Quercetin-loaded Nanoparticles Research Articles

Neurotherapeutic effects of quercetin-loaded nanoparticles and Biochanin-A extracted from Trifolium alexandrinum on PI3K/Akt/GSK-3β signaling in the cerebral cortex of male diabetic rats.

Diabetes mellitus (DM) is a severe metabolic disease that can have significant consequences for cognitive health. Bioflavonoids such as Trifolium alexandrinum (TA), quercetin (Q), and Biochanin-A (BCA) are known to exert a wide range of pharmacological functions including antihyperglycemic activity. This study aimed to investigate the neurotherapeutic effects of quercetin-loaded nanoparticles (Q-LNP) and BCA extracted from TA against diabetes-induced cerebral cortical damage through modulation of PI3K/Akt/GSK-3β and AMPK signaling pathways. Adult male Wistar albino rats (N = 25) were randomly assigned to one of five groups: control, diabetics fed a high-fat diet (HFD) for 2 weeks and intraperitoneally (i.p.) injected with STZ (40 mg/kg), and diabetics treated with Q-LNP (50 mg/kg BW/day), BCA (10 mg/kg BW/day), or TA extract (200 mg/kg BW/day). Treatments were applied by oral gavage once daily for 35 days. Diabetic rats treated with Q-LNP, BCA, and TA extract showed improvement in cognitive performance, cortical oxidative metabolism, antioxidant parameters, and levels of glucose, insulin, triglyceride, and total cholesterol. In addition, these treatments improved neurochemical levels, including acetylcholine, dopamine, and serotonin levels as well acetylcholinesterase and monoamine oxidase activities. Furthermore, these treatments lowered proinflammatory cytokine production for TNF-α and NF-κB; downregulated the levels of IL-1β, iNOS, APP, and PPAR-γ; and attenuated the expressions of PSEN2, BACE, IR, PI3K, FOXO 1, AKT, AMPK, GSK-3β, and GFAP. The histopathological examinations of the cerebral cortical tissues confirmed the biochemical results. Overall, the present findings suggest the potential therapeutic effects of TA bioflavonoids in modulating diabetes-induced cerebral cortical damage.

Novel nanocomposites improve functional recovery of spinal cord injury by regulating NF-κB mediated microglia polarization

Secondary neuroinflammation caused by proinflammatory microglia exacerbates the disability of patients with spinal cord injury (SCI), while low drug delivery efficiency reduces the therapeutic effect of conventional drugs on promoting functional recovery. Nowadays, resorting to nanocomposites has been regarded as a promising approach to overcome such an obstacle. Herein, neutrophil membrane-coated quercetin-loaded nanoparticles (denoted NQNPs) were developed to improve drug delivery efficiency and repolarize microglia thereby inhibiting secondary neuroinflammation in SCI. Quercetin-loaded nanoparticles (QNPs), which have the capacity to reprogram proinflammatory microglia toward anti-inflammatory microglia, act as the inner core of NQNPs. The neutrophil membrane was further coated onto the inner core for targeted drug delivery and co-neutralizing inflammatory factors. In vitro and in vivo studies demonstrated that NQNPs could controllably release quercetin under the reactive oxygen species (ROS) abundant environment, reprogram microglia polarization toward M2 phenotype via nuclear factor kappa-B (NK-κB) pathway, thereby inhibiting excessive neuroinflammation, increasing the density and functional status of neurons, and finally promoting motor recovery of SCI with outstanding biocompatibility. We believe that the current research brings a novel strategy and sheds new light on the treatment of SCI.

Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study.

Quercetin is a hydrophobic molecule with short blood circulation times and instability. The development of a nano-delivery system formulation of quercetin may increase its bioavailability, resulting in greater tumor suppressing effects. Triblock ABA type polycaprolactone-polyethylenglycol- polycaprolactone (PCL-PEG-PCL) copolymers have been synthetized using ring-opening polymerization of caprolactone from PEG diol. The copolymers were characterized by nuclear magnetic resonance (NMR), diffusion-ordered NMR spectroscopy (DOSY), and gel permeation chromatography (GPC). The triblock copolymers self-assembled in water forming micelles consisting of a core of biodegradable polycaprolactone (PCL) and a corona of polyethylenglycol (PEG). The core-shell PCL-PEG-PCL nanoparticles were able to incorporate quercetin into the core. They were characterized by dynamic light scattering (DLS) and NMR. The cellular uptake efficiency of human colorectal carcinoma cells was quantitatively determined by flow cytometry using nanoparticles loaded with Nile Red as hydrophobic model drug. The cytotoxic effect of quercetin-loaded nanoparticles was evaluated on HCT 116 cells, showing promising results.

