Phytoglycogen and Its Derivatives to Incorporate Curcumin for Enhanced Solubility and Efficacy

Randol Jose Rodríguez-Rosales, Purdue University

Abstract

There have been great interests in exploring practical approaches to solubilize and enhance the efficacy of poorly water-soluble active ingredients (AIs). In this research, phytoglycogen (PG) and its two derivatives were evaluated as carriers of curcumin, an important poorly water-soluble AI. Studies were conducted to: (1) evaluate the ability of native PG to solubilize curcumin and improve its in vitro permeation with caco-2 cell monolayers, and increase its anticancer efficacy (i.e., reduction in cancer cell viability) with HeLa and PC3 cell lines, (2) determine the effects of degrees of substitution (DS) on the capability of PG octenyl succinate (PG-OS) to enhance the solubility and efficacies of curcumin, (3) examine the same effects for molar substitution (MS) of hydroxypropyl phytoglycogen (HPP), and (4) evaluate the performance of a high-MS HPP in solubilizing and enabling curcumin efficacy. The results showed that native PG effectively solubilized curcumin, increased its in vitro permeation, and reduced its half maximal inhibitory concentration (IC50) against HeLa and PC3. For PG-OS, a DS-dependent enhancing effect was found on curcumin solubilization and in vitro efficacies, suggesting the interactions between the octenyl succinate groups with curcumin molecules. For HPP, MS-dependent effects were also identified on the solubilization and efficacy enhancement of curcumin, and the highest MS led to the greatest enabling effect on curcumin. In all studies, the carrier-to-curcumin ratio was an important factor as related to the properties and performances of curcumin solid dispersions. Overall, this research provided further information on the interactions between PG (and its derivatives) and poorly water-soluble AIs. PG-based biopolymers are dendrimer-like, which may offer fundamental structural characteristics for incorporating, stabilizing, and enabling active food ingredients.

Degree

Ph.D.

Advisors

Yao, Purdue University.

Subject Area

Food Science|Chemistry|Agriculture

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