ENTERIC-COATED CAPSULES FOR EXTENDED RELEASE OF ESOMEPRAZOLE MUCOADHESIVE MULTIPLE-UNIT MINI PATCHES

Abstract

The present study aims to formulate and evaluate oral mucoadhesive multiple-unit mini patches (MMMP) of Esomeprazole (ESO) for extended-release MMMP of ESO in enteric-coated capsules were prepared and evaluated using chitosan in combination with xanthan gum, guar gum, tragacanth or acacia in the ratios of 19:1, 9:1, 4:1, 1.5:1 and 0.66:1 employing 2% acetic acid as a solvent for chitosan, purified water as a solvent for natural gum polymers and glycerin 0.12mL as a plasticizer. The prepared films were punched into MMMP with 0.5 mm diameter and filled into hard gelatin capsules and further the filled capsules were treated with HPMCAS/Eudragit L dispersion (10% w/v) with a blend ratio of 1:3 for enteric coating. The prepared MMMP were characterized for surface texture, thickness, folding endurance, moisture content, moisture uptake, mucoadhesive strength, drug content uniformity, In vitro drug release and accelerated physical stability studies. The SEM photographs showed the rough to smooth pattern of surfaces of patches. The thickness of MMMP was found between 43.62±0.27 and 49.53±0.11 m. Mean weight of mini-patch was measured and found between 13.81+0.14 and 14.94+0.15 mg. The percentage of swelling was between 215±5.39 and 473±6.72. The moisture content was between 1.04±0.06 and 2.67±0.24. The mucoadhesion in terms of time required to detach all the MMMP from mucosal surface was found between 5.5+0.2 and 12.3+0.6 h. Percentage of drug content uniformity was between 95.08±3.42% and 99.16±4.73% for all formulations. The FTIR and DSC spectra indicated no drug-polymer interactions. The in vitro dissolution studies showed extended release of ESO from MMMP in pH 6.8 phosphate buffer where as no significant of drug release found in acidic environment showing that MMMP in enteric coated capsules could be employed to delivery ESO to intestine directly. Formulations EXF5, EGF5, ETF5 and EAF5 were optimized based on physical characteristics and in vitro drug release patterns. In all the cases the drug dissolution was reciprocal to the polymer concentration in the formulations. Among all natural polymers employed in this specification the decreasing order of drug release from the polymers was Xanthan gum > Tragacanth > Guar gum > Acacia. Accelerated stability studies showed no significant change (p.05) in drug content and dissolution profile of all optimized formulations before and after the test. The prepared mucoadhesive multiple-unit mini patches (MMMP) in enteric coated capsules for controlled release of Esomeprazole using natural polymers and could be successfully employed for intestinal delivery while minimizing the drug degradation and providing extended release of the drug.