Fabrication of quercetin-loaded nanoparticles based on Hohenbuehelia serotina polysaccharides and their modulatory effects on intestinal function and gut microbiota in vivo

This research was aimed to construct the nanoparticles based on Hohenbuehelia serotina polysaccharides for encapsulation of quercetin (QC-HSP NPs), and investigate their effects on intestinal function and gut microbiota in mice. Results showed that in comparison with HSP and control, QC-HSP NPs significantly improved immune organ indexes, colon length, fecal moisture content and intestinal peristalsis capacity of mice. The productions of short-chain fatty acids (SCFAs) in colon were also increased after treatment with QC-HSP NPs, while the colonic fecal pH was decreased and defecation time was shortened. Through analysis of 16S rRNA sequencing, QC-HSP NPs could increase α and β diversities of gut microbiota, modulate their structure and composition, and increase the relative abundance of beneficial bacteria together with reducing the richness of harmful bacteria. In addition, QC-HSP NPs ameliorated the metabolic functions of gut microbiota by modulating metabolic pathways. This study suggested that QC-HSP NPs might be served as a prebiotic for protecting intestinal health.

Hohenbuehelia serotina polysaccharides self-assembled nanoparticles for delivery of quercetin and their anti-proliferative activities during gastrointestinal digestion in vitro

In this study, the self-assembled nanoparticles based on Hohenbuehelia serotina polysaccharides (QC-HSP NPs) were fabricated to encapsulate quercetin for improving its bioavailability. The structural characteristics, physicochemical properties as well as the cytotoxicity activities of QC-HSP NPs during gastrointestinal digestion in vitro were respectively investigated. The results showed that QC-HSP NPs possessed the spherical and smooth surface morphology, with the average particle size of 360 nm and zeta potential of −38.8 mV. Moreover, QC-HSP NPs had excellent physiochemical stabilities, and presented sustained-release characteristics during gastrointestinal digestion in vitro. Compared with undigested ones, QC-HSP NPs after gastrointestinal digestion exhibited the more significant anti-proliferative activity on HeLa cells through accumulation of intracellular ROS, arrest of cell cycle at G2/M phase by regulation of cyclin B1, CDK1, p53 and p21 and induction of apoptosis by ER apoptosis pathway. This study provides a new strategy for designing quercetin-loaded nanoparticles based on natural polysaccharides to improve the bioavailability of quercetin.

Novel, bioactive film based on methylcellulose incorporated with quercetin-loaded nanoparticles: Bifunctional antioxidant and ultraviolet- shielding properties

Novel, bioactive film based on methylcellulose incorporated with quercetin-loaded nanoparticles: Bifunctional antioxidant and ultraviolet- shielding properties

Corrigendum to Bioactivity and cytotoxicity of quercetin-loaded lecithin-chitosan nanoparticles

Corrigendum to Bioactivity and cytotoxicity of quercetin-loaded lecithin-chitosan nanoparticles

Quercetin Extracted from Trifolium Alexandrinum Enhances wound healing in 1 Streptozotocin-induced Diabetic rats through Antioxidant and Anti-inflammatory effects

Background: Diabetes-induced abnormal wound healing stimulates the generation of inflammatory mediators, including reactive oxygen species. Objective: Our study aimed to examine the antioxidant and anti-inflammatory effects of quercetin extracted from Trifolium alexandrinum (TA) on enhancing wound healing in diabetic rats. Methods: Seventy-five male Wistar albino rats were divided into 5 groups as follows: Gp1 (control wounded nondiabetic group), Gp2 (untreated wounded diabetic group), Gp3 (diabetic wounds treated with quercetin-loaded nanoparticles (Q-LNs) group), Gp4 (wounded diabetic rats treated with quercetin (Q) group) and Gp5 (wounded diabetic rats treated with TA extract group). Key findings: The wounded diabetic rats were treated orally and topically with Q-LNs, Q and TA extract at doses of 50 mg/kg BW, 50 mg/kg BW and 200 mg/kg BW, respectively, for 15 days. The wound closure percent was calculated on the 5th, 10th and 15th days and was noticeably increased as a result of topical and oral treatment of wounded diabetic rats with Q-LNs, Q and TA. The elevated blood glucose and the reduced serum insulin levels were significantly improved in treated wounded diabetic rats. Oxidative stress markers were improved. The increased levels of cytokines, as well as MIF, were decreased in treated wounded diabetic rats, while the decreased levels of TGF-β and hexosamine were enhanced. Histological examination showed marked amelioration in the treated wounded skin. Conclusion: It can be concluded that treatment with Q-LNs, Q and TA extract improved the diabetic state, cytokines involved in inflammation and the antioxidant defense system and may play essential roles in promoting the wound healing process.

