Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles
We aimed to investigate which base was suitable for preparing transdermal formulations incorporating tulobuterol (TUL) nanoparticles (30–180 nm) in this study. Three bases (water-soluble, absorptive, and aqueous ionic cream) were selected to prepare the transdermal formulations, and TUL nanoparticle...
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| Format: | Article |
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MDPI AG
2022-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/11/2431 |
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| author | Noriaki Nagai Fumihiko Ogata Saori Deguchi Aoi Fushiki Saki Daimyo Hiroko Otake Naohito Kawasaki |
| author_facet | Noriaki Nagai Fumihiko Ogata Saori Deguchi Aoi Fushiki Saki Daimyo Hiroko Otake Naohito Kawasaki |
| author_sort | Noriaki Nagai |
| collection | DOAJ |
| description | We aimed to investigate which base was suitable for preparing transdermal formulations incorporating tulobuterol (TUL) nanoparticles (30–180 nm) in this study. Three bases (water-soluble, absorptive, and aqueous ionic cream) were selected to prepare the transdermal formulations, and TUL nanoparticles were prepared with a bead-milling treatment. In the drug release study, the TUL release from the water-soluble ointment was higher than that from the other two ointments. Moreover, the addition of <i>l</i>-menthol enhanced TUL nanoparticle release from the ointment, and the rat skin penetration of the TUL water-soluble ointment was also significantly higher than that of the other two ointments. In addition, the drug penetration of the TUL water-soluble ointment with <i>l</i>-menthol sustained zero-order release over 24 h, and the skin permeability of TUL increased with TUL content in the ointment. On the other hand, this penetration was significantly inhibited by treatment with a caveolae-mediated endocytosis inhibitor (nystatin). In conclusion, we found that the water-soluble base incorporating TUL nanoparticles and <i>l</i>-menthol was the best among those assessed in this study. Furthermore, the pathway using caveolae-mediated endocytosis was related to the skin penetration of TUL nanoparticles in the TUL water-soluble ointment with <i>l</i>-menthol. These findings are useful for the design of a transdermal sustained-release formulation based on TUL nanoparticles. |
| first_indexed | 2024-03-09T18:45:28Z |
| format | Article |
| id | doaj.art-d64e5d3eb42e4a2aade1e394144a80b6 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T18:45:28Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-d64e5d3eb42e4a2aade1e394144a80b62023-11-24T06:22:10ZengMDPI AGPharmaceutics1999-49232022-11-011411243110.3390/pharmaceutics14112431Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol NanoparticlesNoriaki Nagai0Fumihiko Ogata1Saori Deguchi2Aoi Fushiki3Saki Daimyo4Hiroko Otake5Naohito Kawasaki6Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanFaculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, JapanWe aimed to investigate which base was suitable for preparing transdermal formulations incorporating tulobuterol (TUL) nanoparticles (30–180 nm) in this study. Three bases (water-soluble, absorptive, and aqueous ionic cream) were selected to prepare the transdermal formulations, and TUL nanoparticles were prepared with a bead-milling treatment. In the drug release study, the TUL release from the water-soluble ointment was higher than that from the other two ointments. Moreover, the addition of <i>l</i>-menthol enhanced TUL nanoparticle release from the ointment, and the rat skin penetration of the TUL water-soluble ointment was also significantly higher than that of the other two ointments. In addition, the drug penetration of the TUL water-soluble ointment with <i>l</i>-menthol sustained zero-order release over 24 h, and the skin permeability of TUL increased with TUL content in the ointment. On the other hand, this penetration was significantly inhibited by treatment with a caveolae-mediated endocytosis inhibitor (nystatin). In conclusion, we found that the water-soluble base incorporating TUL nanoparticles and <i>l</i>-menthol was the best among those assessed in this study. Furthermore, the pathway using caveolae-mediated endocytosis was related to the skin penetration of TUL nanoparticles in the TUL water-soluble ointment with <i>l</i>-menthol. These findings are useful for the design of a transdermal sustained-release formulation based on TUL nanoparticles.https://www.mdpi.com/1999-4923/14/11/2431tulobuterolnanoparticleointmenttransdermal delivery systemendocytosis |
| spellingShingle | Noriaki Nagai Fumihiko Ogata Saori Deguchi Aoi Fushiki Saki Daimyo Hiroko Otake Naohito Kawasaki Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles Pharmaceutics tulobuterol nanoparticle ointment transdermal delivery system endocytosis |
| title | Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles |
| title_full | Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles |
| title_fullStr | Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles |
| title_full_unstemmed | Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles |
| title_short | Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles |
| title_sort | design of a transdermal sustained release formulation based on water soluble ointment incorporating tulobuterol nanoparticles |
| topic | tulobuterol nanoparticle ointment transdermal delivery system endocytosis |
| url | https://www.mdpi.com/1999-4923/14/11/2431 |
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