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Drug Delivery Letters

Editor-in-Chief

ISSN (Print): 2210-3031
ISSN (Online): 2210-304X

Research Article

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

Author(s): Radha Rani, Manish Kumar*, Ravinder Verma, Pravin Gupta, Beena Kumari, Rakesh Pahwa, Vineet Mittal, Shailendra Bhatt and Deepak Kaushik

Volume 12, Issue 4, 2022

Published on: 01 September, 2022

Page: [287 - 301] Pages: 15

DOI: 10.2174/2210303112666220602123548

Price: $65

Abstract

Background: Microspheres are controlled drug delivery systems (CDDS) due to their potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include greater biocompatibility, increased bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects, which has restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to improve the absorption of the drug in the stomach for better anti-ulcer action and fewer side effects.

Objective: This study aimed to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interacting 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: The drug follows a mechanism for prolonged release, known as diffusion. Prolonged drug release (12 hrs) was 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 maximum percentage protection of 97.29%.

Conclusion: The prepared floating microspheres can make potential candidates adaptable to any intra- gastric conditions for multiple-unit delivery devices.

Keywords: Chitosan, sodium lauryl sulphate, capillary extrusion method, floating microspheres, berberine hydrochloride, GIT.

Graphical Abstract
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