Sahiner Mehtap, Suner Selin S, Yilmaz Aynur S, Sahiner Nurettin
Bioengineering Department, Engineering Faculty, Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, Turkey.
Department of Chemistry & Nanoscience and Technology Research and Application Center, Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, Turkey.
Polymers (Basel). 2022 Oct 14;14(20):4324. doi: 10.3390/polym14204324.
Polyelectrolyte microgels derived from natural sources such as chondroitin sulfate (CS) possess considerable interest as therapeutic carriers because of their ionic nature and controllable degradation capability in line with the extent of the used crosslinker for long-term drug delivery applications. In this study, chemically crosslinked CS microgels were synthesized in a single step and treated with an ammonia solution to attain polyelectrolyte CS[NH] microgels via a cation exchange reaction. The spherical and non-porous CS microgels were injectable and in the size range of a few hundred nanometers to tens of micrometers. The average size distribution of the CS microgels and their polyelectrolyte forms were not significantly affected by medium pH. It was determined that the -34 ± 4 mV zeta potential of the CS microgels was changed to -23 ± 3 mV for CS [NH] microgels with pH 7 medium. No important toxicity was determined on L929 fibroblast cells, with 76 ± 1% viability in the presence of 1000 μg/mL concentration of CS[NH] microgels. Furthermore, these microgels were used as a drug carrier material for rosmarinic acid (RA) active agent. The RA-loading capacity was about 2.5-fold increased for CS[R] microgels with 32.4 ± 5.1 μg/mg RA loading, and 23% of the loaded RA was sustainably release for a long-term period within 150 h in comparison to CS microgels. Moreover, RA-loaded CS[R] microgels exhibited great antioxidant activity, with 0.45 ± 0.02 μmol/g Trolox equivalent antioxidant capacity in comparison to no antioxidant properties for bare CS particles.
源自天然来源如硫酸软骨素(CS)的聚电解质微凝胶因其离子性质和与用于长期药物递送应用的交联剂用量相关的可控降解能力而作为治疗载体备受关注。在本研究中,通过一步合成化学交联的CS微凝胶,并用氨溶液处理,通过阳离子交换反应获得聚电解质CS[NH]微凝胶。球形且无孔的CS微凝胶可注射,尺寸范围在几百纳米到几十微米之间。CS微凝胶及其聚电解质形式的平均尺寸分布不受介质pH的显著影响。已确定在pH 7介质中,CS微凝胶的-34±4 mV的zeta电位变为CS[NH]微凝胶的-23±3 mV。在L929成纤维细胞上未测定到重要毒性,在1000μg/mL浓度的CS[NH]微凝胶存在下,细胞活力为76±1%。此外,这些微凝胶用作迷迭香酸(RA)活性剂的药物载体材料。CS[R]微凝胶的RA负载量增加了约2.5倍,RA负载量为32.4±5.1μg/mg,与CS微凝胶相比,负载的RA中有23%在150小时内长期持续释放。此外,负载RA的CS[R]微凝胶表现出很强的抗氧化活性,与裸CS颗粒无抗氧化性能相比,其Trolox当量抗氧化能力为0.45±0.02μmol/g。