title: Gemcitabine-loaded smart carbon nanotubes for effective targeting to cancer cells.
abstract: Carbon nanotubes (CNTs) are the three-dimensional sp(2) hybridized nano-containers that have attracted considerable interest in drug delivery by offering potential advantages such as biocompatibility, non-immunogenicity, high loading efficiency, intrinsic stability and low toxicities. The aim of the present investigation was to assess the potential of gemcitabine-loaded folic acid (FA) conjugated multi-walled CNTs (GEM/FA-NT) for targeting to breast cancer cells. Pristine MWCNTs was functionalized by FA followed by carboxylation, acylation and amidation and characterized by electron microscopy, FT-IR spectroscopy, X-ray diffraction, entrapment efficiency, cytotoxicity and in vivo studies. FDA-approved GEM was loaded to the purified (GEM-NT) and GEM/FA-NT, and % entrapment efficiency was found to be approximately 71.60 ± 0.25 and 79.60 ± 0.45, respectively. The developed formulation GEM/FA-NT was found to have significantly less hemolytic toxicity (8.23 ± 0.65) as compared to free GEM (17.34 ± 0.56). The in vitro release was found to be in sustained pattern at the lysosomal pH, which depicts more cytotoxic response on human breast cancer cell line (MCF-7). It may be interpreted that the GEM/FA-NT formulation is capable to carry drug and deliver it selectively at the tumor site while minimizing side effects and thus holds promise in chemotherapy.
authors.affiliation: Department of Pharmaceutical Sciences, Pharmaceutics Research Laboratory, Dr H. S. Gour University, Sagar, Madhya Pradesh, India.
authors.forename: Ravendra
authors.initials: R
authors.lastname: Singh
authors.forename: Neelesh Kumar
authors.initials: NK
authors.lastname: Mehra
authors.forename: Vikas
authors.initials: V
authors.lastname: Jain
authors.forename: Narendra Kumar
authors.initials: NK
authors.lastname: Jain
mesh_terms: D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005492:Folic Acid / Q000008:administration & dosage / Q000737:chemistry; D006801:Humans; D061986:MCF-7 Cells; D037742:Nanotubes, Carbon / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy*; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods; D000093542:Gemcitabine
chemical_list: D004337:Drug Carriers; D037742:Nanotubes, Carbon; D003841:Deoxycytidine; D005492:Folic Acid; D000093542:Gemcitabine