Agiba Ahmed M, Nasr Maha, Abdel-Hamid Sameh, Eldin Ahmed B, Geneidi Ahmed S
R&D Department, SIGMA Pharmaceutical Industries, 6 October, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Curr Drug Deliv. 2018;15(6):907-916. doi: 10.2174/1567201815666180123100148.
Liposomes are promising systems for the delivery of macromolecules and poorly absorbed drugs, owing to their ability to compartmentalize drugs, their biodegradability and biocompatibility.
The aim of the present study was to formulate and evaluate conventional and modified glucosamine sulphate (GluS) and chondroitin sulphate (CS) liposomal formulations, to enhance their oral permeation for the treatment of osteoarthritis (OA).
Liposomal formulations were prepared by the thin-film hydration method using two types of phospholipids; Epikuron 200© and Epikuron 200© SH, and three permeation enhancers; poloxamer 407, cetylpyridinium chloride, and sodium deoxycholate. In-vitro characterization of liposomal formulations was conducted in terms of entrapment efficiency, particle size, zeta potential, viscosity, physical stability and mucoadhesive strength. Surface morphology and vesicle shape, ex-vivo intestinal permeation, and histopathological studies were further carried out on the selected formulation.
Results showed that the liposomal formulation containing sodium deoxycholate was the most optimum formula, showing high entrapment efficiency (60.11% for GluS and 64.10% for CS) with a particle size of 4.40 µm, zeta potential of -17.2 mV and viscosity of 2.50 cP.
The aforementioned formula displayed the highest cumulative % permeated of GluS and CS through rabbit intestinal mucosa compared to the solution of drugs and other liposomal formulations (64.20% for GluS and 78.21% for CS) after 2 hours. There were no histopathological alterations in the intestinal tissue, suggesting the safety of the utilized liposomal formulation. In light of the above, liposomes can be considered promising oral permeation-enhancer system for GluS and CS, which is worthy of future bioavailability experimentation.
脂质体是用于递送大分子和吸收不良药物的有前景的系统，这归因于它们分隔药物的能力、生物可降解性和生物相容性。
本研究的目的是制备并评估常规和改良的硫酸葡萄糖胺（GluS）和硫酸软骨素（CS）脂质体制剂，以增强其口服渗透性用于骨关节炎（OA）的治疗。
采用薄膜水化法，使用两种磷脂（Epikuron 200©和Epikuron 200© SH）以及三种渗透促进剂（泊洛沙姆407、十六烷基吡啶氯化物和脱氧胆酸钠）制备脂质体制剂。从包封率、粒径、ζ电位、粘度、物理稳定性和粘膜粘附强度方面对脂质体制剂进行体外表征。对所选制剂进一步进行表面形态和囊泡形状、离体肠道渗透和组织病理学研究。
结果表明，含有脱氧胆酸钠的脂质体制剂是最优化的配方，显示出高包封率（GluS为60.11%，CS为64.10%），粒径为4.40 µm，ζ电位为-17.2 mV，粘度为2.50 cP。
与药物溶液和其他脂质体制剂相比，上述配方在2小时后通过兔肠粘膜的GluS和CS的累积渗透百分比最高（GluS为64.20%，CS为78.21%）。肠道组织没有组织病理学改变，表明所使用的脂质体制剂的安全性。鉴于上述情况，脂质体可被认为是用于GluS和CS的有前景的口服渗透增强系统，值得未来进行生物利用度实验。
