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Materials Express
2158-5849/2020/10/1589/010
Copyright © 2020 by American Scientific Publishers
All rights reserved. doi:10.1166/mex.2020.1796
Printed in the United States of America www.aspbs.com/mex
Comparison of two nanocarriers for quercetin in
morphology, loading behavior, release
kinetics and cell inhibitory activity
Tao Wang1, 2 , Caie Wu1, 3, ∗ , Tingting Li1, 3 , Gongjian Fan1, 3 , Hao Gong4 , Peng Liu5 ,
Yunxiao Yang6 , and Lingling Sun7
1
College of Light Industry and Food Engineering, Nanjing Forestry University, Nanjing 210037, China
2
Department of Chemistry Engineering, Xuzhou College of Industrial Technology, Xuzhou 221140, China
3
Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University, Nanjing 210037, China
4
College of Food Science, Xuzhou University of Technology, Xuzhou, 221008, China
5
Weifang Institute for Food and Drug Control, Weifang 261100, China
6
Department of Biomedical Engineering, Johns Hopkins University, Baltimore, Maryland, 21218, USA
7
Qingdao Jimo Comprehensive Inspection and Testing Center, Qingdao 266200, China
Article
IP: 5.10.31.151 On: Sat, 22 Jan 2022 09:55:29
Copyright: American Scientific Publishers
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ABSTRACT
Recently, nanocarrier loading drugs have caused widespread concern. However, there are few reports about
comparison of drug loading behavior of different nanoparticles. In this study, we prepared two nanocarri-
ers (starch nanoparticles and F127 nanoparticles) for oral and intravenous injections, respectively. We used
dynamic light scattering and transmission electron microscopy to study the morphology of the nanocarriers.
Moreover, the loading behavior of nanoparticles on quercetin (QC) and the release behavior of nanoparticles
at different pH levels were studied. In artificial gastric (pH 2.0) and intestinal (pH 6.8) juices, QC showed a
sustained release in two nanoparticles. Meanwhile starch nanoparticle-QC and F127-QC nanosystems both
showed relatively higher inhibitory activities than free QC on five kinds of cells, especially for cell A549, the
cell inhibition ratio achieved to 55.16% and 64.06%, respectively. This study provided a reference for oral and
injection of drug-loaded nanoparticles.
Keywords: Nanoparticle, Quercetin, Loading Behavior, Release Kinetics, Cell Inhibitory.
1. INTRODUCTION biocompatibility. Qin et al. prepared SNPs by nanoprecip-
Nanoparticles (NPs) have been widely used for vari- itation using starch with different amylose contents as a
ous biomedical and industrial applications, such as drug raw material [10]. Liu et al. used oxidized starch to obtain
delivery [1, 2], active material loading, material enhance- SNPs [11]. Debranched SNPs were obtained by nanopre-
ment [3, 4], and emulsification [5]. NPs have shown to cipitation [12]. Lu et al. obtained SNPs by borax crosslink-
be especially promising in drug loading, for they form ing for improving the strength of films [4]. All the above
small compound with highly specific surface area [6–9]. outcomes affirmed that SNPs are suitable for delivering
Starch NPs (SNPs) have aroused great interest in aca- medicine into human body.
demic research because of their biodegradability and
Pluronic F127 is a poloxamer that is biocompatible and
widely used in clinics for various purposes [13]. Pluronics
∗
Author to whom correspondence should be addressed. are triblock copolymers composed of poly(ethylene oxide)
Mater. Express, Vol. 10, No. 10, 2020 1589
Materials Express Comparison of two nanocarriers for quercetin
Wang et al.
