Improving permeability and oral absorption of mangiferin by phospholipid complexation

Ma, Hequn; Chen, Hongming; Sun, Le; Tong, Lijin; Zhang, Tianhong

doi:10.1016/j.fitote.2013.10.016

Cited by 108Drug Solubulity and Delivery SystemsMangiferin and Mango ExtractsAdvanced Drug Delivery Systems

Improving permeability and oral absorption of mangiferin by phospholipid complexation

Ma, Hequn, Chen, Hongming, Sun, Le, Tong, Lijin, Zhang, Tianhong·2014·Fitoterapia

DOI 10.1016/j.fitote.2013.10.016

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Abstract

Mangiferin is an active ingredient of medicinal plant with poor hydrophilicity and lipophilicity. Many reports focused on improving aqueous solubility, but oral bioavailability of mangiferin was still limited. In this study, we intended to increase not only solubility, but also membrane permeability of mangiferin by a phospholipid complexation technique. The new complex's physicochemical properties were characterized in terms of scanning electron microscopy (SEM), differential scanning calorimetry (DSC), infrared absorption spectroscopy (IR), aqueous solubility, oil-water partition coefficient and in vitro dissolution. The intestinal absorption of the complex was studied by the rat in situ intestinal perfusion model. After oral administration of mangiferin-phospholipid complex and crude mangiferin in rats, the concentrations of mangiferin were determined by a validated RP-HPLC method. Results showed that the solubility of the complex in water and in n-octanol was enhanced and the oil-water partition coefficient was improved by 6.2 times and the intestinal permeability in rats was enhanced significantly. Peak plasma concentration and AUC of mangiferin from the complex (Cmax: 377.66 μg/L, AUC: 1039.94 μg/L*h) were higher than crude mangiferin (Cmax: 180 μg/L, AUC: 2355.63 μg/L*h). In view of improved solubility and enhanced permeability, phospholipid complexation technique can increase bioavailability of mangiferin by 2.3 times in comparison to the crude mangiferin.

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Orally administered MGF has low aqueous solubility and limited intestinal permeability, resulting in poor systemic exposure at conventional doses.
“Orally administered MGF shows low aqueous solubility and limited intestinal permeability, resulting in poor systemic exposure at conventional doses (157-160).”
From Mangiferin in human disease: Multifaceted mechanisms and applications (Review) (2026) · cites this paper as [157]
Mangiferin derivatives with improved solubility, bioavailability and potency were obtained by chemical or biotransformation methods.
“In order to identify more effective therapeutic compounds, mangiferin derivatives with improved solubility, bioavailability and potency were obtained by chemical or biotransformation methods (9).”
From Mangiferin: An effective therapeutic agent against several disorders (Review) (2018) · cites this paper as [9]
Oral absorption of mangiferin is low.
“As the fat and water distribution coefficient of mangiferin is relatively high, oral absorption is low (9), which suggests that mangiferin may be better absorbed through the skin.”
From Mangiferin: An effective therapeutic agent against several disorders (Review) (2018) · cites this paper as [9]
The fat and water distribution coefficient of mangiferin is relatively high.
“As the fat and water distribution coefficient of mangiferin is relatively high, oral absorption is low (9), which suggests that mangiferin may be better absorbed through the skin.”
From Mangiferin: An effective therapeutic agent against several disorders (Review) (2018) · cites this paper as [9]

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Authors: Ma, H., Chen, H., Sun, L., Tong, L., & Zhang, T.
Affiliations: Shenyang Pharmaceutical University (CN)
Corresponding author: Zhang, Tianhong
ORCID: Chen, Hongming
Sun, Le
Zhang, Tianhong
Venue: Fitoterapia
Publisher: Elsevier BV
Published: 2014-03
Volume: 93
Pages: 54-61
ISSN: 0367-326X (ISSN-L)
DOI: 10.1016/j.fitote.2013.10.016
OpenAlex: W1997597510
Semantic Scholar: 3e15df2c36d7e6d4d4d047ce49aea5bb2fc49e6e
Cited by: 108
References: 31
Citations by year: 2026: 8 · 2025: 16 · 2024: 8 · 2023: 9 · 2022: 7 · 2021: 13 · 2020: 6 · 2019: 6 · 2018: 11 · 2017: 4 · 2016: 11 · 2015: 7 · 2014: 2
FWCI: 3.63
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Fitoterapia (publishedVersion)
PubMed (publishedVersion)
Funders: Shenyang Pharmaceutical University
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Health Sciences › Medicine › Complementary and alternative medicine › Mangiferin and Mango Extracts
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Keywords: mangiferin, phospholipid complexation, oral bioavailability, intestinal permeability, water solubility, oil-water partition coefficient, in situ intestinal perfusion, plasma pharmacokinetics, poorly water-soluble drugs, drug solubilization
MeSH terms: Administration, Oral, Animals, Biological Availability, Calorimetry, Differential Scanning, Drug Compounding, Intestinal Absorption, Male, Phytotherapy, Microscopy, Electron, Scanning, Permeability, Phospholipids, Random Allocation, Solubility, Spectrophotometry, Infrared, Rats, Sprague-Dawley, Xanthones, Rats

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Improving permeability and oral absorption of mangiferin by phospholipid complexation

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