Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid
Sinapic acid (SA) is a bioactive phenolic acid; its diverse properties are its anti-inflammatory, antioxidant, anticancer, and antibacterial activities. The bioactive compound SA is poorly soluble in water. Our goal was to formulate SA-transethosomes using thin-film hydration. The prepared formulati...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
MDPI AG
2023-09-01
|
Series: | Pharmaceutics |
Subjects: | |
Online Access: | https://www.mdpi.com/1999-4923/15/10/2391 |
_version_ | 1797572564926595072 |
---|---|
author | Yousef A. Bin Jardan Abdul Ahad Mohammad Raish Fahad I. Al-Jenoobi |
author_facet | Yousef A. Bin Jardan Abdul Ahad Mohammad Raish Fahad I. Al-Jenoobi |
author_sort | Yousef A. Bin Jardan |
collection | DOAJ |
description | Sinapic acid (SA) is a bioactive phenolic acid; its diverse properties are its anti-inflammatory, antioxidant, anticancer, and antibacterial activities. The bioactive compound SA is poorly soluble in water. Our goal was to formulate SA-transethosomes using thin-film hydration. The prepared formulations were examined for various parameters. In addition, the optimized formulation was evaluated for surface morphology, in-vitro penetration studies across the Strat M<sup>®</sup>, and its antioxidant activity. The optimized formulation (F5) exhibited 74.36% entrapment efficacy. The vesicle size, zeta potential, and polydispersity index were found to be 111.67 nm, −7.253 mV, and 0.240, respectively. The surface morphology showed smooth and spherical vesicles of SA-transethosomes. In addition, the prepared SA-transethosomes exhibited enhanced antioxidant activity. The SA-transethosomes demonstrated considerably greater penetration across the Strat M<sup>®</sup> membrane during the study. The flux of SA and SA-transethosomes through the Strat M<sup>®</sup> membrane was 1.03 ± 0.07 µg/cm<sup>2</sup>/h and 2.93 ± 0.16 µg/cm<sup>2</sup>/h. The enhancement ratio of SA-transethosomes was 2.86 ± 0.35 compared to the control. The SA-transethosomes are flexible nano-sized vesicles and are able to penetrate the entrapped drug in a higher concentration. Hence, it was concluded that SA-transethosome-based approaches have the potential to be useful for accentuating the penetrability of SA across the skin. |
first_indexed | 2024-03-10T20:58:41Z |
format | Article |
id | doaj.art-63deae04d67c48d294b2a94e136f1fc7 |
institution | Directory Open Access Journal |
issn | 1999-4923 |
language | English |
last_indexed | 2024-03-10T20:58:41Z |
publishDate | 2023-09-01 |
publisher | MDPI AG |
record_format | Article |
series | Pharmaceutics |
spelling | doaj.art-63deae04d67c48d294b2a94e136f1fc72023-11-19T17:43:51ZengMDPI AGPharmaceutics1999-49232023-09-011510239110.3390/pharmaceutics15102391Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic AcidYousef A. Bin Jardan0Abdul Ahad1Mohammad Raish2Fahad I. Al-Jenoobi3Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaSinapic acid (SA) is a bioactive phenolic acid; its diverse properties are its anti-inflammatory, antioxidant, anticancer, and antibacterial activities. The bioactive compound SA is poorly soluble in water. Our goal was to formulate SA-transethosomes using thin-film hydration. The prepared formulations were examined for various parameters. In addition, the optimized formulation was evaluated for surface morphology, in-vitro penetration studies across the Strat M<sup>®</sup>, and its antioxidant activity. The optimized formulation (F5) exhibited 74.36% entrapment efficacy. The vesicle size, zeta potential, and polydispersity index were found to be 111.67 nm, −7.253 mV, and 0.240, respectively. The surface morphology showed smooth and spherical vesicles of SA-transethosomes. In addition, the prepared SA-transethosomes exhibited enhanced antioxidant activity. The SA-transethosomes demonstrated considerably greater penetration across the Strat M<sup>®</sup> membrane during the study. The flux of SA and SA-transethosomes through the Strat M<sup>®</sup> membrane was 1.03 ± 0.07 µg/cm<sup>2</sup>/h and 2.93 ± 0.16 µg/cm<sup>2</sup>/h. The enhancement ratio of SA-transethosomes was 2.86 ± 0.35 compared to the control. The SA-transethosomes are flexible nano-sized vesicles and are able to penetrate the entrapped drug in a higher concentration. Hence, it was concluded that SA-transethosome-based approaches have the potential to be useful for accentuating the penetrability of SA across the skin.https://www.mdpi.com/1999-4923/15/10/2391stratum corneumlipid-based vesiclesultra-deformable vesiclesdermal/transdermal |
spellingShingle | Yousef A. Bin Jardan Abdul Ahad Mohammad Raish Fahad I. Al-Jenoobi Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid Pharmaceutics stratum corneum lipid-based vesicles ultra-deformable vesicles dermal/transdermal |
title | Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid |
title_full | Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid |
title_fullStr | Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid |
title_full_unstemmed | Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid |
title_short | Preparation and Characterization of Transethosome Formulation for the Enhanced Delivery of Sinapic Acid |
title_sort | preparation and characterization of transethosome formulation for the enhanced delivery of sinapic acid |
topic | stratum corneum lipid-based vesicles ultra-deformable vesicles dermal/transdermal |
url | https://www.mdpi.com/1999-4923/15/10/2391 |
work_keys_str_mv | AT yousefabinjardan preparationandcharacterizationoftransethosomeformulationfortheenhanceddeliveryofsinapicacid AT abdulahad preparationandcharacterizationoftransethosomeformulationfortheenhanceddeliveryofsinapicacid AT mohammadraish preparationandcharacterizationoftransethosomeformulationfortheenhanceddeliveryofsinapicacid AT fahadialjenoobi preparationandcharacterizationoftransethosomeformulationfortheenhanceddeliveryofsinapicacid |