Polyethylene Glycol Conjugation for Solubility Enhancement of Cefadroxil, a Poorly Soluble Antibiotic

Abstract

Introduction: Cefadroxil is the most widely used antibiotic for many bacterial infections but has the drawback of poorly solubility. In an attempt to provide an easier technique which can be scaled up on large scale to provide a simple method to enhance its aqueous solubility, this present work has exploited polyethylene glycol conjugation to enhance its aqueous solubility of cefadroxil.
 Objective: The main aim of the work is preparation of Polyethylene glycol conjugates of cefadroxil by solvent evaporation technique and to evaluate its solubility enhancement by solubility analysis and to assess drug content uniformity, drug - excipient interaction studies by FTIR spectroscopy.
 Methodology: Polyethylene glycol conjugates of cefadroxil are prepared by solvent evaporation technique using PEG 6000. Five conjugates of Cefadroxil to PEG6000 taken in weight proportions of (1:0.5), (1:1), (1:2) (1:3) and (1:4) were prepared.
 Results: Reasonable enhancement of solubility of cefadroxil was evidenced from all the prepared polyethylene glycol conjugates of cefadroxil. Among all CFDL: PEG 6000 (1:4) evidenced high percentage solubility of 81±0.61. IR spectrum of CFDL: PEG6000 (1:4) evidenced disappearance of amide group of cefadroxil indicating conjugate formation which is reversible to release cefadroxil to exhibit its therapeutic effect
 Conclusion: Polyethylene glycol conjugates of cefadroxil can be prepared easily by solvent evaporation and the conjugate made by weight proportion of CFDL: PEG 6000 (1:4) enhances solubility of cefadroxil by 88% and is promising to be used in formulations cefadroxil with enhanced dissolution and bioavailability.