Formulation of fenofibrate capsules by dropping method using PEG 6000 and PEG 4000 to enhance solubility

Abstract

The primary aim of the study was to enhance the dissolution rate of fenofibrate, a poorly soluble drug classified under BCS class II. To achieve this, solid dispersions were formulated using the dropping method with polyethylene glycol (PEG) 4000 and PEG 6000 at ratios of 1:1 and 1:2. These formulations were encapsulated and subjected to various evaluations, including solubility tests, assays, FTIR, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and in-vitro dissolution studies. The most effective formulation was then compared to a commercially available product. The formulation identified as D4, which utilized PEG 6000 at a 1:2 ratio via the dropping method, exhibited the highest solubility at 0.678 ± 0.07 mg/ml, a significant improvement over the pure drug's solubility of 0.018 mg/ml. The assay of D4 showed 98.14 ± 12%, with a practical yield of 95.25 ± 0.17%. In vitro dissolution testing revealed that the solid dispersions released the drug within 60 minutes, while the D4 formulation achieved a release of 99.10 ± 0.18% in just 30 minutes. This performance was notably superior to the pure drug, which had a release rate of 27.38 ± 0.10% in 60 minutes, and comparable to the marketed micronized fenofibrate capsule (Lipicard), which had a release rate of 93.91 ± 0.12% in 30 minutes. FTIR analysis indicated no interaction between the drug and the excipients, while XRD and DSC studies confirmed that the drug in the solid dispersion was in an amorphous state. The optimized formulations demonstrated stability over time. Thus, employing the dropping method with a minimal carrier ratio of 1:2 significantly improved the drug release profile, making it comparable to the micronized fenofibrate (Lipicard).