ABSTRACT
OBJECTIVE: The aim of this study was to prepare solid lipid microparticles (SLM) with incorporated ofloxacin, suitable for oral delivery. METHODS: Ofloxacin-loaded SLM were prepared using stearic acid and chloroform as lipid matrix and Tween-80 as surfactant, by high shear homogenization technique and followed by lyophilization. The physiochemical characterization of SLMs were investigated by scanning electron microscopy, transmission electron microscopy, zeta potential, zone of inhibition, in-vitro study, ex-vivo study and stability study. RESULTS: The result demonstrated that the entrapment efficiency, particle size and zeta potential of microparticles were 86.02%, 203.7nm and -32.68mv, respectively. The in-vitro and ex-vivo studies showed sustained release of drug from formulation. CONCLUSION: These results indicate that SLM might be a promising delivery system to enhance the pharmacological activity of ofloxacin.
Subject(s)
Anti-Bacterial Agents/chemistry , Drug Carriers/chemistry , Lipids/chemistry , Ofloxacin/chemistry , Anti-Bacterial Agents/pharmacology , Chemistry, Pharmaceutical , Delayed-Action Preparations , Drug Liberation , Drug Stability , Excipients/chemistry , Humans , Microbial Sensitivity Tests , Microspheres , Ofloxacin/pharmacology , Particle Size , Polysorbates/chemistry , Stearic Acids/chemistryABSTRACT
The current study involves the development and optimization of their drug entrapment and ex vivo bioadhesion of multiunit chitosan based floating system containing Ranitidine HCl by ionotropic gelation method for gastroretentive delivery. Chitosan being cationic, non-toxic, biocompatible, biodegradable and bioadhesive is frequently used as a material for drug delivery systems and used to transport a drug to an acidic environment where it enhances the transport of polar drugs across epithelial surfaces. The effect of various process variables like drug polymer ratio, concentration of sodium tripolyphosphate and stirring speed on various physiochemical properties like drug entrapment efficiency, particle size and bioadhesion was optimized using central composite design and analyzed using response surface methodology. The observed responses were coincided well with the predicted values given by the optimization technique. The optimized microspheres showed drug entrapment efficiency of 74.73%, particle size 707.26 µm and bioadhesion 71.68% in simulated gastric fluid (pH 1.2) after 8 h with floating lag time 40s. The average size of all the dried microspheres ranged from 608.24 to 720.80 µm. The drug entrapment efficiency of microspheres ranged from 41.67% to 87.58% and bioadhesion ranged from 62% to 86%. Accelerated stability study was performed on optimized formulation as per ICH guidelines and no significant change was found in drug content on storage.