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Drug release optimization from microparticles of poly(epsilon-caprolactone) and hydroxypropyl methylcellulose polymeric blends: formulation and characterization

机译:来自聚(ε-己内酯)和羟丙基甲基纤维素聚合物共混物的微粒的药物释放优化:配方和表征

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摘要

In this study, polymeric blend microparticles are prepared with tunable drug releasing behavior, imparted by using poly(epsilon-caprolactone)(PCL) as hydrophobic and hydroxypropyl methylcellulose (HPMC) as hydrophilic biodegradable polymeric constituents. Microparticles were prepared by simple oil in water emulsion-solvent evaporation method and evaluated for their sustained release profile by using nifedipine (half-life is about 2 h) as model drug. Hydrophilic PCL is added to optimize the drug release in simulated aqueous body fluid. Polyvinyl alcohol (PVA), used as emulsifier, was found to improve shape while HPMC increased surface smoothness of microparticles. High encapsulation efficiency was achieved, controllable by HPMC concentration. In vitro dissolution studies in acidic and neutral pH showed sustained release profile for all formulations. Synthesized microparticles, provided control over hydrophobic drug release by changing the proportion of HPMC and PCL in formulation at both acidic and intestinal pH.
机译:在该研究中,通过使用聚(ε-己内酯)(PCL)作为疏水性和羟丙基甲基纤维素(HPMC)作为亲水性可生物降解的聚合物成分来制备聚合物混合物微粒。通过简单的油制备微粒在水乳液溶剂蒸发方法中制备,并通过使用硝苯地平(半衰期为约2小时)作为模型药物评价它们的持续释放曲线。加入亲水PCL以优化模拟水性体液中的药物释放。发现用作乳化剂的聚乙烯醇(PVA),以改善形状,同时HPMC增加了微粒的表面平滑度。实现了高封装效率,可通过HPMC浓度控制。在酸性和中性pH中的体外溶解研究显示所有配方的缓释曲线。合成的微粒,通过在酸性和肠pH的配方中改变HPMC和PCL的比例来提供对疏水药物释放的控制。

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