Abstract
Objective: The present work entails design and characterization of enteric coated mucoadhesive microcapsules loaded with amoxicillin trihydrate as a novel chronotherapeutic approaches for the treatment and management of bacterial infection.Methods: The microcapsules were prepared by solvent evaporation technique using ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) as rate-controlling and mucoadhesive polymers, followed by a triple coating with Eudragit L100 as enteric coating polymer. Box-Behnken statistical design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The optimized microcapsules were also characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity.Results: The optimized microcapsules exhibited good entrapment efficiency, particle size and mucoadhesive property. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical in shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient (r2) value indicated that drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all the prepared formulations at P < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 month showed there was no change in drug content and release characteristics during storage.
Highlights
Amoxicillin trihydrate (AMT) is a semi-synthetic broad-spectrum βlactam antibiotic used for the treatment of bacterial infections
The preliminary screening showed that microcapsules prepared with mucoadhesive polymer ethyl cellulose-based HPMCK100M provides higher stability and protection to the drug and they were found to be non-aggregated
The response variables considered for systematic optimization, i.e., %drug entrapment, % drug release in 24 h and % mucoadhesion were allowed to fit in the quadratic equations with added interaction terms to correlate the studied responses with the examined factors
Summary
Amoxicillin trihydrate (AMT) is a semi-synthetic broad-spectrum βlactam antibiotic used for the treatment of bacterial infections. It is primarily active against gram positive bacteria by inhibiting their cell wall synthesis [1, 2]. I. d) requires the development of a novel once-a-day oral chronomodulated drug delivery systems of AMT for the management of bacterial infections [4, 5]. Microparticles are less affected by pH change, gastric transit time, attain more constant plasma levels, give higher accuracy in reproducibility by dose and provide desired controlled release profile of drug delivery [7]
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