Preparation and evaluation of microspheres with dual polymeric film to minimize burst effect of highly water soluble drug

Liaqat Ali, Mahmood Ahmad, Usman Minhas, Jawad Ahmad Khan, Muhammad Yousuf, Muhammad Sohail, Khaleeq Anwer
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Abstract

Double-layered controlled release microspheres of venlafaxine were prepared using ethyl cellulose (EC) as a wall forming hydrophobic polymer. Usually, it is difficult to control initial sudden release of highly water-soluble drugs. In this regard, double-layered microparticles were prepared not only for controlling initial burst effect but also to sustain the release of venlafaxine for an extended period of time. Solvent evaporation technique based on O/O emulsion was applied to prepare modified release microparticles. To minimize initial burst effect, developed microparticles were again coated with same hydrophobic polymer. Percent recovery, drug loading efficiency and particle size were measured. FTIR, SEM and kinetic models were applied to characterize venlafaxine microspheres. Packing and flow properties of microparticles were satisfactory. FTIR spectra of EC, venlafaxine and venlafaxine loaded microspheres were recorded. SEM analysis showed the formation of spherical microspheres with slightly rough surface. Burst effect of venlafaxine was significantly retarded in double-layered microparticles. Drug release databased on highest values of correlation coefficient, was suitably explained by Higuchi kinetics and mechanism of release was Fickian diffusion. This study strongly suggests that double-layered microspheres can successfully be applied for controlling the dose dumping and sustaining the release of highly water-soluble drug for an extended period of time.
双聚合物膜微球的制备及评价以减少高水溶性药物的破裂效应
以乙基纤维素(EC)为成壁疏水聚合物制备了文拉法辛双层控释微球。高水溶性药物的初始突然释放通常难以控制。在这方面,制备双层微颗粒不仅可以控制初始爆发效应,而且可以延长文拉法辛的释放时间。采用基于O/O乳液的溶剂蒸发技术制备了改性释放微粒。为了减少最初的破裂效应,显影的微颗粒再次涂覆相同的疏水性聚合物。测定了回收率、载药效率和粒径。利用FTIR、SEM和动力学模型对文拉法辛微球进行表征。微粒的堆积和流动性能令人满意。记录了EC、文拉法辛和载文拉法辛微球的FTIR光谱。扫描电镜分析表明,形成的微球呈球状,表面略粗糙。在双层微颗粒中,文拉法辛的爆发效应明显延迟。药物释放以相关系数最高为基准,用Higuchi动力学解释,释放机制为菲克扩散。本研究表明,双层微球可以成功地用于控制高水溶性药物的剂量倾倒和长时间维持释放。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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