Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8412998 | European Journal of Pharmaceutics and Biopharmaceutics | 2015 | 9 Pages |
Abstract
Polymer mediated drug delivery system represents a novel promising platform for tumor-targeting with reduced systemic side effects and improved chemotherapeutical efficacy. In this study, we report the preparation and characterization of herceptin targeted, diglycolamic acid (DGA) functionalized polyamidoamine (PAMAM) dendrimer as a potent drug carrier for cisplatin. DGA dendrimers carrying cisplatin demonstrated enhanced anticancer activity when targeted with herceptin. In vitro cell line studies with herceptin-DGA-G4-cisplatin in HER-2 +ve and HER-2 âve human ovarian cancer cell lines showed that these nanoparticles possessed remarkable features such as lower IC50 value, improved S-phase arrest, and enhanced apoptosis due to increased cellular uptake and accumulation than the untargeted DGA-G4-cisplatin and free cisplatin. Furthermore, in vivo results in SCID mice bearing SKOV-3 tumor xenografts, herceptin-DGA-G4-cisplatin, appeared to be more effective in inducing tumor regression as compared to free cisplatin. Collectively, these results indicate that herceptin targeted DGA functionalized PAMAM-cisplatin conjugates serve as better anti-tumor agents than individual therapeutic agents.
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Authors
Akila Kesavan, P. Ilaiyaraja, W. Sofi Beaula, Vuttaradhi Veena Kumari, J. Sugin Lal, C. Arunkumar, G. Anjana, Satish Srinivas, Anita Ramesh, Suresh Kumar Rayala, D. Ponraju, Ganesh Venkatraman,