TY - JOUR
T1 - Insights into therapeutic liquid mixtures and formulations towards tuberculosis therapy
AU - Santos, Filipa
AU - Pires, David
AU - Anes, Elsa
AU - Duarte, Ana Rita C.
N1 - info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT#
info:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FSAU-INF%2F28182%2F2017/PT#
info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FDTP%2F04138%2F2019/PT#
Funding Information:
This project has received funding from the European Union’s Horizon 2020 (European Research Council) under grant agreement No ERC-2016-CoG 725034 and was supported by the Associate Laboratory for Green Chemistry-LAQV. We also thank the support of ADEIM-FFUL (Associação para o Ensino e a Investigação em Microbiologia).
Publisher Copyright:
© 2023 The Author(s)
PY - 2023/4/25
Y1 - 2023/4/25
N2 - Therapeutic liquid mixtures, as deep eutectic systems, are considered a sustainable strategy that can be useful for the modification and enhancement of the pharmacokinetics and pharmacodynamics of different active ingredients. In this study, we assessed the stability and antibacterial activity of therapeutic liquid formulations prepared with anti-tuberculosis drugs. Tuberculosis therapy presents various pitfalls related, for example, to the administration of prolonged regimens of multiple drugs, different severe adverse effects, low compliance of the patient to treatment and the development of drug resistance. During this study, it was possible to assess the physicochemical stability of the formulations for 6 months, by polarized optical microscopy, 1H NMR and FTIR-ATR. Furthermore, the mixtures present an antibacterial effect against a drug-susceptible Mycobacterium tuberculosis strain (H37Rv). This was particularly evident for the mixtures with ethambutol incorporated, making them interesting to pursue with further studies and evaluation of clinical applicability. Upon infection, it was also observed that a single and higher dose appears to be more effective than lower separate doses, which could allow the production of patient-friendly formulations.
AB - Therapeutic liquid mixtures, as deep eutectic systems, are considered a sustainable strategy that can be useful for the modification and enhancement of the pharmacokinetics and pharmacodynamics of different active ingredients. In this study, we assessed the stability and antibacterial activity of therapeutic liquid formulations prepared with anti-tuberculosis drugs. Tuberculosis therapy presents various pitfalls related, for example, to the administration of prolonged regimens of multiple drugs, different severe adverse effects, low compliance of the patient to treatment and the development of drug resistance. During this study, it was possible to assess the physicochemical stability of the formulations for 6 months, by polarized optical microscopy, 1H NMR and FTIR-ATR. Furthermore, the mixtures present an antibacterial effect against a drug-susceptible Mycobacterium tuberculosis strain (H37Rv). This was particularly evident for the mixtures with ethambutol incorporated, making them interesting to pursue with further studies and evaluation of clinical applicability. Upon infection, it was also observed that a single and higher dose appears to be more effective than lower separate doses, which could allow the production of patient-friendly formulations.
KW - Anti-tuberculosis drugs
KW - Eutectic mixtures
KW - Therapeutic liquid mixtures
KW - Tuberculosis
UR - http://www.scopus.com/inward/record.url?scp=85151041781&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2023.122862
DO - 10.1016/j.ijpharm.2023.122862
M3 - Article
C2 - 36965645
AN - SCOPUS:85151041781
SN - 0378-5173
VL - 637
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 122862
ER -