Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation
Malaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein...
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MDPI AG
2024-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/16/3/357 |
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| author | Rafaela de Andrade Rita de Cássia dos Reis Schmidt Leonardo Santos Gomes Legna Colina-Vegas Ruth Hinrichs Marcos Antônio Zen Vasconcellos Tania Maria Haas Costa Monique Deon Wilmer Villarreal Edilson Valmir Benvenutti |
| author_facet | Rafaela de Andrade Rita de Cássia dos Reis Schmidt Leonardo Santos Gomes Legna Colina-Vegas Ruth Hinrichs Marcos Antônio Zen Vasconcellos Tania Maria Haas Costa Monique Deon Wilmer Villarreal Edilson Valmir Benvenutti |
| author_sort | Rafaela de Andrade |
| collection | DOAJ |
| description | Malaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein, magnetic mesoporous silica (magMCM) was synthesized using iron oxide particles dispersed in the silica structure for magnetically driven behavior. The X-ray diffractogram (XRD) and Mössbauer spectra show patterns corresponding to magnetite and maghemite. Furthermore, Mössbauer spectroscopy revealed superparamagnetic behavior, attributed to single magnetic domains in particles smaller than 10 nm. Even in the presence of iron oxide particles, the hexagonal structure of MCM is clearly identified in XRD (low-angle region) and the channels are visible in TEM images. The drug chloroquine (CQ) was encapsulated by incipient wetness impregnation (magMCM-CQ). The N<sub>2</sub> adsorption–desorption isotherms show that CQ molecules were encapsulated in the pores, without completely filling the mesopores. BET surface area values were 630 m<sup>2</sup> g<sup>−1</sup> (magMCM) and 467 m<sup>2</sup> g<sup>−1</sup> (magMCM-CQ). Encapsulated CQ exhibited rapid delivery (99% in 3 h) in buffer medium and improved solubility compared to the non-encapsulated drug, attributed to CQ encapsulation in amorphous form. The biocompatibility assessment of magMCM, magMCM-CQ, and CQ against MRC5 non-tumoral lung fibroblasts using the MTT assay after 24 h revealed no toxicity associated with magMCM. On the other hand, the non-encapsulated CQ and magMCM-CQ exhibited comparable dose–response activity, indicating a similar cytotoxic effect. |
| first_indexed | 2024-04-24T17:55:23Z |
| format | Article |
| id | doaj.art-be487b9a14cb435d8ded9ac126e63d68 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-24T17:55:23Z |
| publishDate | 2024-03-01 |
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| series | Pharmaceutics |
| spelling | doaj.art-be487b9a14cb435d8ded9ac126e63d682024-03-27T13:59:42ZengMDPI AGPharmaceutics1999-49232024-03-0116335710.3390/pharmaceutics16030357Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro EvaluationRafaela de Andrade0Rita de Cássia dos Reis Schmidt1Leonardo Santos Gomes2Legna Colina-Vegas3Ruth Hinrichs4Marcos Antônio Zen Vasconcellos5Tania Maria Haas Costa6Monique Deon7Wilmer Villarreal8Edilson Valmir Benvenutti9Instituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilPrograma de Pós-Graduação em Biociências, Universidade Federal de Ciências da Saúde de Porto Alegre (UFCSPA), Porto Alegre 90050-170, RS, BrazilInstituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilInstituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilInstituto de Geociências, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilInstituto de Física, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilInstituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilPrograma de Pós-Graduação em Biociências, Universidade Federal de Ciências da Saúde de Porto Alegre (UFCSPA), Porto Alegre 90050-170, RS, BrazilInstituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilInstituto de Química, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, RS, BrazilMalaria is a dangerous tropical disease, with high morbidity in developing countries. The responsible parasite has developed resistance to the existing drugs; therefore, new drug delivery systems are being studied to increase efficacy by targeting hemozoin, a parasite paramagnetic metabolite. Herein, magnetic mesoporous silica (magMCM) was synthesized using iron oxide particles dispersed in the silica structure for magnetically driven behavior. The X-ray diffractogram (XRD) and Mössbauer spectra show patterns corresponding to magnetite and maghemite. Furthermore, Mössbauer spectroscopy revealed superparamagnetic behavior, attributed to single magnetic domains in particles smaller than 10 nm. Even in the presence of iron oxide particles, the hexagonal structure of MCM is clearly identified in XRD (low-angle region) and the channels are visible in TEM images. The drug chloroquine (CQ) was encapsulated by incipient wetness impregnation (magMCM-CQ). The N<sub>2</sub> adsorption–desorption isotherms show that CQ molecules were encapsulated in the pores, without completely filling the mesopores. BET surface area values were 630 m<sup>2</sup> g<sup>−1</sup> (magMCM) and 467 m<sup>2</sup> g<sup>−1</sup> (magMCM-CQ). Encapsulated CQ exhibited rapid delivery (99% in 3 h) in buffer medium and improved solubility compared to the non-encapsulated drug, attributed to CQ encapsulation in amorphous form. The biocompatibility assessment of magMCM, magMCM-CQ, and CQ against MRC5 non-tumoral lung fibroblasts using the MTT assay after 24 h revealed no toxicity associated with magMCM. On the other hand, the non-encapsulated CQ and magMCM-CQ exhibited comparable dose–response activity, indicating a similar cytotoxic effect.https://www.mdpi.com/1999-4923/16/3/357antimalarialchloroquineenhanced drug solubilityMCM-41magnetic nanocarriers |
| spellingShingle | Rafaela de Andrade Rita de Cássia dos Reis Schmidt Leonardo Santos Gomes Legna Colina-Vegas Ruth Hinrichs Marcos Antônio Zen Vasconcellos Tania Maria Haas Costa Monique Deon Wilmer Villarreal Edilson Valmir Benvenutti Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation Pharmaceutics antimalarial chloroquine enhanced drug solubility MCM-41 magnetic nanocarriers |
| title | Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation |
| title_full | Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation |
| title_fullStr | Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation |
| title_full_unstemmed | Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation |
| title_short | Magnetic Mesoporous Silica for Targeted Drug Delivery of Chloroquine: Synthesis, Characterization, and In Vitro Evaluation |
| title_sort | magnetic mesoporous silica for targeted drug delivery of chloroquine synthesis characterization and in vitro evaluation |
| topic | antimalarial chloroquine enhanced drug solubility MCM-41 magnetic nanocarriers |
| url | https://www.mdpi.com/1999-4923/16/3/357 |
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