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关于提高壳聚糖基微球性能和药物释放的有效方法。

On an effective approach to improve the properties and the drug release of chitosan-based microparticles.

机构信息

Department of Informatics, Bioengineering, Robotics and Systems Engineering, University of Genoa, Via All'Opera Pia 13, 16145 Genoa, Italy.

Department of Chemistry and Industrial Chemistry, University of Genoa, Via Dodecaneso 31, 16146 Genoa, Italy.

出版信息

Int J Biol Macromol. 2020 Nov 15;163:393-401. doi: 10.1016/j.ijbiomac.2020.07.016. Epub 2020 Jul 6.

DOI:10.1016/j.ijbiomac.2020.07.016
PMID:32645491
Abstract

The work investigated the possibility to develop an easy scalable treatment capable of modifying only the surface of chitosan-based materials, limiting the degradation of the bulk and the burst release of a drug, without compromising the properties of the polymeric matrix. To this aim, microparticles of CHI were superficially coated with poly-(styrene-co-maleic anhydride) (PSMA), taking advantage of the potential reactivity of chitosan amino groups and maleic functionalities of PSMA. The specific reactions/interactions occurring between the two polymers were studied by IR measurements, while FE-SEM analysis evidenced the modification of the morphology of the particles contacted with PSMA. Contact angle measurements demonstrated the change of wettability in the modified systems and TGA analysis allowed to estimate the amount of the deposited PSMA. The above treatment turned out to improve the particle stability both in an acidic environment and in an enzymatic system. The release properties of the treated and of the untreated particles, over a period of 10 h, were tested using, as model drug, the protein Bovine Serum Albumin (BSA). Finally, the cytocompatibility of the developed composite microparticles was assessed on MCF-7 human breast cancer cells, which measurements demonstrated the non-toxicity of the treatment.

摘要

这项工作研究了开发一种简单的可扩展的治疗方法的可能性,这种方法能够仅修饰壳聚糖基材料的表面,限制药物的整体降解和突释,而不影响聚合物基质的性质。为此,利用壳聚糖氨基基团和 PSMA 的马来酸官能团的潜在反应性,将 CHI 微球的表面涂覆有聚(苯乙烯-co-马来酸酐)(PSMA)。通过红外测量研究了两种聚合物之间发生的特定反应/相互作用,而 FE-SEM 分析表明与 PSMA 接触的颗粒的形态发生了变化。接触角测量证明了改性体系润湿性的变化,TGA 分析允许估计沉积的 PSMA 的量。结果表明,上述处理可提高颗粒在酸性环境和酶系统中的稳定性。使用牛血清白蛋白(BSA)作为模型药物,测试了处理和未处理颗粒在 10 小时内的释放性能。最后,对开发的复合微球的细胞相容性进行了评估,MCF-7 人乳腺癌细胞的测量结果表明该处理无毒性。

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