RRC ID 54818
著者 Uchiyama H, Wada Y, Hatanaka Y, Hirata Y, Taniguchi M, Kadota K, Tozuka Y.
タイトル Solubility and Permeability Improvement of Quercetin by an Interaction Between α-Glucosyl Stevia Nanoaggregates and Hydrophilic Polymer.
ジャーナル J Pharm Sci
Abstract The effect of composite formation between α-glucosyl stevia (Stevia-G) and hydrophilic polymers on solubility and permeability enhancement of quercetin hydrate (QUE) was evaluated. Polyvinylpyrrolidone K-30 (PVP), hydroxypropyl methylcellulose 2910-E (HPMC), and hydroxypropyl cellulose SSL (HPC) were selected as candidate hydrophilic polymers. Fluorescence studies with pyrene and curcumin suggested composite formation occurs between Stevia-G aggregate and polymers. Furthermore, the strength of interaction between Stevia-G aggregate and polymers was as follows: PVP > HPMC > HPC. Evaporated particles (EVPs) of QUE with Stevia-G and polymers showed synergic QUE solubility enhancement. Solubility of QUE from the EVPs was enhanced in the following order: Stevia-G/PVP > Stevia-G/HPMC > Stevia-G/HPC, in accordance with the degree of interaction. Enhanced membrane permeability of QUE from the EVPs of Stevia-G/PVP was confirmed using Caco-2 cells. The amount of QUE that permeated Caco-2 cells from the EVPs of Stevia-G/PVP was 13.7-, 4.7-, and 2.1-fold higher than that of the untreated QUE powder, EVPs of Stevia-G, and EVPs of PVP, respectively. These results indicated that the composite formed by Stevia-G and PVP can dramatically enhance the solubility and membrane permeability of QUE.
巻・号 108(6)
ページ 2033-2040
公開日 2019-6-1
DOI 10.1016/j.xphs.2019.01.007
PII S0022-3549(19)30014-0
PMID 30653971
MeSH Antioxidants / administration & dosage Antioxidants / chemistry Antioxidants / pharmacology* Caco-2 Cells Cell Membrane Permeability / drug effects Cellulose / analogs & derivatives Cellulose / chemistry Diterpenes, Kaurane / chemistry* Diterpenes, Kaurane / pharmacology Drug Carriers / chemistry* Drug Carriers / pharmacology Glucosides / chemistry* Glucosides / pharmacology Humans Hydrophobic and Hydrophilic Interactions Hypromellose Derivatives / chemistry Povidone / analogs & derivatives Povidone / chemistry Quercetin / administration & dosage Quercetin / chemistry Quercetin / pharmacokinetics* Solubility
IF 3.197
引用数 4
リソース情報
ヒト・動物細胞 CACO-2(RCB0988)