Gelatinized core liposomes: A new Trojan horse for the development of a novel timolol maleate glaucoma medication

Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Rania M. Hathout, Heba A. Gad, Salma M. Abdel-Hafez, Naira Nasser, Noha Khalil, Toka Ateyya, Alaa Amr, Nesreen Yasser, Sandy Nasr, Abdelkader A. MetwallyAbstractGlaucoma treatment with ocular medications requires overcoming the corneal barrier to drug penetration. Liposomes have a great corneal penetration ability and affinity while suffering from poor stability and low entrapment of hydrophilic drugs accompanied by rapid drug release. This work aims to develop a new, effective and stable glaucoma medication with sustained drug release properties; Timolol maleate gelatinized core liposomes. A full factorial design was utilized to study the effects of three formulation variables on drug loading and vesicle particle size. Vesicles were prepared by the thin-film hydration method, and characterized for in-vitro drug release and stability. Intra-ocular pressure (IOP) reduction was evaluated in-vivo on glaucomatous rabbit’s eyes. The safety profile was assessed using histolopthological examinations. Gelatin significantly increased the drug entrapment percentage reaching 50% with a particle size of 38.81 µm. Sustained drug release was recorded compared to a marketed product and to a conventional liposomal formulation. The prepared vesicles caused the highest reduction in IOP accompanied by safe histological findings. This work provided a new, safe and effective ocular gluca...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research