Division of Traumatology, Department of Surgery, Chi Mei Medical Center, Tainan, Taiwan.
Int J Colorectal Dis. 2012 Jul;27(7):869-78. doi: 10.1007/s00384-011-1393-3. Epub 2012 Jan 7.
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.
The mucoadhesive strength and rheological properties were measured as a function of poloxamer loaded with curcuminoids.
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.
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.
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。
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。
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。