Int. J. Mol. Sci. 2011, 12(7), 4591-4608; doi:10.3390/ijms12074591
Article

Enhanced Anti-Tumoral Activity of Methotrexate-Human Serum Albumin Conjugated Nanoparticles by Targeting with Luteinizing Hormone-Releasing Hormone (LHRH) Peptide

1email, 1,2,* email, 1,2email, 1email, 1email, 2,3email, 2,3email, 4email and 5email
Received: 22 May 2011; in revised form: 20 June 2011 / Accepted: 30 June 2011 / Published: 15 July 2011
(This article belongs to the Special Issue Bioactive Nanoparticles)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: Active targeting could increase the efficacy of anticancer drugs. Methotrexate-human serum albumin (MTX-HSA) conjugates, functionalized by luteinizing hormone-releasing hormone (LHRH) as targeting moieties, with the aim of specifically targeting the cancer cells, were prepared. Owing to the high expression of LHRH receptors in many cancer cells as compared to normal cells, LHRH was used as the targeting ligand in this study. LHRH was conjugated to MTX-HSA nanoparticles via a cross-linker. Three types of LHRH targeted nanoparticles with a mean particle size between 120–138 nm were prepared. The cytotoxicity of LHRH targeted and non-targeted nanoparticles were determined on the LHRH positive and negative cell lines. The internalization of the targeted and non-targeted nanoparticles in LHRH receptor positive and negative cells was investigated using flow cytometry analysis and fluorescence microscopy. The cytotoxicity of the LHRH targeted nanoparticles on the LHRH receptor positive cells were significantly more than non-targeted nanoparticles. LHRH targeted nanoparticles were also internalized by LHRH receptor positive cells significantly more than non-targeted nanoparticles. There were no significant differences between the uptake of targeted and non-targeted nanoparticles to the LHRH receptor negative cells. The active targeting procedure using LHRH targeted MTX-HSA nanoparticles could increase the anti-tumoral activity of MTX.
Keywords: nanoparticles; drug targeting; conjugates; anti-cancer; human serum albumin; LHRH
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MDPI and ACS Style

Taheri, A.; Dinarvand, R.; Atyabi, F.; Ahadi, F.; Nouri, F.S.; Ghahremani, M.H.; Ostad, S.N.; Borougeni, A.T.; Mansoori, P. Enhanced Anti-Tumoral Activity of Methotrexate-Human Serum Albumin Conjugated Nanoparticles by Targeting with Luteinizing Hormone-Releasing Hormone (LHRH) Peptide. Int. J. Mol. Sci. 2011, 12, 4591-4608.

AMA Style

Taheri A, Dinarvand R, Atyabi F, Ahadi F, Nouri FS, Ghahremani MH, Ostad SN, Borougeni AT, Mansoori P. Enhanced Anti-Tumoral Activity of Methotrexate-Human Serum Albumin Conjugated Nanoparticles by Targeting with Luteinizing Hormone-Releasing Hormone (LHRH) Peptide. International Journal of Molecular Sciences. 2011; 12(7):4591-4608.

Chicago/Turabian Style

Taheri, Azade; Dinarvand, Rassoul; Atyabi, Fatemeh; Ahadi, Fatemeh; Nouri, Farank Salman; Ghahremani, Mohammad Hossein; Ostad, Seyed Nasser; Borougeni, Atefeh Taheri; Mansoori, Pooria. 2011. "Enhanced Anti-Tumoral Activity of Methotrexate-Human Serum Albumin Conjugated Nanoparticles by Targeting with Luteinizing Hormone-Releasing Hormone (LHRH) Peptide." Int. J. Mol. Sci. 12, no. 7: 4591-4608.

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