(PEO) and poly(propylene oxide) (PPO) with a PEO- was centrifuged at 3500 rpm and washed three times
PPO-PEO structure [14–16]. Several pluronics have been by ethanol. Eventually, the SNP products underwent
approved by the Food and Drug Administration [17]. The lyophilization.
biocompatibility and relatively small size of pluronic F127
triblock copolymer prevent their micelles from being rec- 2.3. Preparation of F127 NPs
ognized by proteins and macrophages, thereby allowing First dissolve 0.1 gram of Pluronic F127 into 100 mL of
a long circulation time [18]. Gao et al. found that F127 deionized water. The solution was then sonicated by using
NPs can used to deliver [19]. Therefore, F127 has good ultrasonic (CPX5800H, EMERSON) and high-pressure
prospects for loading drug and active substance. homogenized with a high-pressure homogenizer (SMC
Ginkgo biloba can be widely found in parts of China. VH201-N02, AVESTIN, Canada). Eventually after dis-
Numerous researchers have found that Ginkgo biloba stan- solving cryoprotectants into the prepared solution, dry-
dard extract contains flavonoids (24%) and terpenes (6%). freeze it overnight to get solid F127 NPs.
Flavonoids are efficient antioxidants against superoxide
anion, hydroxyl radical, and peroxy radical. Flavonoids
2.4. Preparation of Loaded QC NPs
have free-radical-scavenging activity because of their
Nanoparticles (5 mg) were incubated in 10 mL QC solu-
ability to chelate the transition metal involved in the
tion (2 mM) in a 50 mL centrifuge tube for different
production of reactive oxygen species via the Fenton
time spans from 1 min to 10 h. Moreover, nanoparticles
reaction [20]. And Meng have reported the antioxida-
tion of phosphites including the free phenolic hydroxyl were in incubated 10 mL Qc solution (2–25 mM) for 2 h.
group in polypropylene [21]. Quercetin (QC) is a flavonoid Then under room temperature, this mixture was stirred at
demonstrating good therapeutic effect on the treatment 300 rotation/minute. After the given contact times, cen-
of coronary heart disease, angina pectoris, cerebral arte- trifuge the suspension fluid at 12,000 g for 10 min. Collect
riosclerosis, and senile dement. Because of such effect the supernatant as much as possible without disturbing the
on treating diseases, many researchers investigated in precipitated solid, and then wash the remaining sediment
related application; though, unfortunately, the applica- with deionized water meanwhile collect the supernatant
Article
tion of flavonoids, including QC, is limited given the again. Repeat the above process three times. The collected
IP: 5.10.31.151
low amount of medicine reached blood stream. We On: Sat, 22 Jan 2022
supernatant 09:55:29
was for calculations of the loading efficiency
Copyright: American Scientific
and Publishers
loading amounts. Measure the amount of free-floating
speculate that using nano-loading materials withDelivered
good dis-by Ingenta
persibility in water can improve the dissolution proper- QC with ultraviolet spectroscopy, where the absorbance
ties of quercetin and enhance its bioavailability. Thus, of the supernatant should be obtained at the wavelength
we selected ginkgo starch and F127 as raw materials of 510 nm. Eventually, dry freeze sediments for further
to prepare nanosystems with QC extracted from ginkgo downstream analysis.
leaves, respectively. We prepared two nanocarriers (starch The loading efficiency and loading amount of
nanoparticles (SNPs) and F127 NPs) for the slow release polyphenols were calculated with Eqs. (1) and (2),
of QC. Moreover, we studied the release of drug-loaded correspondingly:
NPs in different environments and investigated the cell
inhibitory activity of these two kinds of NPs on five kinds Loading efficiency %
of cells. = total content of QC − content of QC in supernatant
/total content of QC × 100 (1)
2. MATERIALS AND METHODS
2.1. Materials Loading amount
Damaling starch (amylose content is 26.7%) was pur- = total content of QC − content of QC in supernatant
chased from Ingredion China Ltd. (Guangdong, China).
