Sustained Release Floating Microspheres Of Acyclovir: Formulation, Optimization, Characterization And In Vitro Evaluation
Sustained Release Floating Microspheres Of Acyclovir: Formulation, Optimization, Characterization And In Vitro Evaluation
复制标题
阿昔洛韦缓释漂浮微球：配方、优化、表征和体外评价
DOI：
--
复制
发表时间：
2011
期刊：
影响因子：
--
通讯作者：
S. Suthar
中科院分区：
文献类型：
--
作者：
Parmar Kunal Vinodbhai;M. Gohel;S. Suthar
本工作的目的是制备阿昔洛韦漂浮微球，以延长阿昔洛韦在胃中的停留时间并持续释放阿昔洛韦。采用双乳化溶剂蒸发法制备阿昔洛韦漂浮微球。采用32全因子设计优化配方。评估所得微球的平均粒径、包封率百分比、体外药物释放和模型拟合动力学。使用扫描电子显微镜、傅里叶变换红外（FTIR）光谱和差示扫描量热法研究微球中药物的物理状态。微球的粒径在275-340μm范围内。包封率百分比在 59%-77% w/w 之间。微球保持浮力超过约12小时。傅里叶变换红外光谱和差示扫描量热法的结果表明了阿昔洛韦在微球中的稳定性，并且还表明不存在药物聚合物相互作用。体外药物释放研究表明，阿昔洛韦从微球中释放缓慢且持续约10小时以上。药物释放遵循 Korsemeyer-pepas 模型。批次分析结果表明，乙基纤维素浓度和搅拌速度显着影响药物包封率和微球粒径。因此我们可以得出结论，可以成功开发漂浮微球来维持药物释放。
The aim of the present work was to prepare floating microspheres of acyclovir to prolong residence time in stomach and to sustain the release of acyclovir. Acyclovir loaded floating microspheres were prepared by double emulsion solvent evaporation method. The 32 full factorial design was applied to optimize the formulation. The resultant microspheres were evaluated for average particle size, percentage encapsulation efficiency, in vitro drug release and model fitting kinetics. Scanning electron microscopy, Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry were used to investigate the physical state of the drug in the microspheres. The particle size of microspheres was in the range of 275-340 µm. Percentage encapsulation efficiency was between 59%-77% w/w. Microspheres remained buoyant for more than about 12 h. The results of FT-IR spectroscopy and differential scanning calorimetry indicated the stable character of acyclovir in microspheres and also revealed absence of drugpolymer interaction. The in vitro drug release study showed that acyclovir release from the microspheres was slow and sustained for more than about 10 h. Drug release followed Korsemeyer-peppas model. The results of factorial batches revealed that the concentration of ethyl cellulose and stirring speed significantly affected drug encapsulation efficiency and particle size of the microspheres. Thus we can conclude that floating microspheres can successfully be developed to sustain the drug release.