Evaluation of the biocompatibility and skin hydration potential of vitamin E-loaded lipid nanosystems formulations: In vitro and human in vivo studies

Vaz, Sara; Silva, R.; Amaral, Maria Helena; Gil-Martins, Eva; Lobo, José Manuel Sousa; Silva, Ana Catarina

doi:10.1016/j.colsurfb.2019.03.036

Cited by 40 publications

(27 citation statements)

References 36 publications

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“…Consequently, stearic acid in its undissolved state, possibly provides a residual layer on the skin surface that enables improved occlusivity [ 26 , 97 ]. Occlusion, which is also established via the increased viscosity of a formulation, decreases transepidermal water loss and thus enhances swelling of the SC, which sequentially disrupts the strictly packed lipid structure of the SC rendering improved drug diffusion [ 98 , 99 ].…”

Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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“…Commercially, vitamin E is available mainly as alpha-tocopherol [9,10] or tocopheryl acetate [11][12][13] which are used above all to oral [14,15] and skin [10,12,16] applications, respectively. Among vitamin E derivatives are tocopheryl acetate, tocopheryl glucoside and tocopheryl phosphate.…”

Section: Vitamin E Isoforms and Derivativesmentioning

confidence: 99%

Vitamin E and Derivatives in Skin Health Promotion

Santos¹,

Tavares²,

Barradas³

2021

Biochemistry

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Vitamin E is fundamental for a proper function of human cells. Mostly obtained from vegetable oils, it has antioxidant and non-antioxidant actions. At times, its oral intake or skin application are employed. Oral intake is recommended in some cases. Differently, the topical application is a part of daily skin routine. Both in oral or in topical formulations, it is employed in its isoforms or derivatives. Tocopherols and tocotrienols are isoforms while derivatives are synthetic forms. In pharmaceutical and cosmetic formulations, vitamin E and its derivatives are widely used due to its antioxidant and photoprotective properties. However, the clinical success treatment is often impaired by its low skin penetration, high lipophilicity, and chemical instability. A rational formulation design in the development of novel vitamin E dosage forms is required. In this chapter, the most successful and innovative approaches towards Vitamin E and its derivatives loaded in formulations for skin health promotion are reviewed. Conventional and nanoparticle-based formulations enable vitamin E chemical stabilization, and they are suitable vehicles for its release on the skin. Further, nano-sized carriers can increase vitamin E content in formulations as well as favor its skin penetration.

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“…The interfacial tension between the lipophilic and hydrophobic components of SEDDSs are reduced by surfactants. They create an interfacial film between the two immiscible phases for the purpose of generating a dispersion [3][4][5][6][7][8]72]. During formulation of SEDDSs, higher emulsification properties are achieved by including surfactants with HLB values exceeding a value of 12.…”

Section: Surfactantsmentioning

confidence: 99%

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

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Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected.

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Evaluation of the biocompatibility and skin hydration potential of vitamin E-loaded lipid nanosystems formulations: In vitro and human in vivo studies

Cited by 40 publications

References 36 publications

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Vitamin E and Derivatives in Skin Health Promotion

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

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