Department of Pharmaceutical Sciences, Calabria University, Ponte P. Bucci, Ed. Polifunzionale, 87030 Rende, Italy.
Colloids Surf B Biointerfaces. 2010 Jan 1;75(1):319-22. doi: 10.1016/j.colsurfb.2009.09.003. Epub 2009 Sep 8.
A commercial sucrose cocoate surfactant was used to obtain a new vesicular system for transdermal drug delivery. The preparation, the dimensional and morphological characterizations and the skin permeation profile of these new niosomes were evaluated. Moreover we studied the possible employment of mixture of sucrose cocoate and cholesterol at different weigh ratios for the vesicles preparation and we analyzed the influence of cholesterol on niosomes properties. Diclofenac and Sulfadiazine were used as model drugs. Results suggest that sucrose cocoate was able to form vesicles in the presence or not of cholesterol and the addition of cholesterol leads to a variation of size: larger vesicles were obtained in the absence of cholesterol both in empty and drug-loaded niosomes. All vesicles were spherical and regular in shape. In vitro skin permeation profiles were significantly higher than the free drug solution, indicating the favourable relations between skin and niosomes. The faster release of the drug was found for niosomes with no cholesterol or with a reduced amount of this membrane additive, in particular the optimal formulation was that in which the cholesterol content was about 27 wt% of total lipid amount: probably this value is a good compromise between the membrane stability and its deformation capacity, allowing a higher drug permeation across the skin.
一种商用蔗糖椰油酸酯表面活性剂被用于获得一种新的用于透皮给药的囊泡体系。评估了这些新的类脂囊泡的制备、尺寸和形态特征以及透皮渗透特性。此外，我们研究了蔗糖椰油酸酯和胆固醇以不同重量比混合用于囊泡制备的可能性，并分析了胆固醇对囊泡性质的影响。双氯芬酸和磺胺嘧啶被用作模型药物。结果表明，蔗糖椰油酸酯能够在有或没有胆固醇的情况下形成囊泡，并且胆固醇的添加导致了大小的变化：在没有胆固醇的情况下，无论是空囊泡还是载药囊泡，都得到了更大的囊泡。所有囊泡均呈球形且形状规则。体外皮肤渗透特性明显高于游离药物溶液，表明囊泡与皮肤之间存在有利关系。发现没有胆固醇或胆固醇添加量减少的囊泡中药物释放更快，特别是胆固醇含量约为总脂质量的 27wt%的最佳配方：这种值可能是在膜稳定性和变形能力之间的良好折衷，允许药物更有效地渗透皮肤。
