Mishra Renuka, Joshi Priyanka, Mehta Tejal
Department of Pharmaceutics and Pharmaceutical Technology, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, India.
Int J Pharm Investig. 2016 Jan-Mar;6(1):47-55. doi: 10.4103/2230-973X.176487.
The objective of the present investigation was formulation, optimization and characterization of mucoadhesive film of clotrimazole (CT) which is patient-convenient and provides an effective alternative for the treatment of vaginal candidiasis. CT is an antimycotic drug applied locally for the treatment of vaginal candidiasis.
Mucoadhesive vaginal films were prepared by solvent casting technique using hydroxyl propylcellulose and sodium alginate as polymers. Propylene glycol and polyethylene glycol-400 were evaluated as plasticizers. The mucoadhesive vaginal films were evaluated for percentage elongation, tensile strength, folding endurance, drug content, in vitro disintegration time, in vitro dissolution study, swelling index, bioadhesive strength, and diffusion study.
Among various permeation enhancers used, isopropyl myristate was found to be suitable. To evaluate the role of the concentration of permeation enhancer and concentration of polymers in the optimization of mucoadhesive vaginal film, 3(2) full factorial design was employed. Optimized batch showed in vitro disintegration time, 18 min; drug content, 99.83%; and tensile strength, 502.1 g/mm(2). In vitro diffusion study showed that 77% drug diffusion occurred in 6 h. This batch was further evaluated by scanning electron microscopy indicating uniformity of the film. In vitro Lactobacillus inhibition and in vitro antifungal activity of optimized batch showed an inhibitory effect against Candida albicans and no effect on Lactobacillus, which is a normal component of vaginal flora.
Mucoadhesive vaginal film of CT is an effective dosage form for the treatment of vaginal candidiasis.
本研究的目的是制备克霉唑（CT）黏膜黏附膜并进行优化和表征，该膜剂方便患者使用，为治疗阴道念珠菌病提供一种有效的替代方法。CT是一种局部应用于治疗阴道念珠菌病的抗真菌药物。
采用溶剂浇铸技术，以羟丙基纤维素和海藻酸钠为聚合物制备黏膜黏附阴道膜。评估了丙二醇和聚乙二醇-400作为增塑剂的效果。对黏膜黏附阴道膜进行了伸长率、拉伸强度、耐折性、药物含量、体外崩解时间、体外溶出度研究、溶胀指数、生物黏附强度和扩散研究。
在所使用的各种渗透促进剂中，发现肉豆蔻酸异丙酯是合适的。为了评估渗透促进剂浓度和聚合物浓度在黏膜黏附阴道膜优化中的作用，采用了3（2）全因子设计。优化后的批次显示体外崩解时间为18分钟；药物含量为99.83%；拉伸强度为502.1 g/mm²。体外扩散研究表明，在6小时内药物扩散率为77%。通过扫描电子显微镜对该批次进行进一步评估，表明膜的均匀性。优化批次的体外乳酸菌抑制和体外抗真菌活性显示对白色念珠菌有抑制作用，对作为阴道菌群正常成分的乳酸菌无影响。
CT黏膜黏附阴道膜是治疗阴道念珠菌病的一种有效剂型。
