Enhanced in vitro release and permeability of glibenclamide by proliposomes: Development, characterization and histopathological evaluation

• Published in: Journal of drug delivery science and technology 2021-06, Vol.63, p.102450, Article 102450
• Main Authors: Khan, Safiullah, Madni, Asadullah, Rahim, Muhammad Abdur, Shah, Hassan, Jabar, Abdul, Khan, Muhammad Muzamil, Khan, Arshad, Jan, Nasrullah, Mahmood, Muhammad Ahmad
• Format: Article
• Language: English
• Subjects: Glibenclamide; In vitro drug dissolution; Liposomal gel; Liposomes; Vesicular drug delivery system
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2021.102450

Proliposomes (PLs) are smart provesicular drug delivery system regarding improvement in solubility, oral bioavailability, stability, and permeability of the therapeutic agents. In this study, glibenclamide (GLB) loaded PLs and liposomes for oral delivery, and liposomal gel for transdermal delivery of GLB has been developed. A slurry method was employed to fabricate PLs, followed by hydration and incorporation of gelling agent for liposomes and liposomal gel, respectively. The developed proliposomes (PLs) were dry, free-flowing (θ; 29.0°–37.1°) with optimum percentage yield (81–92%), entrapment efficiency (67.68–83.11%), compatibility, solid-state stability, and thermal stability. In addition, the liposomal formulations produced suitable vesicle size (510 nm–1436 nm), optimum colloidal stability and monodispersity, such that the optimized formulation (FGP-4) presented vesicle size of 510 ± 4 nm, zeta potential −11.5 ± 2.0 mV and PDI of 0.41 ± 0.06. The in vitro drug dissolution data showed the enhanced GLB release (>90% in 12 h) from the system. Moreover, the permeation studies revealed 2.27 folds enhanced permeability of liposomal gel (FGP-4 gel) compared to drug-loaded gel. An acute oral toxicity study utilizing Wistar rats revealed the safety of PLs. The developed PLs provided enhanced in vitro drug dissolution and liposomal gel provided improved ex vivo permeation. The GLB loaded PLs and liposomal gel may better control Diabetes Mellitus through oral and topical routes. [Display omitted]