Development of Amphotericin B Micellar Formulations Based on Copolymers of Poly(ethylene glycol) and Poly(ε-caprolactone) Conjugated with Retinol

Yeimy, J. Rodriguez (2020) Development of Amphotericin B Micellar Formulations Based on Copolymers of Poly(ethylene glycol) and Poly(ε-caprolactone) Conjugated with Retinol. MDPI, 12 (3). ISSN 1999-4923

[img] Text
pharmaceutics 2020 (3).pdf
Download (367MB)

Abstract

Amphotericin B (AmB) is a broad spectrum of antifungal drug used to treat antifungal diseases. However, due to the high toxicity of AmB, treated patients may suffer the risk of side effects, such as renal failure. Nanoencapsulation strategies have been reported to elicit low toxicity, albeit most of them possess low encapsulation efficiency. The aim of this research is to develop micellar delivery systems for AmB with reduced toxicity while maintaining its affectivity by employing retinol (RET)-conjugated amphiphilic block copolymers (ABCs) as precursors. Copolymers composed of poly(ε-caprolactone) (A) and polyethylenglycol (B) of types AB and ABA were synthesized by ring opening polymerization and subsequently conjugated with RET by Steglich esterification. 1H-NMR spectroscopy was used to corroborate the structure of copolymers and their conjugates and determine their molecular weights. Analysis by gel permeation chromatography also found that the materials have narrow distributions. The resulting copolymers were used as precursors for delivery systems of AmB, thus reducing its aggregation and consequently causing a low haemolytic effect. Upon conjugation with RET, the encapsulation capacity was enhanced from approximately 2 wt % for AB and ABA copolymers to 10 wt %. AmB encapsulated in polymer micelles presented improved antifungal efficiency against Candida albicans and Candida auris strains compared with Fungizone®, as deduced from the low minimum inhibitory concentration.

Item Type: Article
Subjects: R Medicine > RS Pharmacy and materia medica
Divisions: Library of Congress Subject Areas > P Language and Literature > Farmasi
Library of Congress Subject Areas > P Language and Literature > Fakultas Farmasi > Farmasi
Fakultas Farmasi > Farmasi
Depositing User: Unnamed user with email repo@umsb.ac.id
Date Deposited: 27 Sep 2022 08:59
Last Modified: 27 Sep 2022 08:59
URI: http://eprints.umsb.ac.id/id/eprint/459

Actions (login required)

View Item View Item
Test Repository is powered by EPrints 3 which is developed by the School of Electronics and Computer Science at the University of Southampton. More information and software credits.