Effects of Quercetin-Loaded Nanoparticles on MCF-7 Human Breast Cancer Cells.

Background and objectives: Previous studies have shown anti-tumor activity of quercetin (QT). However, the low bioavailability of QT has restricted its use. This study aimed to assess the toxic effect of QT encapsulated in solid lipid nanoparticles (QT-SLNs) on the growth of MCF-7 human breast cancer cells. Materials and Methods: MCF-7 and MCF-10A (non-tumorigenic cell line) cell lines treated with 25 µmol/mL of QT or QT-SLNs for 48 h. Cell viability, colony formation, oxidative stress, and apoptosis were evaluated to determine the toxic effects of the QT-SLNs. Results: The QT-SLNs with appropriate characteristics (particle size of 85.5 nm, a zeta potential of −22.5 and encapsulation efficiency of 97.6%) were prepared. The QT-SLNs showed sustained QT release until 48 h. Cytotoxicity assessments indicated that QT-SLNs inhibited MCF-7 cells growth with a low IC50 (50% inhibitory concentration) value, compared to the free QT. QT-SLNs induced a significant decrease in the viability and proliferation of MCF-7 cells, compared to the free QT. QT-SLN significantly increased reactive oxygen species (ROS) level and MDA contents and significantly decreased antioxidant enzyme activity in the MCF-7 cells. Following QT-SLNs treatment, the expression of the Bcl-2 protein significantly decreased, whereas Bx expression showed a significant increase in comparison with free QT-treated cells. Furthermore, The QT-SLNs significantly increased apoptotic and necrotic indexes in MCF-7 cells. Viability, proliferation, oxidative stress and apoptosis of MCF-10A cells were not affected by QT or QT-SLNs. Conclusions: According to the results of this study, SLN significantly enhanced the toxic effect of QT against human breast cancer cells.

Inclusion of Quercetin in Gold Nanoparticles Decorated with Supramolecular Hosts Amplifies Its Tumor Targeting Properties.

Despite the anticancer potential of natural products (NPs), their limited bioavailability necessitates laborious derivatization or covalent conjugation to delivery vehicles. To unleash their potential, we developed a nanohybrid delivery platform with a noncovalently tunable surface. Initially, the active compound was encapsulated in a macrocycle, p-sulfonatocalix[4]arene, enabling a 62 000-fold aqueous solubility amplification as also a 2.9-fold enhancement in its cytotoxicity with respect to the parent compound in SW-620 colon cancer cells. A pH stimuli responsive behavior was recorded for this formulate, where a programmable release of quercetin from the macrocycle was monitored in an acidic environment. Then, a nanoparticle gold core was decorated with calixarene hosts to accommodate noncovalently NPs. The loaded nanocarrier with the NP quercetin dramatically enhanced the cytotoxicity (>50-fold) of the parent NP in colon cancer and altered its cell membrane transport mode. In vivo experiments in a mouse 4T1 tumor model showed a reduction of tumor volume in mice treated with quercetin-loaded nanoparticles without apparent toxic effects. Further analysis of the tumor-derived RNA highlighted that treatment with quercetin-loaded nanoparticles altered the expression of 27 genes related to apoptosis.

Self-assembly, functionality, and in-vitro properties of quercetin loaded nanoparticles based on shellac-almond gum biological macromolecules.

