Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations
Background: Tocopherol acetate (TA) is known as a skin moisturizing and photoprotective agent. One major drawback with tocopherol and its derivatives remains its limited stability. Aim: To develop highly stable TA-containing ethosomal gel (TAEG) as an advanced dosage form. Methods: A cold method tec...
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| Format: | Article |
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MDPI AG
2022-05-01
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| Series: | Gels |
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| Online Access: | https://www.mdpi.com/2310-2861/8/6/335 |
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| author | Naheed Akhtar Naveed Akhtar Farid Menaa Walaa Alharbi Fatima Saad Salem Alaryani Ali Musfer Alqahtani Faizan Ahmad |
| author_facet | Naheed Akhtar Naveed Akhtar Farid Menaa Walaa Alharbi Fatima Saad Salem Alaryani Ali Musfer Alqahtani Faizan Ahmad |
| author_sort | Naheed Akhtar |
| collection | DOAJ |
| description | Background: Tocopherol acetate (TA) is known as a skin moisturizing and photoprotective agent. One major drawback with tocopherol and its derivatives remains its limited stability. Aim: To develop highly stable TA-containing ethosomal gel (TAEG) as an advanced dosage form. Methods: A cold method technique was used to produce the ethosomes. An in vitro evaluation of viscosity, conductivity, and pH stability was carried out for three months. An in vitro physical characterization of the nanoparticles (NPs) that included particle size (PS), zeta potential (ZP), transmission electron microscopy (TEM), and Fourier-transform infrared (FTIR) spectroscopy analysis was then performed. Organoleptic evaluation, thermostability at 8 °C, 25 °C, 40 °C and 40 °C ± 75% RH, pH, conductivity, viscosity, and spreadability measurements were also performed in vitro for three months. An ex vivo permeation study was performed in phosphate-buffered solution (1× PBS; pH 5.5 or pH 7.4) at 37 ± 0.2 °C by using rat abdominal skin and the Franz diffusion cell method. The data of three independent experiments were expressed as mean ± SD. A two-way ANOVA was applied to compare data on TAEG versus TA control gel (TACG). Results: PS of the ethosomes was in the range of 144–289 nm. A total of nine formulations were developed. Optimized TAEG formulation (TA-5) was selected based on the highest entrapment efficiency (EE) of 99.71%, while the stability, the PS, and the uniformity-based polydispersity index (PDI) were also among the best. TA-5 exhibited smooth spherical ethosomal NPs with PS of 200.6 nm, ZP value of −18.6 V, and PDI of 0.465. Stability data obtained for TA-5 in terms of rheology, conductivity, and pH presented no significant change (<i>p</i> > 0.05) during the entire study duration. Rheological studies indicated that TA-5 followed a non-Newtonian behavior of shear thinning system. The ex vivo drug permeation was 44.55 ± 0.01% in TA-5 and the drug retention in skin was 51.20%, which was significantly higher than TACG as observed after 24 h permeation study (<i>p</i> < 0.05). Conclusions: The newly developed TAEG formulation appears promising to enhance the effectivity of TA and its topical application. |
| first_indexed | 2024-03-09T23:45:01Z |
| format | Article |
| id | doaj.art-abc2e78420bd47ddb82ac7e3422fd550 |
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| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-09T23:45:01Z |
| publishDate | 2022-05-01 |
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| record_format | Article |
| series | Gels |
| spelling | doaj.art-abc2e78420bd47ddb82ac7e3422fd5502023-11-23T16:45:10ZengMDPI AGGels2310-28612022-05-018633510.3390/gels8060335Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo CharacterizationsNaheed Akhtar0Naveed Akhtar1Farid Menaa2Walaa Alharbi3Fatima Saad Salem Alaryani4Ali Musfer Alqahtani5Faizan Ahmad6Department of Pharmacy, Islamia University of Bahawalpur, Bahawalpur 63100, PakistanDepartment of Pharmacy, Islamia University of Bahawalpur, Bahawalpur 63100, PakistanDepartment of Nanomedicine, California Innovations Corporation, San Diego, CA 92037, USADepartment of Chemistry, Science and Arts College, King Abdulaziz University, Rabigh Campus, Jeddah 21911, Saudi ArabiaDepartment of Biology, College of Science, University of Jeddah, Jeddah 21959, Saudi ArabiaDepartment of Pharmacology, College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Saudi ArabiaDepartment of Pharmacy, Bahawalpur Medical and Dental College (BMDC), Bahawalpur 63100, PakistanBackground: Tocopherol acetate (TA) is known as a skin moisturizing and photoprotective agent. One major drawback with tocopherol and its derivatives remains its limited stability. Aim: To develop highly stable TA-containing ethosomal gel (TAEG) as an advanced dosage form. Methods: A cold method technique was used to produce the ethosomes. An in vitro evaluation of viscosity, conductivity, and pH stability was carried out for three months. An in vitro physical characterization of the nanoparticles (NPs) that included particle size (PS), zeta potential (ZP), transmission electron microscopy (TEM), and Fourier-transform infrared (FTIR) spectroscopy analysis was then performed. Organoleptic evaluation, thermostability at 8 °C, 25 °C, 40 °C and 40 °C ± 75% RH, pH, conductivity, viscosity, and spreadability measurements were also performed in vitro for three months. An ex vivo permeation study was performed in phosphate-buffered solution (1× PBS; pH 5.5 or pH 7.4) at 37 ± 0.2 °C by using rat abdominal skin and the Franz diffusion cell method. The data of three independent experiments were expressed as mean ± SD. A two-way ANOVA was applied to compare data on TAEG versus TA control gel (TACG). Results: PS of the ethosomes was in the range of 144–289 nm. A total of nine formulations were developed. Optimized TAEG formulation (TA-5) was selected based on the highest entrapment efficiency (EE) of 99.71%, while the stability, the PS, and the uniformity-based polydispersity index (PDI) were also among the best. TA-5 exhibited smooth spherical ethosomal NPs with PS of 200.6 nm, ZP value of −18.6 V, and PDI of 0.465. Stability data obtained for TA-5 in terms of rheology, conductivity, and pH presented no significant change (<i>p</i> > 0.05) during the entire study duration. Rheological studies indicated that TA-5 followed a non-Newtonian behavior of shear thinning system. The ex vivo drug permeation was 44.55 ± 0.01% in TA-5 and the drug retention in skin was 51.20%, which was significantly higher than TACG as observed after 24 h permeation study (<i>p</i> < 0.05). Conclusions: The newly developed TAEG formulation appears promising to enhance the effectivity of TA and its topical application.https://www.mdpi.com/2310-2861/8/6/335tocopherol acetateethosomesgel formulationpermeation studiesdrug deliverycosmetics |
| spellingShingle | Naheed Akhtar Naveed Akhtar Farid Menaa Walaa Alharbi Fatima Saad Salem Alaryani Ali Musfer Alqahtani Faizan Ahmad Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations Gels tocopherol acetate ethosomes gel formulation permeation studies drug delivery cosmetics |
| title | Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations |
| title_full | Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations |
| title_fullStr | Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations |
| title_full_unstemmed | Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations |
| title_short | Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations |
| title_sort | fabrication of ethosomes containing tocopherol acetate to enhance transdermal permeation in vitro and ex vivo characterizations |
| topic | tocopherol acetate ethosomes gel formulation permeation studies drug delivery cosmetics |
| url | https://www.mdpi.com/2310-2861/8/6/335 |
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