title: Physicochemical characterization of in situ drug-polymer nanocomplex formed between zwitterionic drug and ionomeric material in aqueous solution.
abstract: Biocompatible polymeric materials with the potential to form functional structures, in association with different therapeutic molecules, in physiological media, represent a great potential for biological and pharmaceutical applications. Therefore, here the formation of a nano-complex between a synthetic cationic polymer and model drug (ampicillin trihydrate) was studied. The formed complex was characterized by size and zeta potential measurements, using dynamic light scattering and capillary electrophoresis. Moreover, the chemical and thermodynamically stability of these complexes were studied. The ionomeric material, here referred as EuCl, was obtained by equimolar reaction between Eudragit E and HCl. The structural characterization was carried out by potentiometric titration, FTIR spectroscopy, and DSC. The effect of pH, time, polymer concentration and ampicillin/polymer molar ratio over the hydrodynamic diameter and zeta potential were established. The results show that EuCl ionomer in aqueous media presents two different populations of nanoparticles; one of this tends to form flocculated aggregates in high pH and concentrations, by acquiring different conformations in solution by changing from a compact to an extended conformation. Moreover, the formation of an in situ interfacial polymer-drug complex was demonstrated, this could slightly reduce the hydrolytic degradation of the drug while affecting its solubility, mainly under acidic conditions.
authors.affiliation: Pharmaceutical physical chemistry laboratory, Department of Pharmacy, Faculty of Natural Sciences, ICESI University, Cali, Colombia. Electronic address: chsalamanca@icesi.edu.co.
authors.forename: Constain H
authors.initials: CH
authors.lastname: Salamanca
authors.affiliation: Pharmaceutical physical chemistry laboratory, Department of Pharmacy, Faculty of Natural Sciences, ICESI University, Cali, Colombia.
authors.forename: Duvan F
authors.initials: DF
authors.lastname: Castillo
authors.affiliation: Pharmaceutical physical chemistry laboratory, Department of Pharmacy, Faculty of Natural Sciences, ICESI University, Cali, Colombia.
authors.forename: Juan D
authors.initials: JD
authors.lastname: Villada
authors.affiliation: SIT Biotech GmbH, BMZ 2 Otto-Hahn-Str. 15, 44227 Dortmund, Germany.
authors.forename: Gustavo R
authors.initials: GR
authors.lastname: Rivera
mesh_terms: D000667:Ampicillin / Q000737:chemistry* / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D055664:Electrochemical Techniques; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008768:Methylmethacrylates / Q000737:chemistry; D053761:Nanocomposites / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water / Q000737:chemistry*
chemical_list: D008768:Methylmethacrylates; D011108:Polymers; D014867:Water; C102808:Eudragit-E; D000667:Ampicillin
keywords: Ampicillin; Cationic polymer; Eudragit E; Interfacial nano-complex; Zwitterionic drug