DESIGN, FORMULATION AND EVALUATION OF SOLUBLE, SUB-CONJUNCTIVAL IMPLANTS OF MOXIFLOXACIN HYDROCHLORIDE

Abstract

Keywords: HME, in-vitro release, sub-conjunctival, antimicrobial efficacy, soluble implants Aim & Objectives: To design, develop and evaluate rod-shaped, soluble, sub-conjunctival implants; fitting in the lower cul-de-sac of eye, which are not only target specific but are stable and counter the odds of expulsion from the eye, and have increased ocular bioavailability and patient ompliance, hence leading to accurate dosing and lesser systemic side effects. Methodology: Cylindrical evices were prepared using suitable mixtures of HPC-L, MOX and PEG- 6000 using Hot Melt Extrusion (HME). These formulations were evaluated for mechanical properties like tensile strength, % elongation at break, strain and physicochemical properties like thickness, weight variation, surface pH, % moisture absorption, % oisture loss, compatibility, and drug content. In vitro release studies of the implants using modified Franz diffusion cells were carried out, for the release kinetics to be studied. All the formulations were sterilised using UV radiation and subjected to Draize eye test on rabbits. Results and Discussion: The implants were easured to be 1mm in diameter, 4-4.5 mm in length and 4.5-5 mg in weight. The tensile strength varied from 0.19-0.22 kg/mm2. The surface pH of the prepared inserts varied between 6.5 to 7.5, indicating that the inserts did not have an irritation potential as the pH is within the accepted ocular range. The weight variation and thickness of the prepared inserts were within 2%. The % moisture loss and absorption came out to be 4% and 13% respectively, as the polymer is hygroscopic. The compatibility studies showed no significant change. The drug content of the inserts varied from 95.5 ±1% to 99.6 ±1. The in-vitro release studies showed the maximum concentration to be achieved at 8 hours and eye irritancy studies showed no redness, swelling, watering of the rabbit eye.Conclusion: Our research and data suggests that aforementioned soluble implants could prove to be efficient therapeutic systems for chemotherapy of ocular bacterial infections such as conjunctivitis, keratitis and gonorrhoea. Acknowledgement: Authors are grateful to the Research and Development Wing of Sun Pharmaceutical Industries Ltd for providing necessary materials and equipment for research