Title In vitro and in vivo evaluation of oridonin-loaded long circulating nanostructured lipid carriers
Authors Jia, Lejiao
Shen, Jingyi
Zhang, Dianrui
Duan, Cunxian
Liu, Guangpu
Zheng, Dandan
Tian, Xiaona
Liu, Yue
Zhang, Qiang
Affiliation Shandong Univ, Dept Pharmaceut, Coll Pharm, Jinan 250012, Peoples R China.
Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100083, Peoples R China.
Shandong Univ, Dept Pharmaceut, Coll Pharm, 44 Wenhua Xilu, Jinan 250012, Peoples R China.
Keywords Oridonin
Nanostructured lipid carriers
Long circulating
In vitro release properties
Pharmacokinetics
NANOPARTICLES
NLC
DELIVERY
CELLS
BIODISTRIBUTION
STEARATE
BRAIN
SLN
Issue Date 2012
Publisher 国际生物大分子杂志
Citation INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES.2012,50,(3),523-529.
Abstract The purpose of this study was to develop poly(ethylene glycol)-coated nanostructured lipid carriers (PEG-NLC) for parenteral delivery of oridonin (ORI) to prolong drug circulation time in blood. Oridonin-loaded PEG-NLC (ORI-PEG-NLC) consisting of PEG(2000)-stearate, glycerol monostearate and medium chain triglycerides were prepared by emulsion-evaporation and low temperature-solidification technique. Oridonin-loaded NLC (ORI-NLC) were also prepared as control. ORI-PEG-NLC were observed by transmission election microscope and the morphology was in rotiform shape. The mean particle size of ORI-PEG-NLC was 329.2 nm and entrapment efficacy was 71.18%. The results of differential scanning calorimetry and X-ray diffraction revealed a low-crystalline structure of ORI and verified the incorporation of ORI into the nanoparticles. In vitro drug release of ORI-PEG-NLC exhibited biphasic drug release patterns with burst release initially and prolonged release afterwards. Pharmacokinetic analysis showed that the mean residence time of ORI-PEG-NLC was prolonged and AUC (area under tissue concentration-time curve) value was also improved compared with ORI-NLC and ORI solution. In conclusion, ORI-PEG-NLC could be a potential carrier to get prolonged retention time of oridonin in blood. (C) 2012 Elsevier B.V. All rights reserved.
URI http://hdl.handle.net/20.500.11897/233870
ISSN 0141-8130
DOI 10.1016/j.ijbiomac.2012.01.024
Indexed SCI(E)
Appears in Collections: 药学院
天然药物与仿生药物国家重点实验室

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