Octenylsuccinate Hydroxypropyl Phytoglycogen, a Potent and Non-Specific Solubilizer for Poorly Water-Soluble Active Ingredients
Among active food and pharmaceutical ingredients, many are poorly water-soluble due to their lipophilicity and/or highly crystalline structure. Poorly water-soluble active food ingredients, which include a number of vitamins, nutrients, and phytochemicals, often meet difficulties with effective formulations that may offer desirable health benefits. In medical areas, around 30-40% of top-selling drugs and 75% of drug candidates are practically water-insoluble. In general, the development of non-specific solubilizers for active ingredients (AIs) is highly desirable for enhancing the efficacy, safety, and other benefits of AIs. In this study, a novel solubilizer, octenylsuccinate hydroxypropyl phytoglycogen (OHPP), was introduced. OHPP is an amphiphilic dendrimer-like biopolymer derived from phytoglycogen (PG). PG is a highly branched alpha-D-glucan synthesized by some plants with the deficiency of starch debranching enzyme(s). Due to their dendrimer-like structure, PG and its derivatives have shown properties similar to those of synthetic dendrimers. PG is plant-based and abundant, which makes it more a sustainable biobased material than synthetic dendrimers. As a novel derivative of PG, OHPP has shown highly superior functionalities in solubilizing AIs. With the octenylsuccinate hydroxypropyl external layer, OHPP particulates are able to interact and host hydrophobic molecules. In this research, eight AIs were used to evaluate the solubilization capability of OHPP in the form of solid dispersion (SD). All AI-OHPP SDs have shown reduced crystallinity of AIs. AI-OHPP SDs increased the solubility of AIs by 39 to 15,893 times compared with AIs alone. Importantly, in vitro tests showed that AIs were bioaccessible in the aqueous solutions of AI-OHPP SDs, showing an effective release of AIs from OHPP particulates. OHPP is a biobased, highly potent, and non-specific solubilizer for poorly water-soluble AIs. The examples provided through this study have demonstrated the potential of OHPP as a new excipient and carrier to enable or enhance poorly water-soluble AIs, including active food ingredients and active pharmaceutical ingredients.
Yao, Purdue University.
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