含有他克莫司的主动天然油基纳米乳剂，具有协同的抗银屑病疗效。
Active natural oil-based nanoemulsion containing tacrolimus for synergistic antipsoriatic efficacy.
机构信息
Department of Pharmaceutics, Centre for Pharmaceutical Nanotechnology, National Institute of Pharmaceutical Education & Research, Sector 67 SAS Nagar, Punjab - 160 062, India.
出版信息
Nanomedicine (Lond). 2018 Aug;13(16):1985-1998. doi: 10.2217/nnm-2018-0135. Epub 2018 Sep 6.
AIM
The current study is emphasized on development of a nanoemulsion system that simultaneously delivers two antipsoriatic agents viz. Tacrolimus and Kalonji oil (functional excepient) topically.
MATERIALS & METHODS: A nanoemulsion was characterized for quality attributes; a nanoemulsion gel was evaluated for spreadability, viscosity, dermal bioavailability, and in vitro efficacy in A-431 cell line, and so forth. In vivo performance was evaluated on psoriasis model in BALB/c mice.
RESULTS
Nanoemulsion depicted droplet size: 93.37 ± 2.58 nm with PDI (Polydispersity Index) 0.330 ± 0.025. The nanoemulsion gel exhibited desirable spreadability with sustained release pattern (biphasic). Dermal bioavailability enhancement (4.33-fold) accompanied significant in vitro results. A significant reduction in serum cytokines and improvement in psoriatic condition was achieved in vivo, indicating formulation efficacy compared with marketed formulation (Tacroz Forte, Glenmark Pharmaceuticals Ltd, Maharashtra, India).
CONCLUSION
Nanoemulsion gel thus provides an effective alternative for psoriasis treatment.
目的
本研究强调开发一种纳米乳系统，该系统可同时局部递送达普卢利沙星和卡隆吉油（功能性赋形剂）这两种治疗银屑病的药物。
材料与方法
对纳米乳进行了质量属性的特征描述；对纳米乳凝胶的铺展性、黏度、皮肤生物利用度和在 A-431 细胞系中的体外功效等进行了评价。在 BALB/c 小鼠的银屑病模型中评价了体内性能。
结果
纳米乳的粒径为 93.37±2.58nm，PDI（多分散指数）为 0.330±0.025。纳米乳凝胶表现出良好的铺展性和持续释放模式（两相）。皮肤生物利用度提高了 4.33 倍，体外结果显著。与市售制剂（印度马哈拉施特拉邦 Glenmark 制药有限公司的他克莫司乳膏）相比，体内试验能显著降低血清细胞因子水平并改善银屑病状况，表明该制剂具有疗效。
结论
纳米乳凝胶为治疗银屑病提供了一种有效的替代方案。
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