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载姜黄素的温敏型液体黏附性制剂的体外生物相容性在结直肠肿瘤化学预防中的研究

In vitro biocompatibility of thermally gelling liquid mucoadhesive loaded curcuminoids in colorectal cancer chemoprevention.

机构信息

Division of Traumatology, Department of Surgery, Chi Mei Medical Center, Tainan, Taiwan.

出版信息

Int J Colorectal Dis. 2012 Jul;27(7):869-78. doi: 10.1007/s00384-011-1393-3. Epub 2012 Jan 7.

DOI:10.1007/s00384-011-1393-3
PMID:22222465
Abstract

PURPOSE

Colorectal cancer (CRC) is the third leading cause of cancer death in Taiwan; it ranks top three in the cancer mortality rate. Curcuminoids are derived from the rhizome of Curcuma longa. It has shown anti-cancer activity and apoptosis induction in a variety of cancer cell lines. This aims to study the potential of Poloxamer 407 as the thermogelling and mucoadhesive polymer for development of a site-targeting delivery system to enhance the localized delivery of curcuminoids to the colorectal cells for CRC chemotherapy.

METHODS

The mucoadhesive strength and rheological properties were measured as a function of poloxamer loaded with curcuminoids.

RESULTS

The gelation temperature of Poloxamer 407 was found to vary with its concentration and start gelling at 37°C at the concentration of 15.5% (w/v). To ensure gelation at physiological temperature after intra-rectal application, gelation temperature was determined by rheological measurement as well as by its physical appearance. The results indicated that its mucoadhesive strength also shows a dependency on temperature, which appears to be related to the increment in the maximum strength and average strength of the polymer.

CONCLUSION

The results have suggested that Poloxamer 407 could be a potential thermogelling and mucoadhesive polymer for the development of a site-targeting colorectal drug delivery system for curcuminoids in colorectal cancer therapy.

摘要

目的

结直肠癌(CRC)是台湾癌症死亡的第三大原因;它在癌症死亡率中排名前三。姜黄素类化合物来源于姜黄的根茎。它在多种癌细胞系中表现出抗癌活性和诱导细胞凋亡的作用。本研究旨在研究泊洛沙姆 407 作为热熔胶和黏膜黏附聚合物的潜力,开发一种靶向部位的递药系统,以增强姜黄素类化合物向结直肠细胞的局部递药,用于结直肠癌化疗。

方法

测量了载有姜黄素类化合物的泊洛沙姆的黏膜黏附强度和流变性能。

结果

发现泊洛沙姆 407 的胶凝温度随其浓度而变化,在浓度为 15.5%(w/v)时在 37°C 开始胶凝。为了确保在直肠内给药后在生理温度下胶凝,通过流变学测量和外观确定胶凝温度。结果表明,其黏膜黏附强度也表现出对温度的依赖性,这似乎与聚合物最大强度和平均强度的增加有关。

结论

结果表明,泊洛沙姆 407 可能是一种潜在的热熔胶和黏膜黏附聚合物,可用于开发针对结直肠的姜黄素类化合物靶向递药系统,用于结直肠癌治疗。

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