Involvement of metabolism-permeability in enhancing the oral bioavailability of curcumin in excipient-free solid dispersions co-formed with piperine

International Journal of Pharmaceutics
Ruoning WangJunsong Li

Abstract

Curcumin (CUR) has gained increasing interest worldwide due to multiple biological activities. However, the therapeutic application remains limited because of its low aqueous solubility, intestinal metabolism and poor membrane permeability. In present study, an excipient-free CUR solid dispersion co-formed with piperine (PIP), the absorption enhancer involving metabolism-permeability, was successfully prepared by melting and quench cooling (co-amorphous CUR-PIP). The co-amorphous CUR-PIP exhibited superior performance in non-sink dissolution compared with crystalline and amorphous CUR, and showed physically stable at least 3 months, attributing to the strong molecular interactions between CUR and PIP as evaluated by FTIR spectra. Furthermore, the combination of PIP with CUR in the co-amorphous formulation could inhibit the glucuronidation of CUR, as exhibited in the in vitro assay of rat intestinal microsomes. The co-amorphous CUR-PIP would also exhibit higher gastrointestinal membrane permeability of CUR, as confirmed by Papp of CUR in Caco-2 model. After administration of co-amorphous CUR-PIP, the AUC of CUR significantly increased by 2.16- and 1.92-fold those in crystalline and amorphous CUR, respectively. This study demonst...Continue Reading

Citations

Dec 4, 2019·Drug Delivery and Translational Research·Shimon Ben-ShabatArik Dahan
Jul 21, 2020·Expert Opinion on Drug Delivery·Jiawei HanShuai Qian
Jul 28, 2020·Critical Reviews in Food Science and Nutrition·Isabella Rosa da MataSimone Morelo Dal Bosco
Oct 27, 2020·Critical Reviews in Food Science and Nutrition·Devendrasingh TomarKamal Dua
May 1, 2021·International Journal of Molecular Sciences·Anna StasiłowiczJudyta Cielecka-Piontek
Apr 30, 2021·International Journal of Pharmaceutics·Dani Lakshman YarlagaddaKrishnamurthy Bhat
Jul 10, 2020·Anti-cancer Agents in Medicinal Chemistry·Phuong H L Tran, Thao T D Tran
Aug 29, 2021·Pharmaceutics·Do-Hyun KimJaeh-Wi Lee
Nov 15, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Meng TongZhenhai Zhang
Nov 18, 2021·Journal of Biomolecular Structure & Dynamics·Princy ChoudharySangeeta Singh

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