Natesan Subramanian, Sugumaran Abimanyu, Ponnusamy Chandrasekar, Jeevanesan Vinoth, Girija Gangarani, Palanichamy Rajaguru
Laboratory for Lipid Based Systems, Department of Pharmaceutical Technology, Bharathidasan Institute of Technology, Anna University , Tiruchirappalli, Tamil Nadu , India and.
J Drug Target. 2014 Dec;22(10):913-26. doi: 10.3109/1061186X.2014.948878. Epub 2014 Aug 14.
Development and evaluation of camptothecin-loaded-microemulsion (ME) and -magnetic microemulsion (MME) for passive/active-targeted delivery to BALB/c mice-bearing breast cancer.
Based on the pseudo-ternary phase diagrams camptothecin-loaded-MEs and -MMEs were developed using benzyl alcohol:Captex 300 (3:1), TPGS:Tween 80 (2:1) and water. Furthermore, characterized for their droplet size distribution, magnetic susceptibility and effect of droplet size in plasma and evaluated for in vitro and in vivo targeting potential, drug release, haemolytic potential, cytotoxicity, genotoxicity, in vivo biodistribution and lactone ring stability.
Drug-loaded MEs showed uniform droplet distribution, extended drug release (76.07 ± 4.30% at 24 h), acceptable level of haemolytic activity (<20%), significant cytotoxicity (129 ± 3.9 ng/mL) against MCF-7 cancer cells and low DNA damage in lymphocytes. Targeting potential of MMEs was documented in 4T1 breast cancer-induced BALB/c mice. MMEs were concentrated more at the target tissue on introduction of external magnetic field. In vivo biodistribution study documented the active targeting of 5067.56 ± 354.72 ng/gm and passive targeting of 1677.58 ± 134.20 ng/gm camptothecin to breast cancer from MME and ME, respectively. Lactone stability study shows around 80% of the lactone stable at 24 h.
Developed ME and MME may act as a promising nanocarrier for efficient targeting of breast cancer tissues.
开发并评估载有喜树碱的微乳（ME）和磁性微乳（MME），用于被动/主动靶向递送至荷乳腺癌的BALB/c小鼠。
基于伪三元相图，使用苯甲醇：Captex 300（3:1）、TPGS：吐温80（2:1）和水制备载有喜树碱的ME和MME。此外，对其粒径分布、磁化率以及粒径在血浆中的影响进行表征，并评估其体外和体内靶向潜力、药物释放、溶血潜力、细胞毒性、遗传毒性、体内生物分布和内酯环稳定性。
载药ME显示出均匀的液滴分布，药物释放延长（24小时时为76.07±4.30%），溶血活性水平可接受（<20%），对MCF-7癌细胞具有显著的细胞毒性（129±3.9 ng/mL），且对淋巴细胞的DNA损伤较低。在4T1乳腺癌诱导的BALB/c小鼠中记录了MME的靶向潜力。引入外部磁场后，MME在靶组织中聚集更多。体内生物分布研究记录了MME和ME分别将5067.56±354.72 ng/g和1677.58±134.20 ng/g的喜树碱主动和被动靶向至乳腺癌。内酯稳定性研究表明，24小时时约80%的内酯保持稳定。
所开发的ME和MME可能成为有效靶向乳腺癌组织的有前景的纳米载体。
