乙醇脂质体、二元醇脂质体及传递体对多奈哌齐经皮转运的对比性研究

目的:制备多奈哌齐乙醇脂质体、二元醇脂质体和传递体,并比较皮肤渗透性,从而进一步有效优化药物的经皮转运。方法:通过形态,粒径分布,Zeta电位值和包封率对多奈哌齐乙醇脂质体、二元醇脂质体及传递体进行了初步表征,运用Franz扩散池和共聚焦激光扫描电镜考察了3种囊泡的经皮转运情况。结果:当二元醇脂质体包封率最高(89.1±0.42)%时,乙醇-丙二醇=7∶3,且二元醇脂质体(乙醇-丙二醇为7∶3,W/W)在皮肤中24 h的累积渗透百分数分别是乙醇脂质体和传递体的3.9和5.4倍。结论:二元醇醇脂质体(乙醇-丙二醇为7∶3,W/W)时,有效地改善了药物在醇脂质体中的包封率,且显著增加的药物在皮肤中的累积量。

Comparison of ethosomes,binary ethosomes and transfersomes in the transdermal delivery of donepezil

OBJECTIVE To prepare donepezil ethosomes,binary ethosomes and transfersomes under non-occlusive conditions,and further optimize the transdermal delivery of donepezil.METHODS Ethosomes,binary ethosomes and transfersomes were prepared and characterized for shape,size and entrapment efficiency.Franz diffusion cells and confocal laser scanning microscopy (CLSM) were used for the percutaneous absorption studies.RESULTS The doses of drug in the skin (Q_s) from ethosomes and transfersomes were 3.9 and 5.4 times of that of donepezil from binary ethosomes (ethanol-PG=7:3,W/W).CONCLUSION The binary ethosomes (ethanol-PG=7:3,W/W) can markedly improve the EE and enhance drugs absorption into the skin.