Development of Polyelectrolyte Complex Nanoparticles-PECNs Loaded with Ampicillin by Means of Polyelectrolyte Complexation and Ultra-High Pressure Homogenization (UHPH)
Laboratorio de Diseño y Formulación de Productos Químicos y Derivados, Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Naturales, Universidad ICESI, Calle 18 No. 122-135, Cali 760035, Colombia
Grupo de Investigación en Química y Biotecnología (QUIBIO), Facultad de Ciencias Básicas, Universidad Santiago de Cali, calle 5 No. 62-00, Cali 760035, Colombia
Author to whom correspondence should be addressed.
Polymers 2020, 12(5), 1168; https://doi.org/10.3390/polym12051168
Received: 1 April 2020 / Revised: 9 May 2020 / Accepted: 14 May 2020 / Published: 20 May 2020
(This article belongs to the Section Polymer Physics)
This study was focused on synthesizing, characterizing and evaluating the biological potential of Polyelectrolyte Complex Nanoparticles (PECNs) loaded with the antibiotic ampicillin. For this, the PECNs were produced initially by polyelectrolytic complexation (bottom-up method) and subsequently subjected to ultra-high pressure homogenization-UHPH (top-down method). The synthetic polymeric materials corresponding to the sodium salt of poly(maleic acid-alt-octadecene) (PAM-18Na) and the chloride salt of Eudragit E-100 (EuCl) were used, where the order of polyelectrolyte complexation, the polyelectrolyte ratio and the UHPH conditions on the PECNs features were evaluated. Likewise, PECNs were physicochemically characterized through particle size, polydispersity index, zeta potential, pH and encapsulation efficiency, whereas the antimicrobial effect was evaluated by means of the broth microdilution method employing ampicillin sensitive and resistant S. aureus strains. The results showed that the classical method of polyelectrolyte complexation (bottom-up) led to obtain polymeric complexes with large particle size and high polydispersity, where the 1:1 ratio between the titrant and receptor polyelectrolyte was the most critical condition. In contrast, the UHPH technique (top-down method) proved high performance to produce uniform polymeric complexes on the nanometric scale (particle size < 200 nm and PDI < 0.3). Finally, it was found there was a moderate increase in antimicrobial activity when ampicillin was loaded into the PECNs.