School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.
School of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing 210009, PR China.
Int J Pharm. 2014 Apr 25;465(1-2):32-41. doi: 10.1016/j.ijpharm.2014.02.001. Epub 2014 Feb 7.
In this paper, a lipid material glycerol monooleate was used as the starting material to synthesize the oxidized glycerol monooleate (OGMO). OGMO was subsequently linked to chitosan (CS) via imine bonds (-C=N-) to obtain a new chitosan-based polymer (OGMO-CS), which can form hydrogels rapidly in aqueous media. Scanning electron microscopy, swelling behavior studies and degradation kinetics studies were performed to demonstrate the effect of this synthetic modification on the hydrogels formation of chitosan network and in vitro drug release. The effects of OGMO-CS type, dry hydrogels percentage, release media and drug loading on the sustained release of the model drug trimetazidine hydrochloride were evaluated. The release profiles of the hydrogels could be described by the Peppas-Sahlin mechanism, a combination of Fickian diffusion and Case-II relaxation. Based on the fact that numerous pharmaceutical lipids are available, the present study may pave the way for other lipids to be employed as modifiers of chitosan for more innovative chitosan derivatives with versatile properties and pharmaceutical applications.
本文以甘油单油酸酯为起始原料合成了氧化甘油单油酸酯(OGMO)。随后,OGMO 通过亚胺键(-C=N-)与壳聚糖(CS)连接,得到了一种新型壳聚糖基聚合物(OGMO-CS),它可以在水介质中迅速形成水凝胶。通过扫描电子显微镜、溶胀行为研究和降解动力学研究,证明了这种合成修饰对壳聚糖网络水凝胶形成和体外药物释放的影响。考察了 OGMO-CS 类型、干水凝胶百分比、释放介质和载药量对模型药物盐酸曲美他嗪的缓释效果。水凝胶的释放曲线可以用 Peppas-Sahlin 机制来描述,这是 Fickian 扩散和 Case-II 松弛的结合。鉴于有大量的药用脂质可用,本研究可能为其他脂质作为壳聚糖改性剂开辟道路,以获得具有多种性能和药用应用的更具创新性的壳聚糖衍生物。