Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125 001, India.
Int J Biol Macromol. 2012 Dec;51(5):756-62. doi: 10.1016/j.ijbiomac.2012.07.009. Epub 2012 Jul 16.
The purpose of the present study was to synthesize gum kondagogu-g-poly(N-vinyl-2-pyrrolidone) and to evaluate its mucoadhesive properties. UV-assisted graft co-polymerization of N-vinyl-2-pyrrolidone on gum kondagogu was carried out employing three-factor, three-level central composite experimental designs. It was observed that the concentrations of N-vinyl pyrrolidone and ammonium persulphate exerted a significant antagonistic and synergistic influence on grafting efficiency respectively. The graft co-polymer was characterized by FT-IR, DSC and SEM study. Mucoadhesive properties of the graft-copolymer were evaluated by formulating buccal discs employing metronidazole as the model drug. On comparative evaluation buccal discs formulated using gum kondagogu-g-poly(N-vinyl pyrrolidone) showed higher ex vivo bioadhesion time than the discs formulated using gum kondagogu. In vitro release study showed an almost similar release profile of metronidazole from the buccal discs of gum kondagogu and gum kondagogu-g-poly(N-vinyl-2-pyrrolidone). Thus, grafting of N-vinyl-2-pyrrolidone on gum kondagogu enhances its mucoadhesion without significantly affecting the release behaviour.
本研究的目的是合成胶 Kondagogu-g-聚（N-乙烯基-2-吡咯烷酮），并评价其粘膜粘附性能。采用三因素三水平的中心复合实验设计，在紫外光辅助下进行 N-乙烯基-2-吡咯烷酮在胶 Kondagogu 上的接枝共聚反应。结果表明，N-乙烯基吡咯烷酮和过硫酸铵的浓度分别对接枝效率产生显著的拮抗和协同影响。通过傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）和扫描电子显微镜（SEM）研究对接枝共聚物进行了表征。采用甲硝唑作为模型药物，通过制定颊片来评价接枝共聚物的粘膜粘附性能。在比较评价中，使用胶 Kondagogu-g-聚（N-乙烯基-2-吡咯烷酮）制备的颊片显示出比使用胶 Kondagogu 制备的颊片更高的体外生物粘附时间。体外释放研究表明，甲硝唑从胶 Kondagogu 和胶 Kondagogu-g-聚（N-乙烯基-2-吡咯烷酮）颊片中的释放行为几乎相似。因此，在胶 Kondagogu 上接枝 N-乙烯基-2-吡咯烷酮可以增强其粘膜粘附性，而不会显著影响释放行为。
