Journal
NANOSCALE RESEARCH LETTERS
Volume 14, Issue 1, Pages -Publisher
SPRINGEROPEN
DOI: 10.1186/s11671-019-3164-y
Keywords
Daidzein; Long-circulating liposome; Encapsulation efficiency; In vitro release; Pharmacokinetics
Funding
- major technological innovation project of Hubei Province [2016ACA140]
- united fund for innovation and entrepreneurship of Ministry of Education of China [201610512001]
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In this study, daidzein long-circulating liposomes (DLCL) were prepared using the ultrasonication and lipid film-hydration method. The optimized preparation conditions by the orthogonal design was as follows: 55 to 40 for the molar ratio of soybean phosphatidylcholine (SPC) to cholesterol, 1 to 10 for the mass ratio of daidzein to total lipid (SPC and cholesterol) (w:w), the indicated concentration of 5% DSPE-mPEG2000 (w:w), 50 degrees C for the hydration temperature, and 24 min for the ultrasonic time. Under these conditions, the encapsulation efficiency and drug loading of DLCL were 85.3 +/- 3.6% and 8.2 +/- 1.4%, respectively. The complete release times of DLCL in the medium of pH 1.2 and pH 6.9 increased by four- and twofold of that of free drugs, respectively. After rats were orally administered, a single dose of daidzein (30 mg/kg) and DLCL (containing equal dose of daidzein), respectively, and the MRT0-t (mean residence time, which is the time required for the elimination of 63.2% of drug in the body), t(1/2) (the elimination half-life, which is the time required to halve the plasma drug concentration of the terminal phase), and AUC(0-t) (the area under the plasma drug concentration-time curve, which represents the total absorption after a single dose and reflects the drug absorption degree) of daidzein in DLCL group, increased by 1.6-, 1.8- and 2.5-fold as compared with those in the free group daidzein. Our results indicated that DLCL could not only reduce the first-pass effect of daidzein to promote its oral absorption, but also prolong its mean resident time to achieve the slow-release effect.
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