Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis

In this study, hesperidin was loaded into a transethosome and was developed employing the rotary evaporator method. The formulation was optimized using the Box–Behnken design (BBD). The optimized HSD-TE formulation has a spherical shape, vesicle size, polydispersity index, entrapment efficiency, and...

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Main Authors: Perwez Alam, Mohd Imran, Samreen Jahan, Ali Akhtar, Zafrul Hasan
Format: Article
Language:English
Published: MDPI AG 2023-10-01
Series:Gels
Subjects:
Online Access:https://www.mdpi.com/2310-2861/9/10/791
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author Perwez Alam
Mohd Imran
Samreen Jahan
Ali Akhtar
Zafrul Hasan
author_facet Perwez Alam
Mohd Imran
Samreen Jahan
Ali Akhtar
Zafrul Hasan
author_sort Perwez Alam
collection DOAJ
description In this study, hesperidin was loaded into a transethosome and was developed employing the rotary evaporator method. The formulation was optimized using the Box–Behnken design (BBD). The optimized HSD-TE formulation has a spherical shape, vesicle size, polydispersity index, entrapment efficiency, and zeta potential within the range of 178.98 nm; the PDI was 0.259 with a zeta potential of −31.14 mV and % EE of 89.51%, respectively. The in vitro drug release shows that HSD-TE exhibited the release of 81.124 ± 3.45% in comparison to HSD suspension. The ex vivo skin permeation showed a 2-fold increase in HSD-TE gel permeation. The antioxidant activity of HSD-TE was found to be 79.20 ± 1.77% higher than that of the HSD solution. The formulation showed 2-fold deeper HSD-TE penetration across excised rat skin membranes in confocal laser microscopy scanning, indicating promising in vivo prospects. In a dermatokinetic study, HSD-TE gel was compared to HSD conventional gel where TE significantly boosted HSD transport in the epidermis and dermal layers. The formulation showed greater efficacy than free HSD in the inhibition of microbial growth, as evidenced by antibacterial activity on the Gram-negative and positive bacteria. These investigations found that the HSD-TE formulation could enhance the topical application in the management of cutaneous bacterial infections.
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spelling doaj.art-904436c4e23f4b27a83bb5bbf8e4faa32023-11-19T16:35:25ZengMDPI AGGels2310-28612023-10-0191079110.3390/gels9100791Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic AnalysisPerwez Alam0Mohd Imran1Samreen Jahan2Ali Akhtar3Zafrul Hasan4Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmacognosy, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Medical Surgical Nursing, College of Nursing, King Saud University, Riyadh 11451, Saudi ArabiaIn this study, hesperidin was loaded into a transethosome and was developed employing the rotary evaporator method. The formulation was optimized using the Box–Behnken design (BBD). The optimized HSD-TE formulation has a spherical shape, vesicle size, polydispersity index, entrapment efficiency, and zeta potential within the range of 178.98 nm; the PDI was 0.259 with a zeta potential of −31.14 mV and % EE of 89.51%, respectively. The in vitro drug release shows that HSD-TE exhibited the release of 81.124 ± 3.45% in comparison to HSD suspension. The ex vivo skin permeation showed a 2-fold increase in HSD-TE gel permeation. The antioxidant activity of HSD-TE was found to be 79.20 ± 1.77% higher than that of the HSD solution. The formulation showed 2-fold deeper HSD-TE penetration across excised rat skin membranes in confocal laser microscopy scanning, indicating promising in vivo prospects. In a dermatokinetic study, HSD-TE gel was compared to HSD conventional gel where TE significantly boosted HSD transport in the epidermis and dermal layers. The formulation showed greater efficacy than free HSD in the inhibition of microbial growth, as evidenced by antibacterial activity on the Gram-negative and positive bacteria. These investigations found that the HSD-TE formulation could enhance the topical application in the management of cutaneous bacterial infections.https://www.mdpi.com/2310-2861/9/10/791hesperidintransethosomepositive bacterianegative bacteriaantimicrobial activitybacterial skin infection
spellingShingle Perwez Alam
Mohd Imran
Samreen Jahan
Ali Akhtar
Zafrul Hasan
Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
Gels
hesperidin
transethosome
positive bacteria
negative bacteria
antimicrobial activity
bacterial skin infection
title Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
title_full Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
title_fullStr Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
title_full_unstemmed Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
title_short Formulation and Characterization of Hesperidin-Loaded Transethosomal Gel for Dermal Delivery to Enhance Antibacterial Activity: Comprehension of In Vitro, Ex Vivo, and Dermatokinetic Analysis
title_sort formulation and characterization of hesperidin loaded transethosomal gel for dermal delivery to enhance antibacterial activity comprehension of in vitro ex vivo and dermatokinetic analysis
topic hesperidin
transethosome
positive bacteria
negative bacteria
antimicrobial activity
bacterial skin infection
url https://www.mdpi.com/2310-2861/9/10/791
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