International University, Vietnam National University - Ho Chi Minh City, Viet Nam.
Int J Pharm. 2013 Oct 15;455(1-2):235-40. doi: 10.1016/j.ijpharm.2013.07.025. Epub 2013 Jul 19.
Recently, we synthesized novel amphiphilic gelatin-oleic acid (GO) conjugate to prepare self-assembled nanoparticles for drug delivery. The aim of this study was to investigate pharmaceutical potentialities of self-assembled GO nanoparticles for solubility enhancement and modified release of poorly water-soluble drugs. Three poorly water-soluble model drugs with different pH-dependent solubility (valsartan and aceclofenac, insoluble at pH 1.2; telmisartan, insoluble at pH 6.8) were chosen to investigate the potential contributions of self-assembled GO nanoparticles to solubility enhancement and controlled release. The particle size of the drug-loaded nanoparticles was 200-250 nm. Zeta potential was calculated, and instrumental analysis such as powder X-ray diffraction (PXRD) and Fourier transform infrared (FT-IR) spectroscopy were used to investigate the physicochemical properties of the drug-loaded nanoparticles. Compared to the drug alone, the drug-loaded nanoparticles showed enhanced solubility. Furthermore, the release profiles of the model drugs were modified in a controlled manner. The current self-assembled GO nanoparticles can provide a versatile potential in drug delivery and tumor targeting.
最近,我们合成了一种新型的两亲性明胶-油酸(GO)缀合物,用于制备用于药物递送的自组装纳米粒子。本研究的目的是研究自组装 GO 纳米粒子在提高难溶性药物的溶解度和改善药物释放方面的药物潜力。选择了三种难溶性模型药物(缬沙坦和醋氯芬酸,在 pH 1.2 下不溶;替米沙坦,在 pH 6.8 下不溶)来研究自组装 GO 纳米粒子对溶解度增强和控制释放的潜在贡献。载药纳米粒子的粒径为 200-250nm。计算了 Zeta 电位,并使用粉末 X 射线衍射(PXRD)和傅里叶变换红外(FT-IR)光谱等仪器分析方法研究了载药纳米粒子的物理化学性质。与单独的药物相比,载药纳米粒子显示出增强的溶解度。此外,模型药物的释放曲线得到了控制修饰。目前的自组装 GO 纳米粒子可为药物输送和肿瘤靶向提供多功能潜力。