Statistical Optimization and Characterization of Microballoons for Intestinal Delivery of Acid Labile Drug Utilizing Acrylic Polymer

Objective: The present work was to formulate buoyant system in order to protect the drug from gastric acid degradation, increasing the gastric residence time, control the drug leaching by use of enteric polymers, prolong the half life for longer duration of action, furthermore to prevent dosage form adherence to the mucous wall in order to avoid incomplete drug release. Moreover the side effects of effervescent dosage form could be well controlled. Methods: Employed was emulsion solvent diffusion, using 23factorial design with Eudragit®L100 and RS100 in solvent mixture dichloromethane and ethanol whereas the optimization and validation were carried out through Design-Expert 9.0.3 software. Result: Optimized formulation (LRS-O) showed buoyancy (B %) of 78.88±0.23 %, entrapment efficiency (EE %) of 71.12±0.04 % and drug release over 12 h (CDR12 h %) of 99.50±0.08 % in PB pH 6.8. Whereas in PB pH 7.4 the actual values for B %, EE % and CDR12 h % was 87.35±0.68 %, 89.30±0.05 % and 98.68±0.37 %. Smaller error values for both showed that actual responses were within the predicted range. Particles were in the size range 80-100 μm with spherical, rough, porous and internal hollow cavity. Drug-polymer interactions were negligible and showed zero order patterns over 12 hrs. Conclusion: Enhanced bioavailability of the drug was achieved with excellent responses of B %, EE % and CDR12 h % and the software used for the optimization and validation of formulation design, was economical and reduces the number of trials.