基于聚乙烯亚胺构建pH响应性口服甲氨蝶呤纳米递送系统

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Abstract ObiectiveTo construct pH-responsive oral Methotrexate(MTX)nanoparticles based polyethylenimine(PEI)for improving the oral bioavailability of Methotrexate.MethodsMTX nanoparticles were prepared by dialysis with MTX and PEI based on multiple non-covalent interactions between them.Physicochemical characteristics of nanoparticles containing morphology,particle size,zeta potential,drug loading,and entrapment efficiency were observed and determined,and in vivo and in vitro drug release profiles were employed to evaluate the pH responsive release ability and the oral bioavailability of MTX/PEI nanoparticles.ResultsThe nanoparticles were successfully prepared as discrete and uniform spheres with positive charges,which exhibited an excellent MTX loading performance,and an obvious pH responsive release behavior that no released in pH=1.2 solvent,but rapidly released in pH=7.4 solvent.Compared with the raw MTX and tablet of MTX,MTX/PEI nanoparticles showed a shorter peak time and higher peak concentration after oral administration,and also a larger area undercurve (AUC).ConclusionOral bioavailability of MTX is significantly improved by MTX/PEI nanoparticle system.Based on this,the MTX/PEI nanoparticlesystem is expected to significantly enhance the oral MTX antitumor activity with a good prospect in application.

Key words： Nanoparticles Methotrexate Polyethyleneimine Oral administration

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	MENG Xiao-li
	LONG Ling
	CHEN Xiao-yong

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MENG Xiao-li,LONG Ling,CHEN Xiao-yong. The construction of pH-responsive oral Methotrexate nanoparticles based polyethylenimine[J]. 中国当代医药, 2018, 25(4): 20-24.

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http://dangdaiyiyao.com/EN/ OR http://dangdaiyiyao.com/EN/Y2018/V25/I4/20

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