Delivery of drugs applied topically to the skin

Leite-Silva, Vânia Rodrigues; Almeida, Mariana Mandelli de; Fradin, Aurélie; Grice, Jeffrey E.; Roberts, Michael S.

doi:10.1586/edm.12.32

Cited by 56 publications

(41 citation statements)

References 155 publications

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“…Otherwise, the other concentrations had a high viscosity, which can affect snakehead fish powder penetration into skin cell membrane. This is in line with Leite-Silva et al (2012) stated that the viscosity of a formulation can affect the permeation of active compounds into the skin which is directly related to the concentration of the a material's viscosity.…”

Section: Optimization Of Gel Basissupporting

confidence: 86%

Formulation, optimization, and characterization of snakehead fish (Ophiocephalus Striatus) powder nanoemulgel

Tungadi

Wicita

2020

Braz. J. Pharm. Sci.

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The aim of the present study was to characterize and evaluate nanoemulgel of snakehead fish powder (SFP) for the poorly water-soluble drug. SFP was formulated into nanoemulsion utilizing the best comparison of surfactant, co-surfactant, and oil. Diverse nanoemulsion components (oil, surfactant, and co-surfactant) were chosen based on solvency and emulsification capacity. SFP 0.1% loaded nanoemulsion which tested by stress-stability testing which carried out for all formulations and those that passed these tests were characterized for droplet size, polydispersity index (PDI), zeta potential, pH, viscosity, and transmittance. After that, nanoemulsion was added with 1.5%, 2.0%, and 2.5% of HPMC in different concentrations and mixed until nanoemulgel form and evaluated for pH, viscosity, spreadability, and extrudability measurement. The results of this research showed that SF nanoemulsion produced clear, stable, and transparent formula having the transmittance value 99.87%. Mean droplet size and zeta potential of the optimized nanoemulsion (NE4) were found to be 98.6±0.93 nm (PDI 0.1±0.20) and -57.5±0.3 MV respectively. Meanwhile, the evaluation results of nanoemulgel (NEG) showed NEG 1.5 gave pH 6.0, viscosity 210 cP, spreadability 5.8 g cm/s and extrudability 1.4 g/cm 2 . Otherwise, NEG 2.0 and NEG 2.5 had high viscosity and pH generating low spreading on the skin i.e. 3.9 g cm/s and 2.8 g cm/s respectively. The results of the evaluation and preparation stability test showed a good level of stability of NEG 1.5 with the viscosity and pH by one way ANOVA which did not change significantly.

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Section: Optimization Of Gel Basissupporting

confidence: 86%

Formulation, optimization, and characterization of snakehead fish (Ophiocephalus Striatus) powder nanoemulgel

Tungadi

Wicita

2020

Braz. J. Pharm. Sci.

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“…Both for the hydrogels with HEC and HPMC, penetration depths were reduced as the viscosity of the gels increased. The diffusion of the model drug out of the formulation and into the skin might have been hindered by the high viscosity of the systems and thus resulted in a limited total penetration depth . In conclusion, drug distribution within the skin appeared to be affected by the viscosity of the vehicle.…”

Section: Discussionmentioning

confidence: 90%

The role of viscosity on skin penetration from cellulose ether‐based hydrogels

Binder

Mazál

Petz

et al. 2019

Skin Research and Technology

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BackgroundThe rheological properties of dermal drug delivery systems are of importance when designing new formulations. Viscosity not only affects features such as spreadability and skin feel, but may also affect the skin penetration of incorporated actives. Data on the latter aspect are controversial. Our objective was to elucidate the relation between viscosity and drug delivery performance of different model hydrogels assuming that enhanced microviscosity might delay drug release and penetration.Materials and MethodsHydrogels covering a broad viscosity range were prepared by adding either HPMC or HEC as gelling agents in different concentrations. To investigate the ability of the gels to deliver a model drug into the skin, sulphadiazine sodium was incorporated and its in vitro skin penetration was monitored using tape stripping/HPLC analysis and non‐invasive confocal Raman spectroscopy.ResultsThe trends observed with the two different experimental setups were comparable. Drug penetration depths decreased slightly with increasing viscosity, suggesting slower drug release due to the increasingly dense gel networks. However, the total penetrated drug amounts were independent of the exact formulation viscosity.ConclusionDrug penetration was largely unaffected by hydrogel viscosity. Moderately enhanced viscosity is advisable when designing cellulose ether hydrogels to allow for convenient application.

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“…From a drug delivery perspective, the penetration of the stratum corneum (SC) is extremely challenging for such hydrophilic macromolecules . Despite the increasing number of advanced delivery systems, including solid particles, liposomes, microneedles and conjugates, the delivery of biologics through the SC remains a largely unresolved challenge . Furthermore, rosacea patients frequently apply moisturizing creams to relieve symptoms, which means that topical applications have to be considered as a combination therapy with formulations containing a vast array of skin modifying agents .…”

Section: Introductionmentioning

confidence: 99%

Exploring the potential for rosacea therapeutics of siRNA dispersion in topical emulsions

Colombo¹,

Harmankaya

Water³

et al. 2019

Experimental Dermatology

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Rosacea is a prevalent skin condition dependent on the individual genetic profile. The current pharmacological management of this condition is mostly based on small molecule drugs predominately effective in ameliorating the inflammatory condition. Emerging molecular approaches could present an opportunity for managing rosacea conditions at transcriptomic level, and in the future allow personalized approaches. RNA medicines, such as small RNA interference (siRNA), could provide a flexible and applicable tool reaching this aim. However, the topical siRNA delivery by dermatological emulsions, commonly used in the daily management of rosacea, is still largely unexplored. Consequently, RNA interference application to rosacea was defined on molecular bases by genetic expression meta‐data analysis. Based on this, a siRNA directed against TLR2 was designed and validated in vitro on murine macrophages and fibroblasts. Next, siRNA was dispersed in the continuous phase of emulsions and was characterized for commonly used dermatologic bases. Finally, the potential delivery performance of the topical emulsions was tested in vivo on healthy Balb/c mice. It was found that the interaction of siRNA with combination of excipients, such as urea and glycerol, is likely to favour the siRNA delivery, inducing genetic silencing of TLR2. These findings provide a foundation for the future development of topical RNA‐based dispersions for topical molecular medicines, by emphasizing on the formulation and therapeutic‐based opportunities with dermatological treatments.

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Delivery of drugs applied topically to the skin

Cited by 56 publications

References 155 publications

Formulation, optimization, and characterization of snakehead fish (Ophiocephalus Striatus) powder nanoemulgel

Formulation, optimization, and characterization of snakehead fish (Ophiocephalus Striatus) powder nanoemulgel

The role of viscosity on skin penetration from cellulose ether‐based hydrogels

Exploring the potential for rosacea therapeutics of siRNA dispersion in topical emulsions

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