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 a 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±0.5 °C 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 to estimate In vitro In vivo correlation.Results: All the prepared ocuserts showed the 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 the slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In vitro In vivo correlation showed an 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.
Highlights
Eye is an essential organ with unique qualities and enable us to see the world
All the peaks were found in drug-loaded ocusert that confirms the presence of the drug in the polymers without any interaction
Pharmacokinetics and pharmacodynamics studies in human beings are needed to be carried out to establish the therapeutic utility of this system
Summary
Drug delivery through ocular route is local more than systemic to bypass the high blood concentration of the drug, which may cause eye damage [1]. The solitary anatomy, biochemistry, and physiology of the eye challenge the formulator to circumvent the protective barriers of the eye without causing any tissue damage because of the impervious nature of the eye [2]. About 70% of the total ophthalmic preparations available in market are conventional ophthalmic dosage forms (eye drops and ointments). For these dosage forms, frequent dosing is the net result of the availability of just a little amount for its therapeutic effect. That’s why to overthrow these issues, newer pharmaceutical technologies such as iontophoresis, nanoparticles, liposomes, nanosuspension, microemulsion, in situ gel and bioadhesive ocuserts have been developed to improve patient compliance by increasing the bioavailability of the drug in a controlled and sustained manner [3,4,5,6]
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