Design of Coenzyme Q10 solid dispersion for improved solubilization and stability.

Abstract

Solubilization and stabilization of poorly soluble drugs are important issues in the pharmaceutical industry. Herein, a Coenzyme Q10 (CQ10) solid dispersion (SD) formulation was designed to enhance CQ10 solubility, dissolution (%), and stability. CQ10 SD formulations were prepared with a dual polymer system using a melting method. The physicochemical properties of the SD formulations were evaluated. Poloxamer 407 (Kolliphor® P407) was chosen as the main solubilizer based on solubility test results, and polyvinylpyrrolidone (Kollidon® 17) was selected as the co-solubilizer based on pre-dissolution test results. Moreover, Aerosil®200 was chosen as the carrier based on pre-dissolution test results. The SD7 formulation (weight ratio, CQ10 : Aerosil® 200 : P407®: K17® = 1 : 4 : 4 : 1) showed 29-/95-/26-fold enhancement if dissolution (%), compared to that of commercial products at pH 1.2 buffer, distilled water, and pH 6.8 buffer, respectively. Moreover, the SD7 formulation was more stable than the other SD formulations at room temperature following 9 months of storage. In conclusion, a CQ10 SD formulation with significantly improved dissolution (%) and stability was developed. Thus, the SD7 formulation is expected to show improved bioavailability and effectiveness in the treatment of aging-related and cardiovascular diseases.