正极性驻极体与氮酮联合调控5-氟尿嘧啶在SD大鼠皮肤中的储存

为寻求临床上5-氟尿嘧啶（简称5-FU）治疗增生性瘢痕更安全有效的给药方式,以5-FU为模型药物,以质量分数为3%的氮酮（简称3%氮酮）为化学促渗剂,通过改良的Franz扩散池和高效液相色谱仪研究了经不同等效表面电位正极性驻极体与3%氮酮联合作用时5-FU药物体外经SD大鼠腹部、背部和瘢痕皮肤的渗透规律以及在这3类皮肤中的储存特性。研究结果表明：（1）等效表面电位为500 V、1 000 V、2 000 V的正极性驻极体分别与3%氮酮联合作用对5-FU药物的经皮渗透均具有促进作用,等效表面电位越高,5-FU累积透皮量就越小;（2）5 000 V正极性驻极体与3%氮酮联合作用促进药物经皮渗透的作用明显被削弱;（3）不同等效表面电位正极性驻极体均可增加皮肤角质层和去角质层皮肤中5-FU滞留量,5-FU滞留量与驻极体的等效表面电位正相关;（4）在瘢痕、背部和腹部皮肤中5-FU滞留量从大到小的顺序依次为背部皮肤、瘢痕皮肤、腹部皮肤。综上所述,不同等效表面电位正极性驻极体与3%氮酮联合作用均可促进5-FU体外经SD大鼠皮肤的渗透,高等效表面电位驻极体可使更多5-FU滞留于皮肤组织中,符合增生性瘢痕治疗中5-FU用药的预期效果,可为增生性瘢痕的临床治疗提供新技术、新方法。     

Evaluations of dielectric property and drug release profile of 5-FU patches based on plasma charged electrets

In the present study, the electret 5-fluorouracil patch was developed, the effective surface potential, piezoelectric coefficient d33, open-circuit thermally stimulated discharge (TSD) current spectra and shear adhesion of the patch were measured. The drug release profile of the patch was determined by using high performance liquid chromatography method. A stable potential difference which was positively dependent on the surface potential of the electret was generated on two sides of the patch. The measurements of d33 coefficient, TSD current spectra and adhesion performance showed that the electrostatic field of the electret could cause polarization and cohesive strength decreasing of the matrix molecules, change the distribution and interaction of the drug molecules in patch, therefore to increase the release of drug from the transdermal patch.