5-氟尿嘧啶聚己内酯针状植入剂的研究

Study on Acicular Poly(ε-Caprolactone) Implants Containing 5-Fluorouracil

目的以聚己内酯(PCL)为载体材料、聚乙二醇(PEG)或明胶为添加剂,制备和表征含有5-氟尿嘧啶(5-Fu)的针状植入剂,研究植入剂的体外释放行为。方法采用熔融挤出法制备针状含5-Fu的植入剂,利用XRD和SEM表征植入剂的结晶性和形貌。考察药物含量(12.5%,25%,50%)、添加剂种类(PEG,明胶)、添加剂含量(5%,10%,25%)对药物释放行为的影响。结果植入剂表面光滑,药物在植入剂中分布均匀;植入剂中的5-Fu、PCL和PEG均具有一定程度的结晶性;植入剂中药物含量越大、释放越快;添加PEG或明胶,药物释放加快。结论植入剂制备工艺简单可行,改变载药量、添加剂及其用量可调节植入剂中5-Fu的释放行为,针状植入剂可通过注射器直接注入肿瘤部位,可能在瘤内给药方面有很好的应用前景。

OBJECTIVE To prepare 5-fluorouracil （5-Fu） loaded acicular implants and to investigate the in vitro 5-Fu release behaviors. METHODS The 5-Fu loaded implants were fabricated by hot-melting extrusion method, using PCL as matrix, PEG or gelatin as additive. X-ray diffraction （XRD） and scanning electron microscopy （SEM） were used to character the crystallinity and morphology of implants respectively. The influences of drug loading （12.5%, 25%, 50% ）, types of additives （ PEG and gelatin）, PEG or gelatin content （5%, 10%, 25%）on drug release behaviors were investigated. RESULTS The obtained implants were with smooth surface. 5-Fu was dispersed uniformly in implants. Crystalline of 5-Fu, PCL and PEG in implants were observed. The higher drug loading, the faster drug release. The addition of PEG or gelatin accelerated drug release. CONCLUSION The fabrication process of implants was easy and feasible, drug release behaviors could be adjusted by changing drug loading, types of additives and additive content. Acicular implants could be potential for drug delivery within tumor.