School of Pharmacy, The Queen's University of Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, United Kingdom.
Eur J Pharm Sci. 2012 Aug 15;46(5):315-22. doi: 10.1016/j.ejps.2012.02.003. Epub 2012 Feb 15.
Mucosally-administered vaccine strategies are widely investigated as a promising means of preventing HIV infection. This study describes the development of liposomal gel formulations, and novel lyophilised variants, comprising HIV-1 envelope glycoprotein, CN54gp140, encapsulated within neutral, positively charged or negatively charged liposomes. The CN54gp140 liposomes were evaluated for mean vesicle diameter, polydispersity, morphology, zeta potential and antigen encapsulation efficiency before being incorporated into hydroxyethyl cellulose (HEC) aqueous gel and subsequently lyophilised to produce a rod-shaped solid dosage form for practical vaginal application. The lyophilised liposome-HEC rods were evaluated for moisture content and redispersibility in simulated vaginal fluid. Since these rods are designed to revert to gel form following intravaginal application, mucoadhesive, mechanical (compressibility and hardness) and rheological properties of the reformed gels were evaluated. The liposomes exhibited good encapsulation efficiency and the gels demonstrated suitable mucoadhesive strength. The freeze-dried liposome-HEC formulations represent a novel formulation strategy that could offer potential as stable and practical dosage form.
黏膜给予疫苗策略被广泛研究，作为预防 HIV 感染的一种有前途的方法。本研究描述了包含 HIV-1 包膜糖蛋白 CN54gp140 的脂质体凝胶制剂和新型冻干变体的开发，所述 CN54gp140 被包裹在中性、正电荷或负电荷脂质体中。在将 CN54gp140 脂质体掺入羟乙基纤维素 (HEC) 水性凝胶中并随后冻干以产生用于实际阴道应用的棒状固体剂型之前，评估了 CN54gp140 脂质体的平均囊泡直径、多分散性、形态、Zeta 电位和抗原包封效率。评估了冻干脂质体-HEC 棒的水分含量和在模拟阴道液中的再分散性。由于这些棒旨在在阴道内应用后恢复凝胶形式，因此评估了重构凝胶的粘膜粘附性、机械（可压缩性和硬度）和流变学性质。脂质体表现出良好的包封效率，并且凝胶表现出合适的粘膜粘附强度。冻干脂质体-HEC 制剂代表了一种新的制剂策略，可能作为稳定且实用的剂型提供潜力。
