Preparation of bionic lovastatin-loaded nanostructured lipid carrier and its<i> in vitro</i> targeting and<i> in vivo</i> pharmacokinetics in rabbits

CHEN Yao; GU Xiao

doi:10.11665/j.issn.1000-5048.20140507

Journal of China Pharmaceutical University > 2014 > 45(5): 544-550. > DOI: 10.11665/j.issn.1000-5048.20140507

CHEN Yao, GU Xiao. Preparation of bionic lovastatin-loaded nanostructured lipid carrier and its in vitro targeting and in vivo pharmacokinetics in rabbits[J]. Journal of China Pharmaceutical University, 2014, 45(5): 544-550. DOI: 10.11665/j.issn.1000-5048.20140507

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Preparation of bionic lovastatin-loaded nanostructured lipid carrier and its in vitro targeting and in vivo pharmacokinetics in rabbits

CHEN Yao¹,
GU Xiao²

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Abstract

Lovastatin-loaded nanostructured lipid carrier(LT-NLC)was prepared by lovastatin(LT)and the lipid components of high density lipid protein(HDL). The physicochemical parameters of LT-NLC were characterized in terms of morphology, particle size, Zeta potential, entrapment efficiency, and crystallization behavior. The LT-NLC-apoprotein(LT-NLC-apo), represented effective form in vivo, was prepared by incubating LT-NLC with native HDL. The escaping ability from macrophage cells phagocytosis and targeting effect to foam cells were evaluated, and the pharmacokinetic behavior was invesigated on rabbits. The results showed that LT-NLC was solid spherical or oval in shape with an average diameter of(14. 6±2. 0)nm, Zeta potential of(-32. 3±0. 4)mV and entrapment efficiency of(96. 2±1. 3)%. Phagocytosis studies showed that endogenous LT-NLC-apo can escape phagocytosis and target to foam cells. Pharmacokinetic data also prove that LT-NLC can escape phagocytosis effectively and extend the circulating time in vivo. The study indicated that non-protein NLC-resembling HDL could be a useful tool to deliver lipophilic anti-atherogenic drugs to foam cells.
- lovastatin,
- nanostructured lipid carrier,
- targeting,
- pharmacokinetics

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