Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery
In this pilot study, ethosomes and transethosomes were investigated as potential delivery systems for cholecalciferol (vitamin D3), whose deficiency has been correlated to many disorders such as dermatological diseases, systemic infections, cancer and sarcopenia. A formulative study on the influence...
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| Format: | Article |
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MDPI AG
2021-05-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/10/5341 |
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| author | Manuela Costanzo Elisabetta Esposito Maddalena Sguizzato Maria Assunta Lacavalla Markus Drechsler Giuseppe Valacchi Carlo Zancanaro Manuela Malatesta |
| author_facet | Manuela Costanzo Elisabetta Esposito Maddalena Sguizzato Maria Assunta Lacavalla Markus Drechsler Giuseppe Valacchi Carlo Zancanaro Manuela Malatesta |
| author_sort | Manuela Costanzo |
| collection | DOAJ |
| description | In this pilot study, ethosomes and transethosomes were investigated as potential delivery systems for cholecalciferol (vitamin D3), whose deficiency has been correlated to many disorders such as dermatological diseases, systemic infections, cancer and sarcopenia. A formulative study on the influence of pharmaceutically acceptable ionic and non-ionic surfactants allowed the preparation of different transethosomes. In vitro cytotoxicity was evaluated in different cell types representative of epithelial, connective and muscle tissue. Then, the selected nanocarriers were further investigated at light and transmission electron microscopy to evaluate their uptake and intracellular fate. Both ethosomes and transethosomes proven to have physicochemical properties optimal for transdermal penetration and efficient vitamin D3 loading; moreover, nanocarriers were easily internalized by all cell types, although they followed distinct intracellular fates: ethosomes persisted for long times inside the cytoplasm, without inducing subcellular alteration, while transethosomes underwent rapid degradation giving rise to an intracellular accumulation of lipids. These basic results provide a solid scientific background to in vivo investigations aimed at exploring the efficacy of vitamin D3 transdermal administration in different experimental and pathological conditions. |
| first_indexed | 2024-03-10T11:15:55Z |
| format | Article |
| id | doaj.art-2fc966a920b448f497b3086fbc51bf33 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T11:15:55Z |
| publishDate | 2021-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-2fc966a920b448f497b3086fbc51bf332023-11-21T20:24:02ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-05-012210534110.3390/ijms22105341Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 DeliveryManuela Costanzo0Elisabetta Esposito1Maddalena Sguizzato2Maria Assunta Lacavalla3Markus Drechsler4Giuseppe Valacchi5Carlo Zancanaro6Manuela Malatesta7Department of Neurosciences, Biomedicine and Movement Sciences, University of Verona, I-37134 Verona, ItalyDepartment of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, I-44121 Ferrara, ItalyDepartment of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, I-44121 Ferrara, ItalyDepartment of Neurosciences, Biomedicine and Movement Sciences, University of Verona, I-37134 Verona, ItalyBavarian Polymer Institute (BPI) Keylab Electron and Optical Microscopy, University of Bayreuth, D-95440 Bayreuth, GermanyDepartment of Neurosciences and Rehabilitation, University of Ferrara, I-44121 Ferrara, ItalyDepartment of Neurosciences, Biomedicine and Movement Sciences, University of Verona, I-37134 Verona, ItalyDepartment of Neurosciences, Biomedicine and Movement Sciences, University of Verona, I-37134 Verona, ItalyIn this pilot study, ethosomes and transethosomes were investigated as potential delivery systems for cholecalciferol (vitamin D3), whose deficiency has been correlated to many disorders such as dermatological diseases, systemic infections, cancer and sarcopenia. A formulative study on the influence of pharmaceutically acceptable ionic and non-ionic surfactants allowed the preparation of different transethosomes. In vitro cytotoxicity was evaluated in different cell types representative of epithelial, connective and muscle tissue. Then, the selected nanocarriers were further investigated at light and transmission electron microscopy to evaluate their uptake and intracellular fate. Both ethosomes and transethosomes proven to have physicochemical properties optimal for transdermal penetration and efficient vitamin D3 loading; moreover, nanocarriers were easily internalized by all cell types, although they followed distinct intracellular fates: ethosomes persisted for long times inside the cytoplasm, without inducing subcellular alteration, while transethosomes underwent rapid degradation giving rise to an intracellular accumulation of lipids. These basic results provide a solid scientific background to in vivo investigations aimed at exploring the efficacy of vitamin D3 transdermal administration in different experimental and pathological conditions.https://www.mdpi.com/1422-0067/22/10/5341cell culturecholecalciferolcryogenic transmission electron microscopyin vitro testlight microscopylipid nanocarriers |
| spellingShingle | Manuela Costanzo Elisabetta Esposito Maddalena Sguizzato Maria Assunta Lacavalla Markus Drechsler Giuseppe Valacchi Carlo Zancanaro Manuela Malatesta Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery International Journal of Molecular Sciences cell culture cholecalciferol cryogenic transmission electron microscopy in vitro test light microscopy lipid nanocarriers |
| title | Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery |
| title_full | Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery |
| title_fullStr | Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery |
| title_full_unstemmed | Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery |
| title_short | Formulative Study and Intracellular Fate Evaluation of Ethosomes and Transethosomes for Vitamin D3 Delivery |
| title_sort | formulative study and intracellular fate evaluation of ethosomes and transethosomes for vitamin d3 delivery |
| topic | cell culture cholecalciferol cryogenic transmission electron microscopy in vitro test light microscopy lipid nanocarriers |
| url | https://www.mdpi.com/1422-0067/22/10/5341 |
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