Smart pH-Sensitive Nanogels for Controlled Release in an Acidic Environment.,Biomacromolecules

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Smart pH-Sensitive Nanogels for Controlled Release in an Acidic Environment.
Biomacromolecules ( IF 5.5 ) Pub Date : 2018-11-08 , DOI: 10.1021/acs.biomac.8b01228
Peng Wei _{1,

2} , Gauri Gangapurwala _{1,

2} , David Pretzel _{1,

2} , Meike N Leiske _{1,

2} , Limin Wang _{1,

2} , Stephanie Hoeppener _{1,

2} , Stephanie Schubert _{2,

3} , Johannes C Brendel _{1,

2} , Ulrich S Schubert _{1,

2}

Affiliation

The encapsulation of therapeutic compounds into nanosized delivery vectors has become an important strategy to improve efficiency and reduce side effects in drug delivery applications. Here, we report the synthesis of pH-sensitive nanogels, which are based on the monomer N-[(2,2-dimethyl-1,3-dioxolane)methyl]acrylamide (DMDOMA) bearing an acid cleavable acetal group. Degradation studies revealed that these nanogels hydrolyze under acidic conditions and degrade completely, depending on the cross-linker, but are stable in physiological environment. The best performing system was further studied regarding its release kinetics using the anticancer drug doxorubicin. In vitro studies revealed a good compatibility of the unloaded nanogel and the capability of the doxorubicin loaded nanogel to mediate cytotoxic effects in a concentration and time-dependent manner with an even higher efficiency than the free drug. Based on the investigated features, the presented nanogels represent a promising and conveniently prepared alternative to existing carrier systems for drug delivery.

中文翻译：

在酸性环境中可控释的智能pH敏感纳米凝胶。

将治疗化合物封装到纳米尺寸的递送载体中已经成为提高效率并减少药物递送应用中的副作用的重要策略。在这里，我们报告了pH敏感的纳米凝胶的合成，该凝胶基于带有酸可裂解缩醛基团的单体N-[（2,2-二甲基-1,3-二氧戊环）甲基]丙烯酰胺（DMDOMA）。降解研究表明，这些纳米凝胶在酸性条件下会水解并完全降解，具体取决于交联剂，但在生理环境中稳定。使用抗癌药阿霉素对性能最佳的系统进行了进一步的研究。体外研究表明，未负载的纳米凝胶具有良好的相容性，而负载阿霉素的纳米凝胶具有以浓度和时间依赖性方式介导细胞毒性作用的能力，其效率甚至高于游离药物。基于研究的特征，提出的纳米凝胶代表了一种有前途且方便制备的替代方法，可以替代现有的药物输送载体系统。

更新日期：2018-10-26

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