Abstract

Binding parameters of the N-phenyl benzene sulfonyl hydrazide, sulfonamide, and nanosulfonamide interaction with human serum albumin were determined by calorimetry method. The obtained binding parameters indicated that sulfonamide in the second binding sites has higher affinity for binding than the first binding sites. The binding process of sulfonamide to HSA is both enthalpy and entropy driven. The associated equilibrium constants confirm that sulfonamide binds to HSA with high affinity (2.2×106and 3.86105 M−1for first and second sets of binding sites, resp.). The obtained results indicate that sulfonamide increases the HSA antioxidant property. Nanosulfonamide has much more affinity for HSA (3.6×106 M−1) than sulfonamide.

Highlights

  • Physicochemical properties of nanoparticles such as their small size, large surface area, surface charge, and ability to make them potential delivery systems for effective treatments. e pharmacokinetic parameters of therapeutic drugs against the diseases show limitations in their efficacy. e poor bioavailability, side effects due to the high doses administered, long treatment, and the emergence of drug resistant strains are the disadvantages of ordinary drugs. e advances that nanotechnology-based drug delivery systems have made in improving the pharmacokinetics and efficacy of therapeutic drugs [1,2,3,4].Sulfonamides were the rst chemical substances systematically used to treat and prevent bacterial infections in humans

  • Patients who experience side effects such as nausea and vomiting may interpret this as an allergy and subsequently report that they are allergic to sulfas [7]. e binding of the sulfonamides to serum albumins, an important factor of the pharmacokinetic of these drugs, has been extensively studied by several workers, especially regarding the extent of binding, the stoichiometry, and the in uence of the chemical structure on the binding

  • − 󶀢󶀢δδθBθB − δδθAθA󶀲󶀲 󶀲󶀲xx′AALLAA + xx′BBLLBB󶀳󶀳 xx′BB, where qq are the heats of sulfonamide + Human serum albumin (HSA) or nanosulfonamide + HSA interactions, and qqmax represents the heat value upon saturation of all HSA. e parameters δδθAθA and δδθBθB are the indexes of HSA stability in the low and high sulfonamide concentrations, respectively

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Summary

Introduction

Physicochemical properties of nanoparticles such as their small size, large surface area, surface charge, and ability to make them potential delivery systems for effective treatments. e pharmacokinetic parameters of therapeutic drugs against the diseases show limitations in their efficacy. e poor bioavailability, side effects due to the high doses administered, long treatment, and the emergence of drug resistant strains are the disadvantages of ordinary drugs. e advances that nanotechnology-based drug delivery systems have made in improving the pharmacokinetics and efficacy of therapeutic drugs [1,2,3,4].Sulfonamides were the rst chemical substances systematically used to treat and prevent bacterial infections in humans. E parameters δδθAθA and δδθBθB are the indexes of HSA stability in the low and high sulfonamide concentrations, respectively. F 1: Comparison between the experimental heats (▴) at 300 K, for (nanosulfonamide + HSA) interactions and the calculated data (lines) via (1).

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