Particle engineering of fenofibrate for advanced drug delivery system

Joshi, Ramakant; Raje, Srajan; Akram, Wasim; Garud, Navneet

doi:10.1186/s43094-019-0010-0

Cited by 7 publications

(3 citation statements)

References 11 publications

(13 reference statements)

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“…In-vitro drug release [29,30] : Drug release profile of solid dispersions were determined by dissolution rate test apparatus USP Type II by Veego. Phosphate buffer 7.4 used as dissolution media and temperature was maintained at 37±0.1 0 C to simulate body temperature.…”

Section: Mt = Theoretical Amount Of Drug In Solid Dispersionmentioning

confidence: 99%

Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

2022

pnr

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This research work designed to overcome the problems associated with poorly aqueous soluble drug. Fenofibrate (FENO) being BCS Class II drug shows low solubility but permeability is high. Compatibility of the drug and polymer studies was done by FTIR. Physical mixtures (PM) of the drug and polymer HPMCAS were prepared by trituration method. Fenofibrate solid dispersions (SD) were prepared by common solvent technique ascribed feasibility in laboratory scale. Physical state of formulations was characterized by powder XRD, TGA. Solubility of pure drug (FENO), Physical mixture and SD found to be 0.3, 0.78±0.15 to 1.15±0.28 and 2.17±0.37 to 3.25±0.14 mg/ml respectively. Percentage yield and percentage drug content were determined and found within satisfactory range. The maximum cumulative percentage of drug release from pure drug (FENO), Physical mixture and SD found to be 34.5%, 72.1 and 97.2% respectively at 60 minutes. Microscopy (SEM) study was found that the prepared solid dispersion has porous morphology. The present study establishes the increased bioavailability of the optimized batch when compared with the pure FENO. There was significant (50%) increase in absorption of Fenofibrate observed from the in vitro everted gut sac model. SD of FENO was developed successfully. The solubility of FENO was ameliorated significantly while compared with API (pure FENO). This research work found formulation of SD preferable technique to enhance solubility and enhance dissolution of lipophilic drugs.

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Section: Mt = Theoretical Amount Of Drug In Solid Dispersionmentioning

confidence: 99%

Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

2022

pnr

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“…The physicochemical properties of the drug molecule are modified once it gets converted into co-crystal but its intrinsic activity is preserved. Thus co-crystals of many class II drugs have shown improved dissolution rate (comparable to amorphous form) and long term chemical and physical stability [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of buccal films of piroxicam co-crystals

Ammanage¹,

Rodriques²,

Kempwade³

et al. 2020

Futur J Pharm Sci

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Background The aim of the present study was to enhance the solubility of piroxicam (BCS class II drug) using co-crystallization technique and formulate the buccal films of selected co-crystals for improved therapeutic utilization of drug. Co-crystals of drug with various co-formers (molar ratio 1:1) were prepared by solvent evaporation method and were screened for their aqueous solubility and percent drug content. The formation of co-crystals was confirmed by FTIR, DSC and XRD. Piroxicam co-crystals loaded buccal films were prepared and evaluated for in vitro drug release, ex vivo drug permeation while safety of formulation was determined by histopathological study. Results The co-crystals prepared with different co-formers have proved their potential to improve the solubility of the drug. Co-crystals of piroxicam-sucralose have shown six-folds more solubility than parent drug. FTIR analysis indicated shifting in characteristics peaks of piroxicam. DSC analysis showed an extra exothermic peak and alteration in characteristic endothermic peak. The powder x-ray diffraction pattern exhibited changes in 2θ values of intense peaks. Thus, formation of co-crystal was confirmed. Physical characters of buccal films were found to be within limits. Formulation F6 showed highest mucoadhesive strength (5617 ± 636 dynes /cm2) while formulation F2 showed highest in vitro drug release after 8 h, i.e., 94.557%. The ex vivo drug permeation of F2 was found to be 84.74%. The hisopathological study revealed that there was no damage to buccal mucosal tissue and was found to be intact. Conclusion The piroxicam-suralose co-crystals based mucoadhesive films of piroxicam could be a better formulation approach with improved solubility, safety, and therapeutic efficacy as compared to conventional tablets. Graphical abstract

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“…This drug is used mostly in lipid regulation as it decreases low-Density Lipoprotein (LDL) and Very-Low Density Lipoprotein (VLDL) levels and increases High-Density Lipoprotein (HDL) level. The cocrystals of FNO are reported with tartaric acid [3] , saccharin, succinic acid, sucrose [4] , Polyethylene Glycol (PEG) 4000 by ball milling technique [5] , nicotinamide by different techniques like cogrinding, slurry method, antisolvent precipitation and screening by Hansen solubility parameters [6][7][8] .…”

Section: Fenofibratementioning

confidence: 99%

Fenofibrate-Nicotinamide Cocrystals: Molecular Docking Studies and Evaluation in Tablet Dosage Form

Shete¹,

Shah²,

Bhosale³

et al. 2022

IJPS

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The objectives of present investigation were to evaluate prepared cocrystals of fenofibrate and nicotinamide for pre-compression characteristics, docking studies for target peroxisome proliferator-activated receptor alpha, evaluate performance of cocrystals in tablet dosage form and to carry out in vivo antihyperlipidemic activity. The cocrystals were prepared by antisolvent addition method. Docking studies of cocrystals and pure fenofibrate against of target peroxisome proliferator-activated receptor alpha were carried out by using PyRx (version 0.8) docking tool, AutoDock Vina as docking program. The prepared cocrystals were evaluated for pre-compression properties like angle of repose, bulk density and Carr's index. Cocrystals were formulated in tablet dosage form and evaluated for official and unofficial quality control tests. The antihyperlipidemic activity carried out in rats by using Triton X-100 induced hyperlipidemia model. Cocrystals binds with peroxisome proliferator-activated receptor alpha with more binding affinity as compared with fenofibrate. Cocrystal shows binding energy of -9.3 kcal/mol while fenofibrate shows -8.5 kcal/mol. The pre-compression properties were within the limits of United States Pharmacopeia guidelines. The pure fenofibrate tablet showed 24.7 % drug release at the end of 90 min and cocrystal based tablet showed 100 % at 45 min. There was no statistically significant difference in values for all biochemical parameters in case of in vivo activity for cocrystals in comparison with pure fenofibrate. From the docking studies we can conclude that cocrystals showed stronger more substantial formed stable complexes with target peroxisome proliferator-activated receptor alpha, but no statistically significant difference in pharmacodynamic studies.

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Particle engineering of fenofibrate for advanced drug delivery system

Cited by 7 publications

References 11 publications

Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

Formulation and evaluation of buccal films of piroxicam co-crystals

Fenofibrate-Nicotinamide Cocrystals: Molecular Docking Studies and Evaluation in Tablet Dosage Form

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