Octenylsuccinate hydroxypropyl phytoglycogen, a dendrimer-like biopolymer, solubilizes poorly water-soluble active pharmaceutical ingredients.

Effective solubilizers for poorly water-soluble active pharmaceutical ingredients (APIs) are highly desirable. This study introduced an amphiphilic dendrimer-like biopolymer, octenylsuccinate hydroxypropyl phytoglycogen (OHPP) as a new solubilizer. The molar substitution degree of octenylsuccinate and hydroxypropyl groups of OHPP was 0.51 and 1.69, respectively. The weight-average molecular weight, Z-average root mean square radius, and Zeta-potential of OHPP were 1.507×107g/mol, 22.6nm, and -23.6mV, respectively. OHPP was highly soluble in polar organic solvents and aqueous buffers with pH≥5.0. To evaluate its solubilization capability, each of five APIs (celecoxib, docetaxel, fenofibrate, griseofulvin, and resveratrol) was incorporated with OHPP to form solid dispersions (API-OHPP SD). API-OHPP SD reduced API crystallinity and increased API solubility by up to 1755 times. Over the 3h dissolution, the cumulative dissolved API with API-OHPP SD was in the range of 6.8∼84.9%. Evidently, OHPP was a potent and non-specific polymeric solubilizer of poorly water-soluble APIs.