Abstract

Vincristine sulfate (VCS) was used in combination with other chemotherapeutic agents for the treatment of a variety of cancers, including acute lymphoblastic leukemia, cervical cancer, and breast cancer. However, rapid release of the drug at the site of specific action was still a challenge for antitumor treatment. Recently, hybrid carriers bearing the versatile properties of each component were promising materials in order to improve the effects of therapeutic drugs. This work aimed to prepare and characterize chitosan (CHS)–polyethylene glycol (PEG)–oleic acid (OA) composites as a carrier for VCS delivery. The structure, thermal stability, and surface morphology of CHS/PEG/OA composites were characterized by using Fourier transform infrared spectroscopy, thermal gravimetric analysis, differential thermal analysis, differential scanning calorimeter, scanning electron microscopy, and atomic force microscopy. Additionally, swelling degree, water uptake capacity, gas permeability, water contact angle, and in vitro hydrolytic degradation properties of the composites were examined in detail. The VCS-loaded CHS/PEG/OA composites were prepared and drug-loading efficiency was evaluated. CPO-2 sample with a loading efficiency of 64.1 ± 0.6% was selected for in vitro release^. due to the highest drug loading efficiency. In vitro release behavior was performed in phosphate-buffered saline buffer (pH 7.4). The release of VCS was completed in almost 24 h and the release data were best fitted to Korsmeyer–Peppas model. The release results revealed that CHS/PEG/OA composites with slow-release behavior could be a promising drug carrier for therapeutic drugs such as VCS.

摘要

硫酸长春新碱（VCS）与其他化学治疗剂联合使用可治疗多种癌症，包括急性淋巴细胞白血病，宫颈癌和乳腺癌。然而，在特定作用部位快速释放药物仍然是抗肿瘤治疗的挑战。近年来，具有每种组分的通用性质的杂合载体是有前途的材料，以改善治疗药物的效果。这项工作旨在制备和表征壳聚糖（CHS）–聚乙二醇（PEG）–油酸（OA）复合材料作为VCS输送的载体。利用傅里叶变换红外光谱，热重分析，差示热分析，差示扫描量热仪，扫描电子显微镜和原子力显微镜对CHS / PEG / OA复合材料的结构，热稳定性和表面形貌进行了表征。另外，详细检查了复合材料的溶胀度，吸水能力，气体渗透性，水接触角和体外水解降解性能。制备了VCS负载的CHS / PEG / OA复合材料，并评估了药物负载效率。选择加载效率为64.1±0.6％的CPO-2样品进行体外释放^。由于最高的药物装载效率。在磷酸盐缓冲盐水缓冲液（pH 7.4）中进行体外释放行为。VCS的发布在将近24小时内完成，并且发布数据最适合Korsmeyer-Peppas模型。释放结果表明，具有缓慢释放行为的CHS / PEG / OA复合材料可能是治疗性药物（如VCS）的有前途的药物载体。