Spiclin Polona, Homar Miha, Zupancic-Valant Andreja, Gasperlin Mirjana
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000, Ljubljana, Slovenia.
Int J Pharm. 2003 Apr 30;256(1-2):65-73. doi: 10.1016/s0378-5173(03)00063-2.
Sodium ascorbyl phosphate is a hydrophilic derivative of ascorbic acid, which has improved stability arising from its chemical structure. It is used in cosmetic and pharmaceutical preparations since it has many favorable effects in the skin, the most important being antioxidant action. In order to achieve this, it has to be converted into free ascorbic acid by enzymatic degradation in the skin. In the present work, o/w and w/o microemulsions composed of the same ingredients, were selected as carrier systems for topical delivery of sodium ascorbyl phosphate. We showed that sodium ascorbyl phosphate was stable in both types of microemulsion with no significant influence of its location in the carrier system. To obtain liquid microemulsions appropriate for topical application, their viscosity was increased by adding thickening agents. On the basis of rheological characterization, 4.00% (m/m) colloidal silica was chosen as a suitable thickening agent for w/o microemulsions and 0.50% (m/m) xanthan gum for the o/w type. The presence of thickening agent and the location of sodium ascorbyl phosphate in the microemulsion influenced the in vitro drug release profiles. When incorporated in the internal aqueous phase, sustained release profiles were observed. This study confirmed microemulsions as suitable carrier systems for topical application of sodium ascorbyl phosphate.
抗坏血酸钠磷酸酯是抗坏血酸的一种亲水性衍生物,因其化学结构而具有更高的稳定性。它用于化妆品和药物制剂,因为它在皮肤方面有许多有益作用,其中最重要的是抗氧化作用。为了实现这一点,它必须在皮肤中通过酶降解转化为游离抗坏血酸。在本研究中,选择由相同成分组成的水包油型和油包水型微乳作为抗坏血酸钠磷酸酯局部给药的载体系统。我们发现抗坏血酸钠磷酸酯在两种类型的微乳中均稳定,其在载体系统中的位置对其无显著影响。为了获得适合局部应用的液体微乳,通过添加增稠剂来增加其粘度。基于流变学表征,选择4.00%(m/m)的胶体二氧化硅作为油包水型微乳的合适增稠剂,0.50%(m/m)的黄原胶作为水包油型微乳的合适增稠剂。增稠剂的存在以及抗坏血酸钠磷酸酯在微乳中的位置影响体外药物释放曲线。当它被包封在内相水相中时,观察到缓释曲线。本研究证实微乳是抗坏血酸钠磷酸酯局部应用的合适载体系统。