Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution
Ji-Hyun Kang*,1 Jinmann Chon*,2 Young-Il Kim,1 Hyo-Jung Lee,1 Dong-Won Oh,1 Hong-Goo Lee,1 Chang-Soo Han,1 Dong-Wook Kim,3 Chun-Woong Park11College of Pharmacy, Chungbuk National University, Cheongju, Republic of Korea; 2School of Medicine, Kyung Hee University, Seoul, Republic of...
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Dove Medical Press
2019
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oai:doaj.org-article:fadae648d9594052af42964878ab5afb2021-12-02T07:04:23ZPreparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution1178-2013https://doaj.org/article/fadae648d9594052af42964878ab5afb2019-07-01T00:00:00Zhttps://www.dovepress.com/preparation-and-evaluation-of-tacrolimus-loaded-thermosensitive-solid--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ji-Hyun Kang*,1 Jinmann Chon*,2 Young-Il Kim,1 Hyo-Jung Lee,1 Dong-Won Oh,1 Hong-Goo Lee,1 Chang-Soo Han,1 Dong-Wook Kim,3 Chun-Woong Park11College of Pharmacy, Chungbuk National University, Cheongju, Republic of Korea; 2School of Medicine, Kyung Hee University, Seoul, Republic of Korea; 3Department of Pharmaceutical Engineering, Cheongju University, Cheongju, Republic of Korea*These authors contributed equally to this workBackground: Tacrolimus (TCR), also known as FK-506, is a biopharmaceutics classification system (BCS) class II drug that is insoluble in water because of its high log P values. After dermal application, TCR remains in the stratum corneum and passes through the skin layers with difficulty.Purpose: The objectives of this study were to develop and evaluate solid lipid nanoparticles (SLNs) with thermosensitive properties to improve penetration and retention.Methods: We prepared TCR-loaded thermosensitive solid lipid nanoparticles (TCR-SLNs) with different types of surfactants on the shell of the particle, which conferred the advantages of enhancing skin permeation and distribution. We also characterized them from a physic point of view and performed in vitro and in vivo evaluations.Results: The TCR contained in the prepared TCR-SLN was in an amorphous state and entrapped in the particles with a high loading efficiency. The assessment of ex vivo skin penetration using excised rat dorsal skin showed that the TCR-SLNs penetrated to a deeper layer than the reference product (0.1% Protopic®). In addition, the in vivo skin penetration test demonstrated that TCR-SLNs delivered more drug into deeper skin layers than the reference product. FT-IR images also confirmed drug distribution of TCR-SLNs into deeper layers of the skin.Conclusion: These results revealed the potential application of thermosensitive SLNs for the delivery of difficult-to-permeate, poorly water-soluble drugs into deep skin layers.Keywords: tacrolimus, thermosensitive, solid lipid nanoparticle, FT-IR imaging, atopic dermatitis, dermal deliveryKang JHChon JKim YILee HJOh DWLee HGHan CSKim DWPark CWDove Medical PressarticleTacrolimusThermosensitiveSolid lipid nanoparticleFT-IR imagingAtopic dermatitisDermal deliveryMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 5381-5396 (2019) |
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Tacrolimus Thermosensitive Solid lipid nanoparticle FT-IR imaging Atopic dermatitis Dermal delivery Medicine (General) R5-920 |
| spellingShingle |
Tacrolimus Thermosensitive Solid lipid nanoparticle FT-IR imaging Atopic dermatitis Dermal delivery Medicine (General) R5-920 Kang JH Chon J Kim YI Lee HJ Oh DW Lee HG Han CS Kim DW Park CW Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| description |
Ji-Hyun Kang*,1 Jinmann Chon*,2 Young-Il Kim,1 Hyo-Jung Lee,1 Dong-Won Oh,1 Hong-Goo Lee,1 Chang-Soo Han,1 Dong-Wook Kim,3 Chun-Woong Park11College of Pharmacy, Chungbuk National University, Cheongju, Republic of Korea; 2School of Medicine, Kyung Hee University, Seoul, Republic of Korea; 3Department of Pharmaceutical Engineering, Cheongju University, Cheongju, Republic of Korea*These authors contributed equally to this workBackground: Tacrolimus (TCR), also known as FK-506, is a biopharmaceutics classification system (BCS) class II drug that is insoluble in water because of its high log P values. After dermal application, TCR remains in the stratum corneum and passes through the skin layers with difficulty.Purpose: The objectives of this study were to develop and evaluate solid lipid nanoparticles (SLNs) with thermosensitive properties to improve penetration and retention.Methods: We prepared TCR-loaded thermosensitive solid lipid nanoparticles (TCR-SLNs) with different types of surfactants on the shell of the particle, which conferred the advantages of enhancing skin permeation and distribution. We also characterized them from a physic point of view and performed in vitro and in vivo evaluations.Results: The TCR contained in the prepared TCR-SLN was in an amorphous state and entrapped in the particles with a high loading efficiency. The assessment of ex vivo skin penetration using excised rat dorsal skin showed that the TCR-SLNs penetrated to a deeper layer than the reference product (0.1% Protopic®). In addition, the in vivo skin penetration test demonstrated that TCR-SLNs delivered more drug into deeper skin layers than the reference product. FT-IR images also confirmed drug distribution of TCR-SLNs into deeper layers of the skin.Conclusion: These results revealed the potential application of thermosensitive SLNs for the delivery of difficult-to-permeate, poorly water-soluble drugs into deep skin layers.Keywords: tacrolimus, thermosensitive, solid lipid nanoparticle, FT-IR imaging, atopic dermatitis, dermal delivery |
| format |
article |
| author |
Kang JH Chon J Kim YI Lee HJ Oh DW Lee HG Han CS Kim DW Park CW |
| author_facet |
Kang JH Chon J Kim YI Lee HJ Oh DW Lee HG Han CS Kim DW Park CW |
| author_sort |
Kang JH |
| title |
Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| title_short |
Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| title_full |
Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| title_fullStr |
Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| title_full_unstemmed |
Preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| title_sort |
preparation and evaluation of tacrolimus-loaded thermosensitive solid lipid nanoparticles for improved dermal distribution |
| publisher |
Dove Medical Press |
| publishDate |
2019 |
| url |
https://doaj.org/article/fadae648d9594052af42964878ab5afb |
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