International University, Vietnam National University-Ho Chi Minh City 70000, Vietnam.
J Biomed Nanotechnol. 2013 Aug;9(8):1416-31. doi: 10.1166/jbn.2013.1621.
In this work, a novel, biocompatible conjugates of gelatin and oleic acid (GOC) were synthesized by a novel aqueous solvent-based method that overcame challenges of completely contrary solubility between gelatin and oleic acid (OA). The GO nanoparticles (GONs) and Paclitaxel encapsulated nanoparticles (PTX-GON) were prepared by self-assembly in water. These nanoparticles (NPs) were then conjugated with folic acid (FA) for targeting cervical cancer cells (Hela cells) and were characterized for their various physicochemical and pharmaceutical properties. Fourier transform infrared spectroscopy (FT-IR) and 1H NMR studies indicated the successful synthesis of GOC which showed low critical aggregation concentration in water (0.015 mg/ml). All NPs were stable in human blood serum and their mean diameters were below 300 nm suitable for passive targeting. Powder X-ray diffraction (PXRD) diffractograms showed the reduction in drug crystallinity and hence, leading to the solubility enhancement of PTX. The release of PTX from both PTX-GON and FA conjugated PTX-GON (PTX-FA-GON) was controlled for a long time. The cytotoxicity results demonstrated great advantages of PTX-FA-GON and PTX-GON over the conventional dosage form of pacliaxel (Taxol). These results, therefore, indicate that GOC is a promising material to prepare drug encapsulated NP as a controlled delivery system and PTX-FA-GON is a potential targeted delivery system for cancer therapy.
在这项工作中，通过一种新颖的水相溶剂法合成了一种新型的明胶和油酸（GOC）的生物相容性缀合物，该方法克服了明胶和油酸（OA）完全相反的溶解度之间的挑战。GO 纳米粒子（GONs）和紫杉醇包封纳米粒子（PTX-GON）通过自组装在水中制备。然后将这些纳米粒子（NPs）与叶酸（FA）缀合，用于靶向宫颈癌细胞（Hela 细胞），并对其各种物理化学和药物性质进行了表征。傅里叶变换红外光谱（FT-IR）和 1H NMR 研究表明成功合成了 GOC，其在水中的临界聚集浓度低（0.015mg/ml）。所有 NPs 在人血清中均稳定，其平均粒径均低于 300nm，适合被动靶向。粉末 X 射线衍射（PXRD）图谱表明药物结晶度降低，从而提高了 PTX 的溶解度。PTX 从 PTX-GON 和 FA 缀合的 PTX-GON（PTX-FA-GON）中的释放均得到了长时间的控制。细胞毒性结果表明，PTX-FA-GON 和 PTX-GON 优于紫杉醇的常规剂型（Taxol）具有很大优势。因此，这些结果表明 GOC 是一种有前途的材料，可以制备药物包封的 NP 作为控制释放系统，PTX-FA-GON 是癌症治疗的潜在靶向递送系统。
