期刊文献+

奥沙利铂聚乙二醇修饰脂质体的制备及其大鼠体内的药动学 被引量:4

Preparation and Pharmacokinetics of Oxaliplatin PEGylated Liposomes in Rats
原文传递
导出
摘要 采用逆相蒸发-挤出法制备奥沙利铂聚乙二醇(PEG)修饰脂质体,处方中蛋黄卵磷脂E80-胆固醇-聚乙二醇修饰二硬脂酰磷脂酰乙醇胺(PEG 2000-DSPE)重量比为100∶25∶34,药脂比为1∶10。所得制品平均粒径为140 nm,包封率97.5%。采用HPLC法测定大鼠血浆中的奥沙利铂,考察奥沙利铂PEG修饰脂质体静注给予大鼠的药动学情况,并与奥沙利铂溶液相比较。结果显示,奥沙利铂PEG修饰脂质体组的cmax和AUC均显著大于溶液组(P<0.05);平均滞留时间(MRT)比溶液组延长了约20倍。说明奥沙利铂PEG修饰脂质体能延长药物在大鼠体内的循环时间。 Oxaliplatin PEGylated liposomes were prepared by reverse phase evaporation-extrusion method. The liposomal membranes consisted of egg yolk lecithin E80, cholesterin and polyethylene glycol 2000-distearoylphosphatidylethanolamine (PEG 2000-DSPE) with weight ratio of 100 : 25 : 34. And drug-to-lipid ratio was 1 : 10. The average particle size of the product was about 140 nm with the encapsulation efficiency of 97.5 %. The concentration of oxaliplatin in rat plasma was determined by HPLC. The pharmacokinetics of oxaliplatin PEGylated liposomes in rats after iv administration was investigated with oxaliplatin solution as the control. The results showed that the c and A UC of the liposomes group were significantly higher than those of the solution group (P〈0.05). Compared with the solution group, the mean residence time (MRT) of liposomes group was increased by about 20 times. It indicated that the oxaliplatin PEGylated liposomes could prolong the circulation time in rats.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2012年第11期913-916,926,共5页 Chinese Journal of Pharmaceuticals
基金 2010年度上海市科技启明星(B类)(10QB1404100) 2009年上海市自然科学基金项目(09ZR1430900)
关键词 奥沙利铂 PEG修饰脂质体 制备 药动学 oxaliplatin PEGylated liposome preparation pharmacokinetics
  • 相关文献

参考文献12

  • 1Siegel R, Desantis C, Virgo K, et al. Cancer treatment and survivorship statistics, 2012 [J]. CA Cancer J Clin, 2012, 62 (4) : 220-241.
  • 2Ibrahim A, Hirschfeld S, Cohen MH, et al. FDA drug approval summaries: oxaliplatin [J]. Oncologist, 2004, 9 (1): 8-12.
  • 3Grolleau F, Gamelin L, Boisdron-Celle M, et al. A possible explanation for a neurotoxie effect of the anticancer agent oxaliplatin on neuronal voltage-gated sodium channels[J]. J Neurophysiol, 2001, 85 (5) : 2293-2297.
  • 4Cavaletti G, Tredici G, Petruccioli MG, et al. Effects of different schedules of oxaliplatin treatment on the peripheral nervous system of the rat [J]. Eur J Cancer, 2001, 37 (18): 2457-2463.
  • 5Krishnan AV, Goldstein D, Friedlander M, et al. Oxaliplatin and axonal Na+ channel function in vivo [J]. Clin Cancer Res, 2006, 12 (15) : 4481-4484.
  • 6Ehrsson H, Wallin I, Yachnin J. Pharmacokinetics of oxaliplatin in humans [J]. Med Oncol, 2002, 19 (4) : 261-265.
  • 7顾芃,陈建明.PEG化隐形纳米脂质体的研究进展[J].药学与临床研究,2011,19(1):47-50. 被引量:4
  • 8国家约典委员会编.曰家蓟舳标准新约转正标水笫35册[S].北京:化学工业出版社,2004.
  • 9Delord JP, Umlil A, Guimbaud R, et al. Population pharmacokinetics of oxaliplatin [J]. Cancer Chemother Pharmacol, 2003, 51 (2) : 127-131.
  • 10Brouwers EE, Tibben MM, Joerger M, et al. Determination of oxaliplatin in human plasma and plasma ultrafiltrate by graphite-furnace atomic-absorption spectrometry [J]. Anal Bioanal Chem, 2005, 382 (7) : 1484-1490.

二级参考文献28

  • 1施斌,方超,游美羡,裴元英.聚乙二醇修饰对羟喜树碱隐形纳米囊泡的肿瘤靶向和抑瘤作用的影响[J].中国临床药学杂志,2006,15(1):46-49. 被引量:15
  • 2Wang HJ,Zhao PQ,Liang XF,et al.Folate-PEG coated cationic modified chitosan-cholesterol liposomes for tumor-targeted drug delivery[J].Biomaterials,2010,31(14):4129-38.
  • 3Song SX,Liu D,Peng JL,et al.Novel peptide ligand directs liposomes toward EGF-R high-expressing cancer cells in vitro and in vivo[J].FASEB J,2009,23(5):1396-404.
  • 4Jung SH,Jung HS,Seong H,et al.Polyethylene glycolcomplexed cationic liposome for enhanced cellular uptake and anticancer activity[J].Int J Pharm,2009,382 (1-2):254-61.
  • 5Hong MH,Zhu SJ,Jiang YY,et al.Novel anti-tumor strategy:PEG -hydroxycamptothecin conjugate loaded transferrin-PEG-nanoparticles[J].J Control Release,2010,141 (1):22-9.
  • 6Orditura M,Quaglia F,Morgillo F,et al.Pegylated liposomal doxorubicin pharmacologic and clinical evidence of potent antitumor activity with reduced anthracycline-induced cardiotoxicity[J].Oncol Rep,2004,12 (3):549-56.
  • 7Dadashzadeh S,Vall AM,Rezaie M.The effect of PEG coating on in vitro cytotoxicity and in vivo disposition of topotecan loaded liposomes in rats[J].Int J Pharm,2008,353 (2):251-9.
  • 8Yang T,Choi MK,Cui FD,et al.Preparation and evaluation of paclitaxel -loaded PEGylated immunolip osome[J].J Control Release,2007,120(3):169-77.
  • 9Ryo S,Tomoko T,Yasubiro K,et al.Effective antitumor activity of oxaliplatin encapsulated in transferring -PEG-liposome[J].Int J Pharm,2008,346(2):143-50.
  • 10Phan G,Herbet A,Cholet S,et al.Pharmacokinetics of DTPA entrapped in conventional and long-circulating liposomes of different size for plutonium decorporation[J].J Control Release,2005,110(1):177-88.

共引文献3

同被引文献29

引证文献4

二级引证文献7

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部