Folic Acid Conjugated Chitosan Nanoparticles for Tumor Targeting of Therapeutic and Imaging Agents

Abstract

Folic acid-conjugated temozolomide (TMZ)-loaded chitosan nanoparticles (CS-TMZ-FLA-NP) were developed to target lung cancer in the anticipation that folic acid would increase the affinity of nanoparticles for cancer cells. CS-TMZ-FLA-NP showed the highest anti-proliferative effect on the lung cancer cells in comparison to free TMZ and CS-TMZ-NP (nanoparticles without folic acid). A cellular uptake assay was performed on two different cell lines, L132 and A549. Cellular uptake efficiencies of CS-TMZ-NP and CS-TMZ-FLA-NP were found to be concentration-dependent in both cell lines. CS-TMZ-FLA-NP produced a 2.5 fold greater accumulation of TMZ than CS-TMZ-NP in both cell lines. CS-TMZ-FLA-NP maintained a significantly higher deposition of TMZ in lung tissue (approximately 7.5 μg/g of lung tissue) when compared to free TMZ and CS-TMZ-NP. Mice treated with CS-TMZ-FLA-NP had a 100% survival rate with significant suppression of tumor growth. Histopathological and immunohistochemical studies also demonstrated that CS-TMZ-FLA-NP had superior anticancer activity compared to the other two treatments. Our results indicate that CS-TMZ-FLA-NP can effectively facilitate targeting to human lung cancer cell lines in vitro and to lung tumors in vivo in a sustained manner and so improve the therapeutic efficacy of TMZ.

Fabrication of Electrospun PLA-nHAp Nanocomposite for Sustained Drug Release in Dental and Orthopedic Applications

“…In this regard, treating the infection using in situ drug-release composites can be an optimal solution to prevent orthopedic post-surgical complications. An in situ drug-release composite can promote drug action by delivering sufficient doses of the pharmaceutical agent to a specific site of the body and limit further infections and side effects [ 13 ].…”

Targeted doxorubicin delivery to hepatocarcinoma cells by lactobionic acid-modified laponite nanodisks

“…8 However, those systems still inevitably cause undesirable side effects due to the lack of tumor-specific delivery. Therefore, specific peptides (RGD 9,10 ) or biological ligands (folic acid, 11,12 hyaluronic acid, 13 etc. [14][15][16] ) with an enhanced binding affinity toward certain receptors expressed by cancer cells have been attached onto the surface of nanocarriers to construct targeted drug delivery systems.…”

Folic Acid Decorated Chitosan Nanoparticles and its Derivatives for the Delivery of Drugs and Genes to Cancer Cells

“…On the contrary, chitosan dissolves in acidic solutions and is insoluble in organic solvents. Hence aqueous buffers or in particular combinations with organic solvents miscible with water are chosen as a medium for conjugation reaction 26 . The coupling agents may be used for direct conjugation of folic acid to the -COOH group of chitosan.…”