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叶酸纳米偶联紫杉醇在人卵巢癌裸鼠移植瘤中抗肿瘤效应的实验研究 被引量:2

Experimental Research of FR-targeted Liposomal Formulation of Paclitaxel against Human Ovarian Cancer Xenografts in Nude Mice Models
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摘要 目的通过动物实验探究叶酸纳米偶联紫杉醇对卵巢癌的治疗作用。方法体外培养人卵巢癌SKOV-3细胞,裸鼠皮下接种SKOV-3细胞建立裸鼠移植瘤动物模型,随机分为叶酸纳米偶联紫杉醇组(实验组,10mg/kg尾静脉注射)、紫杉醇组(对照组,10mg/kg尾静脉注射,每周给药2次,共4疗程)、每组各8只。观察移植瘤的生长情况,绘制裸鼠移植瘤的生长曲线,实验结束依肿瘤体积,计算肿瘤生长抑制率,光学显微镜及透射电子显微镜下观察组织形态和细胞超微结构的改变,同时采用TUNEL法检测各组细胞凋亡指数(apoptosis index,AI)。结果实验组裸鼠移植瘤体积明显小于对照组(P<0.05),实验组抑瘤率为38.1%。光学显微镜和透射电子显微镜观察可见实验组凋亡改变明显多于对照组。TUNEL法显示,实验组的AI为(53.45±6.82)%,与对照组比较差异有统计学意义(P<0.01)。结论叶酸纳米偶联紫杉醇药物,可能利用叶酸受体为作用靶点,将药物主动靶向肿瘤细胞,提高药物在肿瘤细胞内的分布,显示出了比传统的紫杉醇药物更好的抗肿瘤疗效。 Objective To explore the influence of folic acid receptor (FR)-targeted liposomal formulation of paclitaxel on human ovarian'cancer xenografts in nude mice models. Methods Human ovarian cancer xenografts in nude mice models were established by using of human ovary cancer cell line SKOV3, and randomly divided into 2 groups (n = 8) :the FR targeted liposomal formulation of paelitaxel (the experi ment group) group and the paclitaxel (the control group) group. The volumes and weight of tumor mass were detected, and the tumor inhibitory rates were calculated. The growth curves of xenograft tumors were draw up. Morphological changes and ultramicrostructure of ceils were observed with inverted phase contrast microscope and transmission electron microscope, respectively. Meanwhile,cell apoptosis was in vestigated with TUNEL staining. Results The tumor inhibitory rate of the experiment group was 38. 1%,which was significantly lower than that of the control group (P〈0. 05). The apoptosis index (AI) of the experiment group was(53.45 ±6.82)%, significant difference was found between the two groups(P〈0. 01 ). Conclusions FR-targeted liposomal formulation of paclitaxel may actively targeting the folie acid receptor,enable to deliver the nanoscale drugs directively into cancer cells,which could in- crease therapeutic effect of drug largely. Compared to traditional preparations, the novel FR-targeted nanoscale drug may offer a more promising approach for tumor targeting therapy.
作者 陈卫 李红霞
出处 《肿瘤防治研究》 CAS CSCD 北大核心 2013年第1期32-35,共4页 Cancer Research on Prevention and Treatment
基金 北京市科委资助项目(Z080507030808028)
关键词 叶酸受体 卵巢癌 紫杉醇 靶向治疗 Folic acid receptor Ovarian cancer Paclitaxei Tumor targeting therapy
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  • 1Ferlay J, Parkin DM, Steliarova-Foucher E. Estimates of cancer incidence and mortality in Europe in 2008[J]. Eur J Cancer, 2010,46(4):765-81.
  • 2Haley B, Frenkel E. Nanoparticles for drug delivery in cancer treatment[J]. Urol Oncol, 2008,26 ( 1 ) : 57- 64.
  • 3Li PY, Del Veccio S, Fonti R, et al. Local concentration of folate binding protein GP38 in sections of human ovarian carcino- ma by in vitro quantitative autoradiography[J]. J Nucl Med, 1996,37(4) :665-72.
  • 4Gabizon A, Shmeeda, H, Horowitz AT, et al. Tumor cell targeting of liposome entrapped drugs with phospholipid-anchored folic acid-PEG conjugates[J]. Adv Drug Deliv Rev, 2004, 56 (8):1177-92.
  • 5Low PS, Henne WA, Doorneweerd DD. Discovei:y and development of folic-acid based receptor targeting for imaging and therapy of cancer and inflammatory diseases [J]. Acc Chem Res,2008,41(1) :120-9.
  • 6Reddy JA,Westrick E, Santhapuram HK, et al. Folate recep tor specific antitumor activity of EC131, a folate-maytansinoid conjugate[J]. Cancer Res, 2007,67 (13): 6376-82.
  • 7lanes MG. Nanomaterials for practical functional uses[J]. J Alloys Compd, 2008,449 : 242-5.
  • 8Singh R, Lillard JW Jr. Nanoparticle-based targeted drug delivery[J]. Exp Mol Pathol,2009,86(3):215-23.
  • 9Letchford K,Burt H. A review of the formation and classification of amphiphilic block eopolymer nanopartieulate structures: micelles, nanospheres, nanocapsules and polymersomes [J]. Eur J Pharm Biopharm,2007,65(3) :259-69.
  • 10Xia W, Low PS. Folate-targeted therapies for cancer [J]. J Med Chem,2010,53(19) :6811-24.

同被引文献20

  • 1陈永法,龚明涛,张钧寿,谢燕.紫杉醇冻干纳米乳在大鼠体内的药动学[J].中国天然药物,2005,3(6):370-372. 被引量:6
  • 2易村犍,凌晟荣,陈克明.C-Kit和PDGFR-α在卵巢上皮性癌组织中的表达及临床意义[J].中国实用妇科与产科杂志,2006,22(4):295-296. 被引量:5
  • 3Ganta S,Devalapally H,Shahiwala A. A review of stimuli -responsive nanocarriers for drug and gene delivery. J ControlRelease, 2008,126 : 187 - 204.
  • 4Ruoslahti E,Bhatia SN, Sailor MJ. Targeting of drugs andnanoparticles to tumors. Cell Biol, 2010,188: 6759 - 6768.
  • 5WuJ,Liu Q , Lee RJ. A folate receptor - targeted liposomalformulation for paclitaxel. Int J of Pharm, 2006,316 : 148 -153.
  • 6Low PS,Henne WA,Doorneweered D. Discovery and de-velopment of folic - acid diseases . Acc Chem Res, 2008,41 :120-129.
  • 7Reddy JA, Westrick E, Santhapuram HK,et al. Folate re-ceptor- specific antitumor activity of EC 131,a folate - may-tansinoid conjugate . Cancer Res, 2007, 67: 6376 - 6382.
  • 8Xia W, Low PS. Folate - targeted therapies for cancer. JMed Chem, 2010, 53: 6811 - 6824.
  • 9Aronov 0,Horowitz AT,Gabizon A, et al. Folate~ targe-ted PEG as a potential carrier for carboplatin analogs. Syn-thesis and in vitro studys. Bioconjugate Chem,2003,14:563- 574.
  • 10Paranjpe PV, Chen Y, Kholodovych V, et al. Tumor - tar-geted bio - conjugate based delivery of camptothecin: design,synthesis and in vitro evaluation. J Control Release,2004,100: 275 - 292.

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