Publicação
Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems
| Resumo: | A therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems. |
|---|---|
| Autores principais: | Aroso, Ivo Manuel Ascensão |
| Outros Autores: | Silva, João C.; Mano, Francisca; Ferreira, Ana S. D.; Dionísio, Madalena; Nogueira, Isabel Sá; Barreiros, Susana; Reis, R. L.; Paiva, Alexandre; Duarte, Ana Rita C. |
| Assunto: | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| Ano: | 2016 |
| País: | Portugal |
| Tipo de documento: | artigo |
| Tipo de acesso: | acesso restrito |
| Instituição associada: | Universidade do Minho |
| Idioma: | inglês |
| Origem: | RepositóriUM - Universidade do Minho |
| _version_ | 1867438125116030976 |
|---|---|
| author | Aroso, Ivo Manuel Ascensão |
| author2 | Silva, João C. Mano, Francisca Ferreira, Ana S. D. Dionísio, Madalena Nogueira, Isabel Sá Barreiros, Susana Reis, R. L. Paiva, Alexandre Duarte, Ana Rita C. |
| author2_role | author author author author author author author author author |
| author_facet | Aroso, Ivo Manuel Ascensão Silva, João C. Mano, Francisca Ferreira, Ana S. D. Dionísio, Madalena Nogueira, Isabel Sá Barreiros, Susana Reis, R. L. Paiva, Alexandre Duarte, Ana Rita C. |
| author_role | author |
| contributor_name_str_mv | RepositóriUM - Universidade do Minho |
| country_str | PT |
| creators_json_txt | [{\"Person.name\":\"Aroso, Ivo Manuel Ascensão\"},{\"Person.name\":\"Silva, João C.\"},{\"Person.name\":\"Mano, Francisca\"},{\"Person.name\":\"Ferreira, Ana S. D.\"},{\"Person.name\":\"Dionísio, Madalena\"},{\"Person.name\":\"Nogueira, Isabel Sá\"},{\"Person.name\":\"Barreiros, Susana\"},{\"Person.name\":\"Reis, R. L.\"},{\"Person.name\":\"Paiva, Alexandre\"},{\"Person.name\":\"Duarte, Ana Rita C.\"}] |
| datacite.contributors.contributor.contributorName.fl_str_mv | RepositóriUM - Universidade do Minho |
| datacite.creators.creator.creatorName.fl_str_mv | Aroso, Ivo Manuel Ascensão Silva, João C. Mano, Francisca Ferreira, Ana S. D. Dionísio, Madalena Nogueira, Isabel Sá Barreiros, Susana Reis, R. L. Paiva, Alexandre Duarte, Ana Rita C. |
| datacite.date.Accepted.fl_str_mv | 2016-01-01T00:00:00Z |
| datacite.rights.fl_str_mv | http://purl.org/coar/access_right/c_16ec |
| datacite.subjects.subject.fl_str_mv | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| datacite.titles.title.fl_str_mv | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| dc.contributor.none.fl_str_mv | RepositóriUM - Universidade do Minho |
| dc.creator.none.fl_str_mv | Aroso, Ivo Manuel Ascensão Silva, João C. Mano, Francisca Ferreira, Ana S. D. Dionísio, Madalena Nogueira, Isabel Sá Barreiros, Susana Reis, R. L. Paiva, Alexandre Duarte, Ana Rita C. |
| dc.date.Accepted.fl_str_mv | 2016-01-01T00:00:00Z |
| dc.format.none.fl_str_mv | application/pdf |
| dc.identifier.none.fl_str_mv | https://hdl.handle.net/1822/40289 |
| dc.language.none.fl_str_mv | eng |
| dc.publisher.none.fl_str_mv | Elsevier |
| dc.rights.none.fl_str_mv | http://purl.org/coar/access_right/c_16ec |
| dc.subject.none.fl_str_mv | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| dc.title.fl_str_mv | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| dc.type.none.fl_str_mv | http://purl.org/coar/resource_type/c_6501 |
| description | A therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems. |
| dirty | 0 |
| eu_rights_str_mv | restrictedAccess |
| format | article |
| fulltext.url.fl_str_mv | https://repositorium.uminho.pt/bitstreams/67dc87cb-c1af-4354-b387-82ef0b3c4743/download |
| id | rum_4868cd168a2d723ca08e6decdfb587bd |
| identifier.url.fl_str_mv | https://hdl.handle.net/1822/40289 |
| instacron_str | repositorium |
| institution | Universidade do Minho |
| instname_str | Universidade do Minho |
| language | eng |
| network_acronym_str | rum |
| network_name_str | RepositóriUM - Universidade do Minho |
| oai_identifier_str | oai:repositorium.uminho.pt:1822/40289 |
| organization_str_mv | urn:organizationAcronym:repositorium |
| person_str_mv | Aroso, Ivo Manuel Ascensão Silva, João C. Mano, Francisca Ferreira, Ana S. D. Dionísio, Madalena Nogueira, Isabel Sá Barreiros, Susana Reis, R. L. Paiva, Alexandre Duarte, Ana Rita C. |
| publishDate | 2016 |
| publisher.none.fl_str_mv | Elsevier |
| reponame_str | RepositóriUM - Universidade do Minho |
| repository_id_str | urn:repositoryAcronym:rum |
| service_str_mv | urn:repositoryAcronym:rum |
| spelling | engElsevierporA therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems.application/pdfporDissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systemsAroso, Ivo Manuel AscensãoSilva, João C.Mano, FranciscaFerreira, Ana S. D.Dionísio, MadalenaNogueira, Isabel SáBarreiros, SusanaReis, R. L.Paiva, AlexandreDuarte, Ana Rita C.HostingInstitutionOrganizationalRepositóriUM - Universidade do Minhoe-mailmailto:repositorium@usdb.uminho.ptrepositorium@usdb.uminho.ptCITATIONAroso I. M., Silva J. C., Mano F., Ferreira A. S., Dionísio M., Sá-Nogueira I., Barreiros S., Reis R. L., Paiva A., Duarte A. R. C. Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems, European Journal of Pharmaceutics and Biopharmaceutics, Vol. 98, pp. 57-66, doi:10.1016/j.ejpb.2015.11.002, 2015PMID26586342ISSNIsPartOf0939-6411DOIIsPartOf10.1016/j.ejpb.2015.11.00220162015-122016-02-01T09:50:01Z2016-01-01T00:00:00ZHandlehttps://hdl.handle.net/1822/40289http://purl.org/coar/access_right/c_16ecrestricted accessTherapeutic deep eutectic systemsDrug solubilityGreen technologiesPharmaceutical and biomedical applications2604819 bytesliteraturehttp://purl.org/coar/resource_type/c_6501journal articlehttp://purl.org/coar/access_right/c_16ecapplication/pdffulltexthttps://repositorium.uminho.pt/bitstreams/67dc87cb-c1af-4354-b387-82ef0b3c4743/download |
| spellingShingle | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems Aroso, Ivo Manuel Ascensão Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| status | SINGLETON |
| subject.fl_str_mv | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| title | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| title_full | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| title_fullStr | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| title_full_unstemmed | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| title_short | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| title_sort | Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems |
| topic | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| topic_facet | Therapeutic deep eutectic systems Drug solubility Green technologies Pharmaceutical and biomedical applications |
| url | https://hdl.handle.net/1822/40289 |
| visible | 1 |