[10] 何治堯， 何穀， 宋相容，等.甘草次酸修飾的長循環陽離子脂質體DNA複合物的製備[J].中國藥學雜誌， 2011， 11（46）： 846.
[11] Tian Q， Wang W， He X T， et al. Glycyrrhetinic acid-modified nanoparticles for drug delivery： preparation and characterization[J]. Chin Sci Bull， 2009， 54（18）： 3927.
[12] 張彥青，解軍波.正交試驗優選石杉堿甲脂質體的製備研究[J].中草藥，2009， 40（6）：896.
[13] 趙誌英，謝俊，劉文一，等.羥喜樹堿脂質體的製備及其大鼠體內組織分布的研究[J].中國中藥雜誌，2011， 36（4）：450.
[14] Ishida T， Ichihara M， Wang X， et al. Injection of PEGylated liposomes in rats elicits PEG-specific IgM， which is responsible for rapid elimination of a second dose of PEGylated liposomes[J]. J Controlled Release， 2006， 112： 15.
[15] 霍美蓉，張勇，周建平，等. N-辛基-O， N-羧甲基殼聚糖聚合物膠束對紫杉醇的增溶、緩釋及其安全性初步評價[J]. 藥學學報， 2008， 43（ 8）： 855.
[16] Dong Y， Feng S S. Methoxy poly （ethylene glycol） -poly （lactide） （MPEG-PLA） nanoparticles for controlled delivery of anticancer drugs [J]. Biomaterials， 2004， 25： 2843.
[17] Zhang Z，Feng S S. Nanoparticles of poly（lactide）/vitamin E TPGS copolymer for cancer chemotherapy： synthesis， formulation， characterization and in vitro drug release[J]. Biomaterials，2006，27（2）：262.
[18] Yu Fan， He Chenghua， Ayman Y Waddad， et al. N-octyl-N-arginine-chitosan （OACS） micelles for gambogic acid oral delivery： preparation， characterization and its study on in situ intestinal perfusion[J]. Drug Dev Ind Pharm， 2013， doi： 10.3109/03639045.
[19] Nicholas A R， Scott M J， Kennedy N I， et al. Effect of grafted polyethylene glycol （PEG） on the size， encapsulation efficiency and permeability of vesicles[J]. Biochim Biophys Acta，2000，1463：167.
[20] Li Jing， Huo Meirong， Wang Jing， et al. Redox-sensitive micelles self-assembled from amphiphilic hyaluronic aciddeoxycholic acid conjugates for targeted intracellular delivery of paclitaxel[J]. Biomaterials， 2011， 33： 2310.
[21] 喻樊，楊錦明.β-穀甾醇替代膽固醇構建槲皮素脂質體的可行性研究[J].中草藥， 2013，44（23）：3303.
[22] Moghimi S M， Davis S S. Innovations in avoiding particle clearance from blood by Kupffer cells： cause for reflection[J]. Crit Rev Ther Drug Carrier Syst， 1994， 11： 31.
Preparation of novel gypenosides long-circulating liposomes consisted by
sphingomyelin and β-sitosterol modified by PEG
YU Fan*， YANG Jing-ming， LI Jin-juan
（College of Pharmacy， Yancheng Teachers University， Yancheng 224051， China）
[Abstract] Objective： To explore the feasibility of preparing novel gypenosides long-circulating liposomes with PEG grafted on β-sitosterol （PEG-Sito）. Method： Succinicanhydride was adopted to connect β-sitosterol and PEG 2000. Sphingomyelin and PEG-Sito was used as material to prepare gypenosides long-circulating liposomes by using ethanol injection method. Encapsulation efficiency was determined by using protamine precipitation method. 1H-NMR was used to verify the synthesis of PEG-Sito， the novel gypenosides long-circulating liposomes were characterized by particle size， zeta potential and atomic force microscope. Result： The synthesis of PEG-Sito was verified by 1H-NMR. Encapsulation efficiency of long-circulating liposomes prepared by ethanol injection method was 74.3%， particle size was 288.1 nm，zeta potential was -20.25 mV， the morphology were round observed by AFM. Conclusion： The novel gypenosides long-circulating liposomes prepared with PEG-Sito was feasible， it had a high encapsulation efficiency and good morphology.
[Key words] gypenosides； long-circulating liposomes； β-sitosterol； PEG
doi：10.4268/cjcmm20140608