Vaginal inserts based on chitosan and carboxymethylcellulose complexes for local delivery of chlorhexidine: Preparation, characterization and antimicrobial activity
Vaginal inserts based on chitosan and carboxymethylcellulose complexes for local delivery of chlorhexidine: Preparation, characterization and antimicrobial activity
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DOI：
10.1016/j.ijpharm.2014.12.008
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发表时间：
2015-01-30
影响因子：
5.8
通讯作者：
Luppi, Barbara
中科院分区：
文献类型：
--
作者：
Bigucci, Federica;Abruzzo, Angela;Luppi, Barbara
本工作的目的是制备基于壳聚糖/羧甲基纤维素复合物的阴道插入物，用于二葡萄糖酸氯己定的局部递送。在pH值接近聚合物的pK（a）区间时，用不同的壳聚糖/羧甲基纤维素摩尔比制备复合物，并对其理化性质、复合产率和载药量进行表征。然后用复合物制备阴道剂型插入物，并评价其物理处理、形态、吸水能力和药物释放性能以及对白色念珠菌和大肠杆菌的抗菌活性。结果证实了壳聚糖和羧甲基纤维素之间存在离子相互作用，以及电荷量对络合产率的影响。复合物的特点是高值的药物负载，并表现出增加的吸水能力与羧甲基纤维素量的增加。选择适当的壳聚糖/羧甲基纤维素摩尔比允许获得锥形形状的固体插入物，易于处理并且能够随时间水合释放药物。最后，配制的插入物显示出对导致阴道感染的常见病原体的抗微生物活性。(C)2014爱思唯尔有限公司版权所有。
The aim of this Work was to prepare vaginal inserts based on chitosan/carboxymethylcellulose polyelectrolyte complexes for local delivery of chlorhexidine digluconate. Complexes were prepared with different chitosan/carboxymethylcellulose molar ratios at a pH value close to pK(a) interval of the polymers and were characterized in terms of physico-chemical properties, complexation yield and drug loading. Then complexes were used to prepare inserts as vaginal dosage forms and their physical handling, morphology, water-uptake ability and drug release properties as well as antimicrobial activity toward Candida albicans and Escherichia coli were evaluated. Results confirmed the ionic interaction between chitosan and carboxymethylcellulose and the influence of the charge amount on the complexation yield. Complexes were characterized by high values of drug loading and showed increasing water-uptake ability with the increase of carboxymethylcellulose amount. The selection of appropriate chitosan/ carboxymethylcellulose molar ratios allowed to obtain cone-like shaped solid inserts, easy to handle and able to hydrate releasing the drug overtime. Finally, the formulated inserts showed antimicrobial activity against common pathogens responsible for vaginal infections. (C) 2014 Elsevier B.V. All rights reserved.