Department of Molecular Biology and Immunology, and Institute for Cancer Research, Graduate School of Biomedical Sciences, University of North Texas Health Science Center, Fort Worth, Texas, 76107, USA.
Anticancer Res. 2013 Sep;33(9):3603-9.
Liposome-based drug delivery has been successful in the past decade, with some formulations being Food and Drug Administration (FDA)-approved and others in clinical trials around the world. The major disadvantage associated with curcumin, a potent anticancer agent, is its poor aqueous solubility and hence low systemic bioavailability. However, curcumin can be encapsulated into liposomes to improve systemic bioavailability.
We determined the antitumor effects of a liposomal curcumin formulation against human MiaPaCa pancreatic cancer cells both in vitro and in xenograft studies. Histological sections were isolated from murine xenografts and immunohistochemistry was performed.
The in vitro (IC50) liposomal curcumin proliferation-inhibiting concentration was 17.5 μM. In xenograft tumors in nude mice, liposomal curcumin at 20 mg/kg i.p. three-times a week for four weeks induced 42% suppression of tumor growth compared to untreated controls. A potent antiangiogenic effect characterized by a reduced number of blood vessels and reduced expression of vascular endothelial growth factor and annexin A2 proteins, as determined by immunohistochemistry was observed in treated tumors.
These data clearly establish the efficacy of liposomal curcumin in reducing human pancreatic cancer growth in the examined model. The therapeutic curcumin-based effects, with no limiting side-effects, suggest that liposomal curcumin may be beneficial in patients with pancreatic cancer.
过去十年，基于脂质体的药物递送取得了成功，一些制剂已获得美国食品和药物管理局（FDA）批准，还有一些制剂正在全球范围内进行临床试验。与姜黄素（一种有效的抗癌剂）相关的主要缺点是其水溶性差，因此系统生物利用度低。然而，姜黄素可以被包封在脂质体中以提高系统生物利用度。
我们测定了脂质体姜黄素制剂对体外和异种移植研究中的人 MiaPaCa 胰腺癌细胞的抗肿瘤作用。从鼠异种移植肿瘤中分离出组织学切片，并进行免疫组织化学分析。
体外（IC50）脂质体姜黄素增殖抑制浓度为 17.5 μM。在裸鼠异种移植肿瘤中，每周腹腔注射三次 20mg/kg 的脂质体姜黄素，连续四周，与未治疗的对照组相比，肿瘤生长抑制率为 42%。通过免疫组织化学分析观察到，在治疗的肿瘤中观察到了一种强烈的抗血管生成作用，表现为血管数量减少，血管内皮生长因子和膜联蛋白 A2 蛋白的表达减少。
这些数据清楚地确立了脂质体姜黄素在减少所检查模型中人类胰腺癌细胞生长方面的疗效。基于姜黄素的治疗效果没有限制副作用，表明脂质体姜黄素可能对胰腺癌患者有益。
