Dhamecha Dinesh, Jalalpure Sunil, Jadhav Kiran, Jagwani Satveer, Chavan Ramesh
KLE University's College of Pharmacy, Nehru Nagar, Belgaum, 590010 Karnataka, India; Dr. Prabhakar Kore Basic Science Research Center, KLE University, Belgaum, 590010 Karnataka, India.
KLE University's College of Pharmacy, Nehru Nagar, Belgaum, 590010 Karnataka, India; Dr. Prabhakar Kore Basic Science Research Center, KLE University, Belgaum, 590010 Karnataka, India.
Pharmacol Res. 2016 Nov;113(Pt A):547-556. doi: 10.1016/j.phrs.2016.09.037. Epub 2016 Sep 28.
The present work aims to investigate targeting potential of doxorubicin (Dox) functionalized gold nanoparticles (D-GNPs) for treatment of chemically induced fibrosarcoma in mice. Carrier GNPs were synthesised by green chemistry method and loaded with doxorubicin by incubation method. D-GNPs were studied for its biocompatibility using normal mouse fibroblasts (L929) and found to be cell compatible and non-toxic. D-GNPs (at a dose of 2.5, 2 and 1.5mg/kg equivalent to Dox) demonstrated passive targeting measured as function of antitumor efficacy against chemical induced fibrosarcoma which showed higher latency to the tumour growth as compared to free Dox (2.5mg/kg). D-GNPs exhibited significantly higher therapeutic anticancer efficacy (∼81% tumour suppression at dose of 2.5mg/kg equivalent to Dox) in the same model as compared to that of free doxorubicin (∼48% tumour suppression at dose of 2.5mg/kg). Safety profile and targeting efficiency of developed formulation was established by assessing cardiac and blood markers.
本研究旨在探讨阿霉素（Dox）功能化金纳米颗粒（D-GNPs）对小鼠化学诱导纤维肉瘤的靶向治疗潜力。通过绿色化学方法合成载体金纳米颗粒，并采用孵育法将阿霉素负载于其上。使用正常小鼠成纤维细胞（L929）研究D-GNPs的生物相容性，发现其具有细胞相容性且无毒。D-GNPs（剂量为2.5、2和1.5mg/kg，相当于阿霉素的剂量）表现出被动靶向性，通过对化学诱导纤维肉瘤的抗肿瘤疗效来衡量，与游离阿霉素（2.5mg/kg）相比，其对肿瘤生长的潜伏期更长。在同一模型中，与游离阿霉素（2.5mg/kg剂量下约48%的肿瘤抑制率）相比，D-GNPs表现出显著更高的治疗抗癌疗效（相当于阿霉素剂量为2.5mg/kg时约81%的肿瘤抑制率）。通过评估心脏和血液标志物来确定所开发制剂的安全性和靶向效率。
