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• Taheri, A
• Dinarvand, R
• Atyabi, F
• Ahadi, F
• Nouri, F
• Ghahremani, M
• Ostad, S
• Borougeni, A
• Mansoori, P
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• Taheri, A
• Dinarvand, R
• Atyabi, F
• Ahadi, F
• Nouri, F
• Ghahremani, M
• Ostad, S
• Borougeni, A
• Mansoori, P
• [+] on PubMed
• Taheri, A
• Dinarvand, R
• Atyabi, F
• Ahadi, F
• Nouri, F
• Ghahremani, M
• Ostad, S
• Borougeni, A
• Mansoori, P

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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

Azade Taheri ¹ , Rassoul Dinarvand ^1,2,* , Fatemeh Atyabi ^1,2 , Fatemeh Ahadi ¹ , Farank Salman Nouri ¹ , Mohammad Hossein Ghahremani ^2,3 , Seyed Nasser Ostad ^2,3 , Atefeh Taheri Borougeni ⁴  and Pooria Mansoori ⁵

¹ Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran P. O. Box 14155-6451, Iran ² Nanotechnology Research Centre, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14174, Iran ³ Department of Pharmacology, Faculty of Pharmacy, Tehran University of Medical sciences, Tehran 14174, Iran ⁴ Department of Oral and Maxillofacial Pathology, Faculty of Dentistry, Tehran University of Medical Sciences, Tehran 14174, Iran ⁵ Faculty of Medicine, Ahvaz Jundishapur University of Medical Sciences, Ahvaz 73166, Iran

* Author to whom correspondence should be addressed.

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)

Download PDF Full-Text [685 KB, Updated Version, uploaded 18 July 2011 09:26 CEST]

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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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