Details

Autor(en) / Beteiligte

• Hathout, Rania M.
• Gad, Heba A.
• Abdel-Hafez, Salma M.
• Nasser, Nayera
• Khalil, Noha
• Ateyya, Toka
• Amr, Alaa
• Yasser, Nesreen
• Nasr, Sandy
• Metwally, Abdelkader A.

Titel

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

Ist Teil von

• International journal of pharmaceutics, 2019-02, Vol.556, p.192-199

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2019

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Gelatinized-core liposomes as a new Trojan horse for the development of a novel glaucoma medication. [Display omitted] Glaucoma 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 histopathological 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 glaucoma medication; Timolol maleate gelatinized core liposomes, solving the main problems of ocular liposomal formulations of hydrophilic drugs, suitable for the pharmaceutical industry and comprising abundant and relatively cheap components.