Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations

The liposomal amphotericin B (AmB) formulation, AmBisome<sup>®</sup>, still represents the best therapeutic option for cutaneous and visceral leishmaniasis. However, its clinical efficacy depends on the patient’s immunological status, the clinical manifestation and the endemic region. Mo...

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Main Authors: Frédéric Frézard, Marta M. G. Aguiar, Lucas A. M. Ferreira, Guilherme S. Ramos, Thais T. Santos, Gabriel S. M. Borges, Virgínia M. R. Vallejos, Helane L. O. De Morais
Format: Article
Language:English
Published: MDPI AG 2022-12-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/15/1/99
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author Frédéric Frézard
Marta M. G. Aguiar
Lucas A. M. Ferreira
Guilherme S. Ramos
Thais T. Santos
Gabriel S. M. Borges
Virgínia M. R. Vallejos
Helane L. O. De Morais
author_facet Frédéric Frézard
Marta M. G. Aguiar
Lucas A. M. Ferreira
Guilherme S. Ramos
Thais T. Santos
Gabriel S. M. Borges
Virgínia M. R. Vallejos
Helane L. O. De Morais
author_sort Frédéric Frézard
collection DOAJ
description The liposomal amphotericin B (AmB) formulation, AmBisome<sup>®</sup>, still represents the best therapeutic option for cutaneous and visceral leishmaniasis. However, its clinical efficacy depends on the patient’s immunological status, the clinical manifestation and the endemic region. Moreover, the need for parenteral administration, its side effects and high cost significantly limit its use in developing countries. This review reports the progress achieved thus far toward the understanding of the mechanism responsible for the reduced toxicity of liposomal AmB formulations and the factors that influence their efficacy against leishmaniasis. It also presents the recent advances in the development of more effective liposomal AmB formulations, including topical and oral liposome formulations. The critical role of the AmB aggregation state and release rate in the reduction of drug toxicity and in the drug efficacy by non-invasive routes is emphasized. This paper is expected to guide future research and development of innovative liposomal formulations of AmB.
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spelling doaj.art-821d450cbc634ade8b1f7492d52770ff2023-11-30T23:57:38ZengMDPI AGPharmaceutics1999-49232022-12-011519910.3390/pharmaceutics15010099Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral FormulationsFrédéric Frézard0Marta M. G. Aguiar1Lucas A. M. Ferreira2Guilherme S. Ramos3Thais T. Santos4Gabriel S. M. Borges5Virgínia M. R. Vallejos6Helane L. O. De Morais7Department of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilFaculty of Pharmacy, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilFaculty of Pharmacy, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartment of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartment of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilFaculty of Pharmacy, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartment of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilDepartment of Physiology and Biophysics, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, MG, BrazilThe liposomal amphotericin B (AmB) formulation, AmBisome<sup>®</sup>, still represents the best therapeutic option for cutaneous and visceral leishmaniasis. However, its clinical efficacy depends on the patient’s immunological status, the clinical manifestation and the endemic region. Moreover, the need for parenteral administration, its side effects and high cost significantly limit its use in developing countries. This review reports the progress achieved thus far toward the understanding of the mechanism responsible for the reduced toxicity of liposomal AmB formulations and the factors that influence their efficacy against leishmaniasis. It also presents the recent advances in the development of more effective liposomal AmB formulations, including topical and oral liposome formulations. The critical role of the AmB aggregation state and release rate in the reduction of drug toxicity and in the drug efficacy by non-invasive routes is emphasized. This paper is expected to guide future research and development of innovative liposomal formulations of AmB.https://www.mdpi.com/1999-4923/15/1/99liposomesamphotericin Bleishmaniasisoral routePEGylationtopical route
spellingShingle Frédéric Frézard
Marta M. G. Aguiar
Lucas A. M. Ferreira
Guilherme S. Ramos
Thais T. Santos
Gabriel S. M. Borges
Virgínia M. R. Vallejos
Helane L. O. De Morais
Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
Pharmaceutics
liposomes
amphotericin B
leishmaniasis
oral route
PEGylation
topical route
title Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
title_full Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
title_fullStr Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
title_full_unstemmed Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
title_short Liposomal Amphotericin B for Treatment of Leishmaniasis: From the Identification of Critical Physicochemical Attributes to the Design of Effective Topical and Oral Formulations
title_sort liposomal amphotericin b for treatment of leishmaniasis from the identification of critical physicochemical attributes to the design of effective topical and oral formulations
topic liposomes
amphotericin B
leishmaniasis
oral route
PEGylation
topical route
url https://www.mdpi.com/1999-4923/15/1/99
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