Patel Keyur S, Patel Mandev B
Research Scholar, Department of Pharmaceutics, Bhagwant University, Ajmer, Rajasthan, India.
A-One Pharmacy College, Enasan, Ahmedabad, Gujarat, India.
Int J Pharm Investig. 2014 Jan;4(1):32-7. doi: 10.4103/2230-973X.127738.
The objective of present study was to develop chitosan-based sustained release nicorandil microspheres to reduce the dosing frequency.
The nicorandil-loaded chitosan microspheres were formulated by emulsion crosslinking method. A 3(2) factorial design was employed to study the influence of drug: Polymer ratio and volume of glutaraldehyde (GA) on percentage entrapment efficiency, particle size, and % drug release at 8 h.
The entrapment efficiency was found to be 41.67 ± 1.43-77.33 ± 1.97% and particle size range 65.67 ± 2.08-146.67 ± 2.18 μm. The batch CH5 showed 79.11 ± 2.23 and 96.21 ± 2.41% drug release at 8 and 12 h, respectively.
DRUG: Polymer ratio and volume of GA had significant effect on % entrapment efficiency, particle size, and % drug release. From the scanning electron microscopy (SEM) study observed that microspheres were spherical and fairly smooth surface. Fickian diffusion was the mode of drug release from nicorandil-loaded chitosan microspheres formulations.
本研究的目的是开发基于壳聚糖的缓释尼可地尔微球,以降低给药频率。
采用乳液交联法制备载尼可地尔壳聚糖微球。采用3(2)析因设计研究药物与聚合物比例和戊二醛(GA)体积对包封率、粒径及8小时药物释放率的影响。
包封率为41.67±1.43 - 77.33±1.97%,粒径范围为65.67±2.08 - 146.67±2.18μm。批次CH5在8小时和12小时的药物释放率分别为79.11±2.23%和96.21±2.41%。
药物与聚合物比例和GA体积对包封率、粒径及药物释放率有显著影响。通过扫描电子显微镜(SEM)研究观察到微球呈球形且表面相当光滑。菲克扩散是载尼可地尔壳聚糖微球制剂的药物释放方式。