Pluronic F127 was purchased from Sigma (chemical struc- /total weight of dry SNPs (2)
tural formula was shown in Fig. 10). QC (purity > 98%)
was supplied by Xi’an Best Technology Co., Ltd. All other 2.5. Transmission Electron Microscopy (TEM)
chemicals were at analytical grade. The morphology of the SNPs was observed by TEM
H-7650 (Hittach, Tokyo, Japan). A drop of the diluted NP
2.2. Preparation of Damaling SNPs suspension was added to a 300-mesh copper grid. The cop-
The SNPs were fabricated according to the method per grid was freeze-dried at −40 C for analysis.
described by Qiu et al. In brief, 10 mL DML starch
suspension (1%, w/v) was heated in boiling water for 2.6. Dynamic Light Scattering (DLS)
30 min [22]. Then, ethanol (40 mL) was added drop- The average particle diameter, diameter distribution, and
wise to the gelatinized and cooling starch slurry imme- polydispersity of the SNPs were measured by DLS using a
diately and incubated for another hour. The mixture Malvern Zetasizer Nano (Malvern, Worcestershire, U.K.).
1590 Mater. Express, Vol. 10, 2020Comparison of two nanocarriers for quercetin
Wang et al.
Materials Express
Samples re-dissolved in deionized water through sonica- with Duncan’s test using a common threshold of p < 0.05
tion (0.05%, w/v) and analyzed at 25 C. via SPSS 10.0 Statistical Software Program (SPSS Inc.,
Chicago, IL, USA).
2.7. In Vitro Release of QC
The release of free QC and SNPs was estimated with 3. RESULTS AND DISCUSSION
the equilibrium dialysis method described by Liu et al.
3.1. Morphology of SNPs and Loaded SNPs
with some modifications [23]. First disperse medicine-
The TEM image and particle size distribution of the SNPs
containing SNPs into pH 2.0 and pH 6.8 phosphate buffer
are shown in Figure 1. The size of the SNPs was about
saline (PBS), and then use a dialysis membrane (molecular
60 nm, and the particles aggregated (Fig. 1(A)). Qin et al.
weight cut-off, 5 kDa) to seal up the suspension fluid. At
also reported that aggregation occurs between SNPs pre-
37 C, shake the mixtures for various durations. For each
pared by nanoprecipitation [10]. When the QC was loaded
mixture sample, 2 mL of the release medium was with-
drawn at predetermined time intervals and replaced by the in the SNPs, the size of the loaded SNPs increased. As
same medium under the same conditions. Then use ultravi- shown in Figure 1(B), a crown appeared around the NPs.
olet spectrophotometer to measure the amount of QC drug We speculate that the crown was QC adsorbed on the SNP
release in each sample. Loaded F127 NPs were released surface. This was due to the hydrogen bonding interaction
in PBS at pH 7.4. Other steps were similar to those in the between the hydroxyl groups of SNPs and the hydroxyl
loaded SNPs. Use free-floating QC as the baseline control. group of QC. As Table I shows that the average sizes of
the SNPs and loaded SNPs were 93 and 212 nm, corre-
spondingly, which are both higher than the diameter mea-
2.8. Cell Culture
sured under TEM. During DLS measurement, the SNPs
Culture A549 in solution with 90% RPMI-1640 and 10%
were swollen in water. Hebeish et al. also reported that the
FBS, HEPG-2 was cultured in 90% MEM with 10% FBS,
hydraulic radius of SNPs is higher than the size from the
BGC-823 was cultured in 90% RPMI-1640 with 10% FBS,
TEM image [24].
MCF-7 was cultured in 90% MEM (contain 0.01 mg/mL
Article
insulin) with 10% FBS, HCT116 was cultured in 90%
McCoy’s 5A with 10% FBS. AllIP:cells were grown
5.10.31.151 a 223.2.
On:inSat,
Morphology of F127 NPs and Loaded F127 NPs
Jan 2022 09:55:29
humidified atmosphere with 5% CO2 Copyright:
at 37 C.American The Figure 2 suggests that F127 NPs are rod shaped with
Gently Scientific Publishers
Delivered
remove cell with trypsin once they reached confluence by length
Ingenta and width of 200–500 and 20–100 nm, respectively,
stage. and show rod aggregations (Fig. 2(A)). The loaded F127
NPs are larger and irregularly shaped compared with the
2.9. Inhibition Effect on Five Different Kinds of F127 NPs. We speculated that the hydroxyl group of QC
Cells of F127-QC and SNPs-QC reacts with the C C bond of the F127 NPs. The longi-
Cells were adjusted to 5 × 10 cells/mL and planted into
4 tudinal and lateral dimensions of the rod structure showed
96-well plate at the concentration of 100 L per well. large differences. Moreover, the hydraulic radius of F127
Upon incubated in 5% CO2 atmosphere at 37 C for NPs was similar to the TEM size. This finding indicated
24 hours, the culture liquid was discarded and various that the F127 NPs were less swollen in water than the
concentration of F127-QC and SNPs-QC with suitable SNPs.
