摘要
目的:观察葡聚糖接枝聚乳酸载吗啡缓释纳米粒胶束(MP/DEX-PLA)对急性疼痛大鼠的镇痛效应。方法:SD雄性大鼠40只,随机均分为4组,A组(空白对照组),B组(空白纳米胶束对照组),C组(普通吗啡组),D组(载吗啡纳米胶束组)。制备可生物降解的载吗啡葡聚糖接枝聚乳酸共聚物,皮下用药后测定急性疼痛大鼠的累计疼痛评分(CPS)和痛阈,评价药物的镇痛效果,观察其副作用。结果:MP/DEX-PLA纳米胶束呈球形,平均载药量为20.94%,平均包封率为36.27%。建模手术后,各组大鼠痛阈明显降低(P<0.05);给药后,C组和D组CPS明显低于B组,痛阈明显升高(P<0.05);C组和D组分别于给药后30 m in和2h时达到最大镇痛效应,C组镇痛持续时间明显短于D组(P<0.05),C组和D组痛阈最高值和CPS无明显差异(P>0.05),C组不良反应发生率显著高于D组(P<0.05)。结论:皮下单次给予MP/DEX-PLA可通过吗啡缓慢释放发挥持续镇痛作用,副作用小于普通吗啡。
investigate the analgesic effect of morphine encapsulated in polylactide-grafted dextran copolymer （MP/DEX-PLA） nano-micelles on acute nociception in rats. Methods： 40 male adult SD rats, weighing 220 - 280g, were randomly allocated to four groups （ n = 10） ： group A （ control group）, group B （received DEX-PLA without morphine）, group C （received morphine 3mg/kg） and group D （received MP/DEX-PLA 15mg/kg）. The biodegradable morphine encapsulated in polylactide grafted dextran copolymer nano-micelles was prepared and subcutaneous injected in thenar aching model rats, and the analgesic effect was observed. The cumulated pain score （CPS） and pain threshold were measured before thenar incision and after drug administration at 30 min, 1h, 2h, 4h, 6h, and 9h. The side effects were recorded. Results： MP/DEX-PLA nano-micelles were round or elliptical in shape. The percent of drug loading was 20.94% and the encapsulating efficiency was 36.27%. Pain threshold decreased significantly after thenar incision in group B, C and D （ P 〈 0.05 ）. Compared with group B, CPS decreased and pain threshold increased significantly after subcutaneous injection with morphine or MP/DEX-PLA （P 〈 0.05 ）. The maximum analgesia in group C and D were obtained at 30 min and 2h after drug administration respectively. Duration of analgesia in group C was significantly shorter than that in group D （ P 〈 0.05 ）. There were no significantly difference in maximum pain threshold and CPS （ P 〉 0.05 ） between group C and D. The percent of rats with side effects in group C was significantly higher than that in group D （P 〈 0.05 ）. Conclusion ： Compared with equivalent-analgesia dose of common morphine, subcutaneous injection with MP/DEX-PLA could obtain extended duration of analgesia with rare side effects.
出处
《中国疼痛医学杂志》
CAS
CSCD
2010年第4期232-235,共4页
Chinese Journal of Pain Medicine
关键词
吗啡
纳米
急性痛
镇痛
药效学
葡聚糖接枝共聚物
Morphine
Nano-micelles
Acute nociception
Analgesia
Pharmacodynamics
Dextran grafted copolymer
