Manconi Maria, Valenti Donatella, Sinico Chiara, Lai Francesco, Loy Giuseppe, Fadda Anna M
Dipartimento Farmaco Chimico Tecnologico, Via Ospedale 72, 09124 Cagliari, Italy.
Int J Pharm. 2003 Jul 24;260(2):261-72. doi: 10.1016/s0378-5173(03)00268-0.
In this work, we compared the chemical stability of tretinoin (TRA) in methanol and in vesicular suspensions exposed both to UV and artificial daylight conditions with the aim of evaluating the potential of niosomes as topical carriers capable of improving the stability of photosensitive drugs. Tretinoin-loaded niosomes were prepared from polyoxyethylene (4) lauryl ether (Brij 30), sorbitan esters (Span 40 and Span 60) and a commercial mixture of octyl/decyl polyglucosides (Triton CG110). Liposomes made from hydrogenated (P90H) and non-hydrogenated (P90) soy phosphatidylcholines were also prepared and studied. In order to evaluate the influence of vesicle structure on the photostability of tretinoin, TRA-loaded vesicles were prepared by the film hydration method, extrusion technique and sonication. After UV irradiation, TRA dissolved in methanol degraded very quickly while the incorporation in vesicles always led to a reduction of the photodegradation process. The photoprotection offered by vesicles varied depending on the vesicle structure and composition. After fluorescent light irradiation for 21 days, not all the studied vesicular formulations improved TRA stability when compared with the free drug in methanol. Tretinoin incorporated in P90 or Span vesicles presented a half-life shorter or very close to that of the free drug. However, the inclusion of TRA in P90H liposomes and Brij 30 or Triton CG110 niosomes retarded the drug photodegradation.
在本研究中,我们比较了维甲酸(TRA)在甲醇中以及在同时暴露于紫外线和人工日光条件下的囊泡悬浮液中的化学稳定性,目的是评估非离子型脂质体作为能够提高光敏药物稳定性的局部载体的潜力。负载维甲酸的非离子型脂质体由聚氧乙烯(4)月桂醚(Brij 30)、脱水山梨醇酯(Span 40和Span 60)以及辛基/癸基聚葡糖苷的商业混合物(Triton CG110)制备而成。还制备并研究了由氢化大豆磷脂酰胆碱(P90H)和非氢化大豆磷脂酰胆碱(P90)制成的脂质体。为了评估囊泡结构对维甲酸光稳定性的影响,通过薄膜水化法、挤压技术和超声处理制备了负载TRA的囊泡。紫外线照射后,溶解在甲醇中的TRA降解非常迅速,而包封在囊泡中总是会导致光降解过程减缓。囊泡提供的光保护作用因囊泡结构和组成而异。荧光照射21天后,与甲醇中的游离药物相比,并非所有研究的囊泡制剂都能提高TRA的稳定性。包封在P90或Span囊泡中的维甲酸的半衰期比游离药物短或非常接近游离药物的半衰期。然而,将TRA包封在P90H脂质体以及Brij 30或Triton CG110非离子型脂质体中会延缓药物的光降解。