Towards nanoformulations for skin delivery of poorly soluble API: What does indeed matter?

Apolinário, Alexsandra Conceição; Hauschke, Leon; Nunes, Jessica Ribeiro; Lopes, Luciana B.

doi:10.1016/j.jddst.2020.102045

Cited by 15 publications

(14 citation statements)

References 48 publications

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“…Ethosomes are hydroalcoholic preparations enabling encapsulation of both hydrophilic and hydrophobic drugs [ 27 ]. Ethosomes can entrap high amount of drugs, including insoluble or poorly water-soluble compounds, due to their high EE, which is an asset for controlled drug delivery [ 37 ].…”

Section: Resultsmentioning

confidence: 99%

Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations

Akhtar

Menaa

et al. 2022

Gels

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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 (p > 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 (p < 0.05). Conclusions: The newly developed TAEG formulation appears promising to enhance the effectivity of TA and its topical application.

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Section: Resultsmentioning

confidence: 99%

Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations

Akhtar

Menaa

et al. 2022

Gels

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“…Ethosomal system has many advantage as it has solved the instability issues of highly light sensitive drugs and rapid degradation issues of these compounds. Poorly water‐soluble drugs and water insoluble drugs can be incorporated into ethosomes for controlled drug delivery 19 …”

Section: Resultsmentioning

confidence: 99%

Development of stable tocopherol succinate‐loaded ethosomes to enhance transdermal permeation: In vitro and in vivo characterizations

Akhtar

2022

J of Cosmetic Dermatology

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Background Tocopherol succinate (TS) represents synthetic derivative of α‐tocopherol (vitamin E), it act as anti‐aging, moisturizing, and antioxidant. Ultraviolet (UV) photo stability of TS is low, and it cause skin irritation. Aim To develop tocopherol succinate loaded ethosomal gel for topical TS delivery and to evaluate its moisturizing and anti‐aging effects. Method Cold method technique was used to produce ethosomal formulations (N = 9) by varying ethanol and lipid concentrations (F1–F9). The most optimized formulation (F5) was selected for further study on the basis of characterization. F5 Formulation was incorporated into gel. Ex vivo permeation study was done by using Franz diffusion cell. Non‐invasive in vivo study was performed using corneometer for the evaluation of skin moisture content and skin mechanical properties by using cutometer, for 12 weeks on human subjects (N = 13). Results Particle size (PS), zeta potential (ZP) and polydispersity index (PDI), Entrapment efficiency were found to be 179.1 nm, −13.7 mV and 0.345, and 99.71%, respectively. Transmission electron microscopy (TEM) depicted spherical ethosomal particles. Ethosomal gel and control gel were evaluated for conductivity and pH. Rheological analysis revealed a non‐Newtonian flow. The release profile showed initial burst and then, sustained release, release data followed Korsmeyer–Peppas model. TS‐loaded ethosomal gel appeared physically stable and showed significant results in terms of skin capacitance and mechanical properties. Conclusion The prepared ethosomal gel formulation containing TS is more stable with enhanced antioxidant, moisturizing properties, and increased TS deposition into the skin layer.

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“…Tween 80 is employed in the ethosomal system at concentrations ranging from 10% to 50% of total phospholipid content and showed a potential to minimize vesicular size and improve system stability and skin-permeation qualities in ethosomal systems. Tween 80's effects on the ethosomal system are mostly related to its solubilizing characteristic and ability to prevent vesicle fusion (20,54,60). In a similar pattern, oleic acid modulates vesicular size, elasticity, zeta potential, and skin permeability via enhancing the fluidity of the stratum corneum.…”

Section: Other Components Of Ethosomal Systemmentioning

confidence: 99%

Ethosomes: a potential nanocarrier for transdermal drug delivery‏

Abubakr

Ibrahem

salah

2023

ERU Research Journal

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Ethosomal system is a lipid vesicular nanocarrier that holds a high concentration of alcohols. This nanocarrier is optimized for the dermal and transdermal delivery of medicinal drugs with various physicochemical features. Since its release in 1996, ethosomes have been subjected to subsequent studies to modify the original formula via the addition of different components, leading to the development of novel ethosomal system types. These new carriers are prepared via a variety of methods and characterized through different parameters, including vesicular size, zeta potential, entrapment efficiency, and skin permeation. The ethosomes efficacy in dermal/transdermal administration is evaluated via clinical studies as well as a wide range of in vivo models.Ethosomal dispersions are frequently incorporated into topical preparations, including gels, patches, and lotions, due to their stability and convenience. This article provides a thorough overview of ethosomal systems from the standpoint of ethosomal types, beginning with classical ethosomes and progressing to binary ethosomes and transethosomes. In addition, this work provides a comprehensive overview of the components of the ethosomal system and their contribution to the final properties of ethosomes, besides highlighting the different methods of preparation and the common dosage forms used as ethosomes' vehicles.

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Towards nanoformulations for skin delivery of poorly soluble API: What does indeed matter?

Cited by 15 publications

References 48 publications

Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations

Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations

Development of stable tocopherol succinate‐loaded ethosomes to enhance transdermal permeation: In vitro and in vivo characterizations

Ethosomes: a potential nanocarrier for transdermal drug delivery‏

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