Ma Man, Wang Jinping, Guo Fang, Lei Mingzhu, Tan Fengping, Li Nan
Tianjin Key Laboratory of Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, 300072, People's Republic of China.
J Mater Sci Mater Med. 2015 Jun;26(6):191. doi: 10.1007/s10856-015-5524-1. Epub 2015 May 20.
The aim of the current investigation was to develop and statistically evaluate nanovesicular systems for dermal imiquimod delivery. To this purpose, transethosomes were prepared with phospholipid, ethanol and different permeation enhancers. Conventional ethosomes, with soy phospholipid and ethanol, were used as control. The prepared vesicles were characterized for size, zeta potential, stability and entrapment efficiency. The optimal transethosomal formulation with mean particle size of 82.3 ± 9.5 nm showed the higher entrapment efficiency (68.69 ± 1.7%). In vitro studies, permeation results of accumulated drug and local accumulation efficiency were significantly higher for transethosomes (24.64 µg/cm(2) and 6.70, respectively) than control (14.45 µg/cm(2) and 3.93, respectively). Confocal laser scanning microscopy of rhodamine 6G-loaded transethosomes revealed an enhanced retention into the deeper skin layers as compared to conventional ethosomes. Besides, Fourier-transform infra-red spectroscopy studies were also performed to understand the mechanism of interaction between skin and carriers. What's more, results of in vivo studies indicated the transethosomes of imiquimod providing the most effectiveness for dermal delivery among all of the formulations. These results suggested that transethosomes would be a promising dermal carrier for imiquimod in actinic keratose treatment.
本研究的目的是开发用于皮肤递送咪喹莫特的纳米囊泡系统并进行统计学评估。为此，用磷脂、乙醇和不同的渗透促进剂制备了传递体。以大豆磷脂和乙醇制备的传统醇质体作为对照。对制备的囊泡进行了粒径、zeta电位、稳定性和包封率的表征。平均粒径为82.3±9.5 nm的最佳传递体制剂显示出较高的包封率（68.69±1.7%）。体外研究中，传递体的累积药物渗透结果和局部累积效率（分别为24.64 µg/cm²和6.70）显著高于对照（分别为14.45 µg/cm²和3.93）。对负载罗丹明6G的传递体进行共聚焦激光扫描显微镜观察发现，与传统醇质体相比，其在皮肤深层的滞留增强。此外，还进行了傅里叶变换红外光谱研究以了解皮肤与载体之间的相互作用机制。更重要的是，体内研究结果表明，在所有制剂中，咪喹莫特传递体在皮肤递送方面最有效。这些结果表明，传递体将是光化性角化病治疗中咪喹莫特的一种有前景的皮肤载体。
