Bioactive Molecules Research Laboratory, Faculty of Sciences, Lebanese University, Lebanon; Laboratoire d'Automatique, de Génie des Procédés et de Génie Pharmaceutique (LAGEPP), Université Claude Bernard Lyon 1, France.
Bioactive Molecules Research Laboratory, Faculty of Sciences, Lebanese University, Lebanon.
Int J Pharm. 2020 Nov 15;589:119721. doi: 10.1016/j.ijpharm.2020.119721. Epub 2020 Aug 3.
Despite the high aqueous solubility of cysteamine, its unpleasant organoleptic properties, hygroscopicity, instability in solutions, and poor pharmacokinetic profile are the main drawbacks that limit its use for medical and cosmetic purposes. In this study, cysteamine-loaded liposomes were prepared using the ethanol injection method. Liposomes were characterized for their size, homogeneity, surface charge, and morphology. The incorporation ratios of cholesterol and phospholipids, the encapsulation efficiency and the loading ratio of cysteamine in liposomes were determined. Moreover, the stability of free and encapsulated cysteamine was assessed at different temperatures (4, 25, and 37 °C) in the presence and absence of light. Cysteamine-loaded liposomes were freeze-dried and reconstituted liposomes were characterized. Finally, the storage stability of the freeze-dried cysteamine-loaded liposomes was studied. Liposomes were nanometric, oligolamellar, and spherical. The encapsulation efficiency and the loading ratio of cysteamine varied between 12 and 40% in the different formulations. The encapsulation improved the stability of cysteamine in the various storage conditions. The dried form of cysteamine-loaded liposomes conserved the size of the vesicles and retained 33% of cysteamine present in the liposomal suspension before lyophilization. The freeze-dried liposomes formulations were stable after four months of storage at 4 °C.
尽管半胱胺的水溶性很高，但它具有令人不快的感官特性、吸湿性、溶液不稳定性和不良的药代动力学特性，这些都是限制其在医疗和美容用途的主要缺点。在本研究中，使用乙醇注入法制备了载半胱胺的脂质体。对脂质体的粒径、均一性、表面电荷和形态进行了表征。测定了胆固醇和磷脂的包封比、包封效率和脂质体中半胱胺的载药量。此外，在有光和无光的情况下，分别在 4、25 和 37°C 下评估了游离和包封的半胱胺的稳定性。对半胱胺载脂质体进行了冷冻干燥，并对重构的脂质体进行了表征。最后，研究了冷冻干燥的半胱胺载脂质体的储存稳定性。脂质体为纳米级、寡层和球形。不同配方的半胱胺包封效率和载药量在 12%至 40%之间变化。包封提高了半胱胺在各种储存条件下的稳定性。载半胱胺脂质体的干燥形式保持了囊泡的大小，并在冻干前保留了脂质体悬浮液中存在的 33%的半胱胺。在 4°C 下储存四个月后，冻干的脂质体配方稳定。
