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ZHANG Yong, GAO Minjiao, ZHANG Laifang, HUO Meirong, PENG Xiaoling, ZHOU Jianping. Cyclosporine A-loaded albumin nanoparticles:preparation, in vitro release and evaluation of pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2013, 44(3): 239-243. DOI: 10.11665/j.issn.1000-5048.20130310
Citation: ZHANG Yong, GAO Minjiao, ZHANG Laifang, HUO Meirong, PENG Xiaoling, ZHOU Jianping. Cyclosporine A-loaded albumin nanoparticles:preparation, in vitro release and evaluation of pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2013, 44(3): 239-243. DOI: 10.11665/j.issn.1000-5048.20130310

Cyclosporine A-loaded albumin nanoparticles:preparation, in vitro release and evaluation of pharmacokinetics in rats

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  • Cyclosporine A-loaded human serum albumin nanoparicles(CyA-HSA)were prepared and physicochemical properties including entrapment efficiency, drug-loading capability, particles size, Zeta potential, morphology, pH value and osmotic pressure were evaluated. Dialysis was undertaken to investigate the release of CyA from CyA-HSA nanoparticles in vitro. The obtained CyA-HSA nanoparticles showed spherical shape with mean particle sizes of 240. 5 nm and Zeta potential of -32. 0 mV. The drug-loading amount and entrapment efficiency were 14. 7% and 85. 8%, respectively. The pH and osmotic pressure of nanoparticles were 7. 0 and 314. 7 mOsmol/kg, respectively. CyA-HSA nanoparticles exhibited better dilution stability than commercial cyclosporine A injection, Sandimmune® . Both CyA-HSA and Sandimmune® exhibited significant sustained release behavior in vitro and both release profiles displayed a zero-order process. The pharmacokinetic study at equal administration dosage(7 mg/kg)in rats showed that cyclosporine A concentration-time data were in accordance with the two-compartment model. The CL and k10 of CyA-HSA significantly decreased and AUC significantly increased compared to those of Sandimmune® (P< 0. 05). CyA-HSA nanoparticles showed obvious solubility enhancement, sustained release and less side effect and toxicity resulting from solubilizing agent of Sandimmune® , Cremophor EL, and might be developed as the next generation dosage form of cyclosporine A.
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