Camptothecin (
CPT) exerts very strong antitumor activities by suppressing the activity of
DNA topoisomerase I, but its application is greatly limited owing to its low solubility and the instability of the active
lactone form. To overcome this bottleneck, we prepared the novel
camptothecin nanocolloids based on
N-trimethyl chitosan (
CPT-TMC) to efficiently administer
CPT systemically. In this study, we investigated the antitumor activity of
CPT-TMC against both
colon cancer and
lung cancer. In vitro cell experiments both
CPT and
CPT-TMC significantly inhibited the growth of CT26 cells and LL/2 cells, but no statistical difference was observed between
CPT-TMC and
CPT. In vivo studies,
CPT-TMC more effectively inhibited
tumor growth and prolonged survival time than
CPT both in the CT26 colon
carcinoma subcutaneous model and in the LL/2
Lewis lung carcinoma subcutaneous model. In addition, results of
PCNA and CD31 immunohistochemical staining of
tumor tissues also confirmed the improved antitumor effect of
CPT-TMC. These findings suggest that
N-trimethyl chitosan could increase the antitumor effect of
CPT. Consequently,
CPT delivery by
N-trimethyl chitosan is a potential approach for effective treatment of
cancer.