Enhancing solubility and bioavailability of coenzyme Q(10:) formulation of solid dispersions using Soluplus (R) as a carrier

Abstract

Improving the aqueous solubility of poorly soluble compounds have been a major issue in the pharmaceutical industry. In the present study, binary amorphous solid dispersions (SDs) of Coenzyme Q10 (CoQ(10)), a biopharmaceutics classification system (BCS) II compound and Soluplus (R) were prepared to enhance the solubility and pharmacokinetic properties compared to crystalline CoQ(10). SDs were prepared with different ratios of CoQ(10) and Soluplus (R) (1:3, 1:5, and 1:7) using spray drying technology, and the physicochemical properties of the SDs were evaluated. X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy suggested the conversion of the crystalline form of CoQ(10) to a binary amorphous system in the SDs. Fourier transform infrared spectroscopy revealed no potential interactions between CoQ(10) and Soluplus (R). The solubility of the optimal SD formulation (SD 1:7) was approximately 9000-fold higher than that of crystalline CoQ(10,) and the increment was Soluplus(R) concentration dependent. As a result, optimized SD 1:7 also showed significantly enhanced dissolution rate where maximum drug release was observed within 30 min in two different dissolution media. Moreover, in contrast to crystalline CoQ(10,) CoQ(10) SDs showed improved pharmacokinetic parameters. Thus, the SD 1:7 formulation is expected to improve biopharmaceutical properties and therapeutic efficacy of CoQ(10).