TY - JOUR
T1 - Determination of mometasone furoate solubility, using deep eutectic systems, and topical formulation- experimental and computational studies
AU - Craveiro, Rita
AU - Rocha, Ângelo
AU - Fernandes, Cláudio
AU - Duarte, Ana Rita C.
AU - Marto, Joana
AU - Paiva, Alexandre
N1 - Funding Information:
info:eu-repo/grantAgreement/FCT/Concurso para Atribuição do Estatuto e Financiamento de Laboratórios Associados (LA)/LA%2FP%2F0008%2F2020/PT#
info:eu-repo/grantAgreement/FCT/Concurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017%2F2018) - Financiamento Programático/UIDP%2F50006%2F2020/PT#
info:eu-repo/grantAgreement/FCT/Concurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017%2F2018) - Financiamento Base/UIDB%2F50006%2F2020/PT#
info:eu-repo/grantAgreement/FCT/Concurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017%2F2018) - Financiamento Base/UIDB%2F04138%2F2020/PT#
info:eu-repo/grantAgreement/FCT/Concurso de avaliação no âmbito do Programa Plurianual de Financiamento de Unidades de I&D (2017%2F2018) - Financiamento Programático/UIDP%2F04138%2F2020/PT#
info:eu-repo/grantAgreement/FCT/CEEC INST 2018/CEECINST%2F00145%2F2018%2FCP1571%2FCT0001/PT#
info:eu-repo/grantAgreement/FCT//PRT%2FBD%2F154656%2F2023/PT#
This project has received funding from the European Union\u2019s Horizon 2020 (European Research Council) under grant agreement no. ERC-2016-CoG 725034.
Publisher Copyright:
© 2024 The Authors
PY - 2024/12
Y1 - 2024/12
N2 - The low solubility of some drugs in aqueous medium, is currently a challenge for the pharmaceutical industry, affecting drug bioavailability and treatment efficacy, so there is the need to find new solutions for this challenge. In this work, the solubility of a glucocorticoid drug, mometasone furoate (MF), in different deep eutectic systems (DES) is studied. DES present the advantage of being sustainable solvents, which can be used directly in the final formulation, and establish a synergistic effect with the drug. The solubility of MF in different DES is increased, when compared to the solubility of this drug in an aqueous medium, particularly in DES composed by levulinic acid and terpenes such as menthol and thymol, where the solubility of MF was of 24.1 and 103.3 mgMF/gDES, respectively. Solubility was also assessed using the computational determination of the Hansen solubility parameters of MF in these DES, in particular the total solubility parameter (δT) and Relative Energy Difference (RED). The obtained results correlate well with the MF measured experimentally, showing that this computational tool can be further used to predict MF solubility in DES. Furthermore, oil-in-water emulsions containing DES with MF were developed, allowing more versatility compared to the drug in powdered form, and were prepared containing 1 and 5 % of DES with MF. This work highlights that DES can have an important role in drug solubilization and in the development of new formulation strategies for the pharmaceutical industries.
AB - The low solubility of some drugs in aqueous medium, is currently a challenge for the pharmaceutical industry, affecting drug bioavailability and treatment efficacy, so there is the need to find new solutions for this challenge. In this work, the solubility of a glucocorticoid drug, mometasone furoate (MF), in different deep eutectic systems (DES) is studied. DES present the advantage of being sustainable solvents, which can be used directly in the final formulation, and establish a synergistic effect with the drug. The solubility of MF in different DES is increased, when compared to the solubility of this drug in an aqueous medium, particularly in DES composed by levulinic acid and terpenes such as menthol and thymol, where the solubility of MF was of 24.1 and 103.3 mgMF/gDES, respectively. Solubility was also assessed using the computational determination of the Hansen solubility parameters of MF in these DES, in particular the total solubility parameter (δT) and Relative Energy Difference (RED). The obtained results correlate well with the MF measured experimentally, showing that this computational tool can be further used to predict MF solubility in DES. Furthermore, oil-in-water emulsions containing DES with MF were developed, allowing more versatility compared to the drug in powdered form, and were prepared containing 1 and 5 % of DES with MF. This work highlights that DES can have an important role in drug solubilization and in the development of new formulation strategies for the pharmaceutical industries.
KW - Deep eutectic systems
KW - Drug solubility
KW - Drug topical formulations
KW - Hansen parameters
KW - Mometasone furoate
KW - Oil-in-water emulsions
UR - http://www.scopus.com/inward/record.url?scp=85204621364&partnerID=8YFLogxK
U2 - 10.1016/j.scp.2024.101783
DO - 10.1016/j.scp.2024.101783
M3 - Article
AN - SCOPUS:85204621364
SN - 2352-5541
VL - 42
JO - Sustainable Chemistry and Pharmacy
JF - Sustainable Chemistry and Pharmacy
M1 - 101783
ER -