a wide of relationship thisofalginate-methylcellulose-EGF range prospective research to furthernetwork. define theAlginate and methylcellu- structure-property lose were found to form a synergistic gel system that resulted in superior viscosity and relationship of this alginate-methylcellulose-EGF network. Alginate and methylcellulose thermoresponsiveness compared to the individual components due to an increase in hy- were found to form a synergistic gel system that resulted in superior viscosity and ther- drophobic association in the interpenetrated polymer network. The stiffness and elasticity moresponsiveness compared to the individual components due to an increase in hydro- of the gel mixture were directly related to methylcellulose concentration. The addition phobic association in the interpenetrated polymer network. The stiffness and elasticity of of EGF resulted in a decrease in viscosity but an increase in viscoelastic modulus. A the gel mixture were directly related to methylcellulose concentration. The addition of new hydrophobically-associated network is suggested to form with EGF incorporation EGF resulted in a decrease in viscosity but an increase in viscoelastic modulus. A new as shorter relaxation times were observed in the ternary system. EGF concentration also hydrophobically-associated network is suggested to form with EGF incorporation as played a large role in thermoresponsiveness of the hydrogel mixtures attributed to its shorter relaxation times were observed in the ternary system. EGF concentration also inherent thermal instability. Overall, this system presents a great opportunity for a highly played a large role in thermoresponsiveness of the hydrogel mixtures attributed to its in- tunable and effective delivery vehicle for EGF with thermoresponsive behavior. The pro- herent thermal instability. Overall, this system presents a great opportunity for a highly tectivity of the gel is suspected to be dependent on the ratio of polymer to the peptide as tunablewell andaseffective delivery individual vehicle polymer for EGF with composition, but thermoresponsive this aspect requiresbehavior. The pro- further investigation. tectivity of the gel is suspected to be dependent on the ratio of polymer to the peptide as well asAuthor individual polymer composition, Contributions: but and Conceptualization this methodology, aspect requires S.A.;further investigation. investigation and validation, O.E. and G.V.; data curation and visualization, O.E.; supervision and analysis, S.A.; writing, O.E. All authors have read and agreed to the published version of the manuscript. Funding: This research received no external funding. Institutional Review Board Statement: Not applicable. Informed Consent Statement: Not applicable. Data Availability Statement: The data presented in this study are available on request from the corresponding author.
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