Enhancing solubility and bioavailability of coenzyme Q10: formulation of solid dispersions using Soluplus® as a carrier

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 (CoQ₁₀), a biopharmaceutics classification system (BCS) II compound and Soluplus^® were prepared to enhance the solubility and pharmacokinetic properties compared to crystalline CoQ₁₀.

SDs were prepared with different ratios of CoQ₁₀ and Soluplus^® (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 CoQ₁₀ to a binary amorphous system in the SDs. Fourier transform infrared spectroscopy revealed no potential interactions between CoQ₁₀ and Soluplus^®. 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^® 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, CoQ₁₀ SDs showed improved pharmacokinetic parameters. Thus, the SD 1:7 formulation is expected to improve biopharmaceutical properties and therapeutic efficacy of CoQ₁₀.

Read the article here

Article information: Lamichhane, S., Seo, JE., Keum, T. et al. Enhancing solubility and bioavailability of coenzyme Q_10: formulation of solid dispersions using Soluplus^® as a carrier. Arch. Pharm. Res. 45, 29–37 (2022). https://doi.org/10.1007/s12272-022-01368-4