A Fresh Look on Bergenin: Vision of Its Novel Drug Delivery Systems and Pharmacological Activities

Abstract

Bergenin (BER), a key constituent of Bergenia crassifolia (Saxifragaceae), has gained extensive attention, owing to its array of pharmacological actions, including anti-infective, anti-cancer, anti-diabetic, neuroprotective, hepatoprotective, anti-urolithiatic, anti-hyperuricemic, and anti-bradykinin properties. Despite ever-intensifying support for its therapeutic features, the poor solubility, lower oral bioavailability, shorter half-life, and more intestinal pH degradation (pH 6.8 or above) of BER have puzzled researchers. To circumvent these pharmaceutical challenges, and to improve its therapeutic efficacy, newer approaches have been adopted by research scientists. Thus, a discussion of the existing literature may provide complete information about the advances in delivery strategies for enhancing its utility. This paper summarizes up-to-date works on the design and development of novel delivery carriers of this bioactive compound, such as phospholipid complexes, extended-release core tablets, prodrugs, herbal gels, polyherbal ointments, nanoparticles, and poly (lactic acid) polymers, with the objective of harnessing its full potential. This review also provides a deep insight into its bioactivities, along with mechanisms. Additionally, the physicochemical attributes, chemistry, and pharmacokinetics of BER are discussed herein. Hence, the comprehensive information documented in this review may introduce new avenues for research advancements of BER.