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In Vitro and In Vivo Evaluations of Berberine-Loaded Microparticles Filled In-House 3D Printed Hollow Capsular Device for Improved Oral Bioavailability.

Authors
  • Choudhury, Dinesh1, 2
  • Jala, Aishwarya3
  • Murty, Upadhyayula Suryanarayana2, 4
  • Borkar, Roshan M3
  • Banerjee, Subham5, 6
  • 1 Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER)-Guwahati, Changsari, Assam, India. , (India)
  • 2 National Centre for Pharmacoengineering, NIPER-Guwahati, Changsari, Assam, India. , (India)
  • 3 Department of Pharmaceutical analysis, NIPER-Guwahati, Changsari, Assam, India. , (India)
  • 4 NIPER-Guwahati, Changsari, Assam, India. , (India)
  • 5 Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER)-Guwahati, Changsari, Assam, India. [email protected] , (India)
  • 6 National Centre for Pharmacoengineering, NIPER-Guwahati, Changsari, Assam, India. [email protected] , (India)
Type
Published Article
Journal
AAPS PharmSciTech
Publisher
American Association of Pharmaceutical Scientists
Publication Date
Mar 16, 2022
Volume
23
Issue
4
Pages
89–89
Identifiers
DOI: 10.1208/s12249-022-02241-9
PMID: 35296955
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

The low oral bioavailability, short biological half-life, high dose, and frequent dosing of berberine (BBR) contribute to its restricted clinical use despite its extensive pharmacological activity. Thus, the objective of this study was to formulate sustained-release microparticles (MPs) using a pH-independent release polymer and to evaluate their potential to improve the oral bioavailability of BBR. BBR loaded MPs were prepared using the emulsion crosslinking method and evaluated for particle size, circularity, morphology, entrapment efficiency, solid-state analysis, swelling index, and in vitro BBR release study fitted with different models of release kinetics. The MPs exhibited desired particle sizes ranges between 11.09-11.62 μm and were almost spherical in shape, as confirmed by the circularity value and micrographic images. A loss of BBR crystallinity was observed after encapsulation in MPs, as evident from various solid-state analyses. The final optimized batch (F3) showed highest % BBR entrapment efficiency value of 81.63% ± 4.9. The in vitro BBR release performance in both acidic and alkaline media showed the desired sustained release behavior from the crosslinked MPs, where the maximum BBR release was observed at alkaline pH, which is in accordance with the swelling study data. In the in vivo study, the oral absorption profiles of BBR from both pristine and MPs formats were investigated using in-house prototyped 3D printed hollow capsules as a unit dose carrier. In vivo data showed sustained and prolonged absorption behavior of BBR from MPs compared to their pristine counterparts, which resulted in a cumulative increment of relative oral bioavailability to mitigate the aforementioned issues related to BBR. Graphical Abstract. © 2022. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.

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