The potential of glycol chitosan nanoparticles as carrier for low water soluble drugs
The potential of glycol chitosan nanoparticles as carrier for low water soluble drugs
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DOI：
10.1016/j.ijpharm.2009.03.041
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发表时间：
2009-06-22
影响因子：
5.8
通讯作者：
Kissel, Thomas
中科院分区：
文献类型：
--
作者：
Trapani, Adriana;Sitterberg, Johannes;Kissel, Thomas
选择激光染料6-香豆素作为低水溶性药物模型，包封在经粘膜应用的乙二醇壳聚糖纳米颗粒中，同时作为荧光探针，有助于阐明颗粒在细胞内的命运。为了提高示踪剂的水溶性，采用了与不同环糊精络合的方法。对包合物的荧光性质进行了评价。不同的环糊精提供的水溶解度的增加[高达1.4 × 10(-4) M的庚（2,6-二- o -甲基）- β -环糊精]允许根据三聚磷酸钠多阳离子的离子交联制备新型乙二醇壳聚糖纳米颗粒。制备技术的微小变化允许生产两种不同尺寸的颗粒，约200 nm和大于300 nm，其中环糊精的贡献包括最终颗粒中的调制包封效率。共聚焦激光扫描显微照片清楚地显示了6-香豆素纳米颗粒在Caco-2细胞系中的内化。结果表明，这些生物可降解纳米颗粒在生物医学领域具有广阔的应用前景。(C) 2009 Elsevier B.V.版权所有
The laser dye 6-coumarin was selected as model of low water soluble drug to be encapsulated in glycol chitosan nanoparticles intended for transmucosal applications and, at the same time, being a fluorescent probe, it is of aid to elucidate the intracellular fate of the particles. To increase the aqueous solubility of the tracer, the complexation with different cyclodextrins was adopted. The fluorescence properties of the inclusion complexes were evaluated. The increase in aqueous solubility provided by different cyclodextrins [up to 1.4 x 10(-4) M in the case of heptakis (2,6-di-O-methyl)-beta-cyclodextrin] allowed the preparation of novel glycol chitosan nanoparticles according to the ionic cross-linking of the polycation by sodium tripolyphosphate. Small changes in the preparation technique allowed to produce particles of two different sizes, around 200 nm and bigger than 300 nm where the contribution of cyclodextrin consisted of the modulation encapsulation efficiency in the final particles. Confocal laser scanning microphotographs clearly showed the internalization of 6-coumarin nanoparticles in Caco-2 cell line. The results reveal that these biodegradable nanoparticles hold promise as probes in biomedical field. (C) 2009 Elsevier B.V. All rights reserved.