New mucoadhesive polymeric film for ophthalmic administration of acetazolamide

L. TÁRTARA, ; S. PALMA; ALLEMANDI D; LLABOT JM

Recent Patents on Drug Delivery & Formulation

Bentham

Año: 2014 vol. 8 p. 224 - 232

1872-2113

Results concerning the design and manufacture of a novel polymeric film for ocular administration of acetazolamide (AZM) are reported in this article. Also, a patent document was presented in 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 and plasticizer. The amount of AZM able to be incorporated without loss of homogeneity or precipitation of the drug was 0.04 mg AZM / mg of 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 a controlled drug release of about 80% was achieved along 240 minutes. This coating membrane did not affect the mucoadhesive properties of the swellable polymers. The system thus 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 irritants for rabbit ocular mucosa.