Formulation and Characterization of Fenofibrate Loaded Solid Dispersion with Enhanced Dissolution Profile

Ghosh, Milon Kumar; Wahed, Mir Imam Ibne; Ali, M. A.; Barman, Ranjan Kumar

doi:10.4236/pp.2019.107028

Cited by 7 publications

(7 citation statements)

References 36 publications

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“…[ 32,33 ] In this study, we aimed to evaluate the in vivo antihyperlipidaemic efficacy of our newly developed formulation of FF that was previously reported as more efficient than pure drug in respect to in vitro drug release. [ 21 ] The fasting plasma glucose levels were significantly reduced among the treatment groups, of which, the most noticeable effect was found with SDF150 and was concordant with NC group (Figure 2). Almost same efficacy in reduction of blood glucose level was observed between FF150 and SDF50.…”

Section: Discussionmentioning

confidence: 71%

“…SDF was prepared using a blend of PEG‐4000 and Carplex‐80 as carriers in weight ratio of FF: PEG‐4000: Carplex‐80 = 1 : 5 : 6, respectively, by solvent evaporation method. [ 21 ]…”

Section: Methodsmentioning

confidence: 99%

“…This formulation was found with fast drug release (29.6 µg/ml) at 5 min, which was about 3.4‐fold higher than that of pure FF (8.8 µg/ml). [ 21 ] Physicochemical characterizations of SDF proved that this enhancement of dissolution attributed conversion to amorphous form from crystalline FF upon SD formation having no incompatibilities among FF and carriers used. In this study, we performed pharmacological evaluation of this new SDF formulation first time to explore the changes in corresponding biochemical parameters and histology of liver tissues.…”

Section: Introductionmentioning

confidence: 99%

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

Ghosh

Wahed

Khan

et al. 2020

Journal of Pharmacy and Pharmacology

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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.

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Section: Discussionmentioning

confidence: 71%

“…SDF was prepared using a blend of PEG‐4000 and Carplex‐80 as carriers in weight ratio of FF: PEG‐4000: Carplex‐80 = 1 : 5 : 6, respectively, by solvent evaporation method. [ 21 ]…”

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

Ghosh

Wahed

Khan

et al. 2020

Journal of Pharmacy and Pharmacology

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“…The reported approaches are solid dispersion, anti-solvent precipitation, dry suspension and dry emulsion, lipidic dispersion, nanosuspension, drug dispersion in carriers, selective adsorption on insoluble carrier, co-solvents, cryogenic techniques etc. [4][5] In recent years, a number of dispersion techniques have been introduced to stand against the obstacle with poorly water-soluble drugs without requiring expensive equipment or facilities. In dispersion technique, a drug substance is dispersed or embedded in a chemical entity so called carrier or continuous phase.…”

Section: Introductionmentioning

confidence: 99%

Cefuroxime Axetil Loaded Dispersed Formulation for Enhanced Drug Release and Antibacterial Activity

Salam¹,

Kumar²,

Salam³

et al. 2022

Ind. J. Pharm. Edu. Res

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Aim: Aqueous solubility of drugs is a determining factor for bioavailability in systemic circulation and confronts in the unbeaten formulation of therapeutic agents. Cefuroxime axetil (CA) is a broad-spectrum β-lactamase cephalosporin that pertains to class II drugs under Biopharmaceutical Classification System (BCS) with poor aqueous solubility and high absorption permeability after oral administration. The objective of this current work was to achieve the enhanced solubility in water and subsequent antibacterial activity of CA loaded coarse dispersion (CCD) formulations. Materials and Methods: CCDs were prepared by anti-solvent precipitation method by blending CA with a carrier, Microcrystalline cellulose (MCC) at different ratios. In-vitro dissolution test using paddle method and antibacterial study against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) were carried out for both pure CA and CCDs for performance comparison. Results: Among the formulations, CCD-3 exhibited maximized dissolution rate by 1.67-fold higher than that of pure CA with the drug-carrier (CA: MCC) ratio of 1:3. Antibacterial activity of CCD-3 against S. aureus and E. coli was also found by 1.75-fold and 5.25-fold higher relative zone of inhibition (RZOI), respectively than that of pure drug. Conclusion: As an optimized formulation, CCD-3 is a promising to be a fruitful substitute to conventional dosage forms of CA for the modified dissolution rate and antibacterial potency. However, before its recommendation as a novel formulation validation study to point its pharmacokinetics, competence with in-vivo antibacterial property and safety is needed.

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“…So it is necessary to increase the solubility and dissolution rate for poorly soluble drugs because low solubility has poor bioavailability [3]. Fenofibrate is one of the drugs belonging to class II in the BCS system (Biopharmaceutical Classification System), which is a third-generation fibric acid derivative with low solubility and high permeability [4]. Fenofibrate is a drug used to treat atherogenic dyslipidemia, which causes a substantial decrease in triglyceride-rich lipoproteins and increases in high-density lipoprotein (HDL) levels.…”

Section: Introductionmentioning

confidence: 99%

Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

Helsinta¹,

Halim²,

Octavia³

et al. 2021

IJPSM

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This review aimed to find information about the solubility of the fenofibrate solid dispersion system using PEG 6000. Fenofibrate is an antihyperlipidemic drug that belongs to the Biopharmaceutical Classification System Class II (BCS II) with low solubility. To find information was by conducting a literature search in national and international journals in the last ten years (2010-2020) through websites, namely Google Scholar, Science Direct, NCBI, ResearchGate, and other trusted journals. Several keywords were used as follows: fenofibrate, solid dispersion, PEG 6000, and dissolution rate. The results of several research journals showed that the solid dispersion of fenofibrate using PEG 6000 made by various methods causes a reduction in particle size to increase the solubility and dissolution rate of fenofibrate. The solid dispersions system was made using several methods, namely fusion (melting), solvent evaporation, dropping, and co-grinding, which is a technique used to increase the solubility of a drug. PEG 6000 was chosen as the carrier because it has high hydrophilicity, is non-toxic, inert, economical, has a low melting point, and is dense at melting temperature to withstand crystallization. Thus it can be concluded that the manufacture of solid dispersion of fenofibrate using PEG 6000 and several methods showed the same results, namely an increase in solubility and dissolution rate.

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Formulation and Characterization of Fenofibrate Loaded Solid Dispersion with Enhanced Dissolution Profile

Cited by 7 publications

References 36 publications

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

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

Cefuroxime Axetil Loaded Dispersed Formulation for Enhanced Drug Release and Antibacterial Activity

Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

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