Development of Polyelectrolyte Complex Nanoparticles-PECNs Loaded with Ampicillin by Means of Polyelectrolyte Complexation and Ultra-High Pressure Homogenization (UHPH)

Abstract

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.

Peptides with Dual Antimicrobial–Anticancer Activity: Strategies to Overcome Peptide Limitations and Rational Design of Anticancer Peptides

“…In inorganic systems, nanoparticles are used with metallic ions, such as silver, gold, and zinc oxide. On the other hand, in organic systems, liposomes and polymer nanoparticles are found [ 31 ]. Similar to hydrogels, nanoparticles have high biocompatibility and biodegradability, and low cytotoxicity.…”

“…Homopolymers and copolymers of polylactide or polyglycolic acid are frequently used. They are classified according to their architecture into nanospheres, nanocapsules, conjugated polymers, and polyelectrolyte complexes [ 31 ]. Nanoparticles can be used to transport proteins and peptides, whose conjugation generates a synergistic effect that improves the limitations of each one of the materials and achieves uses, such as inhibition of the interactions of pathogenic proteins and high sensitivity in molecular imaging [ 32 , 33 , 34 ].…”

Comparative evaluation study of polycomplex carriers based on Eudragit® EPO/S100 copolymers prepared in different media

“…The products of the interaction between chemically complementary macromolecules, that is, proton donors and acceptors (IPCs stabilized by a cooperative system of H‐bonds), and oppositely charged polyions (interpolyelectrolyte complexes, IPECs), have been widely investigated for several decades 1‐4 . IPCs and IPECs are products with new properties in comparison with the original polymers, which open up a wide range of possibilities for their application, including systems for controlled drug delivery 5‐13 . It is known that the application of new polymer compounds as excipients in pharmaceutical technology can be associated with a risk of toxicity.…”

In Silico Characterization of the Interaction between the PBP2a “Decoy” Protein of Resistant Staphylococcus aureus and the Monomeric Units of Eudragit E-100 and Poly(Maleic Acid-alt-Octadecene) Polymers

“…In contrast, the third study assessed different polyelectrolyte complex nanoparticles (PECNs) formed between PAM-18Na and EuCl polymers loaded with ampicillin. In this case, a moderate increase in antimicrobial activity was found on each of the resistant S. aureus strains [ 18 ]. Therefore, the results described in the three previous studies suggested that depending on the type of nanoparticle there is a particular antimicrobial effect ( Figure 2 ).…”