Polymer type and molecular weight dictate the encapsulation efficiency and release of Quercetin from polymeric micelles

Sunoqrot, Suhair; Alsadi, Aya; Tarawneh, Ola; Hamed, Rania

doi:10.1007/s00396-017-4183-9

Cited by 20 publications

(17 citation statements)

References 43 publications

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“…mPEG-PCL copolymers with two different PCL chain lengths were synthesized in this study by controlling the mPEG:CL weight ratio during synthesis. The structure of the copolymers and MW of PCL was confirmed using 1 H-NMR ( Figure S1 ) by relying on the relative integration ratios between the proton peaks referring to the ethylene oxide repeating units and any one of the proton peaks of CL repeats [ 26 ]. Accordingly, when the feed ratio of mPEG:CL was 1:2, the MW of PCL was calculated to be 10,364 Da.…”

Section: Resultsmentioning

confidence: 99%

“…mPEG-PCL copolymers were synthesized by ring-opening polymerization of CL as previously described [ 24 , 26 ], where mPEG served as the macroinitiator and stannous octoate as the catalyst to form mPEG-PCL block copolymers. PCL chain length was varied by controlling the mPEG:CL feed ratio ( Table S1 ).…”

Section: Methodsmentioning

confidence: 99%

“…TQ release was investigated in phosphate buffer (pH 7.4) and acetate buffer (pH 5.0) to simulate physiologic and lysosomal/tumor microenvironment pH, respectively. All release media contained 0.5% w/v Tween 80 to ensure sink conditions [ 25 , 26 , 27 , 28 ]. For the release test, triplicate samples of freshly prepared NPs (1 mL) were each transferred to a dialysis bag with 12–14 kD MWCO (Spectrum laboratories Inc., Rancho Dominguez, CA, USA) and immersed in 30 mL release media in tightly closed glass vials.…”

Section: Methodsmentioning

confidence: 99%

“…mPEG-PCL can be synthesized with varying chain lengths of the biodegradable block (i.e., PCL) in order to modulate its physicochemical properties. It can also be used to prepare NPs with different architectures such as matrix-type nanospheres (NS) [ 24 ], reservoir-type (core/shell) nanocapsules (NC) [ 25 ], as well as polymeric micelles [ 26 ]. In this study, in order to reach an optimized NP formulation for TQ, mPEG-PCL NPs were fabricated using different PCL chain lengths in the form of matrix-type NS or reservoir-type NC.…”

Section: Introductionmentioning

confidence: 99%

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Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture

et al. 2020

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Thymoquinone (TQ) is a water-insoluble natural compound isolated from Nigella sativa that has demonstrated promising chemotherapeutic activity. The purpose of this study was to develop a polymeric nanoscale formulation for TQ to circumvent its delivery challenges. TQ-encapsulated nanoparticles (NPs) were fabricated using methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL) copolymers by the nanoprecipitation technique. Formulation variables included PCL chain length and NP architecture (matrix-type nanospheres or reservoir-type nanocapsules). The formulations were characterized in terms of their particle size, polydispersity index (PDI), drug loading efficiency, and drug release. An optimized TQ NP formulation in the form of oil-filled nanocapsules (F2-NC) was obtained with a mean hydrodynamic diameter of 117 nm, PDI of 0.16, about 60% loading efficiency, and sustained in vitro drug release. The formulation was then tested in cultured human cancer cell lines to verify its antiproliferative efficacy as a potential anticancer nanomedicine. A pilot pharmacokinetic study was also carried out in healthy mice to evaluate the oral bioavailability of the optimized formulation, which revealed a significant increase in the maximum plasma concentration (Cmax) and a 1.3-fold increase in bioavailability compared to free TQ. Our findings demonstrate that the versatility of polymeric NPs can be effectively applied to design a nanoscale delivery platform for TQ that can overcome its biopharmaceutical limitations.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture

et al. 2020

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“…As previously reported [37,38], drug-core compatibility is one of the most critical factors that may influence the loading efficiency of SNPs. Sunoqrot and colleagues [39] reported that, according to the Flory-Huggins interaction parameter, ideally, the highest drug-core compatibility is achieved when the water solubility values of the drug and hydrophobic core are equal. In our case, the different solubility of poloxamer and Q (50 mg/mL vs. 2 mg/mL in water at 25 • C) may have affected the drug loading and explain the low encapsulation efficiency.…”

Section: Resultsmentioning

confidence: 99%

Polyphenols-Loaded Sericin Self-Assembling Nanoparticles: A Slow-Release for Regeneration by Tissue-Resident Mesenchymal Stem/Stromal Cells

et al. 2020

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Mesenchymal stem/stromal cells (MSCs) are a therapeutic target to promote tissue regeneration, mainly when oxidative stress-mediated damage is involved in disease pathogenesis. Here, slow-release silk sericin nanoparticles (SNPs) loaded with natural antioxidant polyphenols were developed to sustain regeneration by tissue-resident MSCs. SNPs were prepared by exploiting a self-assembly method with poloxamer and were loaded with proanthocyanidins (P), quercetin (Q) or epigallocatechin gallate (E). SNPs, with a diameter less than 150 nm, were able to encapsulate both hydrophilic (P and E) and hydrophobic (Q) drugs. A slow and controlled release was obtained from SNPs for all the actives in PBS, while in EtOH, Q and E showed a burst release but P did not. Kinetic models revealed lower diffusion of P than other biomolecules, probably due to the higher steric hindrance of P. The in vitro anti-oxidant, anti-elastase and anti-tyrosinase properties of SNPs were assessed: loading the P and E into SNPs preserved the in vitro biological activities whereas for Q, the anti-elastase activity was strongly improved. Moreover, all formulations promoted MSC metabolic activity over 72 h. Finally, SNPs exhibited a strong ability to protect MSCs from oxidative stress, which supports their potential use for regenerative purposes mediated by tissue-resident MSCs.

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Optimization of the Process Variables for the Development of Enteric Coated Colon Targeted Nanoparticles of Quercetin and Evaluation of its Pharmacokinetics, Biodistribution and Targeting Potential

Patel,

Patel

2024

BioNanoSci.

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Polymer type and molecular weight dictate the encapsulation efficiency and release of Quercetin from polymeric micelles

Cited by 20 publications

References 43 publications

Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture

Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture

Polyphenols-Loaded Sericin Self-Assembling Nanoparticles: A Slow-Release for Regeneration by Tissue-Resident Mesenchymal Stem/Stromal Cells

Optimization of the Process Variables for the Development of Enteric Coated Colon Targeted Nanoparticles of Quercetin and Evaluation of its Pharmacokinetics, Biodistribution and Targeting Potential

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