Improvement of acetazolamide ocular permeation using ascorbyl laurate nanostructures as drug delivery system.

TÁRTARA I.; QUINTEROS D.; SAINO V.; ALLEMANDI D.; PALMA S.

MARY ANN LIEBERT INC

Lugar: Nueva York; Año: 2012 vol. 28 p. 102 - 102

urpose: To evaluate the performance of 6-O-Lauryl?l-ascorbic acid nanostructures (coagels) as vehicles for acetazolamide (AZM) in ophthalmic administration by in vitro and in vivo experimental tests. Methods: The systems of coagel + AZM were evaluated in terms of their in vitro release (dialysis membrane), permeability (isolated cornea), pharmacological effectiveness [intraocular pressure (IOP)-reduction in normotensive rabbits], and potential irritant effects. Results: The results concerning AZM permeation were better when vehiculized in coagels compared with ringer solution, which was evident from the AZM steady-state flux and Papp values (J=1.43 μg/min and Papp=3.04 cm.s1). As a consequence of this increase in permeation, the coagel-AZMs were more effective in lowering the IOP, according to the results obtained from the in vivo assays. Coagels loaded with 0.4% (W/W) of AZM showed a higher hypotensive effect in rabbits compared with the commercial formulation AZOP