作为药物载体的基托微粒具有修改的表面化学成分:在模拟的肠道微环境中研究它们的相互作用
C S Dhanya1, M R Rekha2, Willi Paul3
1Division of Polymeric Medical Devices, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Trivandrum, 695012, Kerala, India.
International journal of biological macromolecules
|January 11, 2026
概括
用素 (LCS) 修改的基托桑微粒显示了5-甲 (5-FU) 的口服药物递送的增强. 这些阴离子载体提高了药物的透性和粘合性,使它们成为抗癌疗法的前景.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术纳米技术
- 制药科学 制药科学
背景情况:
- 药物载体的表面电荷对于与胃肠道相互作用的口服输送系统至关重要.
- 基托 (CS) 微粒被用于药物输送,但它们的表面特性需要优化以提高疗效.
研究的目的:
- 为了合成和表征用素 (LCS) 和黄素无水化物 (MCS) 功能化的奇托桑微粒,用于口服药物输送.
- 在模拟的肠道条件下,评估从这些修饰的微粒中对5-甲 (5-FU) 的加载和释放.
- 评估这些载体的潜力,通过口服改善抗癌药物输送.
主要方法:
- 合成具有不同表面电荷的CS,LCS和MCS微粒 (zeta电位分别为+13.3,+23.7和-9.54mV).
- 将5-甲 (5-FU) 装入微粒中,并评估不同pH值下吸水和药物释放的情况.
- 用Eudragit®S-100进行涂层,以保护胃和释放肠道;评估紧密的结口开口,穿过Caco-2细胞的明显透性和粘合力.
主要成果:
- 所有微粒在酸性pH下显示出高吸水率和5-FU释放;Eudragit®S-100涂层在肠道pH (6.8-7.4) 时确保了受控的释放.
- 与阳离子MCS相比,阴离子LCS和CS微粒显示出优越的紧接口开口和更高的5-FU表面透性.
- 修改后的微粒体显著增强了粘膜粘附和粘膜透,而液体粘膜透体显示出口服输送的最佳性能.
结论:
- 素功能化奇托 (LCS) 微粒可为口服的5-甲 (5-FU) 提供改善的半细胞通透性和粘合性.
- 这些阴离子微粒是增强抗癌药物的口服生物可用性和治疗功效的有希望的载体.
- 基托表面电荷修饰是一种可行的策略,可以优化胃肠道中药物载体的性能.
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