Experimental Models in Predicting Topical Antifungal Efficacy: Practical Aspects and Challenges

Lai, Juan; Maibach, Howard I.

doi:10.1159/000235827

Cited by 12 publications

(5 citation statements)

References 102 publications

(58 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Measurement of dermal absorption for the purpose of targeted skin delivery, systemic delivery, or toxicological assessment should be done under the correct conditions, ideally using the gold-standard experimental model: in vivo human skin. 13 However, this is not always possible, due to the high cost of human trials and concerns over applying substances or materials with potentially toxic effects. As well, in vivo responses may be difficult to measure and interpret and subject to significant variability.…”

Section: Models Used To Evaluate Dermal Absorptionmentioning

confidence: 99%

Skin models for the testing of transdermal drugs

Abd¹,

Yousef²,

Pastore³

et al. 2016

CPAA

231

227

View full text Add to dashboard Cite

The assessment of percutaneous permeation of molecules is a key step in the evaluation of dermal or transdermal delivery systems. If the drugs are intended for delivery to humans, the most appropriate setting in which to do the assessment is the in vivo human. However, this may not be possible for ethical, practical, or economic reasons, particularly in the early phases of development. It is thus necessary to find alternative methods using accessible and reproducible surrogates for in vivo human skin. A range of models has been developed, including ex vivo human skin, usually obtained from cadavers or plastic surgery patients, ex vivo animal skin, and artificial or reconstructed skin models. Increasingly, largely driven by regulatory authorities and industry, there is a focus on developing standardized techniques and protocols. With this comes the need to demonstrate that the surrogate models produce results that correlate with those from in vivo human studies and that they can be used to show bioequivalence of different topical products. This review discusses the alternative skin models that have been developed as surrogates for normal and diseased skin and examines the concepts of using model systems for in vitro–in vivo correlation and the demonstration of bioequivalence.

show abstract

Section: Models Used To Evaluate Dermal Absorptionmentioning

confidence: 99%

Skin models for the testing of transdermal drugs

Abd¹,

Yousef²,

Pastore³

et al. 2016

CPAA

231

227

View full text Add to dashboard Cite

show abstract

“…Ex vivo permeation studies using human skin and under suitable conditions are successfully used to predict in vivo behavior of topical formulations [54,55]. The results of this assay revealed that APR-ME could be used as an effective local treatment for skin inflammation since the drug was able to cross the SC and remain retained into the skin (479.35 ± 102.85 µg APR/g skin/cm 2 ) without reaching the receptor compartment.…”

Section: Discussionmentioning

confidence: 99%

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation

et al. 2020

View full text Add to dashboard Cite

Apremilast (APR) is a selective phosphodiesterase 4 inhibitor administered orally in the treatment of moderate-to-severe plaque psoriasis and active psoriatic arthritis. The low solubility and permeability of this drug hinder its dermal administration. The purpose of this study was to design and characterize an apremilast-loaded microemulsion (APR-ME) as topical therapy for local skin inflammation. Its composition was determined using pseudo-ternary diagrams. Physical, chemical and biopharmaceutical characterization were performed. Stability of this formulation was studied for 90 days. Tolerability of APR-ME was evaluated in healthy volunteers while its anti-inflammatory potential was studied using in vitro and in vivo models. A homogeneous formulation with Newtonian behavior and droplets of nanometric size and spherical shape was obtained. APR-ME released the incorporated drug following a first-order kinetic and facilitated drug retention into the skin, ensuring a local effect. Anti-inflammatory potential was observed for its ability to decrease the production of IL-6 and IL-8 in the in vitro model. This effect was confirmed in the in vivo model histologically by reduction in infiltration of inflammatory cells and immunologically by decrease of inflammatory cytokines IL-8, IL-17A and TNFα. Consequently, these results suggest that this formulation could be used as an attractive topical treatment for skin inflammation.

show abstract

“…), application (finite or infinite dose? ), and temperature 50 . In 1989, Aly et al carried out three phases of research for topical antifungal, first by research pig skin and human body skin in side‐by‐side comparison and by demonstrating that cyclopyroxolamine 1 percent, in two separate vehicles, lotion, and cream, similarly penetrated all stratum corneum layers in both skin types and inhibited the growth of T. mentagrophytes and Candida albicans 50,51 …”

Section: Classification Of Methodsmentioning

confidence: 99%

Methods for evaluating penetration of drug into the skin: A review

Supe

Takudage

2020

Skin Research and Technology

122

View full text Add to dashboard Cite

Background Skin being the largest organ of the human body plays a very important role in the permeation and penetration of the drug. In addition, the transdermal drug delivery system (TDDS) plays a major role in managing dermal infections and attaining sustained plasma drug concentration. Thus, evaluation of percutaneous penetration of the drug through the skin is important in developing TDDS for human use. Material and methods Various techniques are used for getting the desired drug penetration, permeation, and absorption through the skin in managing these dermal disorders. The development of novel pharmaceutical dosage forms for dermal use is much explored in the current era. However, it is very important to evaluate these methods to determine the bioequivalence and risk of these topically applied drugs, which ultimately penetrate and are absorbed through the skin. Results Currently, numerous skin permeation models are being developed and persuasively used in studying dermatopharmacokinetic (DPK) profile and various models have been developed, to evaluate the TDD which include ex vivo human skin, ex vivo animal skin, and artificial or reconstructed skin models. Conclusion This review discusses the general physiology of the skin, the physiochemical characteristics affecting particle penetration, understand the models used for human skin permeation studies and understanding their advantages, and disadvantages.

show abstract

Experimental Models in Predicting Topical Antifungal Efficacy: Practical Aspects and Challenges

Cited by 12 publications

References 102 publications

Skin models for the testing of transdermal drugs

Skin models for the testing of transdermal drugs

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation

Methods for evaluating penetration of drug into the skin: A review

Contact Info

Product

Resources

About