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采用相反相分离/共凝聚法设计载有环丙沙星的可弯曲 PLGA 植入物。

The design of flexible ciprofloxacin-loaded PLGA implants using a reversed phase separation/coacervation method.

机构信息

Department of Pharmacy Sciences, Creighton University, Omaha, USA.

出版信息

Eur J Pharm Biopharm. 2011 Feb;77(2):233-9. doi: 10.1016/j.ejpb.2010.11.014. Epub 2010 Dec 9.

Abstract

The purpose of this research is to design and characterize flexible PLGA-based implants for the controlled release of ciprofloxacin hydrochloride for up to 6 weeks in vitro. This research uses a reversed phase separation/coacervation method to fabricate flexible PLA and PLGA: excipient implants with dichloromethane/mineral oil as solvent/non-solvent. Physical characterization was performed using thermal and mechanical analyses. Drug loading and release studies were performed with ciprofloxacin HCl as the model drug. Release kinetics was modeled to elucidate possible mechanisms of drug release. Four polymer-excipient combinations with glass transition temperatures less than 20°C and representing a wide range of Young's moduli were shown to entrap up to 8% of ciprofloxacin HCl that could be released at a controlled rate for 65 days in vitro. The release rate could consistently fit a ternary Gaussian pattern with an R(2)>0.99. It was postulated that these release patterns could be related to ciprofloxacin that was loosely or poorly bound (burst release), trapped within the polymer matrix, or encapsulated by the polymer. These studies show that flexible implants can be fabricated from PLGA-based polymers for the controlled release of ciprofloxacin hydrochloride for up to 6 weeks in vitro.

摘要

本研究旨在设计并表征基于 PLGA 的可植入式柔性载体,用于体外长达 6 周时间对盐酸环丙沙星的控制释放。该研究采用反相分离/共凝聚方法,以二氯甲烷/矿物油为溶剂/非溶剂,制备 PLA 和 PLGA:赋形剂可植入物。采用热分析和力学分析进行物理特性表征。以盐酸环丙沙星为模型药物进行药物负载和释放研究。采用模型拟合方法研究药物释放动力学,以阐明药物释放的可能机制。四种玻璃化转变温度低于 20°C、杨氏模量范围较宽的聚合物-赋形剂组合可包封高达 8%的盐酸环丙沙星,在体外可控制释放长达 65 天。释放速率可始终一致地符合三元高斯模式,R(2)>0.99。推测这些释放模式可能与盐酸环丙沙星的松散或较差结合(突释)、被困在聚合物基质内或被聚合物包封有关。这些研究表明,可从基于 PLGA 的聚合物制备用于体外长达 6 周时间对盐酸环丙沙星控制释放的柔性植入物。

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