聚乳酸阿霉素纳米微粒的制备及体内外释药的研究  

The preparation and drug-release study in vivo and in vitro of poly (lactic acid) adriamycin nanoparticles

作　　者：殷香保[1] 黎洪浩[1] 陈汝福[1] 叶华[1] 任山[2] 王捷[1] 区庆嘉[1] 

机构地区：[1]中山大学附属第二医院普外科,广州510120 [2]中山大学纳米技术研究中心

出　　处：《中华实验外科杂志》2006年第2期227-229,共3页Chinese Journal of Experimental Surgery

基　　金：国家高技术研究发展计划(863计划)分课题基金资助项目(2002AA214061)

摘　　要：目的研究聚乳酸阿霉素纳米微粒(ADM-NP)的制备及其在体内外的释药特点。方法以聚乳酸为包封材料,以阿霉素为模型药物,采用复乳法制备ADM-NP。采用扫描电镜、动态光散射法及高效液相色谱法分别考察纳米微粒的形态、粒径分布、载药量及包封率,通过体内外实验探讨纳米微粒的释药特点。结果ADM-NP在扫描电镜下呈球形,粒径为(163±52)nm,载药量为(28.4±4.5)%,包封率为(73.6±9.2)%。ADM-NP在体外释药缓慢,在大鼠体内的消除半衰期(t1/2)、曲线下面积(AUC)、平均滞留时间(MRT)均明显大于游离阿霉素(F-ADM,P<0.01)。结论ADM-NP在体内外均具有良好的缓释性,其化疗效果理论上可望优于F-ADM。Objective To study the preparation and drug-release properties in vivo and in vitro of poly （lactic acid） （PLA） adriamycin nanoparticles （ADM-NP）. Methods ADM-NP were prepared by using double emulsion method, with PLA as embedding materials, adriamycin as embedded drug. Morphology, diameters, drug-loaded amount and embedding ratio of ADM-NP were examined respectively by means of scanning electron microscope （SEM）, dynamic light scatter （DLS）, and high pressure liquid chromatography （HPLC）. Drug-release properties of ADM-NP were investigated by experiments in vivo and in vitro. Results ADM-NP looked like microspheres under SEM, whose diameters were （ 163 ± 52） nm. Their drug-loaded amount and embedding ratio were （28.4±4.5） % and （73.6 ± 9.2） % respectively. Drug-release process of ADM-NP in vitro was slow. Elimination half-life （t1/2）, area under curve （AUC）, and mean residence time （MRT） of ADM-NP in rats were much longer or bigger than those of free adiamycin （F-ADM, P〈0.01）.Conclusion ADM-NP shows excellent sustained release properties both in vitro and in vivo. Its chemotherapeutic effect is theoretically superior to that of F-ADM.

关 键 词：阿霉素 纳米微粒 药代动力学 

分 类 号：TQ460.1[化学工程—制药化工]