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Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes.

Wei Y, Guo J, Zheng X, Wu J, Zhou Y, Yu Y, Ye Y, Zhang L, Zhao L - Int J Nanomedicine (2014)

Bottom Line: 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 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.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China.

ABSTRACT
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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The in vitro release profile of BA solution and BA-LP.Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.
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f2-ijn-9-3623: The in vitro release profile of BA solution and BA-LP.Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.

Mentions: In the in vitro release study, dialysis bag method was chosen for separation of free BA from BA-LP, and the results are shown in Figure 2 and Table 2. BA solution (BA was dissolved in 0.1% NaOH, then HCl was used to adjust to pH 7.3) released rapidly and was almost completed within 8 hours. However, the BA-LP released 35%±0.65%, 68%±1.01% and 82%±1.67% of BA within 2, 8, and 20 hours of dialysis, respectively.


Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes.

Wei Y, Guo J, Zheng X, Wu J, Zhou Y, Yu Y, Ye Y, Zhang L, Zhao L - Int J Nanomedicine (2014)

The in vitro release profile of BA solution and BA-LP.Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4128791&req=5

f2-ijn-9-3623: The in vitro release profile of BA solution and BA-LP.Abbreviations: BA, baicalin; BA-LP, BA-loaded liposome.
Mentions: In the in vitro release study, dialysis bag method was chosen for separation of free BA from BA-LP, and the results are shown in Figure 2 and Table 2. BA solution (BA was dissolved in 0.1% NaOH, then HCl was used to adjust to pH 7.3) released rapidly and was almost completed within 8 hours. However, the BA-LP released 35%±0.65%, 68%±1.01% and 82%±1.67% of BA within 2, 8, and 20 hours of dialysis, respectively.

Bottom Line: 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 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.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China.

ABSTRACT
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.

Show MeSH