摘要
目的:制备和厚朴酚纳米晶体制剂,对其理化特性、抗炎效果及毒性进行考察。方法:采用微量沉淀法制备两种和厚朴酚的纳米晶体制剂,对和厚朴酚纳米晶体的粒径、PDI、电位、储存稳定性、稀释稳定性及药物体外释放进行表征,进一步考察和厚朴酚纳米晶体对小鼠耳肿胀及大鼠毒性的影响。结果:两种和厚朴酚纳米晶体的粒径分别为(27.21±0.231)nm和(25.94±0.038)nm,平均PDI为(0.032±0.011),电位为(-7.03±0.705)Mv,透射电镜下呈球形;4℃下放置14 d,稀释10倍能保持稳定;pH=6.8的释放介质中,和厚朴酚的纳米晶体制剂释放率远高于游离的和厚朴酚;和厚朴酚的纳米晶体制剂治疗组小鼠耳廓肿胀率为34.77%和59.50%,明显低于原料药组;大鼠胃、十二指肠、空肠、回肠HE染色切片表明,和厚朴酚纳米晶体无明显毒副作用。结论:该研究制备的和厚朴酚纳米晶体制剂方法简单,能明显增加和厚朴酚的水溶性和口服吸收,有望提高药物的生物利用度和抗炎作用。
Objective:Preparation of honokiol nanocrystalline preparation,and investigation of its physicochemical prop-erties,anti-inflammatory effect and toxicity.Methods:Two kinds of honokiol nanocrystals were prepared by micro pre-cipitation method.The particle size,PDI,potential,storage stability,dilution stability and drug release in vitro of hono-kiol nanocrystals were characterized,and the effects of honokiol nanocrystals on ear swelling in mice and toxicity in rats were further investigated.Results:The particle sizes of the two kinds of honokiol nanocrystals were(27.21±0.231)nm and(25.94±0.038)nm,respectively.The average PDI was(0.032±0.011),and the potential was(-7.03±0.705)Mv.They were spherical under transmission electron microscopy;Keep it at 4℃for 14days,and keep it stable after 10times dilution;In the release medium of pH=6.8,the release rate of honokiol nanocrystals was much higher than that of free honokiol;The ear swelling rate of mice in the treatment group with nano crystal preparation of honoki-ol was 34.77%and 59.50%,which was significantly lower than that in the bulk drug group;HE staining sections of rat stomach,duodenum,jejunum and ileum showed that honokiol nanocrystals had no obvious toxic and side effects.Conclusion:The preparation method of honokiol nanocrystals prepared in this study is simple,which can significantly increase the water solubility and oral absorption of honokiol,and is expected to improve the bioavailability and anti-in-flammatory effect of the drug.
作者
聂彦丰
王小莉
范永春
Nie Yanfeng;Wang Xiaoli;Fan Yongchun(Pizhou Hospital of Chinese Medicine,Pizhou 221300,China;Department of Pharmacy,The Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine,Nanjing 210028,China;Jiangsu Province Academy of TCM,Nanjing 210028,China)
出处
《亚太传统医药》
2023年第4期15-21,共7页
Asia-Pacific Traditional Medicine
关键词
和厚朴酚
纳米混悬剂
生物利用度
抗炎药效
毒性试验
Honokiol
Nanosuspensions
Bioavailability
Anti-Inflammatory Efficacy
Toxicity Test
