Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes
Gold(III) bisdithiolate complexes have been reported as potential antimicrobial and antitumoral agents. The complex [Au(cdc)<sub>2</sub>]<sup>−</sup> (cdc=cyanodithioimido carbonate) displayed antimicrobial and outstanding antitumor activity against the ovarian cancer cells A...
| Main Authors: | , , , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-02-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/15/2/564 |
| _version_ | 1827755899927658496 |
|---|---|
| author | Andreia Sousa Joana F. Santos Francisco Silva Sílvia A. Sousa Jorge H. Leitão António P. Matos Teresa Pinheiro Rafaela A. L. Silva Dulce Belo Manuel Almeida Fernanda Marques Célia Fernandes |
| author_facet | Andreia Sousa Joana F. Santos Francisco Silva Sílvia A. Sousa Jorge H. Leitão António P. Matos Teresa Pinheiro Rafaela A. L. Silva Dulce Belo Manuel Almeida Fernanda Marques Célia Fernandes |
| author_sort | Andreia Sousa |
| collection | DOAJ |
| description | Gold(III) bisdithiolate complexes have been reported as potential antimicrobial and antitumoral agents. The complex [Au(cdc)<sub>2</sub>]<sup>−</sup> (cdc=cyanodithioimido carbonate) displayed antimicrobial and outstanding antitumor activity against the ovarian cancer cells A2780 and A2780cisR, which are sensitive and resistant to cisplatin, respectively. However, poor water solubility may hamper its clinical use. Block copolymer micelles (BCMs) may solubilize hydrophobic drugs, improving their bioavailability and circulation time in blood. Aiming to provide water solubility, prolonged availability, and enhanced therapeutic indexes, BCMs loaded with [Au(cdc)<sub>2</sub>]<sup>−</sup> were synthesized and characterized. The BCM-[Au(cdc)<sub>2</sub>] micelles were prepared with a loading efficiency of 64.6% and a loading content of 35.3 mg [Au(cdc)<sub>2</sub>]<sup>−</sup>/gBCM. A hydrodynamic diameter of 77.31 ± 27.00 nm and a low polydispersity index of 0.18 indicated that the micelles were homogenous and good candidates for drug delivery. Cytotoxic activity studies against A2780/A2780cisR cells showed that BCM-[Au(cdc)<sub>2</sub>] maintained relevant cytotoxic activity comparable to the cytotoxicity observed for the same concentration of gold complexes. The Au uptake in A2780 cells, determined by PIXE, was ca. 17% higher for BCMs-[Au(cdc)<sub>2</sub>] compared to [Au(cdc)<sub>2</sub>]<sup>−</sup>. The BCMs-[Au(cdc)<sub>2</sub>] presented antimicrobial activity against <i>S. aureus</i> Newman and <i>C. glabrata</i> CBS138. These results evidenced the potential of BCM-[Au(cdc)<sub>2</sub>] for drug delivery and its promising anticancer and antimicrobial activities. |
| first_indexed | 2024-03-11T08:16:34Z |
| format | Article |
| id | doaj.art-1c04959aeb9c47f8b2f7ab4ee32b1046 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:16:34Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-1c04959aeb9c47f8b2f7ab4ee32b10462023-11-16T22:41:38ZengMDPI AGPharmaceutics1999-49232023-02-0115256410.3390/pharmaceutics15020564Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate ComplexesAndreia Sousa0Joana F. Santos1Francisco Silva2Sílvia A. Sousa3Jorge H. Leitão4António P. Matos5Teresa Pinheiro6Rafaela A. L. Silva7Dulce Belo8Manuel Almeida9Fernanda Marques10Célia Fernandes11Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugaliBB-Institute for Bioengineering and Biosciences and Associate Laboratory Institute for Health and Bioeconomy—i4HB, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, PortugaliBB-Institute for Bioengineering and Biosciences and Associate Laboratory Institute for Health and Bioeconomy—i4HB, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, PortugalCentro de Investigação Interdisciplinar Egas Moniz, Campus Universitário, Quinta da Granja, Monte de Caparica, 2829-511 Caparica, PortugaliBB-Institute for Bioengineering and Biosciences and Associate Laboratory Institute for Health and Bioeconomy—i4HB, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalCentro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, PortugalGold(III) bisdithiolate complexes have been reported as potential antimicrobial and antitumoral agents. The complex [Au(cdc)<sub>2</sub>]<sup>−</sup> (cdc=cyanodithioimido carbonate) displayed antimicrobial and outstanding antitumor activity against the ovarian cancer cells A2780 and A2780cisR, which are sensitive and resistant to cisplatin, respectively. However, poor water solubility may hamper its clinical use. Block copolymer micelles (BCMs) may solubilize hydrophobic drugs, improving their bioavailability and circulation time in blood. Aiming to provide water solubility, prolonged availability, and enhanced therapeutic indexes, BCMs loaded with [Au(cdc)<sub>2</sub>]<sup>−</sup> were synthesized and characterized. The BCM-[Au(cdc)<sub>2</sub>] micelles were prepared with a loading efficiency of 64.6% and a loading content of 35.3 mg [Au(cdc)<sub>2</sub>]<sup>−</sup>/gBCM. A hydrodynamic diameter of 77.31 ± 27.00 nm and a low polydispersity index of 0.18 indicated that the micelles were homogenous and good candidates for drug delivery. Cytotoxic activity studies against A2780/A2780cisR cells showed that BCM-[Au(cdc)<sub>2</sub>] maintained relevant cytotoxic activity comparable to the cytotoxicity observed for the same concentration of gold complexes. The Au uptake in A2780 cells, determined by PIXE, was ca. 17% higher for BCMs-[Au(cdc)<sub>2</sub>] compared to [Au(cdc)<sub>2</sub>]<sup>−</sup>. The BCMs-[Au(cdc)<sub>2</sub>] presented antimicrobial activity against <i>S. aureus</i> Newman and <i>C. glabrata</i> CBS138. These results evidenced the potential of BCM-[Au(cdc)<sub>2</sub>] for drug delivery and its promising anticancer and antimicrobial activities.https://www.mdpi.com/1999-4923/15/2/564block copolymer micellesdrug deliverygold(III) complexesantimicrobialantitumoral |
| spellingShingle | Andreia Sousa Joana F. Santos Francisco Silva Sílvia A. Sousa Jorge H. Leitão António P. Matos Teresa Pinheiro Rafaela A. L. Silva Dulce Belo Manuel Almeida Fernanda Marques Célia Fernandes Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes Pharmaceutics block copolymer micelles drug delivery gold(III) complexes antimicrobial antitumoral |
| title | Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes |
| title_full | Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes |
| title_fullStr | Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes |
| title_full_unstemmed | Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes |
| title_short | Antitumoral and Antimicrobial Activities of Block Copolymer Micelles Containing Gold Bisdithiolate Complexes |
| title_sort | antitumoral and antimicrobial activities of block copolymer micelles containing gold bisdithiolate complexes |
| topic | block copolymer micelles drug delivery gold(III) complexes antimicrobial antitumoral |
| url | https://www.mdpi.com/1999-4923/15/2/564 |
| work_keys_str_mv | AT andreiasousa antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT joanafsantos antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT franciscosilva antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT silviaasousa antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT jorgehleitao antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT antoniopmatos antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT teresapinheiro antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT rafaelaalsilva antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT dulcebelo antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT manuelalmeida antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT fernandamarques antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes AT celiafernandes antitumoralandantimicrobialactivitiesofblockcopolymermicellescontaininggoldbisdithiolatecomplexes |