Quercetin-fortified nanoparticles were prepared from almond gum (AG), a novel biological macromolecule, and Tween 80 (T80) as stabilizers and shellac (SH) as core material using an antisolvent precipitation method. The final nanoparticles were prepared by 0.67% SH, 0.02% Q, 0.5% AG and 0.1% w/v T80 using the stirring speed of 750 rpm at a dosing rate of 0.5 ml/min. The morphology of the particles was characterized using Cryo-SEM and TEM microscopy. The average particle size was 135 ± 8 nm with a polydispersity index of 0.252 ± 0.01 and an encapsulation efficiency of 97.7 ± 1.2%. At pH 7.4 (intestinal pH), quercetin-loaded nanoparticles showed significantly (p < 0.05) higher antioxidant activity compared to free quercetin while the degradation of quercetin was lower in the nanoparticles compared to free quercetin at the similar pH. Quercetin loaded in nanoparticles was successfully found to be 2 times more available for uptake than free quercetin at pH 7.4. MTT and SRB assays revealed that no significant (p > 0.05) toxicity was observed for Caco-2 cells treated with quercetin-loaded nanoparticles with a dilution factor of 100. This study provides information about the formulation of promising nanocarriers using biological macromolecules for oral delivery of bioactive compounds.

Quercetin prevent proteoglycan destruction by inhibits matrix metalloproteinase-9, matrix metalloproteinase-13, a disintegrin and metalloproteinase with thrombospondin motifs-5 expressions on osteoarthritis model rats.

Prior study has shown that Ageratum conyzoides L. extract that containing quercetin has been proved to prevent inflammation and proteoglycan degradation by inhibiting tumor necrosis factor-alpha and matrix metalloproteinase (MMP-9) expression. Target of osteoarthritis (OA) treatment was in the synovial joint that requiring a drug delivery system. The aim of this study was to prove the efficacy of quercetin-loaded lecithin-chitosan nanoparticles on the OA model rats by observed its effect on interleukin (IL-1) β, MMP-9, MMP-13, and a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS-5) expressions. In this study, 70 white male Sprague Dawley rats were divided into 14 groups, 7 groups each for destabilization of medial meniscus (DMM) and monoiodoacetate (MIA)-induced OA. After 28 days from induction, SHAM and negative group received gel base topically; positive group received sodium diclofenac gel; three-dose group received each 0.84, 1.68, 3.36 mg/g quercetin-loaded nanoparticles gel; and A. conyzoides L. group received A. conyzoides L. extract gel. Each group gets treatment until day 70, and then, blood sample was collected for serum analysis; knee joint was isolated and subjected to histology samples treatment. Quercetin-loaded nanoparticle gel dose 1 (0.84 mg/g gel), dose 2 (1.68 mg/g gel), dose 3 (3.36 mg/g), and A. conyzoides L. extract gel could decreased the level of IL-1 β, MMP-9, MMP-13, ADAMTS-5, and increasing color intensity significantly on histopathological observations on DMM and MIA-induced OA.

Hepatoprotective and antioxidant activity of quercetin loaded chitosan/alginate particles in vitro and in vivo in a model of paracetamol-induced toxicity

The toxic liver impairment caused by free radical injury or excessive reactive oxigen species (ROS) formation could be effectivelly attenuated by natural antioxidants. The present study aimed to explore and compare the hepatoprotective and antioxidant effects of free and encapsulated quercetin in in vitro and in vivo models of hepatotoxicity. Thus, quercetin was encapsulated in chitosan/alginate nanoparticles by gelation method. Both empty and quercetin-loaded nanoparticles revealed good safety profile in vitro, determined by the lack of cytotoxicity in human hepatoma HepG2 cells. The pretreatment of HepG2 cells with encapsulated quercetin (10μg/ml) significantly attenuated the decrease in cell viability in H2О2-induced oxidative stress (0.1mM H2О2), thus showing an effective in vitro protection.In vivo evaluation of the antioxidant and hepatoprotective potential of free and encapsulated quercetin was performed in a model of paracetamol − induced liver injury in male Wistar rats. The oral pretreatment with encapsulated quercetin (0.18mg/kg b.w., 7days) significantly diminished the increased levels of serum transaminases ALT and AST, attenuated the lipid peroxidation and restored the levels of gluthation (a marker of cell antioxidant defence system). The protective effects of quercetin encapsulated in chitosan-based nanoformulation were superior to those of free quercetin. The results of the study suggest that the encapsulation of quercetin in chitosan/alginate nanoformulations might represent an effective therapeutic approach against oxidative stress induced liver injury.

