Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125 001, India.
Int J Biol Macromol. 2013 Feb;53:114-21. doi: 10.1016/j.ijbiomac.2012.10.033. Epub 2012 Nov 21.
The study was conducted to evaluate carboxymethyl gellan gum as bioadhesive polymer for drug delivery applications. Gellan gum was carboxymethylated by reacting it with monochloroacetic acid. Degree of carboxymethyl substitution was found to be 1.18. Further, carboxymethylation of gellan gum was found to increase its degree of crystallinity, surface roughness and diminish the cation-induced gelation. On comparative evaluation carboxymethyl gellan gum showed 2.71-fold higher mucoadhesive strength than gellan gum. Evaluation of ex vivo ocular tolerance using chorioallantoic membrane of hen's egg and cytotoxicity screening on Vero cells using resazurin assay revealed that caroboxymethyl gellan gum is non-irritant and biocompatible. Ionotiropically gelled beads of carboxymethyl gellan gum formulated using metformin as the model drug and calcium chloride as the cross-linking agent showed ex vivo bioadhesion of 100% over 24h. Further, it was observed that carboxymethyl gellan gum beads released metformin at a rate faster than gellan gum.
本研究旨在评估羧甲基结冷胶作为药物传递应用的生物粘附聚合物。通过将结冷胶与一氯乙酸反应,对结冷胶进行羧甲基化。发现羧甲基取代度为 1.18。此外,结冷胶的羧甲基化被发现增加了其结晶度、表面粗糙度,并减少了阳离子诱导的凝胶化。在比较评估中,羧甲基结冷胶显示出比结冷胶高 2.71 倍的粘膜粘附强度。使用鸡胚的绒尿膜对体外眼耐受性进行评估,以及使用 Resazurin 测定法在 Vero 细胞上进行细胞毒性筛选,结果表明羧甲基结冷胶无刺激性且生物相容性良好。使用二甲双胍作为模型药物和氯化钙作为交联剂,离子型凝胶化的羧甲基结冷胶珠在 24 小时内显示出 100%的体外生物粘附性。此外,观察到羧甲基结冷胶珠释放二甲双胍的速度比结冷胶珠快。