Evaluation of drug release kinetics from polymeric nanoparticles loaded with poorly water-soluble APIs

IF 1 Q4 CHEMISTRY, MULTIDISCIPLINARY Ovidius University Annals of Chemistry Pub Date : 2021-07-01 DOI:10.2478/auoc-2021-0020

Ramona-Daniela Păvăloiu, Fawzia Sha’at, Cristina Hlevca, Mousa Sha’at, G. Sãvoiu, Sibel Osman

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引用次数: 1

Abstract

Abstract The aim of this research was to investigate the release behavior of a combination of two poorly water-soluble active pharmaceutical ingredients (APIs) from poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles. Amlodipine besylate - AML, a calcium channel blocker, and valsartan - VAL, an angiotensin II receptor antagonist drug, were used as poorly water-soluble model drugs. PLGA nanoparticles loaded with AML-VAL (1:16 w/w) were obtained by nanoprecipitation using an amphiphilic block copolymer - Pluronic F127 as stabilizer. The drugs release from the PLGA nanoparticles was determined by a dialysis membrane method under sink conditions. Nanoparticles provided a slow release for both APIs and an attenuated burst effect compared to free drug. Five kinetics models such as Zero-order, First-order, Korsmeyer-Peppas, Higuchi and Hixson-Crowell were applied to predict drug release profiles. The Higuchi and Korsmeyer-Peppas models (R2 > 0.97) best described physicochemical release phenomenon for each PLGA formulations.

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载难水溶性原料药的聚合物纳米颗粒的药物释放动力学评价

摘要:本研究旨在研究两种低水溶性活性药物成分(api)在聚D, l -丙交酯-共聚物(PLGA)纳米颗粒中的释放行为。氨氯地平- AML(一种钙通道阻滞剂)和缬沙坦- VAL(一种血管紧张素II受体拮抗剂)被用作低水溶性模型药物。以两亲嵌段共聚物Pluronic F127为稳定剂，通过纳米沉淀法获得了负载AML-VAL (1:16 w/w)的PLGA纳米颗粒。在沉淀条件下，采用透析膜法测定了PLGA纳米颗粒的药物释放量。与游离药物相比，纳米颗粒对原料药具有缓释作用和减弱的爆发效应。采用零阶、一阶、Korsmeyer-Peppas、Higuchi和Hixson-Crowell 5种动力学模型预测药物释放曲线。Higuchi和Korsmeyer-Peppas模型(R2 > 0.97)最能描述各PLGA配方的理化释放现象。

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Ovidius University Annals of Chemistry CHEMISTRY, MULTIDISCIPLINARY-

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11.10%

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5 weeks