Еvaluation of biocompatibility and antioxidant efficiency of chitosan-alginate nanoparticles loaded with quercetin

The present study deals with development and evaluation of the safety profile of chitosan/alginate nanoparticles as a platform for delivery of a natural antioxidant quercetin. The nanoparticles were prepared by varying the ratios between both biopolymers giving different size and charge of the formulations. The biocompatibility was explored in vitro in cells from different origin: cultivated HepG2 cells, isolated primary rat hepatocytes, isolated murine spleen lymphocytes and macrophages. In vivo toxicological evaluation was performed after repeated 14-day oral administration to rats. The study revealed that chitosan/alginate nanoparticles did not change body weight, the relative weight of rat livers, liver histology, hematology and biochemical parameters. The protective effects of quercetin-loaded nanoparticles were investigated in the models of iron/ascorbic acid (Fe2+/AA) induced lipid peroxidation in microsomes and tert-butyl hydroperoxide oxidative stress in isolated rat hepatocytes. Interesting finding was that the empty chitosan/alginate nanoparticles possessed protective activity themselves. The antioxidant effects of quercetin loaded into the nanoparticles formulated with higher concentration of chitosan were superior compared to quercetin encapsulated in nanoparticles with higher amount of sodium alginate. In conclusion, chitosan/alginate nanoparticles can be considered appropriate carrier for quercetin, combining safety profile and improved protective activity of the encapsulated antioxidant.

Zein nanoparticles for oral delivery of quercetin: Pharmacokinetic studies and preventive anti-inflammatory effects in a mouse model of endotoxemia

Zein nanoparticles were evaluated as nanocarriers to promote the oral bioavailability of quercetin and, thus, improve its anti-inflammatory effect on a mouse model of induced endotoxemia. For this purpose, the flavonoid and 2-hydroxypropyl-β-cyclodextrin were encapsulated in zein nanoparticles. The resulting nanoparticles displayed a mean size of about 300nm and the payload was calculated to be close to 70μg/mg nanoparticle. The release of quercetin from zein nanoparticles followed a zero-order kinetic. After oral administration, nanoparticles provided high and sustained levels of quercetin in plasma and the relative oral bioavailability was calculated to be approx. 60%. Animals treated with quercetin-loaded nanoparticles (1 dose every two days; 1week) presented endotoxic symptoms less severe than those observed in animals treated with the oral solution of the flavonoid (1 dose every day; 1week). This was further corroborated by the significantly low circulating TNF-alpha in the quercetin-loaded nanoparticles treated mice.

Bovine Serum Albumin Nanoparticles Containing Quercetin: Characterization and Antioxidant Activity.

Quercetin is a flavonoid reported as anti-allergic, anti-inflammatory, antiplatelet, anti-microbial, antioxidant, antineurodegenerative and antitumoral. However, due to its low water solubility, its efficacy is restricted. Nanotechnology can be an importante tool to improve the quercetin properties and increase its bioavailability. In this study, bovine serum albumin (BSA) nanoparticles containing quercetin were developed by desolvation technique, characterized the mean particle size, polydispersity, zeta potential, encapsulation efficiency, physical state of drug in nanoparticles and drug release profile as well as their antioxidant activity was evaluated. The influence of glutaraldehyde percentage in nanoparticles properties was evaluated and did not influence the nanoparticles parameters. Nanoparticles presented a mean size around 130 nm and encapsulation efficiency around 85%. Results from X-ray diffractometry showed that the crystal of the drug was converted to an amorphous state in polymeric matrix. Quercetin release profile demonstrated a biphasic pattern and after 96 h approximately 18% of drug was released. Kinetic models demonstrated that the quercetin release followed a second-order model and the release was governed by Fickian diffusion. After 96 h, quercetin-loaded nanoparticles were more effective than free quercetin for scanvenger of radical ABTS + and hypochlorous acid. BSA nanoparticles represents potential carriers for improve quercetin properties.

Morphological and in vitro antibacterial efficacy of quercetin loaded nanoparticles against food-borne microorganisms

Biodegradable nanoparticles have been used regularly as drug delivery carriers owing to its bioavailability augmentation, better entrapment, sustained release and biocompatibility. The present study aimed to compare the antibacterial efficacy of quercetin loaded nanoparticles (QLNs) with free quercetin against Bacillus subtilis, Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium (food-borne microorganisms). Stability study confirmed insignificant variation in particle size, zeta potential and encapsulation efficiency over a period of 90 days of storage. High resolution-transmission electron microscopy (HR-TEM) showed the formation of spherical nanoparticles with smooth surface. The antibacterial activity of free quercetin and QLNs were evaluated for zone of inhibition, percentage retardation of bacterial growth, kinetic measurement, minimum inhibitory concentration and minimum bactericidal concentration studies. The results indicated that QLNs were more efficient than free quercetin owing to control release of quercetin from nanoparticles. The mechanism of antibacterial activity of QLNs was investigated by atomic force microscopy and scanning electron microscopy. Microscopic study revealed the adsorption of nanoparticles on bacterial cell surface followed by increased cell permeability causing cell lysis.

