Ocular administration of acetazolamide microsponges in situ gel formulations.

Autor: Obiedallah MM; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt., Abdel-Mageed AM; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt., Elfaham TH; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Jazyk: angličtina
Zdroj: Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society [Saudi Pharm J] 2018 Nov; Vol. 26 (7), pp. 909-920. Date of Electronic Publication: 2018 Sep 24.
DOI: 10.1016/j.jsps.2018.01.005
Abstrakt: In the present work, the antiglaucoma drug, acetazolamide, was formulated as microsponges in situ gel for ocular drug delivery aiming an improved therapeutic efficacy and reduction in the systemic side effects of oral acetazolamide. The microsponges were prepared by the quasi emulsion solvent diffusion method and were incorporated into 25% pluronic F-127 in situ gel. Ethyl cellulose polymer in different proportions with drug was used to prepare the microsponges. Different parameters were evaluated to select the best formulation. The formula S2 with drug to polymer ratio (2:1) showed high entrapment efficiency of about 82% and mean particle size of about 10 µm with polydispersity index (PDI) of 0.22, which are suitable characters for ocular delivery. The in situ gels were evaluated for physicochemical properties (pH, gelling capacity, gelation time and rheological properties) and in vivo studies. S2 formulation showed higher therapeutic efficacy compared to free drug in gel. It was non irritant to the rabbit's eye. These results indicated that acetazolamide microsponges in situ gel have potential ability for ophthalmic delivery.
Databáze: MEDLINE