Studies on Biotinylated Liposomes as Potential Carries for Enhancing Oral Absorption of Curcumin

Wu Qiuping, Su Kunquan, T. Jin, T. Zeng, Wu Chenyan, Yin Lingzhi, Huiwen Ying
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Abstract

Oral dosage forms have many obvious advantages like simple, painless and self-administered. While the bioavailability of drugs are always low for they are unstable and usually degraded within gastrointestinal tract. Curcumin, a multifunction native compound, can be used in curing many diseases while the oral bioavailability is relatively low, limiting its clinical effectiveness. The aim of this study was to investigate the method of increasing the bioavailability by the addition of biotin, which was a kind of vitamin helping the liposomes to uptake by biotin receptors. In situ rat Single-Pass Intestinal Perfusion Model (SPIP) was applied to investigate the different content of biotin and caco-2 cells monolayer model was established to mimic the intestinal tract in drug transportation study. As the results shows that biotin decorated liposomes (biotin-PEG-DSPE-Lip) had a better cellular uptake and transportation rate compared to biotin undecorated ones (PEG-DSPE-Lip). It indicated that the bioavailability of curcumin had been increased.
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生物素化脂质体作为促进姜黄素口服吸收的潜在载体的研究
口服剂型有许多明显的优点,如简单、无痛和自行给药。而药物的生物利用度一直很低,因为它们不稳定,通常在胃肠道内降解。姜黄素是一种多功能天然化合物,可用于多种疾病的治疗,但口服生物利用度较低,限制了其临床疗效。生物素是一种促进脂质体被生物素受体吸收的维生素,本研究旨在探讨通过添加生物素来提高脂质体生物利用度的方法。采用原位大鼠单遍肠灌注模型(SPIP)研究不同生物素含量,建立caco-2细胞单层模型模拟肠道药物转运研究。结果表明,生物素修饰脂质体(biotin-PEG-DSPE-Lip)比未修饰的生物素脂质体(PEG-DSPE-Lip)具有更好的细胞摄取和运输速率。表明姜黄素的生物利用度有所提高。
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