Synthesis, characterization and in vitro evaluation of methotrexate conjugated fluorescent carbon nanoparticles as drug delivery system for human lung cancer targeting

• Published in: Journal of photochemistry and photobiology. B, Biology Biology, 2015-12, Vol.153, p.111-120
• Main Authors: Ajmal, Muhammad, Yunus, Uzma, Matin, Abdul, Haq, Noaman Ul
• Format: Article
• Language: English
• Subjects: Adhesion assay; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Carbon - chemistry; Carbon nanoparticles–methotrexate conjugates; Cell Line, Tumor; Drug Carriers - chemical synthesis; Drug Carriers - chemistry; Fluorescent carbon nanoparticles; Fluorescent Dyes - chemistry; Humans; Lactate dehydrogenase assay; Lung carcinoma cells; Lung Neoplasms; Methotrexate - chemistry; Methotrexate - pharmacology; Microscopy, Electron, Scanning; Nanoparticles - chemistry; Rhodamines - chemistry; Spectrometry, Fluorescence; Spectroscopy, Fourier Transform Infrared; Sulforhodamine B assay; Thermogravimetry
• ISSN: 1011-1344; 1873-2682
• DOI: 10.1016/j.jphotobiol.2015.09.006

Nanotechnology based cancer therapeutics have rapidly advanced towards the solution of many limitations associated with other drug delivery agents such as nonspecific distribution within the body, low water solubility and non-biocompatibility. Carbon nanoparticles have demonstrated unique properties that are useful to combat with these issues, including their properties dependent on size, high stability in different solvents, compatible size for drug delivery and ease of surface modifications. Fluorescent carbon nanoparticles with good water solubility were obtained from a carbohydrate source by acid assisted ultrasonic treatment at 35kHz for 4h. This simple and economical method can be used for large scale production. Electron microscopic, spectroscopic and thermo gravimetric analysis techniques were used to characterize these carbon nanoparticles. Functionalized CNPs were further conjugated with anticancer drug-methotrexate and used as fluorescent nano-carriers. In this research work, we determined the in vitro bioactivity of CNPs-methotrexate conjugates by lactate dehydrogenase assay, cell adhesion assay and sulforhodamine B assay in human lung carcinoma cell line (H157). The CNPs showed promising biocompatibility and CNPs-MTX conjugates demonstrated potent cytotoxic effects and high anticancer activities in human lung cancer cell line. [Display omitted] •Fluorescent carbon nanoparticles were synthesized from glucose by ultrasonication.•Carbon nanoparticles were characterized by microscopic and spectroscopic techniques.•Functionalized carbon nanoparticles were attached with anti cancer drug-methotrexate.•Bioactivity of CNPs and CNPs-MTX conjugates was evaluated by biological endpoints.•CNPs-MTX conjugates showed promising cytotoxicity against lung carcinoma cell line.