目的根据三阴性乳腺癌(triple negative breast cancer,TNBC)细胞过度表达葡萄糖转运蛋白1(glucose transporter type 1,Glut1),而人参皂苷Rg_(3)(ginsenoside Rg_(3),Rg_(3))的葡萄糖基可与Glut1底物高度结合的特点,以Rg_(3)为脂质体膜...目的根据三阴性乳腺癌(triple negative breast cancer,TNBC)细胞过度表达葡萄糖转运蛋白1(glucose transporter type 1,Glut1),而人参皂苷Rg_(3)(ginsenoside Rg_(3),Rg_(3))的葡萄糖基可与Glut1底物高度结合的特点,以Rg_(3)为脂质体膜材,制备包载雷公藤红素(celastrol,Cel)的靶向治疗TNBC的脂质体(Cel/Rg_(3)-LPs),并对其靶向行为及抗TNBC疗效进行考察。方法采用薄膜分散法制备Cel/Rg_(3)-LPs并采用单因素考察法优化处方,对优化处方的Cel/Rg_(3)-LPs进行形态、粒径、ζ电位、体外释放和稳定性的考察;通过Cel/Rg_(3)-LPs在体外鼠源4T1细胞的摄取实验、及对BALB/c原位荷4T1瘤株小鼠的治疗效果综合评价其靶向性。结果Cel/Rg_(3)-LPs优化处方为水化温度50℃,Cel为1.5 mg,Rg_(3)为3.0 mg,大豆磷脂为21.0 mg,制备得到的脂质体外观呈圆球形,分布均匀,其粒径和PDI分别为(148.4±0.23)nm和0.19±0.01,ζ电位为(-29.70±0.34)mV,Cel在脂质体中包封率为(96.69±0.03)%,载药量为(5.62±0.01)%。Cel/Rg_(3)-LPs在4T1细胞中的摄取作用显著增强,且显著抑制4T1细胞增殖;原位荷瘤小鼠体内实验表明,Cel/Rg_(3)-LPs能降低肿瘤组织脂质,并明显抑制肿瘤生长,具有良好的肿瘤靶向性,无明显肝肾毒性和组织毒性。结论利用Rg_(3)替代胆固醇作为脂质体膜材可使雷公藤红素具有较好的TNBC靶向性,其药效相比胆固醇作为膜材显著增强,值得进一步研究。展开更多
In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by ...In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by thin-film dispersion-ultrasonic method, and the prescription composition and preparation process were optimized by single-factor investigation method. Certainly, the solubility and quality evaluation of dimethyl curcumin niosomes were also investigated. The average particle size of prepared dimethyl curcumin niosomes was （310.3＋0.9） nm. The highest encapsulation rate was 88.1%± 1.7%, and the drug-loading amount was 4.03%±1.05%. Moreover, the leakage rate was below 2% within 45 d. Collectively, all these findings indicated that the niosomes, as a vector, could significantly improve the solubility and stability of dimethyl curcumin, offering a theoretical basis for dimethyl curcumin as an anticancer drug in medicine application.展开更多
目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,...目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,磷脂与胆固醇比例为12∶1,脂药比为15∶1,DSPEMPEG2000摩尔百分比为5%。此条件下制备的脂质体包封率为90.6%,平均粒径为113.4 nm,Zeta电位为-45.9 m V。结论:本实验所制备的呋喃二烯长循环脂质体包封率较高,粒度分布范围较窄,平均粒径较小,具有很好的应用前景。展开更多
基金The National Natural Science Foundation of China(Grant No.31271002)Jiangsu Provincial Department of Education Funded Projects(Grant No.14KJB350001)
文摘In the present work, we aimed to optimize the preparation technology of dimethyl curcumin niosomes, improve its solubility and assess its stability. The novel anti-androgen dimethyl curcumin niosomes were prepared by thin-film dispersion-ultrasonic method, and the prescription composition and preparation process were optimized by single-factor investigation method. Certainly, the solubility and quality evaluation of dimethyl curcumin niosomes were also investigated. The average particle size of prepared dimethyl curcumin niosomes was （310.3＋0.9） nm. The highest encapsulation rate was 88.1%± 1.7%, and the drug-loading amount was 4.03%±1.05%. Moreover, the leakage rate was below 2% within 45 d. Collectively, all these findings indicated that the niosomes, as a vector, could significantly improve the solubility and stability of dimethyl curcumin, offering a theoretical basis for dimethyl curcumin as an anticancer drug in medicine application.
文摘目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,磷脂与胆固醇比例为12∶1,脂药比为15∶1,DSPEMPEG2000摩尔百分比为5%。此条件下制备的脂质体包封率为90.6%,平均粒径为113.4 nm,Zeta电位为-45.9 m V。结论:本实验所制备的呋喃二烯长循环脂质体包封率较高,粒度分布范围较窄,平均粒径较小,具有很好的应用前景。
