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Nanomaterials 2018, 8(7), 482; https://doi.org/10.3390/nano8070482

The Effect of Polymer Microstructure on Encapsulation Efficiency and Release Kinetics of Citropin 1.1 from the Poly(ε-caprolactone) Microparticles

1
Department of Biomaterials Chemistry, Chair of Analytical Chemistry and Biomaterials, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Banacha 1 St., 02-097 Warsaw, Poland
2
Department of Organic Chemistry and Biochemistry, Faculty of Materials Science and Design, Kazimierz Pulaski University of Technology and Humanities in Radom, 27 Chrobrego St., 26-600 Radom, Poland
3
Department of Inorganic Chemistry, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Gdansk, Al. Gen. J. Hallera 107 St., 80-416 Gdansk, Poland
4
Department of Biochemistry and Clinical Chemistry, Faculty of Pharmacy with the Laboratory Medicine Division, Medical University of Warsaw, Banacha 1 St., 02-097 Warsaw, Poland
*
Author to whom correspondence should be addressed.
Received: 26 May 2018 / Revised: 22 June 2018 / Accepted: 28 June 2018 / Published: 30 June 2018
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Abstract

Cationic antimicrobial peptides represent a promising therapeutic option against multidrug-resistant bacteria for the treatment of local infections. However, due to their low stability and potential toxicity, there are limited possibilities for their application in clinical practice. In this study, different poly(ε-caprolactone) (PCL) microparticles (MPs) loaded with citropin 1.1 (CIT) were investigated in order to demonstrate the effect of the polymer microstructure on the encapsulation efficiency (EE) and kinetics of the peptide release from the newly developed devices. The characteristics of the new systems in terms of surface morphology, particle size, EE and zeta potential analysis, as well as the haemolytic activities of the peptide were investigated. The in vitro release kinetics of CIT from the MPs was also investigated. CIT loading was favoured by a high content of negative charged linear polymer chains in the PCL structure. The presence of non-charged, amorphous macrocycle domains results in faster degradation of the PCL matrix. Depending on the crystallinity of the PCL, the peptide release exhibited a near-zero-order or near-first-order profile with no “burst release”. The results indicated that CIT-loaded PCL MPs could potentially be a promising drug delivery system (DDS) for the treatment of local infections. View Full-Text
Keywords: antimicrobial peptides; drug release; hemotoxicity; microparticles; poly(ε-caprolactone) antimicrobial peptides; drug release; hemotoxicity; microparticles; poly(ε-caprolactone)
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Piotrowska, U.; Oledzka, E.; Kamysz, W.; Białek, S.; Sobczak, M. The Effect of Polymer Microstructure on Encapsulation Efficiency and Release Kinetics of Citropin 1.1 from the Poly(ε-caprolactone) Microparticles. Nanomaterials 2018, 8, 482.

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