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载紫杉醇磁脂质体的体外应用于联合化疗和热疗。

In vitro application of paclitaxel loaded magnetoliposomes for combined chemotherapy and hyperthermia.

机构信息

WRCBB, Department of Biosciences and Bioengineering, Indian Institute of Technology, Bombay, Mumbai 400076, India.

出版信息

Colloids Surf B Biointerfaces. 2012 Aug 1;96:1-7. doi: 10.1016/j.colsurfb.2012.02.029. Epub 2012 Mar 3.


DOI:10.1016/j.colsurfb.2012.02.029
PMID:22521681
Abstract

Paclitaxel loaded thermosensitive magnetoliposomes containing 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 1-palmitoyl-2-oleoyl-sn-glycero-3-phospho-rac-glycerol (PG) were prepared by thin film hydration method. Encapsulation efficiencies of paclitaxel and citric acid coated Fe(3)O(4) nanoparticles were 83±3% and 74.6±5%, respectively. Based on the release study, DPPC/PG in 9:1 (w/w) liposomes (PCPG) formulation was found to be thermosensitive and showed 46 fold higher drug release at 43 °C than at 37 °C. Drug release was done under an alternating magnetic field of intensity 10 kA/m and a fixed frequency of 423 kHz. In-vitro cytotoxicity and hyperthermia studies were carried out using a human cervical cancer cell line (HeLa). IC(50) value of the magnetoliposomes formulation was 100 nM. When the magnetoliposomes with 100 nM drug was used to treat HeLa cells in combination with hyperthermia under AC magnetic field, 89% cells were killed and were found to be more effective than either hyperthermia or chemotherapy alone. So, PCPG liposomes which co-encapsulate both Fe(3)O(4) nanoparticles and paclitaxel may be useful for combined chemotherapy and hyperthermia.

摘要

载紫杉醇的热敏感载药磁脂体由 1,2-二棕榈酰-sn-甘油-3-磷酸胆碱 (DPPC) 和 1-棕榈酰基-2-油酰基-sn-甘油-3-磷酸-rac-甘油 (PG) 通过薄膜水化法制备。紫杉醇和柠檬酸包覆的 Fe3O4 纳米粒子的包封效率分别为 83±3%和 74.6±5%。基于释放研究,发现 DPPC/PG(w/w)比为 9:1 的脂(PCPG)制剂具有热敏感性,在 43°C 时比在 37°C 时药物释放增加了 46 倍。在强度为 10 kA/m 和固定频率为 423 kHz 的交变磁场下进行药物释放。采用人宫颈癌细胞系(HeLa)进行体外细胞毒性和热疗研究。磁脂体制剂的 IC50 值为 100 nM。当用 100 nM 药物的载药磁脂体与交变磁场下的热疗联合治疗 HeLa 细胞时,89%的细胞被杀死,比单独热疗或化疗更有效。因此,共包封 Fe3O4 纳米粒子和紫杉醇的 PCPG 脂体可能对联合化疗和热疗有用。

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