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基于硝酰水杨酰亚胺壳聚糖水凝胶的局部治疗长时持续释放药物传递系统。

Nitrosalicyl-imine-chitosan hydrogels based drug delivery systems for long term sustained release in local therapy.

机构信息

"Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, Iasi, Romania; "Alexandru Ioan Cuza" University, Department of Organic Chemistry, Iasi, Romania.

"Gr. T. Popa" University of Medicine and Pharmacy, Iasi, Romania.

出版信息

J Colloid Interface Sci. 2019 Feb 15;536:196-207. doi: 10.1016/j.jcis.2018.10.048. Epub 2018 Oct 19.

DOI:10.1016/j.jcis.2018.10.048
PMID:30368091
Abstract

The paper focuses on the synthesis and characterization of new drug delivery systems for local therapy. They were prepared by in situ hydrogelation of chitosan biopolymer with nitrosalicylaldehyde in the presence of a model drug, varying the crosslinking density. The structural, supramolecular and morphological characteristics of the systems were studied by FTIR spectroscopy, X-ray diffraction and, POM and SEM microscopy. In vitro release of the drug has been explored in simulated physiological conditions and in vivo release was investigated by the somatic pain model on rats. Information on the biodegradation of the systems was gain by simulating experiments of enzymatic degradation. The systems were biodegradable and showed a prolonged drug release, assuring an in vivo efficient therapeutic effect over 5 days, with no systemic toxicity. All these findings demonstrated that the new hydrogels based on nitrosalicyl-imine-chitosan provides a practical approach for sustained drug delivery for local chemotherapy.

摘要

本文专注于新型局部治疗药物传递系统的合成与表征。通过在模型药物存在的情况下,将壳聚糖生物聚合物原位水凝胶化与硝酰水杨醛反应,改变交联密度来制备这些系统。通过傅里叶变换红外光谱、X 射线衍射、偏光显微镜和扫描电子显微镜研究了系统的结构、超分子和形态特征。在模拟生理条件下研究了药物的体外释放,通过大鼠躯体疼痛模型研究了体内释放。通过模拟酶降解实验获得了系统生物降解的信息。这些系统可生物降解,并表现出延长的药物释放,确保了 5 天内体内的有效治疗效果,且无全身毒性。所有这些发现表明,基于硝酰水杨醛亚胺壳聚糖的新型水凝胶为局部化疗的药物持续释放提供了一种实用方法。

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