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Sci. Pharm. 2014, 82(4), 857-872; doi:10.3797/scipharm.1402-03

Physicochemical Characterization and Cytotoxicity Screening of a Novel Colloidal Nanogold-Based Phenytoin Conjugate

1
School of Bio Sciences and Technology, VIT University, Vellore - 632014, Tamil Nadu, India
2
Centre for Nanotechnology Research, VIT University, Vellore - 632014, Tamil Nadu, India
*
Author to whom correspondence should be addressed.
Received: 6 February 2014 / Accepted: 21 August 2014 / Published: 21 August 2014
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Abstract

A novel, colloidal nanogold-based drug delivery system for phenytoin, a well-known anti-epileptic drug with an enhanced efflux via P-glycoprotein, has been proposed in this study. The vital physical properties that would aid in predicting the biological interaction of this system were profiled using various techniques such as UV-Vis, DLS, and TEM in corroboration with theoretical calculations. It was significant to note that the binding of phenytoin to colloidal nanogold was strongly pH-dependent with the optimum at pH 5.5 and a consistently reproducible spectral shift. Analysis of the conjugate by FTIR revealed that the imide functional group of phenytoin mediated a dative coordinate bond to colloidal nanogold at the optimum pH. The amount of the drug bound to the gold was quantified to be 85.8±2.5% (w/v) by HPLC. Hypothetically, the surface charge of the conjugate could possibly imply charge-mediated uptake across the cell membrane. Further, the novel conjugate was screened for its cytotoxicity in two cell lines and the dosage range was identified. Subsequent development, thorough evaluations in suitable model systems, and the potential for bioimaging to track the payload would validate our hypothesis on the conjugate for better intracellular retention at the site of action, and thereby achieve the targeted delivery.
Keywords: Phenytoin; Colloidal gold; In vitro release; Drug delivery Phenytoin; Colloidal gold; In vitro release; Drug delivery
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. (CC BY 4.0).

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MDPI and ACS Style

SUNEETHA, S.C.A.; RAGHUPATHY, B.P.C.; SURESH, P.K. Physicochemical Characterization and Cytotoxicity Screening of a Novel Colloidal Nanogold-Based Phenytoin Conjugate. Sci. Pharm. 2014, 82, 857-872.

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