ABSTRACT

We designed three cholesterol-modified carboxylated pullulan (CHSP) polymers modified with different degrees of substitution (DS). Nuclear magnetic resonance (NMR) was used to characterize CHSP polymer and calculate the DS, which were 2.12%, 4.36% and 6.05% for CHSP1, CHSP2 and CHSP3. The particle sizes identified by dynamic light scattering (DLS) were approximately 229.4 nm, 185.1 nm and 178.0 nm.The mitoxantrone (MTO) loadings of three nanoparticles were 5.28%, 6.71% and 7.68%. At pH 6.8, 72 hours later, the drug release rates were 95.42%, 86.88%, and 80.16%. In the weakly acidic environment, the drug release rate was significantly accelerated but still showed three types of nanoparticles and hydrophobic substitution degree-related slow release characteristics. In the cytotoxicity experiments, it was found that the inhibitory effect of the three nanoparticles on hepatoma cells is related to the degree of hydrophobic substitution, and the nanoparticles with the lowest hydrophobic substitution degree have the strongest inhibitory effect.

摘要

我们设计了三种经不同取代度 (DS) 修饰的胆固醇修饰羧化支链淀粉 (CHSP) 聚合物。核磁共振(NMR)用于表征CHSP聚合物并计算DS，CHSP1、CHSP2和CHSP3的DS分别为2.12%、4.36%和6.05%。动态光散射(DLS)鉴定的粒径约为229.4 nm、185.1 nm和178.0 nm。三种纳米粒子的米托蒽醌(MTO)载量分别为5.28%、6.71%和7.68%。在pH 6.8，72小时后，药物释放率分别为95.42%、86.88%和80.16%。在弱酸性环境下，药物释放速度明显加快，但仍表现出三类纳米粒和疏水取代度相关的缓释特征。在细胞毒性实验中，