Synthesis of Quercetin Loaded Nanoparticles Based on Alginate for Pb(II) Adsorption in Aqueous Solution.

Pb(II) is a representative heavy metal in industrial wastewater, which may frequently cause serious hazard to living organisms. In this study, comparative studies between alginate nanoparticles (AN) and quercetin-decorated alginate nanoparticles (Q-AN) were investigated for Pb(II) ion adsorption. Characterization of AN and Q-AN were analysed by transmission electron microscopy (TEM), Fourier transform infrared spectrometry (FT-IR), X-ray diffractometer (XRD), and thermogravimetric analysis (TG-DTG-DSC). The main operating conditions such as pH, initial concentration of Pb(II), and co-existing metal ions were also investigated using a batch experiment. AN and Q-AN, with a diameter of 95.06 and 58.23 nm, were constituted by many small primary nanoparticles. It revealed that when initial concentration of Pb(II) is between 250 and 1250 mg L−1, the adsorption rate and equilibrium adsorption were increased with the increase of pH from 2 to 7. The maximum adsorption capacities of 147.02 and 140.37 mg L−1 were achieved by AN and Q-AN, respectively, with 0.2 g adsorbents in 1000 mg L−1 Pb(II) at pH 7. The adsorption rate of Pb(II) was little influenced by the co-existing metal ions, such as Mn(II), Co(II), and Cd(II). Desorption experiments showed that Q-AN possessed a higher desorption rate than AN, which were 90.07 and 83.26 %, respectively. AN and Q-AN would probably be applied as adsorbents to remove Pb(II) and then recover it from wastewater for the advantages of simple preparation, high adsorption capacity, and recyclability.

Preparation of PCL/PEG superporous hydrogel containing drug-loaded nanoparticles: The effect of hydrophobic–hydrophilic interface on the physical properties

A series of novel amphiphilic hydrogels were synthesized by photopolymerization of diacrylated polyethylene glycol as hydrophilic parts and polycaprolactone (PCL) terminated with linear acrylates (G0.5) and dendritic ones (G1.5) as hydrophobic segments in the presence of Irgacure 2959 as initiator. Water absorbency, water content percentage and in-vitro degradation of all hydrogels were determined. Due to their fast swelling and high swelling ratios, these hydrogels have the capability of using as superporous hydrogels. Tandem acrylation/Michael addition by acryloyl chloride and diethanolamine were used to prepare the second generation of aminoester–polycaprolactone–aminoester triblock copolymer (G2) with dendritic–linear–dendritic structure. All steps were characterized by FT-IR and 1H NMR spectroscopy. In order to evaluate the ability of synthesized hydrogels as biodevice materials, the release profile of hydrogels containing quercetin-loaded nanoparticles was determined and compared with the free nanoparticles. Drug-loaded nanoparticles with 88nm in diameter were prepared by nanoprecipitation method using G2 as polymeric carrier.

Synthesis and characterization of pH-responsive and folated nanoparticles based on self-assembled brush-like PLGA/PEG/AEMA copolymer with targeted cancer therapy properties: A comprehensive kinetic study

In this study, a novel nanocarrier was synthesized based on methacrylated poly(lactic-co-glycolic acid) (mPLGA) as a lipophilic domain, acrylated methoxy poly(ethylene glycol) (aMPEG) as hydrophilic part and N-2-[(tert-butoxycarbonyl)amino] ethyl methacrylamide (Boc-AEMA) as pH-responsive segment. Radical polymerization of the above-mentioned three modified monomers produces amphiphilic brush-like copolymer. The protecting amine group (Boc) was selectively deprotected and the latter targeted copolymer was produced through the reaction of this copolymer with activated folic acid. Nanoprecipitation method was used to prepare quercetin-loaded nanoparticles. Dynamic light scattering (DLS) analysis showed that the produced nanoparticles had nanometric size (<100nm) and low polydispersity in size at different pHs. Higuchi and Korsmeyer–Peppas models were applied to evaluate release mechanisms and kinetics. Based on in-vitro degradation study, we found that the brush-like copolymer underwent a rapid weight loss in acidic pH.