An Improvement of Efficacy of Moxifloxacin HCl for the Treatment of Bacterial Keratitis by Formulation of Ocular Mucoadhesive Microspheres
| Autor: | Amit Manohar Belekar, AP Gadad, Vivek Wamanrao Sontake, Panchaxari Mallappa Dandagi, VS Mastiholimath, Prashant Sanjivrao Salian |
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| Rok vydání: | 2013 |
| Předmět: |
Moxifloxacin HCl
genetic structures business.industry Sodium medicine.medical_treatment Pharmaceutical Science chemistry.chemical_element Eye drop Mucoadhesion Pharmacology Antimicrobial Microspheres eye diseases chemistry Bacterial keratitis Polymer ratio In vivo Ocular MOXIFLOXACIN HCL Medicine Particle size business Research Article |
| Zdroj: | Scientia Pharmaceutica Volume 81 Issue 1 Pages 259-280 |
| ISSN: | 2218-0532 0036-8709 |
| Popis: | The aim of this study was to prepare novel ocular mucoadhesive microspheres of Moxifloxacin HCl to increase its residence time on the ocular surface and to enhance its therapeutic efficacy in ocular bacterial keratitis. Microspheres were fabricated with different grades of Methocel and Sodium CMC as polymers. Microspheres were evaluated for their particle size, morphology, encapsulation efficiency, mucoadhesion, antimicrobial efficacy, and in vitro drug release studies. In vivo studies were carried out for the promising formulation on eyes of albino rabbits by inducing bacterial keratitis. A sterile microspheres suspension in light mineral oil was applied to infected eyes twice a day. A marketed conventional eye drop was used as a positive control. Eyes were examined daily for improvement of clinical signs of bacterial keratitis by an ophthalmologist. The average particle size of microspheres was found to be less than 80 μm. Methocel microspheres were found to have a smoother surface than Sodium CMC. Entrapment efficiency was enhanced with an increased polymer concentration and viscosity. The formulation containing Methocel K100M with a drug: polymer ratio of 1:2 exerted longer corneal and conjunctival mucoadhesion time of 8.45±0.15 h and 9.40±0.53 h respectively. In vitro release of Moxifloxacin HCl from microspheres was retarded with increased viscosity and concentration of polymers, and was controlled by diffusion as well as polymer relaxation. All formulations showed comparable antimicrobial activity in comparison with conventional marketed eye drops. The formulation containing Methocel K100M with a drug: polymer ratio of 1:2 was found to be a promising formulation and was used for the in vivo studies. The in vivo studies revealed that microspheres demonstrated significantly lower clinical scores and reduced the total duration of therapy than the marketed Moxifloxacin HCl eye drops. In vitro and in vivo studies showed that ocular mucoadhesive microspheres of Moxifloxacin HCl were found to have an improved efficacy in the treatment of ocular bacterial keratitis in comparison with the marketed formulation. |
| Databáze: | OpenAIRE |
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