Pharmacological screening of fenofibrate-loaded solid dispersion in fructose-induced diabetic rat

Abstract

Objectives Hyperlipidaemia is a common phenomenon in diabetes mellitus. Fenofibrate (FF) is a good candidate for the treatment of lipid abnormalities in patients with type 2 diabetes. But the bioavailability as well as therapeutic efficacy of this drug is limited to its dissolution behaviour. Here, the authors assess the therapeutic efficacy of a newly formulated solid dispersion of fenofibrate (SDF) having enhanced dissolution profiles in contrast to pure FF using fructose-induced diabetic rat model. Methods Fructose-induced diabetic rat model was developed to assess the pharmacological efficacy of the formulated SDF, and the results were compared with the effects of conventional FF therapy. Key findings The 14 days treatment showed better improvement in lipid-lowering potency of SDF than pure FF. SDF containing one-third dose of pure FF showed similar effect in terms of triglyceride, total cholesterol and low-density lipoprotein lowering efficacy, whereas increased high-density lipoprotein at same extent. The similar dose of SDF produced more prominent effect than FF. Histological studies also demonstrated the enhanced lipid clearance from liver by SDF than FF that was concordant with the biochemical results. Conclusions This newly formulated SDF would be a promising alternative for conventional fenofibrate in treating hyperlipidaemia.

Development and Evaluation of Stable Paracetamol Loaded Solid Dispersion with Enhanced Analgesic and Hepatoprotective Property

“…In the acetic acid-induced writhing test PSD10 showed a significant decrease in the number of writhing by 1.44-fold greater compared to pure PCM at an equal dose (30 mg/kg). This result indicated that fast dissolution and subsequent rapid absorption of PCM occurred in GIT from the solid dispersion formulation (PSD10) as previously reported by various authors [43] [44] [45].…”

Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

“…[2] Fenofibrate (FENO) is a peroxisome proliferator-activated-α (PPAR α) receptor agonist used as a hypolipidemic drug, effective in the management of various forms of dyslipidemia. [3,4,5] As a PPAR α, it regulates gene/protein interactions which are associated in various pathological processes like regulation of β-oxidation of fatty acids, oxidative stress, inflammation and even cancer progression and tumorigenesis. [6] As a result of PPAR α activation of gene transcription and translation which leads to peroxisomes filled with hydrogen peroxide, reactive oxygen species and hydroxyl radicals act as participant in lipolysis.…”