紫杉醇载聚二氧环酮膜和胶囊的差异药物释放动力学。

Smrithi Padmakumar, Merin Mary Varghese, Deepthy Menon
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引用次数: 0

摘要

背景:满载药物的植入式系统可以提供几个小时到几年的药物释放,最终有助于急性和慢性疾病的治疗。本研究的重点是对植入物的形态、结构、孔隙度、表面积和润湿性等特性在调节载药聚合物基质的药物释放动力学中的影响进行基本评估。方法:以聚二氧环酮(PDS)为聚合物,紫杉醇(Ptx)为模型药物。研究中采用了两种不同形式的基质植入物,即浸渍涂层制备的储层型胶囊和相转化和静电纺丝制备的基质型膜。用简单方法制备的四种不同基质在体外PBS和体外腹膜洗液中释放约4周。药物释放谱随后与聚合物植入物的理化参数相关。结果:储层型膜具有缓慢稳定的零级动力学,而基质型电纺丝膜和相转化膜具有典型的双相动力学。结论:推测PDS聚合物的缓慢降解速率以及植入物的孔隙度、润湿性等特性对药物释放率起重要控制作用。
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Differential Drug Release Kinetics from Paclitaxel-Loaded Polydioxanone Membranes and Capsules.

Background: Drug laden implantable systems can provide drug release over several hours to years, which eventually aid in the therapy of both acute and chronic diseases. The present study focuses on a fundamental evaluation of the influence of implant properties such as morphology, architecture, porosity, surface area, and wettability in regulating the drug release kinetics from drug-loaded polymeric matrices.

Methods: For this, Polydioxanone (PDS) was selected as the polymer and Paclitaxel (Ptx) as the model drug. Two different forms of the matrix implants, viz., reservoir type capsules developed by dip coating and matrix type membranes fabricated by phase inversion and electrospinning, were utilized for the study. Drug release from all the four different matrices prepared by simple techniques was evaluated in vitro in PBS and ex vivo in peritoneal wash fluid for ~4 weeks. The drug release profiles were thereafter correlated with the physicochemical parameters of the polymeric implants.

Results: Reservoir-type capsules followed a slow and steady zero-order kinetics, while matrix-type electrospun and phase inversion membranes displayed typical biphasic kinetics.

Conclusion: It was inferred that the slow degradation rate of PDS polymer as well as the implant properties like porosity and wettability play an important role in controlling the drug release rates.

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