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Drug Transport Mechanisms and In Vitro Release Kinetics of Vancomycin Encapsulated Chitosan-Alginate Polyelectrolyte Microparticles as a Controlled Drug Delivery System

机译:万古霉素封装的壳聚糖-海藻酸酯聚电解质微粒作为药物控制系统的药物转运机理和体外释放动力学

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摘要

In this study, chitosan-alginate polyelectrolyte microparticles containing the antibiotic, vancomycin chloride were prepared using the ionotropic gelation (coacervation) technique. In vitro release and drug transport mechanisms were studied concerning the chitosan only and alginate only microparticles as a control group. Further, the effect of porosity on the drug transport mechanism was also studied for chitosan-alginate mixed particles produced by lyophilizing in contrast to the air-dried non-porous particles. According to the in vitro release data, alginate only and chitosan only microparticles showed burst release and prolonged release respectively. Chitosan-alginate lyophilized microparticles showed the best-controlled release of vancomycin with the average release of 22 μg per day for 14 days. Also, when increasing alginate concentration there was no increase in the release rate of vancomycin. The release data of all the microparticles were treated with Ritger-Peppas, Higuchi, Peppas-Sahlin, zero-order, and first-order kinetic models. The best fit was observed with Peppas-Sahlin model, indicating the drug transport mechanism was controlled by both Fickian diffusion and case II relaxations. Also, Fickian diffusion dominates the drug transport mechanism of all air-dried samples during the study period. However, the Fickian contribution was gradually reducing with time. Porosity significantly effects the drug transport mechanism as case II relaxation dominates after day 10 of the lyophilized microparticles.
机译:在这项研究中,使用离子型凝胶化(凝聚)技术制备了含有抗生素万古霉素氯化物的壳聚糖-海藻酸酯聚电解质微粒。研究了仅壳聚糖和仅藻酸盐的微粒作为对照组的体外释放和药物转运机制。此外,与通过风干的无孔颗粒形成对比,还研究了通过冷冻干燥制得的壳聚糖-海藻酸盐混合颗粒的孔隙率对药物传输机理的影响。根据体外释放数据,仅藻酸盐和仅壳聚糖的微粒分别显示出爆发释放和延长释放。壳聚糖-海藻酸盐冻干微粒显示万古霉素的最佳控制释放,在14天中平均每天释放22μg。同样,当增加藻酸盐浓度时,万古霉素的释放速率也没有增加。用Ritger-Peppas,Higuchi,Peppas-Sahlin,零级和一级动力学模型处理所有微粒的释放数据。 Peppas-Sahlin模型观察到最佳拟合,表明药物转运机制受Fickian扩散和病例II弛豫的控制。而且,在研究期间,菲克扩散控制着所有风干样品的药物传输机制。但是,菲克的贡献随着时间的推移逐渐减少。孔隙率显着影响药物传输机制,因为冻干微粒的第10天后,情况II松弛起主导作用。

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