摘要
在各种不同的药物传递装置中,纳米脂质体是癌症治疗中一个新兴的制剂。在这里,我们已经开发枸橼酸他莫昔芬与磷酸乙醇胺(PE)结合(TC)采用薄膜水化的方法负载纳米脂质体。进行了如药物 - 赋形剂相互作用、表面形态、能量色散x射线分析,电动电势,体外药物释放,细胞吸收,体外细胞毒性试验和体内药代动力学特性的各种物理化学和生物制药表征研究。TC-装载纳米脂质体(TNL1)和PE缀合的TC-装载纳米脂质体(TNL-PE)分别显示3.23±0.26%和3.07±0.05%药物负载值。纳米脂质体的平均直径(Z平均)在100纳米内,负电位电势,TNL1和TNL-PE 30小时药物释放的累积百分比分别为75.77±12.21%和61.04±10.53%。两种纳米脂质在MCF-7中乳腺癌细胞中显现主要摄取。TNL1和TNL-PE降低细胞活力分别从95.95±0.37至12.22±0.64%和从96.51±0.24至13.49±0.08%。体内药代动力学研究表明,TNL-PE的AUC 0-∞,AUMC0-∞,MRT,和T1 / 2值同游离药物相比分别增加(22%,100%,2.66倍和60%)。TNL-PE监管比游离药物减少肾清除率值(大约38%)。TNL1和TNL-PE以持续的方式释放药物。此外,TNL-PE可以作为乳腺癌细胞的有效靶向当其与特定的抗体PE——一个链接器分子标记时。
关键词: MCF-7乳腺癌细胞系、磷酸乙醇胺共轭纳米脂质体、持续方式、他莫昔芬柠檬酸盐
图形摘要
Current Cancer Drug Targets
Title:Development of Linker-Conjugated Nanosize Lipid Vesicles: A Strategy for Cell Selective Treatment in Breast Cancer
Volume: 16 Issue: 4
Author(s): Niladri Shekhar Dey, Biswajit Mukherjee, Ruma Maji, Bhabani Sankar Satapathy
Affiliation:
关键词: MCF-7乳腺癌细胞系、磷酸乙醇胺共轭纳米脂质体、持续方式、他莫昔芬柠檬酸盐
摘要: Among the various drug delivery devices, nanoliposome is an emerging formulation in the treatment of cancer. Here we have developed tamoxifen citrate (TC) loaded nanoliposome conjugated with phosphoethanolamine (PE) by thin film hydration method. Various physicochemical and biopharmaceutical characterization studies such as drug-excipients interaction, surface morphology, energy dispersive X-ray analysis, zeta potential, in vitro drug release, cellular uptake, in vitro cytotoxicity assay and in vivo pharmacokinetic profiles were conducted. TC-loaded nanoliposome (TNL1) and PE-conjugated TC-loaded nanoliposome (TNL-PE) showed 3.23±0.26% and 3.07±0.05% drug loading values, respectively. Average diameters (z-average) of the nanoliposomes were within 100 nm, with negative zeta potentials and cumulative percentages of drug release were 75.77±12.21% and 61.04±10.53% at 30 h for TNL1 and TNL-PE respectively. Predominant uptake of both the types of nanoliposomes was visualized in MCF-7 breast cancer cells. TNL1 and TNL-PE decreased the cell viability from 95.95±0.37 to 12.22±0.64% and from 96.51±0.24 to 13.49±0.08% respectively. In vivo pharmacokinetic study showed that AUC 0-∞, AUMC0-∞, MRT, and t1/2 value of TNL-PE increased (22%, 100%, 2.66 fold and 60% respectively) as compared to the free drug. Administration of TNL-PE decreased the renal clearance value (about 38%) as compared to the free drug. TNL1 and TNL-PE released the drug in a sustained manner. Further, TNL-PE may be used for active targeting for breast cancer cells when it is tagged with specific antibodies to PE, a linker molecule.
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Cite this article as:
Niladri Shekhar Dey, Biswajit Mukherjee, Ruma Maji, Bhabani Sankar Satapathy , Development of Linker-Conjugated Nanosize Lipid Vesicles: A Strategy for Cell Selective Treatment in Breast Cancer, Current Cancer Drug Targets 2016; 16 (4) . https://dx.doi.org/10.2174/1568009616666151106120606
DOI https://dx.doi.org/10.2174/1568009616666151106120606 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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