First People's Hospital of Linping District, Hangzhou, China.
Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals and College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China.
Drug Deliv. 2022 Dec;29(1):1398-1408. doi: 10.1080/10717544.2022.2069879.
Triptolide (TP), a compound isolated from a Chinese medicinal herb, possesses potent anti-tumor, immunosuppressive, and anti-inflammatory properties, but was clinically limited due to its poor solubility, bioavailability, and toxicity. Considering the environment-friendly, low-cost mechanochemical techniques and potential dissolution enhancement ability of NaGA, an amorphous solid dispersion (NaGA&TP-BM) consisting of TP and NaGA were well-prepared to address these issues. The performance of NaGA&TP-BM was improved through ball milling, such as from crystalline state to an amorphous solid dispersion, suitable nano micelle size and surface potential, and increased solubility. This change had a significant improvement of pharmacokinetic behavior in mice and could be able to extend the blood circulation time of the antitumor drug. Moreover, and anti-tumor study showed that NaGA&TP-BM displayed more potent cytotoxicity to tumor cells. The work illustrated an environment-friendly and safe preparation of the TP formulation, which was promising to enhance the oral bioavailability and antitumor ability of TP, might be considered for efficient anticancer therapy.
雷公藤红素（TP）是从一种中药中分离得到的化合物，具有很强的抗肿瘤、免疫抑制和抗炎作用，但由于其溶解度、生物利用度和毒性差，临床上受到限制。考虑到环境友好、低成本的机械化学技术和 NaGA 的潜在溶解增强能力，制备了由 TP 和 NaGA 组成的无定形固体分散体（NaGA&TP-BM）来解决这些问题。球磨可以改善 NaGA&TP-BM 的性能，例如从结晶状态变为无定形固体分散体、合适的纳米胶束大小和表面电位以及增加溶解度。这种变化显著改善了在小鼠体内的药代动力学行为，并可能延长抗肿瘤药物的血液循环时间。此外，抗肿瘤研究表明，NaGA&TP-BM 对肿瘤细胞表现出更强的细胞毒性。这项工作说明了一种环保且安全的 TP 制剂制备方法，有望提高 TP 的口服生物利用度和抗肿瘤能力，可能被认为是有效的抗癌治疗方法。