medium were put into each well (100 L/well). The base- As shown in Table I, the F127 NPs are larger than the
line control was prepared starting at the same time. Then, SNPs. The polydispersity index (PDI) of the loaded SNPs
incubate all plates under the same condition for 48 hours. was slightly smaller than that of the SNPs. We speculated
Mix 10 mL CCK-8 solution into each well of each plate, that the loaded SNPs are mutually exclusive. Thus, the
which was shaken for 10 min and continued to incubate for adsorbed QC can improve the dispersibility of the SNPs.
4 h. Take photos under microscope. The absorbance was This result is consistent with the TEM image. However,
measured at 450 nm and the inhibition rate was calculated the PDIs of the F127 NPs and loaded F127 NPs were
as follows: similar. This might be related to the rod-like structure of
the F127 NPs. We speculate that repulsive force between
Inhibition rate% rod-like structures was weaker than spherical structure.
= Negative control group − Experiment group
3.3. Characterization of NPs Loaded with QC
/Negative control group × 100% The effect of QC concentration on loading content is
shown in Figure 3. The loading amounts of NPs on QC
2.10. Statistical Analysis gradually increased with increasing QC concentration. The
All biological experiments were repeated at least three loading amounts of NPs on QC rapidly increased as the
times. Mean and standard deviations were calculated for QC concentration was increased from 2 mM to 14 mM.
each numerical result. Variance analyses were computed At low QC concentration, NPs have sufficient position
Mater. Express, Vol. 10, 2020 1591Materials Express Comparison of two nanocarriers for quercetin
Wang et al.
A B
14 14 Loaded SNPs
a SNPs b
12 12
10 10
Intensity (%)
Intensity (%)
8 8
6 6
4 4
2 2
0 0
10 100 1000
Article
100 1000
Size (nm) Size (nm)
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Fig. 1. The morphology of SNPs (A, a) and loaded SNPsAmerican
(B, b). Scientific Publishers
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to combine with QC. Therefore, most QC form complex force between QC and F127 was stronger than that of SNP
with NPs. When the concentration of QC was increased and F127.
from 14 mM to 24 mM, the loading amounts of NPs on Figure 4 delineates the effect of time on loading con-
QC slowly increased. As QC concentration continued to tent. For the SNPs and F127 NPs, the loading content grew
increase, the binding sites of NPs gradually became sat- drastically as the time was prolonged from 0 to 250 min. In
urated. Therefore, at high QC concentrations, excessive a short period of time, QC entered the many easily acces-
QC was not adsorbed. When the QC concentration was sible binding sites on the surface of the SNPs and F127
increased from 20 mM to 24 mM, the loading amount NPs. Once the time reached 250 min, the amount of the
of NPs was stable. Qiu et al. found that the number of loaded polyphenols became relatively slow, and the reac-
polyphenols adsorbed to amylopectin and amylose NPs tion essentially reached the state of equilibrium (Fig. 4).
increases markedly with prolonged contact times, then the This result might be due to the saturation of some reactive
absorption rate plateaued out [25]. Moreover, the maxi- sites and repulsive forces between loaded QCand bulk-
mum loading amounts of SNPs and F127 NPs were 1140 free QC. This finding agreed with the previous studies
and 1382 g/mg, respectively. This result indicates that the where Phan found that the amount of dietary polyphe-
F127 NPs have higher loading capacity than the SNPs. We nols adsorbed to cellulose increases markedly with pro-
speculated that there more binding sites are available for longed exposure times and then the adsorption appeared to
the F127 NPs than for the SNPs. Moreover, the binding reach a plateau [26]. Meanwhile the loading content of the
F127 NPs was higher than that of the SNPs. This result
Table I. The PDI, average size of NPs and F127 NPs. indicates that the F127 NPs have more binding sites than
the SNPs.
