Ossama Muhammed, Hathout Rania M, Attia Dalia A, Mortada Nahed D
Department of Pharmaceutics and Industrial Pharmacy, The British University in Egypt (BUE), Cairo 11837, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt.
ACS Omega. 2019 Jun 28;4(6):11293-11300. doi: 10.1021/acsomega.9b01580. eCollection 2019 Jun 30.
The cytotoxic potential of allicin was evaluated on different cancer cell lines, particularly, hepatic (HepG-2), breast (MCF-7), lung (A-549), and prostatic (PC-3), where allicin scored an IC score of 19.26 μM on HepG-2. In order to increase the cell uptake, optimized allicin-loaded gelatin nanoparticles (GNPs) were prepared where the optimum formulation was surface-conjugated to glycyrrhetinic acid. GNPs were optimized using a D-optimal design. The optimum formulation had a particle size of 370.7 ± 6.78 nm and polydispersity index of 0.0363 ± 0.009 and 39.13 ± 2.38% of drug entrapment. The conjugation of the ligand, glycyrrhetinic acid with allicin-loaded GNPs, was confirmed utilizing H NMR. Drug release profiles in the presence/absence of collagenase were obtained. Finally, a cytotoxicity study on HepG-2 was performed for the unconjugated and conjugated allicin-loaded GNPs scoring IC of 10.95 and 5.046 μM, revealing two- and fourfold enhancements in allicin cytotoxicity, respectively. To our knowledge, the ligand-carrier pair, glycyrrhetinic acid-gelatin, was not explored before, and the developed system poses a successful liver cancer therapy.
评估了大蒜素对不同癌细胞系的细胞毒性潜力，特别是肝癌细胞系（HepG-2）、乳腺癌细胞系（MCF-7）、肺癌细胞系（A-549）和前列腺癌细胞系（PC-3），其中大蒜素在HepG-2细胞系上的半数抑制浓度（IC）值为19.26 μM。为了提高细胞摄取量，制备了优化的载大蒜素明胶纳米颗粒（GNP），其中最佳配方与甘草次酸进行了表面共轭。采用D-最优设计对GNP进行了优化。最佳配方的粒径为370.7±6.78 nm，多分散指数为0.0363±0.009，药物包封率为39.13±2.38%。利用氢核磁共振（1H NMR）证实了配体甘草次酸与载大蒜素GNP的共轭。获得了在有/无胶原酶情况下的药物释放曲线。最后，对未共轭和共轭的载大蒜素GNP进行了HepG-2细胞毒性研究，其半数抑制浓度（IC）分别为10.95和5.046 μM，表明大蒜素的细胞毒性分别提高了两倍和四倍。据我们所知，之前尚未探索过甘草次酸-明胶这种配体-载体对，并且所开发的系统为肝癌治疗提供了一种成功的方法。
