Department of Pharmaco-Chemical Technology, University of Cagliari, Cagliari, Italy.
J Liposome Res. 2010 Dec;20(4):269-76. doi: 10.3109/08982100903402962. Epub 2009 Dec 3.
A comparative study between archaeosomes, lipid lamellar vesicles made from archaea polar lipids, and conventional phospholipids liposomes was carried out, aiming at evaluating the properties and the potential of archaeosomes as novel colloidal carriers for effective drug delivery to the skin. Betamethasone dipropionate (BMD)-loaded archaeosomes and conventional liposomes were prepared by the thin-lipid film and sonication procedures, using, respectively, archaeal lipids extracted from archaea Halobacterium salinarum and enriched soy phosphatidylcholine. Vesicular formulations were characterized by assessing vesicle size, zeta potential, incorporation efficiency, and morphology. In order to investigate the effect of the incorporation in the two different colloidal carrier systems on the (trans)dermal delivery of BMD, in vitro drug permeation studies through full-thickness pig skin were carried out by using Franz diffusion vertical cells by testing both archaeal and liposomal dispersions. Interestingly, archaeosomes appeared to be the most effective carriers for the model drug, achieveing a major drug penetration and accumulation in the skin strata, especially in the epidermis. This can, presumably, be due to the enhanced archaeosomal bilayer fluidity, as indicated by the rheological studies that provided insight into the viscoelastic properties of all the studied systems. The available data suggest that suitably developed archaeosomes may hold great promise as delivery vehicles for topical applications.
本研究对来自古生菌极性脂的类脂囊泡（archaeosomes）与传统脂质体（liposomal vesicles）进行了比较，旨在评估类脂囊泡作为新型胶体载体用于将药物有效递送至皮肤的特性和潜力。采用薄脂质膜法和超声处理法，分别用古生菌盐杆菌提取的古生菌脂和富含大豆卵磷脂的古生菌脂制备了载倍他米松二丙酸酯（BMD）的类脂囊泡和传统脂质体。通过测定囊泡粒径、zeta 电位、包封率和形态，对囊泡制剂进行了表征。为了研究将药物包裹于两种不同胶体载体系统对 BMD 经皮传递的影响，通过 Franz 扩散垂直细胞进行了体外全厚猪皮透皮实验，同时对类脂囊泡和脂质体混悬液进行了检测。有趣的是，类脂囊泡似乎是模型药物最有效的载体，可使药物在皮肤各层，尤其是表皮中实现更大的穿透和积累。这可能归因于流变学研究中观察到的类脂囊泡双层流动性增强，该研究深入了解了所有研究系统的粘弹性性质。现有数据表明，经过适当开发的类脂囊泡有望作为用于局部应用的递药载体。
