Cited by 363Berberine and alkaloids researchDrug Transport and Resistance MechanismsDrug Solubulity and Delivery Systems

Research progress on berberine with a special focus on its oral bioavailability

Liu, Chang-Shun, Zheng, Yu-Rong, Zhang, Ying-Feng, Long, Xiao-Ying·2016·Fitoterapia

Abstract

The natural product berberine (BBR) has become a potential drug in the treatment of diabetes, hyperlipidemia, and cancer. However, the oral delivery of BBR is challenged by its poor bioavailability. It is necessary to improve the oral bioavailability of BBR before it can be used in many clinical applications. Understanding the pharmacokinetic characteristics of BBR will enable the development of suitable formulas that have improved oral bioavailability. The key considerations for BBR are how to enhance the drug absorption and to avoid the intestinal first-pass effect. This review summarizes the pharmacological activities of BBR and analyzes the factors that lead to its poor oral bioavailability. In particular, the therapeutic potential of BBR in new indications from the aspect of oral bioavailability is discussed. In conclusion, BBR is a promising drug candidate for metabolic disorders and cancer but faces considerable challenges due to its poor oral bioavailability.

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Crossref · 10.1016/j.fitote.2016.02.001

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Authors
Liu, C.-S., Zheng, Y.-R., Zhang, Y.-F., & Long, X.-Y.
Affiliations
Guangdong Pharmaceutical University (CN)
Venue
Fitoterapia
Publisher
Elsevier BV
Published
2016-03
Volume
109
Pages
274-282
ISSN
0367-326X (ISSN-L)
OpenAlex
W2272399875
Cited by
363
References
128
Citations by year
2026: 33 · 2025: 40 · 2024: 33 · 2023: 37 · 2022: 50 · 2021: 46 · 2020: 44 · 2019: 22 · 2018: 25 · 2017: 28 · 2016: 4
FWCI
3.02
Type
journal article
Language
en
Open access
closed
Locations
  • Fitoterapia (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • National Natural Science Foundation of China (81573353)
  • Medjaden Academy & Research Foundation for Young Scientists (MJA20160107)
Topics
  • Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Keywords
berberine, oral bioavailability, pharmacokinetics, drug absorption enhancement, first-pass metabolism, natural products, diabetes mellitus, hyperlipidemia, cancer, metabolic disorders, pharmacological activity
MeSH terms
Administration, Oral, Animals, Berberine, Biological Availability, Diabetes Mellitus, Humans, Hyperlipidemias, Neoplasms, Molecular Structure

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