2022
DOI: 10.1021/acs.biomac.1c01451
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Covalent Conjugation of Amphotericin B to Hyaluronic Acid: An Injectable Water-Soluble Conjugate with Reduced Toxicity and Anti-Leishmanial Potential

Abstract: Amphotericin B (AmB) is a highly hydrophobic drug with significant leishmanicidal activity whose use is limited by its poor water solubility and adverse effects. Polymer-drug conjugates are proposed as a delivery system designed to overcome those limitations while improving drug bioavailability, safety, and activity. Here, AmB was covalently linked to periodate-oxidized hyaluronic acid (HA) (oxidation degree of 30.1 ± 5.6%) via a Schiff base (HA-AmB imine). The conjugate presents high water solubility and self… Show more

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Cited by 7 publications
(2 citation statements)
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References 84 publications
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“…Pentavalent antimonial is the first-line drug for treating visceral leishmaniasis, but its adverse events or toxic reactions happen frequently, and even ineffective reactions occur [ 51 ]. Amphotericin B, a polyene macrolide antibiotic that binds to sterols in cell membranes, is currently the most effective anti-leishmanial drug [ 52 ]. Due to its poor oral absorption, only dosing concentrations can be achieved by intravenous injection.…”
Section: Liposomes and Lipid Nanoparticles (Lnps)mentioning
confidence: 99%
“…Pentavalent antimonial is the first-line drug for treating visceral leishmaniasis, but its adverse events or toxic reactions happen frequently, and even ineffective reactions occur [ 51 ]. Amphotericin B, a polyene macrolide antibiotic that binds to sterols in cell membranes, is currently the most effective anti-leishmanial drug [ 52 ]. Due to its poor oral absorption, only dosing concentrations can be achieved by intravenous injection.…”
Section: Liposomes and Lipid Nanoparticles (Lnps)mentioning
confidence: 99%
“…In the delivery of antileishmanial drugs to macrophages, a nanocarrier should be capable of delivering the active moiety at the targeted site in macrophages. Most frequently used nanoparticles in macrophage targeting through IV route are liposomes, non-ionic surfactant vesicles, nano emulsions and nano discs, where liposome lipid carriers are the most frequently employed for delivery of anti-leishmania drugs (Silva-Carvalho et al, 2022).…”
Section: Introductionmentioning
confidence: 99%