Ternary Deep Eutectic Solvents System of Colchicine, 4-Hydroxyacetophenone, and Protocatechuic Acid and Characterization of Transdermal Enhancement Mechanism
Abstract This study aimed to prepare colchicine (CO), 4-hydroxyacetophenone (HA), and protocatechuic acid (CA) contained in transdermal rubber plasters into a more releasable and acrylate pressure-sensitive adhesive (PSA) to optimize traditional Touguling rubber plasters (TOU) with enhanced transdermal permeability by using deep eutectic solvents (DES) technology. We compared the difference in the release behavior of CO between rubber plaster and PSA, determined the composition of the patch through pharmacodynamic experiments, explored the transdermal behavior of the three components, optimized the patch formula factors, and improved the penetration of CO through the skin. We also focused on elucidating the interactions among the three components of DES and the intricate relationship between DES and the skin. The melting point of DES was determined using DSC, while FTIR, 13C NMR, and ATR-FTIR were used to explore the intricate molecular mechanisms underlying the formation of DES, as well as its enhancement of skin permeability. The results of this investigation confirmed the successful formation of DES, marked by a discernible melting point at 27.33°C. The optimized patch, formulated with a molar ratio of 1:1:1 for CO, HA, and CA, significantly enhanced skin permeability, with the measured skin permeation quantities being 32.26 ± 2.98 µg/$ cm^{2} $, 117.67 ± 7.73 µg/$ cm^{2} $, and 56.79 ± 1.30 µg/$ cm^{2} $ respectively. Remarkably, the optimized patch also demonstrated similar analgesic and anti-inflammatory effects compared to commercial diclofenac diethylamide patches in different pharmacodynamics studies. The formation of DES altered drug compatibility with skin lipids and increased retention, driven by the interaction among the three component molecules through hydrogen bonding, effectively shielding the skin-binding sites and enhancing component permeation. In summary, the study demonstrated that optimized DES patches can concurrently enhance the penetration of CO, HA, and CA, thereby providing a promising approach for the development of DES in transdermal drug delivery systems. The findings also shed light on the molecular mechanisms underlying the transdermal behavior of DES and offer insights for developing more effective traditional Chinese medicine transdermal drug delivery systems..
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2023 |
|---|---|
| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:24 |
|---|---|
| Enthalten in: |
AAPS PharmSciTech - 24(2023), 8 vom: 14. Nov. |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Piao, Huiqing [VerfasserIn] |
|---|
| Links: |
Volltext [lizenzpflichtig] |
|---|
| Themen: |
Colchicine |
|---|
| Anmerkungen: |
© The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. |
|---|
| doi: |
10.1208/s12249-023-02681-x |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
SPR053738578 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | SPR053738578 | ||
| 003 | DE-627 | ||
| 005 | 20231230064630.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231115s2023 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1208/s12249-023-02681-x |2 doi | |
| 035 | |a (DE-627)SPR053738578 | ||
| 035 | |a (SPR)s12249-023-02681-x-e | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Piao, Huiqing |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Ternary Deep Eutectic Solvents System of Colchicine, 4-Hydroxyacetophenone, and Protocatechuic Acid and Characterization of Transdermal Enhancement Mechanism |
| 264 | 1 | |c 2023 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a Computermedien |b c |2 rdamedia | ||
| 338 | |a Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a © The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. | ||
| 520 | |a Abstract This study aimed to prepare colchicine (CO), 4-hydroxyacetophenone (HA), and protocatechuic acid (CA) contained in transdermal rubber plasters into a more releasable and acrylate pressure-sensitive adhesive (PSA) to optimize traditional Touguling rubber plasters (TOU) with enhanced transdermal permeability by using deep eutectic solvents (DES) technology. We compared the difference in the release behavior of CO between rubber plaster and PSA, determined the composition of the patch through pharmacodynamic experiments, explored the transdermal behavior of the three components, optimized the patch formula factors, and improved the penetration of CO through the skin. We also focused on elucidating the interactions among the three components of DES and the intricate relationship between DES and the skin. The melting point of DES was determined using DSC, while FTIR, 13C NMR, and ATR-FTIR were used to explore the intricate molecular mechanisms underlying the formation of DES, as well as its enhancement of skin permeability. The results of this investigation confirmed the successful formation of DES, marked by a discernible melting point at 27.33°C. The optimized patch, formulated with a molar ratio of 1:1:1 for CO, HA, and CA, significantly enhanced skin permeability, with the measured skin permeation quantities being 32.26 ± 2.98 µg/$ cm^{2} $, 117.67 ± 7.73 µg/$ cm^{2} $, and 56.79 ± 1.30 µg/$ cm^{2} $ respectively. Remarkably, the optimized patch also demonstrated similar analgesic and anti-inflammatory effects compared to commercial diclofenac diethylamide patches in different pharmacodynamics studies. The formation of DES altered drug compatibility with skin lipids and increased retention, driven by the interaction among the three component molecules through hydrogen bonding, effectively shielding the skin-binding sites and enhancing component permeation. In summary, the study demonstrated that optimized DES patches can concurrently enhance the penetration of CO, HA, and CA, thereby providing a promising approach for the development of DES in transdermal drug delivery systems. The findings also shed light on the molecular mechanisms underlying the transdermal behavior of DES and offer insights for developing more effective traditional Chinese medicine transdermal drug delivery systems. | ||
| 650 | 4 | |a colchicine |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a deep eutectic solvents |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a traditional Chinese medicine |7 (dpeaa)DE-He213 | |
| 650 | 4 | |a transdermal patch |7 (dpeaa)DE-He213 | |
| 700 | 1 | |a Xie, Wanchen |4 aut | |
| 700 | 1 | |a Li, Shiqi |4 aut | |
| 700 | 1 | |a Wang, Jiaqi |4 aut | |
| 700 | 1 | |a Liu, Chao |4 aut | |
| 700 | 1 | |a Quan, Peng |4 aut | |
| 700 | 1 | |a Fang, Liang |0 (orcid)0000-0001-9966-3880 |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t AAPS PharmSciTech |d New York, NY : Springer, 2000 |g 24(2023), 8 vom: 14. Nov. |w (DE-627)SPR02478785X |w (DE-600)2052070-0 |x 1530-9932 |7 nnns |
| 773 | 1 | 8 | |g volume:24 |g year:2023 |g number:8 |g day:14 |g month:11 |
| 856 | 4 | 0 | |u https://dx.doi.org/10.1208/s12249-023-02681-x |z lizenzpflichtig |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_SPRINGER | ||
| 951 | |a AR | ||
| 952 | |d 24 |j 2023 |e 8 |b 14 |c 11 | ||