Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment



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Gómez Ballesteros, Miguel and López Cano, José Javier and Bravo Osuna, Irene and Herrero Vanrell, Rocío and Molina Martínez, Irene Teresa (2019) Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment. Polymers, 11 (6). p. 929. ISSN 2073-4360

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Official URL: https://doi.org/10.3390/polym11060929


The combination of acetazolamide-loaded nano-liposomes and Hydroxypropyl methylcellulose (HPMC) with similar components to the preocular tear film in an osmoprotectant media (trehalose and erythritol) is proposed as a novel strategy to increase the ocular bioavailability of poorly soluble drugs. Ophthalmic formulations based on acetazolamide-loaded liposomes, dispersed in the osmoprotectant solution (ACZ-LP) or in combination with HPMC (ACZ-LP-P) were characterized and in vivo evaluated. The pH and tonicity of both formulations resulted in physiological ranges. The inclusion of HPMC produced an increment in viscosity (from 0.9 to 4.7 mPa·s. 64.9 ± 2.6% of acetazolamide initially included in the formulation was retained in vesicles. In both formulations, a similar onset time (1 h) and effective time periods were observed (7 h) after a single instillation (25 µL) in normotensive rabbits’ eyes. The AUC0–8h of the ACZ-LP-P was 1.5-fold higher than of ACZ-LP (p < 0.001) and the maximum hypotensive effect resulted in 1.4-fold higher (p < 0.001). In addition, the formulation of ACZ in the hybrid liposome/HPMC system produced a 30.25-folds total increment in ocular bioavailability, compared with the drug solution. Excellent tolerance in rabbits’ eyes was confirmed during the study.

Item Type:Article
Uncontrolled Keywords:Liposomes; HPMC; glaucoma; acetazolamide; ocular tolerance; intraocular pressure
Subjects:Medical sciences > Medicine > Ophtalmology
Medical sciences > Pharmacy > Pharmacology
ID Code:62950
Deposited On:04 Nov 2020 11:13
Last Modified:18 Nov 2020 10:18

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