Formulation and Evaluation of In Situ forming Polymeric Drug Delivery Systems for Mixed Vaginal Infection

Abstract

Aims: Vaginal preparations are still associated with number of problems including frequent administration and escape from vagina causing discomfort to patient. For efficient vaginal delivery of drugs, the delivery system should reside at the site of infection for a prolonged period of time therefore this work aims to prepare Vaginal Capsules containing sustained release in situ forming polymeric particles containing broad spectrum antibiotics to cover all the common pathogen associated with vaginal infections. Study Design: Characterization for the developed beads, such as determination od, particle size, drug entrapment yield, and drug release profiles, were characterized prior to determining intracellular uptake profile, in vitro, and in vivo tissue distribution patterns of the particles. Place and Duration of Study: Department of pharmaceutical technology in German university in Cairo and Department of Pharmaceutical Technology in National Research Center, Cairo, Egypt between June 2012 and March 2014. Methodology: Calcium alginate, chitosan and mixed polycarbophil beads containing fluconazole (antifungal) and metronidazole (antiprotozoal) were packed in hard gelatin capsule and evaluated as new vaginal drug delivery forms beads were characterized by size, Scanning Electron Microscopy (SEM), weight uniformity and drug entrapment efficiency as well as in –vivo bioadhesion test Results: Results of the in vitro antimicrobial study indicated that the M5 and F4 mixed beads had better antimicrobial action than the commercial intravaginal drug delivery systems and retention was prolonged in an ex vivo retention study showed that the bioadhesion of the beads were 68.88 to 84.3%. Conclusion: Developed beads were found to be more effective in in vitro conditions. The average zone of inhibition of the developed M5 the formulae that contain (Metronidazole: Chitosan: Polycarbophil) in (1:1:1 ratio)and F4the formulae that contain (Fluconazole: Chitosan: Polycarbophil) in (1:1:1 ratio) mixed beads Candida albicans was 28.3±0.6 mm compared to 24.5±1.7 mm of commercial Amrizol®, indicating significantly higher efficacy of M5 and F4 mixed beads (p>0.001). Average zone of inhibition of the developed M5 and F4 mixed beads against E. coli was 31.5±2.2 mm compared to 28.6±1.8 mm of Amrizol®. The developed M5 and F4 mixed beads was more effective than the tested commercial formulations and last for12, 18 and 24 hr.