芒果苷传递体的制备及其经皮给药特性的研究  

Preparation of Mangiferin-loaded Transfersomes and Its Transdermal Delivery Characteristics

作　　者：孙爱珍[1,2] 郑银[1,2] 王亚静[1,2] 皮佳鑫[1,2] 方晓玉[1,2] 王文津[1,2] 

机构地区：[1]天津中医药大学,天津300193 [2]现代中药发现与制剂技术教育部工程研究中心,天津300193

出　　处：《中国药学杂志》2016年第9期727-731,共5页Chinese Pharmaceutical Journal

基　　金：国家科技部"重大新药创制"科技重大专项-现代中药新药发现和评价技术平台建设资助项目(2012ZX09304007)

摘　　要：目的制备芒果苷传递体,并研究其经皮给药特性。方法采用薄膜分散法制备芒果苷传递体,以改良的Franz扩散池法研究其体外经皮渗透特性,用荧光示踪法对传递体在皮肤中的分布特性进行考察,采用大鼠背部气囊炎症模型,以前列腺素E2(PGE2)的含量为指标,对芒果苷传递体的抗炎效果进行初步评价。结果芒果苷传递体平均粒径为(84.50±5.26)nm,多分散指数(PDI)为(0.21±0.012),Zeta电位为(-10.83±0.66)m V,包封率为(64.07±2.10)%,变形性为(20.0±1.30)%;芒果苷传递体24 h累积经皮渗透量和皮内滞留量,分别为(313.672±22.62)和(60.34±8.10)μg·cm-2,荧光示踪法显示,在8 h时FITC传递体在皮内的荧光强度高于FITC溶液;抗炎实验表明,芒果苷传递体中、高剂量组的PGE2含量显著下降,特别是高剂量组,达到与复方地塞米松组相当的抗炎效果。结论传递体能够促进芒果苷的经皮渗透,增加其皮内滞留量,并显著增强芒果苷的抗炎作用。OBJECTIVE To prepare mangiferin transfersomes and investigate its transdermal delivery characteristics. METH- ODS Mangiferin transfersomes were prepared by the method of film-dispersion, the in vitro percutaneous penetration study was con- ducted in the modified Franz diffusion cell, the distribution of transfersomes in skin was investigated by fluorescent tracer method, and the rat back airbag inflammation model was used to preliminarily evaluate the anti-inflammatory effect of mangiferin transfersomes with prostaglandin E2 （PGE2） content as the indicator. RESULTS The average particle size of mangiferin transfersomes was （ 84. 50 ± 5.26） nm, the polydispersity index （PDI） was （0. 21 ± 0. 012）, the Zeta potential was （ - 10. 83 ± 0. 66） mV, the encapsulation effi- ciency （ EE ） was （ 64. 07 ± 2. 10 ） %, and the deformability was （ 20. 00 ± 0. 30 ） % ; the cumulative permeation quantities in 24 h and intradermal retention of mangiferin transfersomes were （313.67 ± 22. 62 ） and （60. 34 ± 8.10 ） μg · cm-2, respectively. Fluorescent tracer method showed that the fluorescence intensity of FITC transfersomes in the inside of skin was stronger than that of FITC solution at 8 h. Anti-inflammatory test showed that the PGE2 contents in the middle and high dose mangiferin transfersomes groups decreased significantly. The anti-inflammatory effect of the high dose mangiferin transfersomes was even close to that of compound dexamethasone cream. CONCLUSION Transfersomes can promote the pereutaneous penetration of mangiferin, increase its intradermal retention, and enhance the anti-inflammatory effect of mangiferin significantly.

关 键 词：芒果苷 传递体 经皮渗透性 皮内分布 抗炎 

分 类 号：R944[医药卫生—药剂学]