3种药物传递体的制备及其包封率、体外释放的比较研究

目的:通过对不同药物所制得传递体的包封率和体外释放差异的探讨,找出药物性质对传递体包封率和体外释放影响的规律。方法:采用相同的原料和方法制备了秋水仙碱(CLC)、硫酸长春新碱(VCR)和盐酸米托蒽醌(DHAD)的传递体(CLC-T,VCR-T,DHAD-T)并测定包封率,探讨了药物的溶解性、分子质量和电性等与包封率的关系;进行传递体体外释放实验,比较不同药物传递体体外释放的差异。结果:VCR和DHAD属于亲脂性或亲水性强、分子质量大和带正电荷的药物,所得传递体的包封率高,而CLC属于两亲性的、分子质量小和不带电荷的药物,所得传递体的包封率很低;由于DHAD有插膜作用,DHAD-T的体外释放明显较VCR-T缓慢。结论:在制备传递体时,应选择亲脂性或亲水性强、分子质量大和与膜带相反电荷的药物,否则不容易制备成传递体。药物与传递体之间的相互作用是影响传递体体外释药速率的因素之一。

Preparation and characterization of transfersomes of three drugs in vitro

Objective: To investigate the influence of drug properties on the encapsulation effiency(EE) and drug release of transfersomes for a proper transfersome preparation.Method: To prepare the transfersomes of colchicines(CLC),vincristine sulfate(VCR) and mitoxantrone hydrochloride(DHAD) with the same materials and methods,and then measure their EE.To find out the relationship between drug properties like solubility,molecular weight and charges,and EE.To performe the drug release experiments of various types of transfersomes in vitro,and compare their differences.Result: VCR and DHAD are lipophilic or hydrophilic,owing positive charges and large molecular weight,as a result,their EE are high,while CLC is amphipathic,neutral,and of small molecular weight,its EE is very low.As DHAD can insert into the membrane of transfersome,the drug release of DHAD-T in vitro is much slower than that of VCR-T.Conclusion: To prepare transfersomes with high EE,drugs that are lipophilic or hydrophilic,high molecular weight and opposite charges to the membrane should be chosen.Interaction between drugs and membrane will influnce the rate of drug release.