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

Zhao, Ling; Wei, Yumeng; Huang, Yu Jui; He, Bing; Zhou, Yang; Fu, Junjiang

doi:10.2147/ijn.s51578

Cited by 110 publications

(51 citation statements)

References 36 publications

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“…6 However, due to its low hydrophilicity and poor absorption following oral administration, the low oral bioavailability of BA limits its therapeutic efficacy and clinical application. 13,16 Therefore, on the basis of our previous studies, 23,24 the novel effervescent dispersion technique was used to develop BA-LP for the first time.…”

Section: Discussionmentioning

confidence: 99%

“…6,9,10 In order to overcome the shortcoming of BA, the development of novel dosages and formulations of BA has attracted an increasing attention in the pharmaceutical field in recent years. These have included microspheres, 11 microcapsules, 12 nanoemulsions, 13 inclusion complexes, 14,15 solid lipid nanoparticles, 16 BA-polyvinylpyrrolidone coprecipitate, and a BA-phospholipid complex. 17,18 Indeed, the studies have shown an increased solubility and improvement of oral bioavailability in the preclinical phase.…”

Section: Introductionmentioning

confidence: 99%

“…However, the currently marketed preparations, including BA capsules and tablets, have to be administered at a large dose to obtain effective drug plasma concentration, due to low oral bioavailability. 13 Therefore, it is necessary for us to develop a novel drug delivery system to improve the oral bioavailability of BA.…”

Section: Introductionmentioning

confidence: 99%

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Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween ® 80, Phospholipon ® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of −20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1−Q)) =0.609 lnt −1.230 ( r =0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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“…Recent reports suggested that the formulation of nanoemulsion and powdered nanocapsule can remarkably improve the bioavailability of the functional ingredients (Ragelle et al, 2012;Zhao et al, 2013). Furthermore, Ganesan et al (2015) reported that nano bioactive compounds from red ginseng are effective to chronic diseases since it has positive role in antidiabetic, aphrodisiac, cardiovascular and protective role in neurodegenerative diseases.…”

Section: Introductionmentioning

confidence: 99%

Optimized conditions to produce water-in-oil-in-water nanoemulsion and spray-dried nanocapsule of red ginseng extract

et al. 2018

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The aim of this study was to optimize conditions for producing water-in-oil-in-water (W/D/W) nanoemulsion and spray-dried nanocapsule of red ginseng extract. Based on emulsion stability and average particle size analysis, optimum conditions to produce W/D/W nanoemulsion were: ratio of core to coating material, 3:7; primary emulsifier, 10% polyglycerol polyricinoleate; ratio of W/D phase to coating material, 1.5:8.5; secondary emulsifier, 10% polyoxyethylene sorbitan monolaurate; solvent, 20% ethyl acetate; secondary coating material, 10% maltodextrin (MD). Under these optimized conditions, particle size of spray-dried nanocapsules coated with MD of red ginseng ranged from 100 nm to 500 nm, based on response surface methodology with the highest yield (up to 99.7%). Results of the present study can be used to further optimize conditions to produce W/D/W nanoemulsion and spray-dried nanocapsule of red ginseng extract.

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“…5 Baicalin is 7-d-glucuronic acid 5,6-dihydroxyflavone derived from the dried root of Scutellaria baicalensis Georgi, known as radix scutellariae, a basic and key medicinal composition unit in the traditional Chinese medicine. 6,7 Extensive studies have shown that baicalin has strong antitumor effects. [8][9][10] For the treatment of lung cancer, in vitro experiments, baicalin could suppress cell proliferation of human lung cancer A549 and mouse Lewis lung cancer in a dose-and time-dependent behavior.…”

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confidence: 99%