Ternary Deep Eutectic Solvents System of Colchicine, 4-Hydroxyacetophenone, and Protocatechuic Acid and Characterization of Transdermal Enhancement Mechanism
© 2023. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists..
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/cm2, 117.67 ± 7.73 µg/cm2, and 56.79 ± 1.30 µg/cm2 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., Seite 229 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Piao, Huiqing [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 16.11.2023 Date Revised 29.12.2023 published: Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1208/s12249-023-02681-x |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM364557133 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM364557133 | ||
| 003 | DE-627 | ||
| 005 | 20240108140215.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231226s2023 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1208/s12249-023-02681-x |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1243.xml |
| 035 | |a (DE-627)NLM364557133 | ||
| 035 | |a (NLM)37964102 | ||
| 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 ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 16.11.2023 | ||
| 500 | |a Date Revised 29.12.2023 | ||
| 500 | |a published: Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2023. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists. | ||
| 520 | |a 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/cm2, 117.67 ± 7.73 µg/cm2, and 56.79 ± 1.30 µg/cm2 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 Journal Article | |
| 650 | 4 | |a colchicine | |
| 650 | 4 | |a deep eutectic solvents | |
| 650 | 4 | |a traditional Chinese medicine | |
| 650 | 4 | |a transdermal patch | |
| 650 | 7 | |a 4-hydroxyacetophenone |2 NLM | |
| 650 | 7 | |a G1L3HT4CMH |2 NLM | |
| 650 | 7 | |a protocatechuic acid |2 NLM | |
| 650 | 7 | |a 36R5QJ8L4B |2 NLM | |
| 650 | 7 | |a Deep Eutectic Solvents |2 NLM | |
| 650 | 7 | |a Colchicine |2 NLM | |
| 650 | 7 | |a SML2Y3J35T |2 NLM | |
| 650 | 7 | |a Rubber |2 NLM | |
| 650 | 7 | |a 9006-04-6 |2 NLM | |
| 700 | 1 | |a Xie, Wanchen |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Shiqi |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Jiaqi |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Chao |e verfasserin |4 aut | |
| 700 | 1 | |a Quan, Peng |e verfasserin |4 aut | |
| 700 | 1 | |a Fang, Liang |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t AAPS PharmSciTech |d 2000 |g 24(2023), 8 vom: 14. Nov., Seite 229 |w (DE-627)NLM126699429 |x 1530-9932 |7 nnns |
| 773 | 1 | 8 | |g volume:24 |g year:2023 |g number:8 |g day:14 |g month:11 |g pages:229 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1208/s12249-023-02681-x |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 24 |j 2023 |e 8 |b 14 |c 11 |h 229 | ||