Department of Health Sciences, University Magna Græcia of Catanzaro, Campus Universitario S. Venuta, Building of BioSciences, Viale S. Venuta, I-88100 Germaneto, Catanzaro, Italy.
J Control Release. 2012 Aug 20;162(1):143-51. doi: 10.1016/j.jconrel.2012.05.050. Epub 2012 Jun 12.
The potentiality of ultradeformable vesicles as a possible topical delivery system for asiaticoside, a natural compound obtained from Centella asiatica was evaluated, because this compound exhibits collagen biosynthesis promoting activity. Ultradeformable vesicles were prepared by the extrusion technique; these vesicles were composed of Phospholipon 100 and different molar fractions of sodium cholate as the edge activator. The physicochemical properties of the ultradeformable vesicles were investigated through differential scanning calorimetry and light scattering techniques. The potential cyctotoxicity and biological activity of asiaticoside-loaded ultradeformable vesicles were evaluated on primary human dermal fibroblast cells by determining the extracellular lactic dehydrogenase activity, the cellular viability and the biosynthetic production of collagen. In vitro permeation experiments through human stratum corneum and epidermis membranes were also carried out. Ultradeformable vesicles having sodium cholate molar fraction of 0.2 proved to be the most suitable topical carriers for asiaticoside. A sodium cholate content of >0.2 was observed to be cytotoxic probably due to its co-existence with other lipid aggregates, an example being mixed micelles. Asiaticoside-loaded ultradeformable vesicles with a sodium cholate molar fraction of 0.2 elicited the greatest degree of collagen biosynthesis in human fibroblasts. Ultradeformable vesicles provided the greatest in vitro skin permeation of asiaticoside showing a 10-fold increase with respect to the free drug solution and favoured an increase in in vivo collagen biosynthesis. Ultradeformable vesicles are therefore suitable carriers for the pharmaceutical and cosmetic application of the natural agent asiaticoside.
超变形囊泡作为一种可能的局部递药系统用于积雪草苷的潜力被评估，因为这种化合物具有促进胶原蛋白生物合成的活性。超变形囊泡通过挤出技术制备；这些囊泡由磷脂 100 和不同摩尔分数的胆酸钠作为边缘活性剂组成。通过差示扫描量热法和光散射技术研究了超变形囊泡的理化性质。通过测定细胞外乳酸脱氢酶活性、细胞活力和胶原蛋白的生物合成来评估载有积雪草苷的超变形囊泡对原代人真皮成纤维细胞的潜在细胞毒性和生物活性。还进行了体外通过人角质层和表皮膜的渗透实验。摩尔分数为 0.2 的胆酸钠的超变形囊泡被证明是最适合积雪草苷的局部载体。观察到超过 0.2 的胆酸钠含量具有细胞毒性，可能是由于其与其他脂质聚集体共存，例如混合胶束。摩尔分数为 0.2 的胆酸钠载有积雪草苷的超变形囊泡在人成纤维细胞中引起最大程度的胶原蛋白生物合成。超变形囊泡提供了积雪草苷的最大体外皮肤渗透，与游离药物溶液相比增加了 10 倍，并有利于体内胶原蛋白生物合成的增加。因此，超变形囊泡是积雪草苷这种天然药物在药物和化妆品应用中的合适载体。
