摘要
合成新型的功能性氧化石墨烯-β-环糊精/盐酸利多卡因包合物(Graphene Oxide-dextran-β-Cyclodextrin/Lidocaine hydrochloride,GO-DEX-β-CD/LDH),并研究其对盐酸利多卡因(lidocaine hydrochloride,LDH)的装载,释放和经皮给药的渗透性能。以高效液相色谱法测定利多卡因含量,并对制剂的高效装载和缓释性进行研究,以离心法测定GO-DEX-β-CD/LDH的包封率。将含药载体应用于离体和在体小鼠皮肤,研究GO-DEX-β-CD/LDH经小鼠皮肤给药的渗透性。GO-DEX-β-CD对盐酸利多卡因的载药率较高,其释放具有较好的缓释,经皮给药的渗透性能良好。结果显示,应用GO-DEX-β-CD/LDH后12 h累积渗透量是(11.029±0.521)μg。在体鼠皮渗透实验中,应用GO-DEX-β-CD/LDH,10 min时皮肤内药物浓度达峰值。GODEX-β-CD/LDH制备工艺可行,渗透速度较快,透皮效果良好,为进一步临床应用提供了良好的实验依据。
The new-type GO-DEX-β-CD/LDH inclusion compound were synthetized, and the high-efficiency loading , sustained-release and permeability as transdermal delivery for Lidocaine hydrochloride composites were studied. The concentration of LDH was determined by high efficiency liquid chromatography. The high-efficiency loading , sustained-release and permeability as transdermal delivery of the GO-DEX-β-CD/LDH were studied, and the encapsulation efficiency of it was determined by centrifugation. The GO-DEX-β-CD/LDH was applied onto the mouse skin in vitro and in vivo to develop the permeability of it. The GO-DEX-β-CD had a high loading rate for LDH and had a good sustained-release performance, and the permeability as transdermal delivery of Lidocaine hydrochloride composites was good . The results showed that the number of the accumulation permeation was （11. 029 ±0. 521 ） μg after GO-DEX-β-CD/LDH had been applied over 12 h. In the penetration experiments of mouse skin in vivo, drug concentration in skin reached the peak on 10 min by the application of GO-DEX-β-CD/ LDH. The preparation techniques of GO-DEX-β-CD/LDH was feasible, and the velocity of permeability of it was fast. GO-DEX-β-CD/LDH is promising in enhancing the permeability across the skin and provide great potential for transdermal drug delivery.
出处
《科学技术与工程》
北大核心
2015年第23期130-135,共6页
Science Technology and Engineering
基金
国家863计划(2007AA021809)资助
