Department of Chemistry, Shahrood Branch, Islamic Azad University, Shahrood, Iran.
Department of Biochemistry, Shahrood Branch, Islamic Azad University, Shahrood, Iran.
Mol Biol Rep. 2024 Feb 27;51(1):369. doi: 10.1007/s11033-024-09325-8.
In this study the formulation of parthenolide (PN), an anticancer agent extracted from a natural product, into a liposome (PN-liposome), was examined. The surface of the PN-liposome was modified using chitosan (PN-chitosome). By using real-time quantitative PCR and flow cytometry, we examined the release of PN-chitosomes, cytotoxicity, and ability to induce apoptosis in vitro.
According to the present study, PN-chitosomes had a size of 251 nm which is acceptable for efficient enhanced permeation and retention (EPR) performance. PN-chitosomes were confirmed to be spherical in shape and size through FESEM analysis. In terms of encapsulation efficiency, 94.5% was achieved. PN-chitosome possessed a zeta potential of 34.72 mV, which was suitable for its stability. According to the FTIR spectra of PN and PN-chitosome, PN was chemically stable due to the intermolecular interaction between the liposome and the drug. After 48 h, only 10% of the PN was released from the PN-chitosome in PBS (pH 7.4), and less than 20% was released after 144 h.
In a dose-dependent manner, PN-chitosome exhibited anticancer properties that were more cytotoxic against cancer cells than normal cells. Moreover, the formulation activated both the apoptosis pathway and cytotoxic genes in real-time qPCR experiments. According to the cytotoxicity and activating apoptosis of the prepared modified particle, PN-chitosome may be helpful in the treatment of cancer.
本研究考察了将天然产物中提取的抗癌剂小白菊内酯（PN）制成脂质体（PN-脂质体）的配方。通过使用壳聚糖（PN-壳聚糖）对 PN-脂质体的表面进行修饰。通过实时定量 PCR 和流式细胞术，我们检测了 PN-壳聚糖的释放、细胞毒性以及体外诱导细胞凋亡的能力。
根据本研究，PN-壳聚糖的粒径为 251nm，这对于有效的增强渗透和保留（EPR）性能是可接受的。FESEM 分析证实 PN-壳聚糖为球形且粒径均匀。包封效率达到 94.5%。PN-壳聚糖的 Zeta 电位为 34.72mV，这有利于其稳定性。根据 PN 和 PN-壳聚糖的傅里叶变换红外（FTIR）光谱，由于脂质体与药物之间的分子间相互作用，PN 化学稳定。在 PBS（pH 7.4）中，48h 后只有 10%的 PN 从 PN-壳聚糖中释放，144h 后释放量不到 20%。
PN-壳聚糖以剂量依赖的方式表现出抗癌特性，对癌细胞的细胞毒性比对正常细胞更强。此外，制剂在实时 qPCR 实验中激活了细胞凋亡途径和细胞毒性基因。根据所制备的改性颗粒的细胞毒性和诱导细胞凋亡的作用，PN-壳聚糖可能有助于癌症的治疗。
