Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour Viswavidyalaya, Sagar 470 003, MP, India.
Chem Phys Lipids. 2012 May;165(4):454-61. doi: 10.1016/j.chemphyslip.2012.01.006. Epub 2012 Jan 31.
The nanoparticulate carrier systems as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have gained interest for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Therefore in this study, SLNs and NLCs loaded fluconazole (FLZ) were prepared by solvent diffusion method in an aqueous system and characterized for different parameters. In addition, antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed albino rats. The results showed that SLNs and NLCs represent the respective mean particle sizes of approx. 178 and 134 nm with encapsulation efficiency of 75.7±4.94% and 81.4±3.89%, respectively. The skin-retention studies of FLZ from in vitro and in vivo experiments revealed significantly higher accumulation of drug in the case of NLCs formulation. The in vivo cumulative amount of FLZ retention from NLCs was more than 5-fold that of the plain solution, while it was 3.3-fold more in the case of an equivalent-dose application in the form of SLNs at 12h after administration. The antifungal study also confirmed the maximum therapeutic efficacy of NLCs, as the lowest number of cfu/ml was recorded. It can be concluded from this study that NLCs provide a good skin targeting effect and may be a promising carrier for topical delivery of FLZ offering the sustained release and maintain the localized effect, resulting in an effective treatment of a life-threatening cutaneous fungal infection.
纳米颗粒载体系统,如固体脂质纳米粒 (SLN) 和纳米结构化脂质载体 (NLC),因其能够促进载药穿透皮肤而引起了人们对治疗皮肤相关真菌感染的兴趣。因此,在本研究中,通过溶剂扩散法在水相体系中制备了负载氟康唑 (FLZ) 的 SLN 和 NLC,并对其进行了不同参数的表征。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,SLN 和 NLC 的平均粒径分别约为 178nm 和 134nm,包封效率分别为 75.7±4.94%和 81.4±3.89%。体外和体内实验的 FLZ 皮肤保留研究表明,NLC 制剂中药物的积累明显更高。NLC 制剂中 FLZ 的体内累积量是普通溶液的 5 倍以上,而以 SLN 形式给予等效剂量时,12h 后体内累积量是普通溶液的 3.3 倍。抗真菌研究也证实了 NLC 的最大治疗效果,因为记录到的 cfu/ml 数量最少。综上所述,NLC 提供了良好的皮肤靶向效果,可能是 FLZ 局部给药的有前途的载体,能够实现药物的持续释放和维持局部作用,从而有效治疗危及生命的皮肤真菌感染。