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Dual Drug Conjugate Loaded Nanoparticles for the Treatment of Cancer

Matlapudi, Megha Shyam and Moin, Afrasim and Medishetti, Raghavender and Rajendra, K and Raichur, Ashok M and Kumar, Prashantha BR (2016) Dual Drug Conjugate Loaded Nanoparticles for the Treatment of Cancer. In: CURRENT DRUG DELIVERY, 12 (6). pp. 782-794.

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Official URL: http://dx.doi.org/10.2174/156720181266615050712045...


Two antineoplastic agents, Imatinib (IM) and 5-Fluorouracil (FU) were conjugated by hydrolysable linkers through an amide bond and entrapped in polymeric Human Serum Albumin (HSA) nanoparticles. The presence of dual drugs in a common carrier has the advantage of reaching the site of action simultaneously and acting at different phases of the cell cycle to arrest the growth of cancer cells before they develop chemoresistance. The study has demonstrated an enhanced anticancer activity of the conjugate, and conjugate loaded stealth HSA nanoparticles (NPs) in comparison to the free drug in A-549 human lung carcinoma cell line and Zebra fish embryos (Danio rerio). Hydrolysability of the conjugate has also been demonstrated with complete hydrolysis being observed after 12 h. In vivo pharmacodynamics study in terms of tumor volume and pharmacokinetics in mice for conjugate (IM-SC-FU) and conjugate loaded nanoparticles showed significant anti-cancer activity. The other parameters evaluated were particle size (86nm), Poly Dispersive Index (PDI) (0.209), zeta potential (-49mV), drug entrapment efficiency (96.73%) and drug loading efficiency (89%). Being in stealth mode gives the potential for the NPs to evade Reticulo-Endothelial system (RES), achieve passive targeting by Enhanced Permeation Retention (EPR) effect with controlled release of the therapeutic agent. As the conjugate cleaves into individual drugs in the tumor environment, this promises better suppression of cancer chemoresistance by delivering dual drugs with different modes of action at the same site, thereby synergistically inhibiting the growth of cancerous tissue.

Item Type: Journal Article
Additional Information: Copy right for this article belongs to the BENTHAM SCIENCE PUBL LTD, EXECUTIVE STE Y-2, PO BOX 7917, SAIF ZONE, 1200 BR SHARJAH, U ARAB EMIRATES
Keywords: Cancer chemoresistance; controlled release; dual drug conjugates; polymeric nanoparticles; Zebrafish embryos (Danio rerio)
Department/Centre: Division of Mechanical Sciences > Materials Engineering (formerly Metallurgy)
Date Deposited: 12 Apr 2016 06:12
Last Modified: 12 Apr 2016 06:12
URI: http://eprints.iisc.ac.in/id/eprint/53653

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