鬼臼毒素脂质体壳聚糖涂膜剂的初步研究

目的：研制宫颈靶向性脂质体鬼臼毒素壳聚糖涂膜剂。方法：反相蒸发法制备脂质体鬼臼毒素混悬液，壳聚糖作为涂膜剂的成膜材料，配置成0．5％的脂质体鬼臼毒素涂膜剂；进行光镜及电镜下的形态观察，库尔特计数仪检测脂质体粒度，HPLC法测定包封率，观察时间稳定性和热稳定性，并进行了治疗阴道内尖锐湿疣的临床观察。结果：反相蒸发法制备的脂质体为单层脂质体，粒度在200nm～800nm之间，平均粒度为350nm，鬼臼毒素平均包封率76．3％，平均回收率96．3％，壳聚糖涂膜荆稳定性较脂质体混悬液高，治疗阴道内尖锐湿疣效果优于鬼臼毒素软膏而局部刺激性小。结论：脂质体鬼臼毒素涂膜剂制备工艺可行，质量控制方法简单、可靠，对阴道内尖锐湿疣疗效肯定，是作用于宫颈上皮的理想的制剂。

RUDIMENTARY STUDY OF PODOPHYLLOTOXIN LIPOSOME CHITOSAN FILM

Objective:To prepare the target podophyllotoxin liposome film for cervix uteri epithelia. Methods:Liposome solution prepared by reverse-phase evaporation and film material prepared by chitosan were used to prepare the 0.5% podophyllotoxin liposome film.The configuration of the liposomes was observed with optics and electronics microscopes , the diameter was measured by coulter counter,and the embedding ratio of podophyllotoxin was examined by HPLC. We also studied the time stability and the hot stability, studied the clinical effect assessment for treating the endovaginal condyloma acuminatum.Results:The liposomes prepared by reverse-phase evaporation were Mono-stratiform and its diameter ranged from 200nm to 800nm, the average diameter was 350nm, the average embedding ratio was 76.3%, and the average reclaim ratio was 96.3 %. The stability of podophyllotoxin liposome film was better than that of podophyllotoxin liposome solution. Podophyllotoxin liposome film was more effective in treating the endovaginal condyloma acuminatum than podophyllotoxin ointment and had less topical lesion.Conclusions:The technics of preparing the podophyllotoxin liposome film is feasible and the method of quality control is simple and reliable, podophyllotoxin liposome film is more effective for treating the endovaginal condyloma acuminatum and expected to be an ideal preparation to cervix uteri epithelia.