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由两亲性壳聚糖衍生物组成的亚微米颗粒,用于口服胰岛素和姜黄素释放应用。

Submicroparticles composed of amphiphilic chitosan derivative for oral insulin and curcumin release applications.

机构信息

Division of Biosurface Technology, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences & Technology, Thiruvananthapuram 695012, India.

出版信息

Colloids Surf B Biointerfaces. 2011 Dec 1;88(2):722-8. doi: 10.1016/j.colsurfb.2011.08.007. Epub 2011 Aug 17.

Abstract

Amphiphilic polymers for dual drug delivery have been a focus of research in recent years. We have previously developed and characterized Lauroyl sulphated chitosan (LSCS). Here biological characterizations like mucoadhesion, cytotoxicity, calcium binding, tight junction opening and enzymatic degradation studies were performed to understand its applicability. In vitro drug release properties of both hydrophilic insulin and hydrophobic curcumin were carried out. The biological activity and stability of released insulin were also studied. The stability studies of encapsulated curcumin and uptake studies have also been carried out. LSCS showed strong mucoadhesion and 100% of non-toxicity. LSCS could transiently open tight junctions between Caco-2 cells and thus increase the paracellular permeability. LSCS enhanced calcium binding properties and decreased enzymatic degradation rate retaining insulin activity. LSCS could protect curcumin from photodegradation and could also enter into the cells. From release studies, LSCS was found to be a suitable candidate for both drugs.

摘要

近年来,两亲性聚合物在双重药物递送上的应用一直是研究热点。我们之前已经开发并表征了月桂酰化硫酸化壳聚糖(LSCS)。在这里,我们进行了黏膜黏附性、细胞毒性、钙结合、紧密连接开放和酶降解研究等生物学特性的研究,以了解其适用性。我们还进行了亲水性胰岛素和疏水性姜黄素的体外药物释放性质研究,并研究了释放胰岛素的生物活性和稳定性。我们还进行了包封姜黄素的稳定性研究和摄取研究。LSCS 表现出很强的黏膜黏附性,且 100%无毒。LSCS 可以瞬时打开 Caco-2 细胞之间的紧密连接,从而增加细胞旁通透性。LSCS 增强了钙结合特性,降低了酶降解率,保持了胰岛素的活性。LSCS 可以保护姜黄素免受光降解,并且可以进入细胞。从释放研究中发现,LSCS 是这两种药物的合适候选物。

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