Evaluation of Intestinal Absorption and Bioavailability of a Bergenin–Phospholipid Complex Solid Dispersion in Rats

Gao, Haoshi; Yue, Wei; Xi, Long; Sun, Yuanyuan; Zhang, Tianhong

doi:10.1208/s12249-018-0984-5

Cited by 15 publications

(2 citation statements)

References 22 publications

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“…The values of C max and AUC 0−t for this bioactive were significantly greater in BERPC-SD then pure bioactive, and were further augmented by verapamil. These findings represent that BERPC-SD can upsurge the bioavailability of BCS class IV moieties [92].…”

Section: Phospholipid Complex Solid Dispersionmentioning

confidence: 69%

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

Mehta

Kadian

Dalal

et al. 2022

Future Pharmacology

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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.

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Section: Phospholipid Complex Solid Dispersionmentioning

confidence: 69%

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

Mehta

Kadian

Dalal

et al. 2022

Future Pharmacology

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“…The perfusion solutions were infused into intestinal segments at the same flow rate for 120 min and collected every 15 min. Finally, the BITC content in the effluent was determined, and the constant of absorption ( K a ) and effective intestinal permeability ( P eff ) of each sample were calculated (Gao, Wei, Xi, Sun, & Zhang, 2018).

K_{a} (1 - \frac{C_{o u t} Q_{o u t}}{C_{i n} Q_{i n}}) \cdot \frac{Q_{i n}}{π r^{2} l}

P_{e f f} = - \frac{Q_{i n} \cdot \ln \frac{C_{o u t}}{C_{i n}}}{2 π r l}

…”

Section: Methodsmentioning

confidence: 99%

Pseudosciaena crocea roe protein‐stabilized emulsions for oral delivery systems: In vitro digestion and in situ intestinal perfusion study

Tang

Wang

Jiang

et al. 2020

Journal of Food Science

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Benzyl isothiocyanate (BITC) was encapsulated in oil‐in‐water emulsions stabilized by Pseudosciaena crocea roe protein isolate (PRPI). The stability, lipid digestion, BITC bioavailability, and retention rate of the emulsions were characterized using a simulated gastrointestinal tract model. Tween‐corn and PRPI‐medium‐chain triglycerides (MCT) emulsions were used as controls. The membrane permeability and BITC absorption from these emulsions were investigated by in situ single‐pass intestinal perfusion. The results showed that the PRPI‐stabilized emulsions were stable under nonacidic environment conditions. Moreover, the PRPI‐corn emulsion had more obvious protective effects than PRPI‐MCT and Tween‐corn emulsions. Atomic force and confocal laser scanning microscopy images showed that the protein hydrolyzed and oil droplets aggregated during simulated gastric phase digestion. Following the exposure of oil droplets in the small intestine phase, the PRPI‐corn emulsion had a high rate of free fatty acid release (99.13 ± 2.49%), and the retention rate and bioavailability of BITC from the PRPI‐corn emulsion were 75.93 ± 7.17% and 77.32 ± 5.36%, respectively, which were significantly higher than those measured for the other emulsions (P < 0.05). Moreover, the Ka and Peff of the PRPI‐corn emulsion reached the maximum value at 45 min and then decreased slowly. These results suggest that the PRPI‐corn emulsion delivery system is effective in encapsulating, delivering, and protecting BITC. Practical Application This study provides some useful information for the food industry to develop a Pseudosciaena crocea roe protein isolate (PRPI) emulsion that could be successfully used to construct a BITC delivery system and improve benzyl isothiocyanate (BITC) bioavailability. The protective effect on BITC assessed in vitro simulated gastrointestinal tract and in situ single‐pass intestinal perfusion are discussed.

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Phospholipid complexation: A versatile technique for delivery of phytomedicine

Biswas¹,

Kar²,

Sharma³

et al. 2022

Evidence-Based Validation of Herbal Medicine

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Evaluation of Intestinal Absorption and Bioavailability of a Bergenin–Phospholipid Complex Solid Dispersion in Rats

Cited by 15 publications

References 22 publications

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

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

Pseudosciaena crocea roe protein‐stabilized emulsions for oral delivery systems: In vitro digestion and in situ intestinal perfusion study

Phospholipid complexation: A versatile technique for delivery of phytomedicine

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