首页> 美国卫生研究院文献>AAPS PharmSciTech >The Improvement of the Anticancer Effect of a Novel Compound Benzoic Acid 2-Hydroxy- 2-d-ribofuranosylhydrazide (BHR) Loaded in Solid Lipid Nanoparticles
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The Improvement of the Anticancer Effect of a Novel Compound Benzoic Acid 2-Hydroxy- 2-d-ribofuranosylhydrazide (BHR) Loaded in Solid Lipid Nanoparticles

机译:固体脂质纳米颗粒中负载新型化合物苯甲酸2-羟基-2-d-呋喃呋喃糖基酰肼(BHR)的抗癌作用的改善

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摘要

A novel drug delivery system consisting of benzoic acid, 2-hydroxy-, 2-d-ribofuranosylhydrazide (BHR)-loaded solid lipid nanoparticles (BHR-SLNs) was prepared using the emulsification–evaporation technique. The mean particle size of the BHR-SLNs measured by photon correlation spectroscopy was about 75 nm. BHR-SLN morphology was assessed by transmission electron microscopy and atomic force microscopy. The drug entrapment efficiency was 70.2%, as determined via Sephadex gel chromatography and high-performance liquid chromatography. Drug release assessment in vitro showed that BHR was gradually released from SLNs in a time-dependent manner. Furthermore, treatment of 293T and Hela cells with BHR-SLNs demonstrated that BHR-SLNs were less toxic to normal cells while more effective in antitumor potency compared with the BHR drug alone. The results imply that BHR-SLNs could be considered as a promising antitumor drug system for a range of new therapeutic applications.
机译:使用乳化-蒸发技术制备了由苯甲酸,2-羟基-,2-d-呋喃呋喃糖基酰肼(BHR)负载的固体脂质纳米颗粒(BHR-SLNs)组成的新型药物递送系统。通过光子相关光谱法测得的BHR-SLN的平均粒径约为75 nm。 BHR-SLN形态通过透射电子显微镜和原子力显微镜进行评估。通过Sephadex凝胶色谱法和高效液相色谱法测定的药物截留率为70.2%。体外药物释放评估表明,BHR以时间依赖性方式逐渐从SLN中释放出来。此外,用BHR-SLNs处理293T和Hela细胞表明,与单独的BHR药物相比,BHR-SLNs对正常细胞的毒性较小,而在抗肿瘤效力方面更为有效。结果表明,对于一系列新的治疗应用,BHR-SLNs可以被视为有希望的抗肿瘤药物系统。

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