Preparation of nanoparticles co-modified with chitosan and cell-penetrating peptides and in vitro cytological evaluation against colon cancer
Objective:To improve the oral efficacy of 5-fluorouracil(5-FU)against colon cancer,PLGA nanoparticles co-modified by N,N,N-trimethyl-N-stearoyl chitosan(TSCS),adenosine and cell-penetrating peptide(TAT)were constructed and evaluated.Methods:TSCS,stearoyl adenosine and 5-fluorouracil phospholipid complexes were synthesized and co-modified nanoparticles AD-CPP-NPs were prepared and evaluated pharmacologically and cytologically in terms of particle size,encapsulation rate and in vitro release.Results:The nanoparticles were sphere-like in appearance and homogeneously distributed.The measured nanoparticle size was about 177 nm,the Zeta potential was 38.2 mV,and the encapsulation rate was 56.6％.Cellular experiments showed that after co-incubation with HT-29 cells for 4 h,the uptake capacity of co-modified nanoparticles was increased by 16.42-fold relative to PVA-NPs compared to PLGA nanoparticles with unmodified surface.Conclusion:Co-modified nanoparticles can actively target colon cancer cells,enhance cell uptake efficiency,and increase the accumulation of 5-FU in cancer cells.
chitosannanoparticlescell-penetrating peptidescolon canceroral drug delivery
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