Development and In Vitro/Ex Vivo Evaluation of Lecithin-Based Deformable Transfersomes and Transfersome-Based Gels for Combined Dermal Delivery of Meloxicam and Dexamethasone

Khan, Muhammad Imran; Yaqoob, Samiya; Madni, Asadullah; Akhtar, Muhammad Furqan; Sohail, Muhammad; Saleem, Ammara; Nawaz, Tahir; Khan, Kashif-ur-Rehman; Qureshi, Omer Salman

doi:10.1155/2022/8170318

Cited by 17 publications

(8 citation statements)

References 86 publications

(99 reference statements)

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“…Moreover, the EE% decreased by increasing the amount of surfactant which may be due to the increase in the solubility of the drug in the aqueous phase by the increasing amount of surfactant [ 36 ]. Other researchers explained the reduction in EE% by increasing the surfactant concentration by the formation of pores in the lipid bilayer membrane which resulted in leakage of the drug [ 37 ]. The previous results were in agreement with Mayangsari et al, who prepared berberine chloride tranferosomes for transdermal use using Tween 80 as a surfactant and found that the EE% was decreased by increasing the surfactant concentration from 15% to 25% [ 38 ].…”

Section: Resultsmentioning

confidence: 99%

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

et al. 2023

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Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier for drug penetration. Therefore, this study aimed to prepare itraconazole as transferosomes (ITZ-TFS) to overcome the barrier function of the skin. ITZ-TFSs were prepared by thin lipid film hydration technique using different surfactants, sodium lauryl sulfate (SLS) and sodium deoxycholate (SDC). The prepared ITZ-TFS were evaluated for entrapment efficiency (EE) %, particle size, polydispersity index (PDI), zeta potential, and in vitro drug release to obtain an optimized formula. The surface morphology of the optimized formula of ITZ-TFS was determined by transmission electron microscope (TEM). The optimized formulation was prepared in the form of gel using hydroxyl propyl methyl cellulose (HPMC) gel base. The prepared ITZ-TFS gel was evaluated for homogeneity, drug content, spreadability, pH, and in vitro antifungal activity in comparison with the free ITZ- gel. The prepared ITZ-TFS formulations exhibited high EE% ranging from 89.02 ± 1.65% to 98.17 ± 1.28% with particle size ranging from 132.6 ± 2.15 nm to 384.1 ± 3.46. The PDI for all ITZ-TFSs was less than 0.5 and had a negative zeta potential. The TEM image for the optimized formulation (ITZ-TFS4) showed spherical vesicles with a smooth surface. The prepared gels had good spreadability, pH, and acceptable drug content. ITZ-TFS gel showed higher antifungal activity than free ITZ gel as determined by zone of inhibition. ITZ was successfully prepared in form of TFSs with higher antifungal activity than the free drug.

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Section: Resultsmentioning

confidence: 99%

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

et al. 2023

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“…Hereinafter, the protein release profile data were fitted into several drug release kinetic models, namely zero-order, first-order, Higuchi, and Korsmeyer-Peppas. The data fitting model was analyzed by Microsoft Excel with DDSolver add-ins (Mazhar et al, 2023;Khan et al, 2022;Zhang et al, 2010), and the coefficient of determination (R 2 ) was used as a goodness-of-fit indicator (Costa and Lobo, 2001).…”

Section: In Vitro Protein Release Assaymentioning

confidence: 99%

Effect of Freeze-Thaw Cycles Method to Transfersome Characteristics for Growth Protein Encapsulation

Khayrani,

Fahmi,

Nurhayati

et al. 2024

IJTech

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Transfersome, a lipid-based nanovesicle, can be a suitable tool to improve the delivery of valuable growth factors. Through transfersome technology, growth factors and active compounds can be transferred transdermally without the need for invasive delivery procedures. In this study, we evaluated the impact of freeze-thaw cycles on transfersome characteristics, particularly particle size, polydispersity, and encapsulation efficiency. Transfersome particles were prepared from dipalmitoylphosphatidylcholine (DPPC) and Tween 80 with a 97.5:2.5 w/w% using thin film hydration at a temperature of 45° -50°C. Then, the transfersome suspension was subjected to repeated freeze-thaw for 1 minute of freezing and 3 minutes of thawing. The protein release from all transfersome samples were evaluated using Bradford assay, while the particle size and polydispersity were determined with a dynamic scattering analyzer. It was found that freeze-thaw increased encapsulation efficiency, particle size, and polydispersity of transfersomes up to 81.63±0.00%, 180.70±0.87 nm, and 0.369±0.02, respectively, from those without freeze-thaw steps (73.35±0.03%, 144.93±0.21 nm and 0.202±0.02). Moreover, freeze-thawed transfersomes exhibited a release of up to 52.80% of loaded protein within 78 hours, in contrast to 37.48% in nonfreeze-thawed transfersomes. This study shows that an additional freeze-thaw step is a promising method to improve the properties of transfersome particles, especially encapsulation efficiency and sustained protein release.

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“…Release studies were performed in triplicate for each sample. In order to study the drug release mechanism, the release data were fitted to zero-order, first-order, Higuchi diffusion and Koresmeyer-Peppas kinetic models, and the correlation coefficient was used as the index of goodness of fit [61,62].…”

Section: In Vitro Drug Release Studymentioning

confidence: 99%

Microemulsion-Based Keratin–Chitosan Gel for Improvement of Skin Permeation/Retention and Activity of Curcumin

Niu

Yuan

Gao

et al. 2023

Gels

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Curcumin (Cur) is a kind of polyphenol with a variety of topical pharmacological properties including antioxidant, analgesic and anti-inflammatory activities. However, its low water solubility and poor skin bioavailability limit its effectiveness. In the current study, we aimed to develop microemulsion-based keratin–chitosan gel for the improvement of the topical activity of Cur. The curcumin-loaded microemulsion (CME) was formulated and then loaded into the keratin–chitosan (KCS) gel to form the CME-KCS gel. The formulated CME-KCS gel was evaluated for its characterization, in vitro release, in vitro skin permeation and in vivo activity. The results showed that the developed CME-KCS gel had an orange-yellow and gel-like appearance. The particle size and zeta potential of the CME-KCS gel were 186.45 ± 0.75 nm and 9.42 ± 0.86 mV, respectively. The CME-KCS gel showed desirable viscoelasticity, spreadability, bioadhesion and controlled drug release, which was suitable for topical application. The in vitro skin permeation and retention study showed that the CME-KCS gel had better in vitro skin penetration than the Cur solution and achieved maximum skin drug retention (3.75 ± 0.24 μg/cm2). In vivo experimental results confirmed that the CME-KCS gel was more effective than curcumin-loaded microemulsion (Cur-ME) in analgesic and anti-inflammatory activities. In addition, the CME-KCS gel did not cause any erythema or edema based on a mice skin irritation test. These findings indicated that the developed CME-KCS gel could improve the skin penetration and retention of Cur and could become a promising formulation for topical delivery to treat local diseases.

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Development and In Vitro/Ex Vivo Evaluation of Lecithin-Based Deformable Transfersomes and Transfersome-Based Gels for Combined Dermal Delivery of Meloxicam and Dexamethasone

Cited by 17 publications

References 86 publications

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

Preparation and Optimization of Itraconazole Transferosomes-Loaded HPMC Hydrogel for Enhancing Its Antifungal Activity: 2^3 Full Factorial Design

Effect of Freeze-Thaw Cycles Method to Transfersome Characteristics for Growth Protein Encapsulation

Microemulsion-Based Keratin–Chitosan Gel for Improvement of Skin Permeation/Retention and Activity of Curcumin

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