Volume 10 ; Issue 1 ; in Month : Jan-June (2026) Article No : 201
Karim MJ, Fazal B, Kori ML.

Abstract

Fenofibrate, a BCS class II drug, exhibits poor aqueous solubility, which limits its dissolution rate and oral bioavailability. The present study aimed to improve the physicochemical, dissolution, and pharmacological properties of fenofibrate through co-crystallization with a Generally Recognized as Safe (GRAS) co-former. Fenofibrate–benzoic acid co-crystals were prepared using the solvent drop grinding method in different stoichiometric ratios. Among the evaluated formulations, the 1:1 drug–co-former ratio produced stable and well-defined co-crystals. The formation of co-crystals was confirmed using Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), and Powder X-ray Diffraction (PXRD), which demonstrated the emergence of a new crystalline phase with altered thermal and structural properties. In-vitro dissolution studies revealed a significant enhancement in drug release from the optimized co-crystals, with approximately 89.83% cumulative drug release within 30 minutes, compared to 39.57% from pure fenofibrate and 61.91% from the marketed formulation. Dissolution kinetics followed a first-order release model. In-vivo antihyperlipidemic evaluation using a Triton X-100–induced hyperlipidemic rat model demonstrated that fenofibrate co-crystals significantly reduced serum total cholesterol, triglycerides, and low-density lipoprotein levels while increasing high-density lipoprotein levels when compared to the pure drug. Accelerated stability studies conducted at 40°C/75% RH for six months indicated improved stability of the co-crystals (73% drug content retained) compared to the pure drug (61%), with both formulations following first-order degradation kinetics. Overall, the study confirms that co-crystallization with benzoic acid is an effective and promising strategy to enhance the dissolution, stability, and antihyperlipidemic efficacy of fenofibrate, thereby offering potential for improved oral drug delivery and therapeutic performance.

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