阴道输送的姜黄素负载聚合物微球:配方设计,体外评价,动力学和稳定性研究

J. Nesalin, Shafiya Khanum
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引用次数: 0

摘要

本研究的主要目的是探讨姜黄素生物黏附微粒子制备的新方法,并设计一种创新的姜黄素阴道给药系统,以提高姜黄素的抗癌活性。采用溶剂蒸发法制备姜黄素包封微球。微球呈离散球形,具有自由流动的特性,并对其粒度分析、形状(扫描电镜)、药物包封效率、FTIR、DSC研究和体外释放性能进行了评估。选择最佳微球制剂(F2,含药高聚物比1:2)与生物黏附聚合物结合成凝胶。对所制备的微胶囊阴道凝胶进行pH、铺展性、挤压性、黏度、体外释药、释药动力学、生物黏附试验、加速稳定性等评价。所选择的微胶囊生物黏附阴道凝胶(FS3凝胶,含1%载药微球w/w和0.6%载药微球w/w)的体外药物释放率超过12小时。然后对结果进行统计比较,得到满意的相关性。综上所述,采用阴道微囊化凝胶制备方案的研究可为其他药物阴道给药的新型给药系统的成功开发提供依据。
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CURCUMIN LOADED POLYMERIC MICROSPHERES FOR VAGINAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES
The main objective of this research is to evaluate a new approach for the preparation of bio adhesive microparticles and to design an innovative vaginal delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated microspheres were prepared by solvent evaporation method. The microspheres were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected microsphere formulation (F2, containing drug: polymer ratio 1:2) was incorporated into gels with a bio adhesive polymer. The microencapsulated vaginal gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected microencapsulated bio adhesive vaginal gel (FS3 gel, containing 1 % w/w of drug loaded microspheres and 0.6 % w/w of Carbopol 934) was found to sustain curcumin over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of microencapsulated vaginal gel study may be adopted for a successful development of newer drug delivery system of other drugs for administration to vagina.
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