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Abstract #81169 Published in IGR 20-3
Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment
Gómez-Ballesteros M; López-Cano JJ; Bravo-Osuna I; Herrero-Vanrell R; Molina-Martínez ITPolymers 2019; 11:
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 AUC of the ACZ-LP-P was 1.5-fold higher than of ACZ-LP ( < 0.001) and the maximum hypotensive effect resulted in 1.4-fold higher ( < 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.
Complutense University, Innovation, Therapy and Pharmaceutical Development in Ophthalmology (InnOftal) Research Group, UCM 920415, Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Plaza Ramón y Cajal s/n, Madrid 28040, Spain. mgballesteros@farm.ucm.es.
Full articleClassification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)