Samples Average size (nm) PDI
SNPs 80 ± 8.23d
0.34 ± 0.08a 3.4. In Vitro Release of QC from Loaded SNPs
Loaded SNPs 165 ± 9.65c 0.28 ± 0.07a
The in vitro release behavior of the loaded SNPs in artifi-
F127 NPs 262 ± 12.42b 0.32 ± 0.05a
Loades F127 NPs 364 ± 15.31a 0.36 ± 0.11a cial gastric juice (pH 2.0) and artificial intestinal juice (pH
6.8) is shown in Figures 5 and 6. The in vitro release pro-
Note: Different letters (a–d) in each column means significant differences.
files of free QC for gastrointestinal juice showed a typical
1592 Mater. Express, Vol. 10, 2020Comparison of two nanocarriers for quercetin
Wang et al.
Materials Express
A B
20 F127 NPs
a 20
18 b Loaded F127
18
16
16
14 Intensity (%) 14
Intensity (%)
12 12
10 10
8 8
6 6
4 4
Article
2 2
0 IP: 5.10.31.151 On: Sat, 22 Jan0 2022 09:55:29
100 Copyright: American 200
1000 Scientific Publishers 400 600 800 1000
Size (nm) Delivered by Ingenta Size (nm)
Fig. 2. The morpology of F127 NPs (A, a) and loaded F127 NPs (B, b).
biphasic pattern. The release behavior of QC from the membrane. Given various durations, the release profile of
SNPs was consistent with previous results [27]. As shown the loaded QC SNPs was roughly divided into three stages
in Figure 5, the free QC was rapidly released in stage I and at pH 2.0. First stage (I): the QC was burst released during
more than 80% of the free QC was released during 1.0 h. 0.6 h, which may be attributed to the presence of free QC
Thus, the free Qc can diffuse freely through the dialysis on the SNP surface. Chuacharoen et al. [28] reported that
1600 1800
SNPs
SNPs F127 NPs
1400 F127 NPs 1600
1400
1200
Loading content (µg/mg)
Loading content (µg/mg)
1200
1000
1000
800
800
600
600
400
400
200 200
0 0
0 5 10 15 20 25 0 100 200 300 400 500 600
Concentration of Qc (mM) Time(min)
Fig. 3. Effect of Qc concentration on loading amount of NPs. Fig. 4. Effect of time on the loading content at 24 mM Qc solution.
Mater. Express, Vol. 10, 2020 1593Materials Express Comparison of two nanocarriers for quercetin
Wang et al.
Free Qc
Cumulative release percentage (%)
100
A Loaded Qc SNPs
a
80
60
40
20
䊠 䊡 䊢
0
0 2 4 6 8 10 12
Time (h)
Fig. 5. In vitro release behavior of loaded SNPs (A) and corresponding TEM image (a) in artificial gastric juice (pH = 2.0).
the release of the non-entrapped compounds available on the soft adsorption between QC and the SNPs. Third stage
the particle surface at the beginning stage of the release is (III): after 6 h, QC was released slowly possibly because
referred to as the “initial burst release.” Second stage (II): the QC inside the SNPs was released after the SNPs were
QC was immediately released (1–6 h), which was due to destroyed.
Free Qc
100
A Loaded Qc SNPs
a
Cumulative release percentage (%)
Article
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60 Delivered by Ingenta
40
20
䊠 䊡 䊢
0
0 2 4 6 8 10 12
Time (h)
Fig. 6. In vitro release behavior of loaded SNPs (A) and corresponding TEM image (a) in artificial intestinal juice (pH = 6.8).
100 Free Qc
Loaded Qc F127
A
a
Cumulative release rate (%)
80
60
40
20
䊠 䊡 䊢
0
0 2 4 6 8 10 12
Time (h)
Fig. 7. In vitro release behavior of loaded F127 NPs (A) and corresponding TEM image (a) in artificial plasma (pH = 7.4).
