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Improving Antitumor Activity with N-Trimethyl Chitosan Entrapping Camptothecin in Colon Cancer and Lung Cancer.

Abstract
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.
AuthorsLu Sun, Xingyi Li, Zhengguang Li, Zhiyong Li, Maling Gou, Zhiyong Qian, Feng Peng
JournalJournal of nanoscience and nanotechnology (J Nanosci Nanotechnol) Vol. 15 Issue 9 Pg. 6397-404 (Sep 2015) ISSN: 1533-4880 [Print] United States
PMID26716193 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Drug Carriers
  • N-trimethyl chitosan chloride
  • Chitosan
  • Camptothecin
Topics
  • Animals
  • Antineoplastic Agents (chemistry, pharmacology, toxicity)
  • Camptothecin (chemistry, pharmacology, toxicity)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Cell Survival (drug effects)
  • Chitosan (chemistry, toxicity)
  • Colonic Neoplasms
  • Drug Carriers (chemistry, toxicity)
  • Female
  • Lung Neoplasms
  • Mice
  • Mice, Inbred BALB C

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