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Fabrication of core–shell PLGA/PLA–pNIPAM nanocomposites for improved entrapment and release kinetics of antihypertensive drugs
Particuology ( IF 3.5 ) Pub Date : 2018-02-03 , DOI: 10.1016/j.partic.2017.10.002
Tanushree Basu , Bonamali Pal , Satnam Singh

Polylactic acid (PLA) and poly(lactic-co-glycolic) acid (PLGA) are two commonly applied biodegradable polymers for the preparation of nanocomposites used in drug-delivery systems. However, these polymers lack desirable attributes such as resistance to aggregation during long-term storage due to lyophilisation. To improve their efficacy, in this work, PLA and PLGA were encapsulated within a shell of poly(N-isopropylacrylamide) (pNIPAM) using a single emulsion technique followed by an aqueous free radical precipitation polymerisation process, yielding core–shell PLA/PLGA–pNIPAM nanocomposites. The nanocomposites were characterised using zeta potential, dynamic light scattering, and transmission electron microscopy analyses and were further applied as a delivery system for ramipril, an antihypertensive drug. The drug-loaded PLGA–pNIPAM core–shell nanoparticles exhibited a higher drug content (91%) and entrapment efficiency (78%) than their PLA counterparts. An in vitro release study of the formulations at pH 7.3 in phosphate-buffered saline indicated that PLGA was more efficient than PLA with a sustained release of 86% of ramipril from the polymer matrix within 24 h. Furthermore, to determine the release kinetics, the data were fitted to Korsmeyer–Peppas and Higuchi models; the release of ramipril from the polymer matrix followed zero-order rate kinetics and an anomalous (non-Fickian) diffusion mechanism.



中文翻译:

核-壳PLGA / PLA-pNIPAM纳米复合材料的制备可改善降压药的包封和释放动力学

聚乳酸(PLA)和聚乳酸-乙醇酸共聚物(PLGA)是两种常用的可生物降解的聚合物,用于制备药物递送系统中使用的纳米复合材料。但是,这些聚合物缺乏合乎需要的特性,例如由于冻干而在长期储存过程中不耐聚集。为了提高其功效,在这项工作中,将PLA和PLGA封装在了聚(N-异丙基丙烯酰胺)(pNIPAM)使用单乳液技术,然后进行水性自由基沉淀聚合过程,得到核-壳PLA / PLGA-pNIPAM纳米复合材料。使用zeta电位,动态光散射和透射电子显微镜分析对纳米复合材料进行表征,并将其进一步用作抗高血压药物雷米普利的递送系统。载有PLGA-pNIPAM核-壳纳米颗粒的药物比PLA药物具有更高的药物含量(91%)和包封率(78%)。在磷酸盐缓冲液中pH 7.3的制剂的体外释放研究表明,PLGA比PLA更有效,在24小时内从聚合物基质中持续释放了86%的雷米普利。此外,要确定释放动力学,数据符合Korsmeyer-Peppas和Higuchi模型;雷米普利从聚合物基质中的释放遵循零级速率动力学和异常(非菲克)扩散机制。

更新日期:2018-02-03
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