1594 Mater. Express, Vol. 10, 2020Comparison of two nanocarriers for quercetin
Wang et al.
Materials Express
A
100 F127 NPs-Qc
SNP-Qc
Free Qc
80 SNP
Cell inhibition rate (%)
F127 NPs
60
40
20
0
0 50 100 150 200
Administration concentration (ug/mL)
B F127 NPs-Qc C
100 SNP-Qc 100
F127 NPs-Qc
Free Qc SNP-Qc
SNP Free Qc
80 F127 NPs 80
Cell inhibition rate (%)
Cell inhibition rate (%)
SNP
F127 NPs
60 60
Article
40 40
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20 Delivered by Ingenta
20
0 0
0 50 100 150 200 0 50 100 150 200
Administration concentration (ug/mL) Administration concentration (ug/mL)
D
100 E
100 F127 NPs-Qc F127 NPs-Qc
SNP-Qc SNP-Qc
Free Qc 80 Free Qc
SNP SNP
80
Cell inhibition rate (%)
Cell inhibition rate (%)
F127 NPs F127 NPs
60
60
40
40
20 20
0 0
0 50 100 150 200 0 50 100 150 200
Administration concentration (ug/mL) Administration concentration (ug/mL)
Fig. 8. Inhibitory activity of SNPs-QC and F127-QC on different cells, (A) A549, (B) HEPG-2 (C) BGC-823, (D) MCF-7, (E) HCT116.
Mater. Express, Vol. 10, 2020 1595Materials Express Comparison of two nanocarriers for quercetin
Wang et al.
At pH 6.8, the loaded SNPs exhibited similar release percentage increased by 31.4% in 5 h at pH 2.0. At pH 6.8,
profiles (Fig. 6), which could be characterized by an initial the accumulative release percentage of the loaded SNPs
burst release within 2 h followed by an immediate release increased by 34.2% in 5 h. This result indicates that
(2–7 h). After 7 h, QC was sustained release. Although QC and F127 have stronger binding ability than QC and
the release profile of the loaded SNPs was divided into SNPs. At stage III, the accumulative release percentage
three stages at pH 2.0 and pH 6.8, the time intervals of the loaded F127 NPs slowly increased. Meanwhile, the
of the first and second stages were different. This result amount of released QC was lower than that of free QC
indicated that the stability of the SNPs at 2.0 and 6.8 possibly because QC has strong binding to F127 and can-
was different. Figures 5 and 6 show the corresponding not be completely released within 12 h. Feng et al. also
TEM images of the loaded SNPs at different pH for 6 h. demonstrated that the intermolecular interaction between
The spherical loaded SNPs were destroyed. Some black F127-CD and honokiol is strong [29]. Figure 7(a) shows
entities corresponding to the released QC were observed the corresponding TEM images. The morphology of the
from the TEM image. The above results indicated that F127 NPs was destroyed and some debris were produced.
the QC loaded by the SNPs can be sustainably released, We speculated that the fragments contain unreleased QC.
which suggests an improvement made in achieving better Therefore, the accumulative release percentage of the F127
bioavailability. This indicated that both SNPs and F127 NPs was lower than that of the SNPs.
