乙醇脂质体对多奈哌齐经皮转运的促进作用

Synergistic Penetration Enhancement Effect of Ethosomes Prodrug on the Transdermal Delivery of Donepezil

目的制备多奈哌齐乙醇脂质体,进一步优化有效药物的经皮转运。方法采用注入法制备多奈哌齐乙醇脂质体;通过形态,粒径分布和包封率对乙醇脂质体进行了初步表征,运用Franz扩散池和共聚焦激光扫描电镜考察乙醇脂质体的经皮转运情况。结果多奈哌齐乙醇脂质体(乙醇含量45%)包封率明显高于多奈哌齐脂质体;多奈哌齐乙醇脂质体透皮量分别为脂质体及乙醇溶液的3倍和1.6倍。结论乙醇脂质体可有效携带药物进入皮肤深层。

OBJECTIVE To prepare donepezil ethosomes, and further optimize the transdermal delivery of drugs. METHODS Infusing method was used to prepare donepezil ethosomes. The systems were characterized for shape, particle size and entrapment efficiency（EE）. Franz diffusion cells and confocal laser scanning microscopy were used for the percutaneous absorption studies. RESULTS The EE of donepezil ethosomes（ethanol content 45%） were much higher than that of liposome. The percentage of the drug in ethosomes retained by isolated skin were 3 and 1.6 times higher than liposomes and hydroalcoholic solution. CONCLUSION Ethosomes may be able to enhance the permeation of donepezil into skin.