Dhankar Vandana, Garg Garima, Dhamija Koushal, Awasthi Rajendra
Pharmaceutics, Spectrum Institute of Pharmaceutical Sciences and Research, Greater Noida, India.
Pharmaceutics, Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, India.
Polim Med. 2014 Apr-Jun;44(2):75-81.
Mucoadhesion enables localization of drugs to a defined region of the gastrointestinal tract through attractive interactions between polymers composing the drug delivery devices and the mucin layer of the intestinal epithelium. Thus, this approach can be used for enhancement of the oral bioavailability of the drug.
The current communication deals with the development of ranitidine hydrochloride-loaded chitosan-based mucoadhesive microspheres.
Microspheres were prepared by water-in-oil emulsion technique, using glutaraldehyde as a cross-linking agent. The effect of independent variables like stirring speed and polymer-to-drug ratio on dependent variables, i.e. percentage mucoadhesion, percentage drug loading, particle size and swelling index, was examined using a 3(2); factorial design.
The microspheres were discrete, spherical, free-flowing and also showed high percentage drug entrapment efficiency (43-70%). An in vitro mucoadhesion test showed that the microspheres adhered strongly to the mucous layer for an extended period of time. The RC 4 batch exhibited a high percentage of drug encapsulation (70%) and mucoadhesion (75%). The drug release was sustained for more than 12 h. The drug release kinetics were found to follow Peppas' kinetics for all the formulations and the drug release was diffusion controlled.
The preliminary results of this study suggest that the developed microspheres containing ranitidine hydrochloride could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.
粘膜粘附通过构成药物递送装置的聚合物与肠上皮粘液层之间的吸引相互作用，使药物能够定位在胃肠道的特定区域。因此，这种方法可用于提高药物的口服生物利用度。
本通讯涉及载有盐酸雷尼替丁的壳聚糖基粘膜粘附微球的研制。
采用油包水乳液技术，以戊二醛为交联剂制备微球。使用3(2)析因设计考察搅拌速度和聚合物与药物比例等自变量对粘膜粘附百分比、载药百分比、粒径和溶胀指数等因变量的影响。
微球呈离散的球形，自由流动，且药物包封率高（43%-70%）。体外粘膜粘附试验表明，微球能长时间牢固地粘附于粘液层。RC 4批次表现出高载药率（70%）和粘膜粘附率（75%）。药物释放持续超过12小时。所有制剂的药物释放动力学均符合Peppas动力学，药物释放受扩散控制。
本研究的初步结果表明，研制的载有盐酸雷尼替丁的微球可提高药物包封率，减少初始突释，并调节药物释放。
