摘要
为了实现疏水性药物和亲水性药物共同包载,采用自由基聚合法和物理交联法制备了羟丙基甲基纤维素(HPMC)/聚异丙基丙烯酰胺(PNIPAm)水凝胶。甲氨蝶呤(MTX)和亚叶酸钙(CaF)被选为模型药物。用相转变分析、差示扫描量热法(DSC)、傅里叶红外光谱(FT-IR)、扫描电子显微镜(SEM)和紫外-可见分光光度计(UV)等考察了水凝胶的理化性能及其体外释药行为。结果表明,该水凝胶最低临界溶解温度(LCST)为32.6℃,呈相互连接3D多孔结构,孔径30~80μm。加入HPMC有利于包载以及药物的减缓释放;体外释放发现,CaF的释放速率略高于MTX,在MTX释放时,其周围环境中已存在部分CaF,预示该水凝胶可能有较好的预防MTX过量或大剂量应用后引起的严重不良反应的效果。
In order to achieve the entrapment of hydrophobic drugs and hydrophilic drugs,hydroxypropyl methylcellulose(HPMC)/polyisopropyl acrylamide(PNIPAm)hydrogels were prepared by free radical polymerization and physical cross-linking.Methotrexate(MTX)and calcium folinate(CaF)were selected as model drugs.The physicochemical properties of the hydrogels and their release behaviors in vitro were investigated by using phase transition analysis,differential scanning calorimetry(DSC),Fourier transform infrared spectroscopy(FT-IR),scanning electron microscopy(SEM)and UV-visible spectrophotometry(UV).The results showed that the lower critical solution temperature(LCST)of the hydrogel was 32.6℃.The hydrogel was connected to a 3 Dporous structure with a pore size of 30 to 80μm.The addition of HPMC helps to entrap the hydrophobic drug.The addition of HPMC facilitates the entrapment of hydrophobic drugs and the sustained release of the drug.In vitro release showed that the release rate of CaF was slightly higher than that of MTX.When MTX was released,part of CaF was already present in its surrounding environment,indicating that the hydrogel may have better effects of preventing serious adverse reactions caused by excessive MTX or high-dose application.
引文
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