title: Probing influence of methodological variation on active loading of acetazolamide into nanoliposomes: biophysical, in vitro, ex vivo, in vivo and rheological investigation.
abstract: In the present work comparative evaluation of acetate and pH gradient techniques for effective drug loading in liposomes has been investigated. The acetazolamide (ACZ) loaded liposomes prepared by two methods were analyzed by vesicle size analysis, zeta potential, percent encapsulation efficiency, in vitro drug release studies and intraocular pressure lowering activity. ICH guidelines were followed for determining stability of the prepared liposomes. The superiority of acetate gradient method for active loading of acetazolamide has been established. The prepared acetate gradient positive liposomes showed extended hypotensive effect when compared to other liposomal formulations. Thus ACZ loaded liposomes prepared by acetate gradient technique may serve as promising ocular delivery system in the treatment of glaucoma. The current work emphasizes the fact that the techniques used for active drug loading into liposomes strongly influence the pharmaceutical performance of the final formulation.
authors.affiliation: Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune 411038, Maharashtra, India.
authors.forename: Prashant B
authors.initials: PB
authors.lastname: Pisal
authors.affiliation: Sai Life Sciences Ltd, Pune 411057, Maharashtra, India.
authors.forename: Manjusha A
authors.initials: MA
authors.lastname: Joshi
authors.affiliation: Sai Life Sciences Ltd, Pune 411057, Maharashtra, India.
authors.forename: Mahesh N
authors.initials: MN
authors.lastname: Padamwar
authors.affiliation: Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune 411038, Maharashtra, India.
authors.forename: Sharvil S
authors.initials: SS
authors.lastname: Patil
authors.affiliation: Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Department of Pharmaceutics, Erandwane, Pune 411038, Maharashtra, India. Electronic address: vbpokharkar@yahoo.co.in.
authors.forename: Varsha B
authors.initials: VB
authors.lastname: Pokharkar
mesh_terms: D000086:Acetazolamide / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D060433:Administration, Ophthalmic; D000818:Animals; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D004355:Drug Stability; D005901:Glaucoma / Q000188:drug therapy / Q000503:physiopathology; D007429:Intraocular Pressure / Q000187:drug effects*; D008081:Liposomes; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D011817:Rabbits; D012212:Rheology
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D008081:Liposomes; D000086:Acetazolamide
keywords: Acetazolamide; Encapsulation efficiency; Glaucoma; Gradient liposomes; Intra-ocular pressure