Dept. Scienze della Vita e dell'Ambiente, Sezione Scienzedel Farmaco, University of Cagliari, CNBS, via Ospedale 72, Cagliari, Italy.
Eur J Pharm Biopharm. 2012 Oct;82(2):352-9. doi: 10.1016/j.ejpb.2012.06.015. Epub 2012 Aug 13.
In this work, we focused on how composition and preparation method of vesicles might affect their morphological features and delivery performances. Penetration Enhancer-containing Vesicles, PEVs, vesicles containing a water miscible penetration enhancer (Transcutol® P; 10%, 20%, 30% v/v) and encapsulating diclofenac sodium, were formulated and compared with conventional liposomes. A cheap and unpurified commercial mixture of phospholipids, fatty acids, and triglycerides (Phospholipon® 50) was used, and the effects of this heterogeneous composition (along with the presence or absence of transcutol and the production method) on vesicle morphology, size, surface charge, drug loading, and stability were investigated. The variations in vesicle structure, bilayer thickness, and number of lamellae were assessed by TEM and Small and Wide Angle X-ray Scattering, which also proved the liquid state of the vesicular bilayer. Further, vesicles were evaluated for ex vivo (trans)dermal delivery, and their mode of action was studied performing a pre-treatment test and confocal laser scanning microscopy analyses. Results showed the formation of multi- and unilamellar vesicles that provided improved diclofenac delivery to pig skin, influenced by vesicle lipid composition and structure. Images of the qualitative CLSM analyses support the conclusion that PEVs enhance drug transport by penetrating intact the stratum corneum, thanks to a synergic effect of vesicles and penetration enhancer.
在这项工作中，我们专注于囊泡的组成和制备方法如何影响其形态特征和传递性能。载药囊泡（PEV）是指含有水混溶性渗透增强剂（Transcutol® P；10%、20%、30%v/v）并包载双氯芬酸钠的囊泡，与传统脂质体进行了比较。我们使用了一种廉价且未纯化的商业混合物磷脂、脂肪酸和甘油三酯（Phospholipon® 50），并研究了这种不均匀组成（以及是否存在 Transcutol 和生产方法）对囊泡形态、大小、表面电荷、载药量和稳定性的影响。TEM 和小角和广角 X 射线散射评估了囊泡结构、双层厚度和层片数的变化，这也证明了囊泡双层的液态。此外，还评估了囊泡用于离体（透皮）给药的性能，并通过预处理试验和共聚焦激光扫描显微镜分析研究了其作用模式。结果表明，形成了多和单室囊泡，这改善了双氯芬酸钠向猪皮的传递，这受到囊泡脂质组成和结构的影响。定性 CLSM 分析的图像支持这样的结论，即载药囊泡通过协同作用增强药物穿透完整的角质层来增强药物输送。
