a Department of Precision Machinery and Precision Instrumentation, School of Engineering Science , University of Science and Technology of China , Hefei , P.R.China.
b Department of Chemistry, Laboratory of Nanomaterials for Energy Conversion (LNEC) , University of Science and Technology of China , Hefei , Anhui, PR China.
Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):957-967. doi: 10.1080/21691401.2019.1576705.
The current clinical paradigm for ovarian cancer treatment has a poor prognosis, partially due to the efficacy and toxicity concerns associated with the available chemotherapeutic formulations. To overcome these limitations, we have designed core-shell-structured paclitaxel (PTX) laden solid lipid microparticles (PTX-SLMPs) for intraperitoneal treatment of ovarian cancer. A single-step coaxial electro hydrodynamic atomization (CEHDA) process has been explored to synthesize core-shell structure of PTX-SLMPs with the particle size of 1.76 ± 0.37 µm. Core-shell PTX-SLMPs have high encapsulation efficiency of 94.73% with sustained drug release profile. In vitro evaluation of PTX-SLMPs in SKOV-3 ovarian cancer cells yield significant enhancement in cytotoxicity when compared with Taxol®. In vivo pharmacokinetic study demonstrated slower absorption of PTX into the systemic circulation after intraperitoneal (i.p.) administration of PTX-SLMPs in Wistar rats implying the PTX-SLMPs remained in the peritoneal cavity and released the PTX for prolonged period of time. Through these studies, we have demonstrated the technical potential of core-shell structured PTX-SLMPs, which can enhance passive targeting of PTX to the tumor in the treatment of not only ovarian cancer but also in other peritoneal cancer.
目前卵巢癌治疗的临床模式预后较差，部分原因是由于现有化疗制剂的疗效和毒性问题。为了克服这些限制，我们设计了载紫杉醇（PTX）的核壳结构固体脂质毫微粒（PTX-SLMPs），用于治疗卵巢癌的腹腔内治疗。探索了一步同轴电动力学雾化（CEHDA）工艺，以合成粒径为 1.76±0.37μm 的核壳结构的 PTX-SLMPs。PTX-SLMPs 的包封效率高达 94.73%，具有持续的药物释放特性。与 Taxol®相比，PTX-SLMPs 在 SKOV-3 卵巢癌细胞中的体外评估显示出显著增强的细胞毒性。在 Wistar 大鼠中的体内药代动力学研究表明，PTX-SLMPs 经腹腔给药后，PTX 进入体循环的吸收速度较慢，这意味着 PTX-SLMPs 仍留在腹腔内，并在较长时间内释放 PTX。通过这些研究，我们证明了核壳结构的 PTX-SLMPs 具有技术潜力，可增强 PTX 对肿瘤的被动靶向作用，不仅可用于治疗卵巢癌，还可用于治疗其他腹膜癌。
