The poor solubility of resveratrol (RES) leads to incomplete absorption and low bioavailability, which may restrict its clinical trials and potential applications. Numerous delivery systems of RES have been proposed for enhanced RES solubility and dissolution rate, however, with various limitations. The objective of this study was to evaluate the capabilities of octenylsuccinate hydroxypropyl phytoglycogen (OHPP), a recently developed amphiphilic dendrimer-like biopolymer, to improve the water solubility, dissolution rate, and Caco-2 monolayer permeation of RES. The RES-OHPP solid dispersion was prepared using spray-drying at OHPP/RES ratio of 4/1. The obtained RES-OHPP solid dispersion was characterized for RES soluble amount, crystallinity, RES-OHPP interactions, dissolution profile, and Caco-2 permeation. Results showed that for RES-OHPP solid dispersion the instant soluble amount of RES reached 638.1 µg/mL, which was over 17 times that of pure RES (35.2 µg/mL). The dissolution study showed that RES in RES-OHPP solid dispersion completely dissolved in 3 h upon dissolution, whereas only 33% of pure RES dissolved. Noticeably, X-ray powder diffraction crystallograms showed a significant reduction of RES crystallinity in RES-OHPP solid dispersion. In addition, FTIR spectra indicated the formation of hydrogen bonds between RES and OHPP in RES-OHPP solid dispersion. For Caco-2 permeation test, only RES-OHPP solid dispersion achieved RES permeation at high RES loading amount (&gt;35 µg/mL), which was associated with improved soluble amount of RES. The study suggested that the hydroxypropyl and octenylsuccinate groups at the surface of OHPP particulates interacted with RES molecules through hydrogen bonding. The dendrimer-like structure of OHPP particulate provided steric hindrance that could prevent the crystallization of dispersed RES molecules. These interactions could facilitate the incorporation of RES with OHPP particulates, and therefore improved the soluble amount of RES. Through increasing the soluble amount of RES, OHPP may improve the bioavailability of RES.

Octenylsuccinate hydroxypropyl phytoglycogen to enhance the solubility and <i>in vitro</i> permeation of resveratrol

2019 Fall National Meeting

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Octenylsuccinate hydroxypropyl phytoglycogen to enhance the solubility and in vitro permeation of resveratrol