FABRICATION OF BIOADHESIVE OCUSERT WITH DIFFERENT POLYMERS: ONCE A DAY DOSE


Aya M. Dawaba, Hamdy M. Dawaba, Amal S. M. Abu El-enin, Maha K. A. Khalifa

Abstract


Objective: The objective of this current study is to fabricate ocuserts to control the drug release from chosen bioadhesive polymeric matrixes to enhance patient compliance. ciprofloxacin HCl (CFX HCl) was selected as a model drug.

Methods: Different bioadhesive polymers with different film forming capabilities namely Hydroxy Propyl Methyl Cellulose (HPMC K4M), Poly Vinyl Alcohol (PVA), Sodium Carboxy Methyl Cellulose (Na CMC), Hydroxy Propyl Cellulose (HPC), Sodium Alginate (Na Alg.), pullulan and Xanthan Gum (XG) in different ratios were used in fabricating ocuserts using solvent-casting technique. Propylene Glycol (PG) was used as plasticizer to facilitate the fabrication process. Characterization tests of the developed ocuserts were performed as well as bioadhesive tests and in-vitro release studies of the incorporated drug. The obtained results were analysed using different release kinetic models. Stability of the selected ocuserts was investigated at 40 ± 0.5oC and 75 ± 5% Relative Humidity (RH) for three months’ storage period. In-vivo ocular irritation test was performed to investigate the safety of the formula in rabbits’ eyes as well as to test the release profile and thus estimating In-vitro In-vivo correlation.

Results: All the prepared ocuserts showed uniformity of film characterization and bioadhesion strength ranged from 240 ± 66 and 158 ± 52dyne/cm2. Selected formula from the in-vitro release study tested for in-vivo study showed slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In-vitro In-vivo correlation showed excellent correlation with R2 value of 0.9982.

Conclusion: PVA based ocuserts proven to be a promising once-daily, effective and safe ocular delivery system of the drug.

 


Keywords


polymeric matrix; ocuserts; In-vivo tests; once-daily.

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