Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour Vishwavidyalaya, Sagar, India.
J Liposome Res. 2010 Dec;20(4):341-50. doi: 10.3109/08982101003596125. Epub 2010 Feb 18.
The localized delivery of fluconazole (FLZ) by conventional therapy is a major impediment in achieving its therapeutic efficacy against skin infections, such as cutaneous candidiasis. Therefore, the present study was aimed to develop FLZ-loaded vesicular construct(s), such as liposomes and niosomes, incorporated into carbopol gel (1%; w/w) for sustained, localized application. The liposomes and niosomes were prepared by the lipid/nonionic surfactant-based dry-film hydration method and were characterized for different parameters. In addition, antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed albino rats. The results showed that the size of liposomes and niosomes was found to be 0.348 ± 0.054 and 0.326 ± 0.033 μm with encapsulation efficiency of 31.8 ± 1.36 and 27.6 ± 1.08%, respectively. The skin-retention studies of FLZ from in vitro and in vivo experiments showed significantly higher accumulation of drug in the case of liposomal gel. The in vivo localization studies in viable skin showed that liposomal gel could produce 14.2-fold higher drug accumulation, compared with plain gel, while it was 3.3-fold more in the case of an equivalent-dose application in the form of niosomal gel. The antifungal study also confirmed the maximum therapeutic efficacy of liposomal gel, as the lowest number of cfu/mL was recorded following liposomal FLZ application. The studies signify the potential of liposomal gel for topical delivery of FLZ with increased accumulation of drug in various strata of skin vis-a-vis through sustained release of drug could maintain the localized effect, resulting in an effective treatment of a life-threatening cutaneous fungal infection.
氟康唑（FLZ）的局部递送是实现其对皮肤感染（如皮肤念珠菌病）治疗效果的主要障碍。因此，本研究旨在开发 FLZ 载体制剂（如脂质体和非离子囊泡），并将其纳入卡波姆凝胶（1%；w/w）中用于持续、局部应用。脂质体和非离子囊泡是通过基于脂质/非离子表面活性剂的干膜水化法制备的，并对不同参数进行了表征。此外，还在免疫抑制白化大鼠的实验性皮肤念珠菌病中进行了抗真菌活性研究。结果表明，脂质体和非离子囊泡的粒径分别为 0.348±0.054μm 和 0.326±0.033μm，包封效率分别为 31.8±1.36%和 27.6±1.08%。体外和体内实验的 FLZ 皮肤滞留研究表明，脂质体凝胶中药物的累积量明显更高。在活皮中的体内定位研究表明，与普通凝胶相比，脂质体凝胶可使药物累积增加 14.2 倍，而以非离子囊泡凝胶的等效剂量给药时，药物累积增加 3.3 倍。抗真菌研究也证实了脂质体凝胶的最大治疗效果，因为在应用脂质体 FLZ 后记录到的 CFU/mL 数量最低。这些研究表明，脂质体凝胶具有将 FLZ 递送至皮肤的潜力，与通过持续释放药物增加药物在皮肤各层的累积量相比，可维持局部效应，从而有效治疗危及生命的皮肤真菌感染。
