Nagda C D, Chotai N P, Nagda D C, Patel S B, Patel U L
Induakaka Ipcowala College of Pharmacy, New Vallabh Vidyanagar, Anand, India.
Pharmazie. 2011 Apr;66(4):249-57.
The objective of the present investigation was to prepare mucoadhesive microspheres of ketorolac for nasal administration by means of a solvent evaporation technique using carbopol (CP), polycarbophil (PL) and chitosan (CS) as mucoadhesive polymers. The prepared microspheres were characterized for morphology, swelling behavior, mucoadhesion, interaction studies, drug encapsulation efficiency, in vitro drug release, release kinetics, and ex vivo nasal cilio toxicity studies. The effects of various process variables on the particle size of the microspheres were investigated. Drug encapsulation efficiency and particle size of the microspheres ranged from 52-78% w/w and 14-46 microm respectively. Interaction studies revealed that there were no drug-polymer interactions. The in vitro release profiles showed prolonged-release of the drug. In vitro release data showed a good fit with the Higuchi model, and indicated Fickian diffusion. No severe damage was found to the integrity of nasal mucosa after ex vivo experiments.
本研究的目的是通过溶剂蒸发技术，以卡波姆（CP）、聚卡波非（PL）和壳聚糖（CS）作为粘膜粘附聚合物，制备用于鼻腔给药的酮咯酸粘膜粘附微球。对制备的微球进行了形态学、溶胀行为、粘膜粘附、相互作用研究、药物包封率、体外药物释放、释放动力学和离体鼻纤毛毒性研究等表征。研究了各种工艺变量对微球粒径的影响。微球的药物包封率和粒径分别为52 - 78% w/w和14 - 46微米。相互作用研究表明不存在药物 - 聚合物相互作用。体外释放曲线显示药物为缓释。体外释放数据与Higuchi模型拟合良好，表明为菲克扩散。离体实验后未发现鼻黏膜完整性受到严重损伤。
