本研究旨在开发负载顺铂的聚乙二醇化壳聚糖纳米粒。负载顺铂的聚乙二醇化壳聚糖纳米粒的最佳批次具有+49.9mV的ζ电位,PDI为0.347,%PDI为58.9。纳米粒子ζ大小为741.4z.d.nm,直径大小为866.7±470.5nm,胶体溶液中纳米粒子的电导率为0.739mS/cm。差示扫描量热法(DSC)显示负载顺铂的聚乙二醇化壳聚糖纳米颗粒在168.6°C的温度下具有尖锐的吸热峰。热重分析(TGA)显示负载顺铂的聚乙二醇化壳聚糖纳米粒的重量损失,在262.76°C下观察到95%。对负载顺铂的聚乙二醇化壳聚糖纳米颗粒的XRD研究在2θ为9.7°处显示出明显的峰,20.4°,22.1°,25.3°,36.1°,38.1°,39.5°,44.3°,和64.5°,确认晶体结构。1HNMR分析显示,负载顺铂的聚乙二醇化壳聚糖纳米颗粒的指纹区在质子维度为0.85、1.73和1.00ppm,并且去屏蔽的质子峰出现在3.57、3.58、3.58、3.59、3.65、3.67、3,67、3.70、3.71、3.77、3.78和4.71ppm。13CNMR谱显示在63.18、69.20和70.77ppm处的特定峰。负载顺铂的聚乙二醇化纳米颗粒的FT-IR光谱显示在3186.52、2931.68、1453.19、1333.98、1253.71、1085.19、1019.60、969.98、929.53、888.80、706.13和623.67cm-1处存在许多指纹区。负载顺铂的聚乙二醇化壳聚糖纳米粒的药物释放动力学表现为零级动力学,药物释放线性为48%,R2值为0.9778。对MCF-7ATCC人乳腺癌细胞系的体外研究表明,IC50值为82.08μg/mL。可注射纳米颗粒具有良好的物理化学和细胞毒性。该方法是新颖的,因为PEG化方法的应用导致壳聚糖纳米颗粒在接近中性pH下的溶解度增加。
The study aimed to develop cisplatin-loaded PEGylated chitosan nanoparticles. The optimal batch of cisplatin-loaded PEGylated chitosan nanoparticles had a + 49.9 mV zeta potential, PDI of 0.347, and % PDI of 58.9. Nanoparticle zeta size was 741.4 z. d.nm, the size in diameter was 866.7 ± 470.5 nm, and nanoparticle conductivity in colloidal solution was 0.739 mS/cm. Differential scanning calorimetry (DSC) revealed that cisplatin-loaded PEGylated chitosan nanoparticles had sharp endothermic peaks at temperatures at 168.6 °C. The thermogravimetric analysis (TGA) showed the weight loss of cisplatin-loaded PEGylated chitosan nanoparticles, which was observed as 95% at 262.76 °C. XRD investigation on cisplatin-loaded PEGylated chitosan nanoparticles exhibited distinct peaks at 2θ as 9.7°, 20.4°, 22.1°, 25.3°, 36.1°, 38.1°, 39.5°, 44.3°, and 64.5°, confirming crystalline structure. The 1H NMR analysis showed the fingerprint region of cisplatin-loaded PEGylated chitosan nanoparticles as 0.85, 1.73, and 1.00 ppm in the proton dimension and de-shielded proton peaks appeared at 3.57, 3.58, 3.58, 3.59, 3.65, 3.67, 3,67, 3,67, 3.70, 3.71, 3.77, 3.78 and 4.71 ppm. The 13C NMR spectrum showed specified peaks at 63.18, 69.20, and 70.77 ppm. The FT-IR spectra of cisplatin loaded PEGylated nanoparticles show the existence of many fingerprint regions at 3186.52, 2931.68, 1453.19, 1333.98, 1253.71, 1085.19, 1019.60, 969.98, 929.53, 888.80, 706.13, and 623.67 cm-1. The drug release kinetics of cisplatin loaded PEGylated chitosan nanoparticles showed zero order kinetics with 48% of drug release linearity fashion which has R2 value of 0.9778. Studies on the MCF-7 ATCC human breast cancer cell line in vitro revealed that the IC50 value 82.08 µg /mL. Injectable nanoparticles had good physicochemical and cytotoxic properties. This method is novel since the application of the PEGylation processes leads to an increased solubility of chitosan nanoparticles at near neutral pH.