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Recent Patents on Drug Delivery & Formulation

Editor-in-Chief

ISSN (Print): 1872-2113
ISSN (Online): 2212-4039

New Mucoadhesive Polymeric Film for Ophthalmic Administration of Acetazolamide

Author(s): Luis I. Tartara, Santiago D. Palma, Daniel Allemandi, Maria I. Ahumada and Juan M. Llabot

Volume 8, Issue 3, 2014

Page: [224 - 232] Pages: 9

DOI: 10.2174/1872211308666140908121632

Price: $65

Abstract

This article reports the results concerning the design and manufacture of a novel polymeric film for ocular administration of acetazolamide (AZM), and a patent document presented to INPI- National Institute of Industrial/Intelectual Property. The system was designed using mucoadhesive polymers, such as carbomer (CB974P) and sodium carboxymethylcellulose (NaCMC), combined with the poloxamer (POL407) which behaves as a swelling modulator, surfactant and slightly plasticizer. The maximum amount of AZM to be incorporated without loss of homogeneity or precipitation of the drug, was 0.04 mg AZM/mg of the film. The addition of a polymeric coating based on Eudragit RSPO (cationic permeable polymethacrylate polymer) allowed optimizing drug release. The coating in a proportion of 10% (determined as percentage of total weight of the film) seemed to be the most adequate, since 80% of controlled drug release was achieved along 240 minutes. This coating membrane did not affect the mucoadhesive properties of the swellable polymers. Thus, the system obtained, showed good efficiency and the intra ocular pressure (IOP) decreased according to the results derived from in vivo studies performed on normotensive rabbits. Finally, irritation scored studies demonstrated that these systems were not irritant for rabbit´s ocular mucosa.

Keywords: Acetazolamide, bioadhesive films, glaucoma, ophthalmic delivery.


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