Xu D H, Zhang Q, Feng X, Xu X, Liang W Q
Department of Pharmacy, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, PR China.
Pharmazie. 2007 Apr;62(4):316-8.
The purpose of this study was to investigate the effects of ethosomes, chemical enhancers and their binary combination on the in vitro permeability enhancement of naloxone through human skin. Franz diffusion cells were used for the percutaneous absorption studies. Propylene glycol (PG), N,N-dimethyl formamide (N,N-DMF), N,N-dimethyl acetamide (N,N-DMA), dimethyl sulfoxide (DMSO), Azone and polyethylene glycol 400 (PEG400), were chosen as the chemical enhancers. Naloxone ethosomes showed 11.68 times increase in steady-state flux compared to phosphate buffered solution (PBS). Ethosomes in combination with chemical enhancers synergistically increased (p < 0.05) in vitro flux of naloxone. Azone 3% + PG7% pretreated in ethosomal form dramatically enhanced the skin permeation of naloxone in vitro compared with ethosomes (steady-state flux: 96.75 +/- 5.70 microg x cm(-2) x h(-1) vs 20.56 +/- 1.67 microg x cm(-2) x h(-1)). Ethosomal carrier and enhancers accumulated in the skin after 24 h were greater than that of PBS.
本研究的目的是考察醇质体、化学渗透促进剂及其二元组合对纳洛酮经人皮肤体外渗透增强作用的影响。采用Franz扩散池进行经皮吸收研究。选择丙二醇（PG）、N，N - 二甲基甲酰胺（N，N - DMF）、N，N - 二甲基乙酰胺（N，N - DMA）、二甲基亚砜（DMSO）、氮酮和聚乙二醇400（PEG400）作为化学渗透促进剂。与磷酸盐缓冲溶液（PBS）相比，纳洛酮醇质体的稳态通量增加了11.68倍。醇质体与化学渗透促进剂联合使用可协同增加（p < 0.05）纳洛酮的体外通量。与醇质体相比，3%氮酮 + 7% PG以醇质体形式预处理后可显著增强纳洛酮的体外皮肤渗透（稳态通量：96.75±5.70μg·cm⁻²·h⁻¹对20.56±1.67μg·cm⁻²·h⁻¹）。24小时后，醇质体载体和渗透促进剂在皮肤中的蓄积量大于PBS。
