基于聚乳酸的负载肝素微球鼻腔给药

Ayca Yıldız , Alper Okyar , Gül Baktır , Ahmet Araman , Yıldız Özsoy
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引用次数: 16

摘要

本研究设计了表面光滑、粒径小的负载肝素微球,以实现肝素通过鼻黏膜的吸收。为此,以聚乳酸为原料,采用溶剂蒸发法制备了不同聚合物/药物比(1:10、1:25、1:1)和不同聚乙烯醇、乳化剂(1.5%、2.5% w/v)浓度的微球。对微球的形状、表面性质、粒径、产率、包封效率和体外释放度进行了评价。在体外实验的基础上,选择的微球经鼻路应用于Wistar白化大鼠。根据体内研究,负载肝素的微球可以通过鼻腔途径作为肠外途径的替代方案。
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Nasal administration of heparin-loaded microspheres based on poly(lactic acid)

In this study, heparin-loaded microspheres having smooth surface and small particle size were designed in order to provide the absorption of heparin through nasal mucosa. For this purpose, microspheres at different polymer/drug ratios (1:10, 1:2.5 and 1:1) and at different concentrations of polyvinyl alcohol, emulsifying agent (1.5% and 2.5% w/v) were prepared by solvent evaporation method with poly(lactic acid). The microspheres were for evaluated shape and surface properties, particle size, production yield, encapsulation efficiency and in vitro drug release. Based on the in vitro data, selected microspheres were applied by nasal route to Wistar albino rats. According to in vivo studies, heparin-loaded microspheres may be used by nasal route as an alternative to parenteral route.

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