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A STUDY ON THE OPTIMIZATION OF ANTIMICROBIAL ACTIVITY OF ERYTHROMYCIN BY COMPLEXATION WITH ?-CYCLODEXTRIN DERIVATES

Assoc. Prof. Dr. Lacramioara Ochiuz, Dr. Cristian Peptu, Lecturer Dr. Catalina Anisoara Peptu, Dr. Anca Grigoras, Assoc. Prof. Dr. Mihai Mares

Abstract

Erythromycin (E), a hydrophobic macrolide antibiotic, is prescribed for the treatment of acute bacterial infections, such as respiratory, urine, skin, and mouth infections. The main disadvantage of ER is its poor water solubility (2 mg/mL) that limits both formulation using hydrophilic bases and skin permeability. Cyclodextrins (CDs) are biocompatible cyclic oligomers of glucose, with a hydrophobic core and a hydrophilic exterior. CDs are used to improve the bioavailability of drugs by increasing their solubility and/or their dissolution rate after including the poorly water-soluble substances (such as ER) in the hydrophobic cavity of CDs. Adding CDs leads to improved solubility and stability of the drug substance, increased permeability of low aqueous solubility, decreased toxicity and even to reduced active dose as a result of increased bioavailability. Specifically, to optimize the physical inclusion of specific guests, the polarity of native CDs molecules should be adjusted. Generally, this is achieved by attaching small alkyl or hydroxyalkyl substituents through ether linkages. Our study aiming at improving the stability and tolerance of E in topical products developed a complex of E with ? cyclodextrin functionalized with a variable number of lactide units (CD-LA_E). The antibacterial activity of the synthesized complex was assessed against S. aureus strains.

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DOI resolver: doi.org/10.5593/sgem2017/61/s24.001

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