A new type of itraconazole amphiphilic chitosan preparation of nanometer antibacterial agent and activity against Candida albicans in vitro
The limitations of antifungal drugs and severe drug resistance make the treatment of invasive fungal infections(IFIs)a great challenge.Itraconazole(ITZ),as a clinical first-line drug,has a wide range of antifungal activity,but it is still limited by adverse reactions such as liver and kidney toxicity,headache and abdominal pain due to its poor water solubility and easy to cause drug accumulation by injection.In this study,the amphiphilic polymer gallic acid-chitosan-cinnamaldehyde(GA-CS-CN)was prepared by amide reaction and Schiff-base reaction.The drug-loaded nanoparticles(GA-CS-CN/ITZ)were prepared by ultrasonic method.The properties of nanoparticles formulations and its in vitro antifungal activity were investigated in the study.Studies have shown that GA-CS-CN/ITZ is spherical,homogeneous and stable,and has good biological safety.The average particle size was 239.57±31.37 nm,ITZ encapsulation efficiency was(93.41±1.12)％,and the cumulative drug release was(62.25±1.88)％at 48 h in vitro.The antifungal activity results of Candida albicans ATCC 10231(C.albicans)showed that it had the optimal antifungal effect and could significantly enhance the antifungal activity of free drugs.GA-CS-CN/ITZ prepared in this study has excellent biological safety and anti-C.albicans performance,which provides a new choice for the treatment of C.albicans infection and has good application potential in the treatment of this fungal infection.
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