Design of fenofibrate microemulsion for improved bioavailability

Hu, Liandong; H, Wu; Niu, F.; Yan, Cong-hua; Yang, Xihua; Jia, Yanhong

doi:10.1016/j.ijpharm.2011.08.043

Cited by 55 publications

(34 citation statements)

References 16 publications

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“…[11][12][13][14][15][16][17][18][19] Nanoemulsion formulations have been widely used to overcome problems related to the poor water solubility and low oral bioavailability of some drugs. [20][21][22][23][24][25][26] Therefore, amongst the various drug delivery systems, nanoemulsions are considered an ideal alternative for the oral administration of drugs with poor water solubility, as they improve absorption and bioavailability. At present, the US Food and Drug Administration has approved nanoemulsions of compounds with poor water solubility, including cyclosporin (Neoral ® , Gengraf ® ), 27,28 saquinavir (Fortovase ® ), 29,30 and ritonavir (Norvir ® ), 31 for clinical use.…”

mentioning

confidence: 99%

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Zhao¹,

Wei²,

Huang³

et al. 2013

IJN

112

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confidence: 99%

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Zhao¹,

Wei²,

Huang³

et al. 2013

IJN

112

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“…The mean droplet size was smaller than those found in other related studies. 10,32,34 The zeta potential of FVSMs was zero according to the result of the zeta potential analysis (data not shown), which indicated that there was no electrostatic action among the microemulsion drops. The morphology of microemulsions observed by TEM was spherical ( Figure 5), and the result of droplet size was consistent with that determined by the particle detector.…”

Section: Long-term Experimentsmentioning

confidence: 98%

“…The FVS could dissolve in the oily core and/or on the interface of these molecules, 32 therefore the selected oily vehicles including IPM and MCT showed higher solubility values than the other oil (soybean oil). Since the IPM is mainly used as a matrix and wetting agent of cosmetics, while MCT is widely used in medicines, food, health products, and cosmetics as a semisynthetic, functional oil, the MCT was consequently selected as the oil phase for further studies.…”

Section: Optimized Preparation Of Fvsms Optimization Of Blank Microemmentioning

confidence: 99%

“…The improvement of the FVS loading using o/w microemulsion depends on the solubility of the sterol in the dispersed oil phase and the percentage of that phase present. 32 The results of the stability tests which were used to select the optimum prescription were as shown in the in the following sections "high temperature experiments" and "long-term experiments. "…”

Section: −1mentioning

confidence: 99%

“…This indicates that FVSMs were physicochemically stable as reported by previous studies. 32 Microemulsions could be diluted by water in the gastrointestinal tract upon oral administration, which could lead to drug precipitation. Therefore, the nonprecipitation of the FVSMs after several dilutions is also a good step in the right direction.…”

Section: Long-term Experimentsmentioning

confidence: 99%

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Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Yi¹,

Zhong²,

Tong³

et al. 2012

IJN

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Purpose:To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluate the optimum microemulsion prescription, as well as the pharmacokinetics of encapsulated FVS. Methods: Molecules present in the FVS isolate were identified by gas chromatography/mass spectrometry analysis. The cell viability of FVS was assessed with methyl thiazolyl tetrazolium (MTT) bioassay. Based on the solubility study, phase diagram and stability tests, the optimum prescription of F. velutipes sterol microemulsions (FVSMs) were determined, followed by FVSMs characterization, and its in vivo pharmacokinetic study in rats. ). The optimal FVSMs prescription consisted of 3.0% medium chain triglycerides, 5.0% ethanol, 21.0% Cremophor EL and 71.0% water (w/w) with associated solubility of FVS being 0.680 mg ⋅ mL −1 as compared to free FVS (0.67 µg ⋅ mL −1 ). The relative oral bioavailability (area-under-the-curve values of ergosterol and 22,23-dihydroergosterol showed a 2.56-fold and 4.50-fold increase, respectively) of FVSMs (mean diameter ∼ 22.9 nm) as against free FVS were greatly enhanced. Our laboratory has been able to screen out lipid soluble sterols with an antitumor effect from F. velutipes by lipidraft chromatography, which was found to be linked to the tyrosine kinase receptor (data not published). In this study, our laboratory was interested in performing a preliminary investigation of the anticancer potential and bioavailability of F. velutipes sterol (FVS) as an in-depth contribution to the research of F. velutipes. FVS is a white powder, which can easily dissolve in ether, chloroform, hot ethanol, and other organic solvents, but barely dissolves in water. As a result, it is necessary to find a method to improve the solubility and oral bioavailability of this sterol. Dovepress 5067 O R I G I N A L R E S E A R C HMicroemulsions are thermodynamically stable nanometer systems with characteristics of easy preparation, small droplet size, low viscosity, and strong solubilization effect. 12It is formed spontaneously by water, oil, surfactant and cosurfactant. 13,14 According to the structure of a microemulsion, it can be divided into water-in-oil (w/o), oil-in-water (o/w) and bicontinuous microemulsion. 15 As a drug carrier, a microemulsion can increase the solubility and oral bioavailability of poorly soluble drugs, ameliorate the localization, improve systemic delivery of the drug, and possess the ability of targeting drug release. [16][17][18] The absolute bioavailability of a poorly soluble drug cyclosporin A which was loaded into a microemulsion system was increased to about 3.3-and 1.25-fold compared with free Sandimmun and Sandimmun Neoral (Novartis, Basel, Switzerland), which were used as commercial cyclosporin A. 19 In addition, it has been confirmed that the microemulsion system containing the poorly soluble drug docetaxel could improve the solubilization property and oral bioavailability of the drug. 20 Presently, there a...

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Microemulsions for Drug Solubilization and Delivery

Wang¹,

Zhang²

2013

Drug Delivery Strategies for Poorly Water‐Soluble Drugs

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Design of fenofibrate microemulsion for improved bioavailability

Cited by 55 publications

References 16 publications

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Microemulsions for Drug Solubilization and Delivery

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