NPs could achieve the slow release of QC. This laid the
foundation for the suppression of cancer cells. 3.6. Inhibition Effect on Five Different Kinds of
Cells of F127-QC and SNPs-QC
3.5. In Vitro Release of QC from Loaded F127 NPs QC was well known with it’s anti-cancer activity, in order
The in vitro release behavior of the loaded F127 NPs to evaluate the inhibition ratio on cancer cell of the nano-
in pH 7.4 is shown in Figure 7(A). The accumulative systems, five sorts of common cancer cells were selected
release percentage of free QC was about 80% at 2 h. and studied. As shown in Figures 8 and 9, that free QC
However, the released rate of the loaded QC F127 NPs and the two nano-loading systems of SNP-QC and F127-
Article
obviously decreased. After 10 h, the maximum accumula- QC all have certain inhibitory effects on the five kinds
tive release percentage of the loaded QC F127 NPs
IP: 5.10.31.151 On: was
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cells,
2022 among which the effect was the most signifi-
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reached. Just like the SNPs, the loaded QC American
F127 NPs Scientific
cant onPublishers
cell A549. The effects on HEPG-2 and BGC-
were burst released at stage I (0–2 h). QC was Delivered
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823 were not as obvious, and the inhibitory impacts on
ately released during 2–8 h. During 6 h, the accumulative MCF-7 and HCT116 cells were the weakest. Compared
release percentage of QC increased by 26.1%. However, with free QC, the two nano-drug loading systems had
at stage II, for the loaded SNPs, the accumulative release some degree of increased inhibition effectiveness. Among
Fig. 9. Microscope imagines of cell A549 after administration different concentrations of QC, SNPs-QC, and F127-QC. ((A) 6.25 g/mL,
(B) 12.5 g/mL, (C) 25 g/mL, (D) 50 g/mL, (E) 100 g/mL, (F) 200 g/mL, all the images use the same scale bar).
1596 Mater. Express, Vol. 10, 2020Comparison of two nanocarriers for quercetin
Wang et al.
Materials Express
spheroidal (SNPs) and rod (F127 NPs), respectively. Load-
ing efficiency and loading amount of F127 NPs was higher
than that of SNP at the same concentration and time. Both
NPs have a high encapsulation rate for QC, the SNPs and
F127 NPs could not only improve the pharmacokinetic
behavior of QC but also reduce the release rate of QC.
Fig. 10. The chemical structure of starch (A) and F127 (B). Moreover, based on the cell experiments, both of the two
NPs have better performance on cell inhibitory activity
them, F127-QC had the best efficacy, such that the rank- compare with free QC. The inhibitory activity of F127 NPs
ing of cell inhibitory effects was F127-QC > SNP-QC > was more significant than SNPs. In terms of application,
free QC. There existed a roughly positive correlation F127 NPs were more suitable for injection while SNPs
between the cell inhibition rate and the dose concentration. were suitable for oral administration. Overall, we designed
When the dose concentration was 200 g/mL, the inhibi- and compared the embedding efficiency, release effect and
tion rates of SNP-QC and F127-QC on A549 cells were cell inhibitory activity of two kinds nano-drugs devel-
55.16% and 64.06%, respectively, which were significantly oped by nanomaterial-embedded QC, which provided a
higher than free QC’s inhibition rate being 48.76%. At theoretical reference for the development of nanomaterial-
this concentration, the inhibition rates of F127-QC, SNP- embedded QC-related drugs.
QC and free QC on HEPG-2 cells were 46.29%, 32.70%
and 28.16% respectively. QC and its nano-loading system Acknowledgments: This work was supported by
appear to have a relatively weak impact on MCF-7 and the Natural Science Foundation of Jiangsu Province
HCT116. As drug dosage increased from 6.25 g/mL to (BE2015315) and Natural Youth Foundation of Jiangsu
200 g/mL, the cell inhibition rates of SNP-QC on MCF-7 Province (BK20150883). The authors also acknowledge
and HCT116 ranged from 1.39% to 26.30% and 7.81%– the support of the Priority Academic Program Develop-
27.10%, respectively. Meanwhile, the cell inhibition rates ment of Jiangsu Higher Education Institutions and Coinno-
vation Centre for Sustainable Forestry in Southern China.
Article
of F127-QC on MCF-7 and HCT116 ranged from 3.98%
to 28.65% and 9.56% to 29.18%.IP: 5.10.31.151 On: Sat, 22 Jan 2022 09:55:29
Given the results above, we can conclude that American
Copyright: when free Scientific
References
Publishersand Notes
QC is loaded into a nano-delivery system, itsDelivered
inhibitory by Ingenta
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Copyright: American
Synthesis and characterization of novel amphiphilic copolymer
Scientific Publishers
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Received: 7 March 2020. Accepted: 31 March 2020.
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