Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use

Cefixime (CEF) is a cephalosporin included in the WHO Model List of Essential Medicines for Children. Liquid formulations are considered the best choice for pediatric use, due to their great ease of administration and dose-adaptability. Owing to its very low aqueous solubility and poor stability, CE...

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Autores principales:	Marzia Cirri, Natascia Mennini, Giulia Nerli, Jessica Rubia, Enrico Casalone, Fabrizio Melani, Francesca Maestrelli, Paola Mura
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	cefixime amino acids pediatric oral formulation sulfobutylether-β-cyclodextrin histidine molecular dynamic studies Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/8ff4b916504049389c223a66506e05f6
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spelling	oai:doaj.org-article:8ff4b916504049389c223a66506e05f62021-11-25T18:41:53ZCombined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use10.3390/pharmaceutics131119231999-4923https://doaj.org/article/8ff4b916504049389c223a66506e05f62021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1923https://doaj.org/toc/1999-4923Cefixime (CEF) is a cephalosporin included in the WHO Model List of Essential Medicines for Children. Liquid formulations are considered the best choice for pediatric use, due to their great ease of administration and dose-adaptability. Owing to its very low aqueous solubility and poor stability, CEF is only available as a powder for oral suspensions, which can lead to reduced compliance by children, due to its unpleasant texture and taste, and possible non-homogeneous dosage. The aim of this work was to develop an oral pediatric CEF solution endowed with good palatability, exploiting the solubilizing and taste-masking properties of cyclodextrins (CDs), joined to the use of amino acids as an auxiliary third component. Solubility studies indicated sulfobutylether-β-cyclodextrin (SBEβCD) and Histidine (His) as the most effective CD and amino acid, respectively, even though no synergistic effect on drug solubility improvement by their combined use was found. Molecular Dynamic and <sup>1</sup>H-NMR studies provided insight into the interactions of binary CEF:His and ternary CEF:His:SBEβCD systems used to prepare CEF solutions, which resulted stable and maintained unchanged antimicrobial activity during the two-weeks-use in therapy. The ternary solution was superior in terms of more tolerable pH (5.6 vs. 4.7) and better palatability, being resulted completely odorless by a panel test.Marzia CirriNatascia MenniniGiulia NerliJessica RubiaEnrico CasaloneFabrizio MelaniFrancesca MaestrelliPaola MuraMDPI AGarticlecefiximeamino acidspediatric oral formulationsulfobutylether-β-cyclodextrinhistidinemolecular dynamic studiesPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1923, p 1923 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	cefixime amino acids pediatric oral formulation sulfobutylether-β-cyclodextrin histidine molecular dynamic studies Pharmacy and materia medica RS1-441
spellingShingle	cefixime amino acids pediatric oral formulation sulfobutylether-β-cyclodextrin histidine molecular dynamic studies Pharmacy and materia medica RS1-441 Marzia Cirri Natascia Mennini Giulia Nerli Jessica Rubia Enrico Casalone Fabrizio Melani Francesca Maestrelli Paola Mura Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
description	Cefixime (CEF) is a cephalosporin included in the WHO Model List of Essential Medicines for Children. Liquid formulations are considered the best choice for pediatric use, due to their great ease of administration and dose-adaptability. Owing to its very low aqueous solubility and poor stability, CEF is only available as a powder for oral suspensions, which can lead to reduced compliance by children, due to its unpleasant texture and taste, and possible non-homogeneous dosage. The aim of this work was to develop an oral pediatric CEF solution endowed with good palatability, exploiting the solubilizing and taste-masking properties of cyclodextrins (CDs), joined to the use of amino acids as an auxiliary third component. Solubility studies indicated sulfobutylether-β-cyclodextrin (SBEβCD) and Histidine (His) as the most effective CD and amino acid, respectively, even though no synergistic effect on drug solubility improvement by their combined use was found. Molecular Dynamic and <sup>1</sup>H-NMR studies provided insight into the interactions of binary CEF:His and ternary CEF:His:SBEβCD systems used to prepare CEF solutions, which resulted stable and maintained unchanged antimicrobial activity during the two-weeks-use in therapy. The ternary solution was superior in terms of more tolerable pH (5.6 vs. 4.7) and better palatability, being resulted completely odorless by a panel test.
format	article
author	Marzia Cirri Natascia Mennini Giulia Nerli Jessica Rubia Enrico Casalone Fabrizio Melani Francesca Maestrelli Paola Mura
author_facet	Marzia Cirri Natascia Mennini Giulia Nerli Jessica Rubia Enrico Casalone Fabrizio Melani Francesca Maestrelli Paola Mura
author_sort	Marzia Cirri
title	Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
title_short	Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
title_full	Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
title_fullStr	Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
title_full_unstemmed	Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use
title_sort	combined use of cyclodextrins and amino acids for the development of cefixime oral solutions for pediatric use
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/8ff4b916504049389c223a66506e05f6
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Combined Use of Cyclodextrins and Amino Acids for the Development of Cefixime Oral Solutions for Pediatric Use

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