Development, characterization and cancer targeting potential of surface engineered carbon nanotubes

Abstract

The aim of the present study was to assess the in vitro and in vivo potential of doxorubicin-loaded, folic acid appended engineered multi-walled carbon nanotubes (DOX/FA-PEG-MWCNTs) for efficient tumor targeting. The loading efficiency was determined to be 92.0 ± 0.92 (DOX/FA-PEG-MWCNTs) in phosphate buffer solution (pH 7.4) ascribed to π–π stacking interaction. The developed nanoconjugates were evaluated for in vitro DOX release, erythrocytes toxicity, ex vivo cytotoxicity and cell uptake studies on MCF-7 (breast cancer cell line). The DOX/FA-PEG-MWCNTs nanoconjugate affords higher efficacy in tumor growth suppression due to its stealth nature and most preferentially taken up by the cultured MCF-7 through caveolae-mediated endocytosis as compared to free DOX. The in vivo studies were performed to determine the pharmacokinetics, biodistribution and antitumor efficacy on tumor bearing female Sprague Dawley rats and improved pharmacokinetics confirm the function of FA-PEG conjugated CNTs. The median survival time for tumor bearing rats treated with DOX/FA-PEG-MWCNTs (30 d) was extended very significantly as compared to free DOX (p < 0.001). The results concluded that developed water-soluble nano-conjugates might emerge as “safe and effective” nano-medicine in cancer treatment by minimizing the side effects with and Generally Regarded as Safe prominence.

• Anti-tumor activity
• carbon nanotubes
• doxorubicin
• drug targeting
• folic acid
• MCF-7 cells
• pharmacokinetic

Acknowledgements

The authors gratefully acknowledge M/s Sun Pharmaceutical Advanced Research Center (SPARC), Vadodara, India, for a gift sample of Doxorubicin hydrochloride, All India Institute of Medical Sciences (AIIMS), New Delhi, India, for Transmission Electron Microscopy (TEM) and Scanning Electron Microscopy (SEM). One of the authors (Neelesh Kumar Mehra) is thankful to the University Grants Commission (UGC), New Delhi, India for providing the Junior Research Fellowship (JRF) during the tenure of these studies.