In this study, we prepared paclitaxel/chitosan (PTX/CS) nanosuspensions (NSs) with different mass ratios of PTX and CS (1.5:2, 2:2, and 2.5:2), for controlled drug delivery purposes. For attachment and dispersion in water medium, a simple ultrasonic disruption technique was employed. The water-dispersed PTX/CS NSs exhibited a rod-shape morphology with an average diameter of 170–210 nm and average length of about 1–10 µm. Transmission electron microscopy, differential scanning calorimetry and X-ray diffraction indicated that the obtained PTX/CS NSs contain a nanocrystalline PTX phase. It was also inferred that presence of CS can promotes the crystalline nature of PTX up to 80%. In addition, efficiency of PTX loading reached over 85% in freeze-dried PTX/CS NSs, showing a slow rate of drug release in vitro for 8 days. The MTT and LDH assessments revealed that PTX/CS NSs significantly inhibit the growth of tumor cells (HeLa), while it is slightly toxic for the normal cells (NIH/3T3). Therefore, PTX/CS NSs is suggested as a potential nanodrug delivery system for cancer therapy.Graphic Abstract

中文翻译：

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紫杉醇/壳聚糖纳米混悬剂的制备，表征及体外细胞毒性评价

在这项研究中，我们制备了紫杉醇/壳聚糖（PTX / CS）纳米混悬剂（NSs），它们具有不同的PTX和CS的质量比（1.5：2、2：2和2.5：2），用于可控药物递送。为了在水介质中附着和分散，采用了一种简单的超声破碎技术。水分散的PTX / CS NSs呈棒状形态，平均直径为170-210 nm，平均长度约为1-10 µm。透射电子显微镜，差示扫描量热法和X射线衍射表明，所获得的PTX / CS NSs包含纳米晶PTX相。还推断CS的存在可以促进PTX的晶体性质高达80％。此外，在冻干的PTX / CS NS中，PTX装载效率达到了85％以上，显示出体外药物释放速度（持续8天）较慢。MTT和LDH评估显示，PTX / CS NSs显着抑制肿瘤细胞（HeLa）的生长，而对正常细胞（NIH / 3T3）则有轻微毒性。因此，PTX / CS NSs被认为是潜在的用于癌症治疗的纳米药物输送系统。