(+)-Usnic acid (UA) is a natural substance that displays pharmacological activity, but it is barely soluble in water, so it was included in liposomes in order to study its properties. First, the effects of phospholipid structure and loading methodology on UA entrapment efficacy were evaluated. Then, the physicochemical and biological properties (UA delivery efficacy to Staphylococcus aureus bacterial cells) of different liposome formulations containing structurally related amphiphiles derived from L-prolinol were fully investigated. Entrapment efficiency of UA with passive loading by incubation was 80–100 molar percentage, which is related to lipophilicity of the drug and to the packing and fluidity of the bilayer. Some of the investigated formulations show the potential of UA in delivery systems (minimum inhibitory concentration of liposomal UA: 8 μg/mL) and even subtle variations of the molecular structure of lipids can significantly affect the liposomes’ physicochemical properties and efficiency of drug release. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

Correlation of physicochemical and antimicrobial properties of liposomes loaded with (+)-usnic acid / Battista, Sara; Bellio, Pierangelo; Celenza, Giuseppe; Galantini, Luciano; Franceschini, Irene; Mancini, Giovanna; Giansanti, Luisa. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 85:5(2020), pp. 1014-1021. [10.1002/cplu.202000125]

Correlation of physicochemical and antimicrobial properties of liposomes loaded with (+)-usnic acid

Galantini, Luciano;
2020

Abstract

(+)-Usnic acid (UA) is a natural substance that displays pharmacological activity, but it is barely soluble in water, so it was included in liposomes in order to study its properties. First, the effects of phospholipid structure and loading methodology on UA entrapment efficacy were evaluated. Then, the physicochemical and biological properties (UA delivery efficacy to Staphylococcus aureus bacterial cells) of different liposome formulations containing structurally related amphiphiles derived from L-prolinol were fully investigated. Entrapment efficiency of UA with passive loading by incubation was 80–100 molar percentage, which is related to lipophilicity of the drug and to the packing and fluidity of the bilayer. Some of the investigated formulations show the potential of UA in delivery systems (minimum inhibitory concentration of liposomal UA: 8 μg/mL) and even subtle variations of the molecular structure of lipids can significantly affect the liposomes’ physicochemical properties and efficiency of drug release. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
2020
(+)-Usnic acid; antioxidant activity; L-prolinol derivatives; liposomes; N-oxide moiety; structure-properties relationship
01 Pubblicazione su rivista::01a Articolo in rivista
Correlation of physicochemical and antimicrobial properties of liposomes loaded with (+)-usnic acid / Battista, Sara; Bellio, Pierangelo; Celenza, Giuseppe; Galantini, Luciano; Franceschini, Irene; Mancini, Giovanna; Giansanti, Luisa. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 85:5(2020), pp. 1014-1021. [10.1002/cplu.202000125]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1415243
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