Berberine Hydrochloride Embedded Chitosan-based Novel Floating Microspheres: Optimization, Characterization, and in vivo Anti-ulcer Potential

Abstract

Background: Microspheres are controlled drug delivery systems (CDDS) because they have the potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include biocompatiblity, greater bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects which restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to absorb the drug in the stomach for better antiulcer potential and fewer side effects. Objective: The rationale of the current investigational effort is to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interaction with the mucosa inside the stomach. Methods: The capillary extrusion technique was used with the aid of chitosan, a polymer in addition to sodium lauryl sulphate, a crosslinking agent. Scanning electron microscopy characterized the surface morphology of the prepared microspheres. The effects of polymeric concentration as well as the concentration of cross-link agent on percent yield, in vitro floating behavior, and in vitro drug release were efficiently assessed. Results: Diffusion has been observed as a popular mechanism for most launches. Prolonged drug release (12 hrs) has been seen in the prepared microspheres and they also remained buoyant for around 10 hrs. In vivo evaluation study was successfully performed. From the values of ulcer indexes for various groups, percentage protection was determined. The treatment group (F-2 formulation) showed the maximum percentage protection of 97.29%. Conclusion: The prepared floating microspheres can thus persuade potential candidates to be adaptable to any intra-gastric conditions for multiple-unit delivery devices.