氟脲嘧啶-羟丙基-β-环糊精包合物的生物黏附凝胶剂的制备与评价

Preparation and characterization of bio-adhesive vaginal gel containing 5-fluorouracil-HP-β-CD inclusion

目的:宫颈癌是导致女性因癌症而死亡的第二大原因,为了提高治疗效果和患者的顺应性,制备了药物5-氟尿嘧啶生物黏附性阴道用凝胶,为了增加药物的溶解度,对药物进行了环糊精包合。方法:在对包合物进行红外光谱、X射线衍射和电镜扫描后,以聚卡波菲为凝胶基质制备生物黏附阴道用凝胶,采用HPLC法,测定制剂在水中的溶出度。结果:羟丙基-β-环糊精显著提高了药物的溶解度,以聚卡波菲为凝胶基质制得的制剂在低浓度下黏附性高,并能延缓药物的释放。结论:以聚卡波菲为基质,制备5-氟尿嘧啶-羟丙基-β-环糊精包合物生物黏附性阴道用凝胶剂,适合于阴道给药治疗宫颈癌。

Objective： Cervical cancer is the second leading cause of cancer deaths among women. To achieve a better therapeutic efficacy and patient compliance,5-fluorouracil has been formulated in a bio-adhesive vaginal gel using the polycarbophil. To increase its aqueous solubility,the drug was incorporated with hydroxypropyl-β-cyclodextrin（ HP-β-CD）. Methods： The inclusion sample was characterized by Fourier-transform infrared（ FT-IR） spectrometry,X-ray diffraction（ XRD）,and scanning electron microscope. The polycarbophil was used to develop vaginal gel,and the dissolutions of gels in pure water were determined. Results： HP-β-CD can increase the solubility of 5-fluorouracil significantly. The formulation containing polycarbophil has high bio-adhesive strength at a low concentration. Furthermore,polycarbophil could sustain the release of 5-FU. Conclusion： The developed bio-adhesive vaginal gel containing 5-fluorouracil-HP-β-CD is suitable to be applied in vagina site to treat cervical cancer.