Whistler Center for Carbohydrate Research, Department of Food Science, Purdue University, West Lafayette, IN 47907, USA.
Carbohydr Polym. 2013 Apr 15;94(1):209-15. doi: 10.1016/j.carbpol.2013.01.008. Epub 2013 Jan 11.
Many challenges arise during the development of new drug carrier systems, and paramount among them are safety, solubility and controlled release requirements. Although synthetic polymers are effective, the possibility of side effects imposes restrictions on their acceptable use and dose limits. Thus, a new drug carrier system that is safe to handle and free from side effects is very much in need and food grade polysaccharides stand tall as worthy alternatives. Herein, we demonstrate for the first time the feasibility of sodium iota-carrageenan fibers and their distinctive water pockets to embed and release a wide variety of drug molecules. Structural analysis has revealed the existence of crystalline network in the fibers even after encapsulating the drug molecules, and iota-carrageenan maintains its characteristic and reproducible double helical structure suggesting that the composites thus produced are reminiscent of cocrystals. The melting properties of iota-carrageenan:drug complexes are distinctly different from those of either drug or iota-carrageenan fiber. The encapsulated drugs are released in a sustained manner from the fiber matrix. Overall, our research provides an elegant opportunity for developing effective drug carriers with stable network toward enhancing and/or controlling bioavailability and extending shelf-life of drug molecules using GRAS excipients, food polysaccharides, that are inexpensive and non-toxic.
在新型药物载体系统的开发过程中会出现许多挑战,其中最重要的是安全性、溶解性和控制释放要求。虽然合成聚合物很有效,但副作用的可能性对其可接受的用途和剂量限制施加了限制。因此,非常需要一种安全易用且无副作用的新型药物载体系统,而食品级多糖则是很好的替代品。在这里,我们首次证明了钠 ι-卡拉胶纤维及其独特的水口袋能够嵌入和释放各种药物分子的可行性。结构分析表明,即使在包裹药物分子后,纤维中仍然存在结晶网络,并且 ι-卡拉胶保持其特征性和可重复的双螺旋结构,这表明所制备的复合材料类似于共晶。ι-卡拉胶:药物复合物的熔融特性明显不同于药物或 ι-卡拉胶纤维。药物从纤维基质中以持续的方式释放。总的来说,我们的研究为开发使用 GRAS 赋形剂(廉价且无毒的食品多糖)的有效药物载体提供了一个优雅的机会,这些药物载体具有稳定的网络,可增强和/或控制药物分子的生物利用度并延长其保质期。