Effective use of transdermal drug delivery in children

Delgado‐Charro, M. Begoña; Guy, Richard H.

doi:10.1016/j.addr.2013.11.014

Cited by 86 publications

(61 citation statements)

References 197 publications

(301 reference statements)

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Section: In Vitro Evaluation Of the Skin Permeation Of Drugsmentioning

confidence: 64%

“…Studies examining the thickness of various skin layers have shown that pig ear skin has a thickness similar to that of human skin (stratum corneum and epidermis). The follicular structure, vascular anatomy, and arrangement of collagen fibers in the dermis of the pig ear, as well as the content of glycosphingolipids and ceramides, are also similar to those of the human skin (Nair et al, 1997;Zorin, Kuylenstierna, Thulin, 1999;Heard et al, 2006;Klang et al, 2012;Chen, Han, Lian, 2013;Delgado-Charro, Guy, 2014).Skin permeation studies using inadequate protocols generate inaccurate data (Godin, Touitou, 2007). Thus, selection of the protocol must be performed by using experimental conditions, such as skin model, experimental apparatus, and receptor medium, appropriate for the formulation to be evaluated, and it must be based on the physicochemical properties of the drug, including aqueous solubility and oil-water partition coefficients.…”

mentioning

confidence: 65%

“…The ideal physicochemical properties of a drug selected for cutaneous administration are low molecular weight (<600 Da) because the diffusion coefficient will be high; solubility in water and oils to achieve a high concentration gradient and increase the diffusion force across the skin; an elevated but balanced partition coefficient because very high partition coefficients may inhibit drug clearance from the skin and increase drug retention; and a low melting point (<200 ºC), which is related to an appropriate solubility Moser et al, 2001;Farahmand, Maibach, 2009;Williams, Barry, 2012;Delgado-Charro, Guy, 2014).…”

Section: Drug Transport Across the Skinmentioning

confidence: 99%

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Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

209

135

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The skin barrier function has been attributed to the stratum corneum and represents a major challenge in clinical practice pertaining to cutaneous administration of drugs. Despite this, a large number of bioactive compounds have been successfully administered via cutaneous administration because of advances in the design of topical and transdermal formulations. In vitro and in vivo evaluations of these novel drug delivery systems are necessary to characterize their quality and efficacy. This review covers the most well-known methods for assessing the cutaneous absorption of drugs as an auxiliary tool for pharmaceutical formulation scientists in the design of drug delivery systems. In vitro methods as skin permeation assays using Franz-type diffusion cells, cutaneous retention and tape-stripping methods to study the cutaneous penetration of drugs, and in vivo evaluations as pre-clinical pharmacokinetic studies in animal models are discussed. Alternative approaches to cutaneous microdialysis are also covered. Recent advances in research on skin absorption of drugs and the effect of skin absorption enhancers, as investigated using confocal laser scanning microscopy, Raman confocal microscopy, and attenuated total reflectance Fourier-transform infrared spectroscopy, are reviewed. Uniterms:Skin absorption/effects/study. Skin absorption/topical formulations. Skin absorption/ transdermal formulations. Skin absorptions/enhancers. INTRODUCTIONTopical and transdermal drug delivery systems have shown significant advantages in clinical practice for drug targeting to the action site in the body; this has reduced the systemic side effects. The administration of drugs by through the skin is also performed to achieve controlled or prolonged drug delivery, and this route can be explored as an alternative to the oral route. The oral route shows some limitations for drugs with irregular absorption in the gastrointestinal tract and low bioavailability and for drugs with increased first pass metabolism and short plasma halflife times (Barry, 2001;Wokovich et al., 2006;Prausnitz, Langer, 2009;Alexander et al., 2012).Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected. This is the case for topical formulations for treatment of skin disorders such as acne and cutaneous inflammatory diseases that include dermatitis, erythematous lupus, and psoriasis. On the other hand, transdermal formulations release drugs that permeate through the skin and enter the systemic circulation. Transdermal therapy must ensure that significant concentrations of the drug are absorbed to reach effective plasma concentrations. Permeation of drugs is targeted in some cases to body regions close to the action site, where a regional effect is expected, e.g., in the muscles, blood vessels, and articulations. In this way, the term "cutaneous absorption" is properly used to characterize the sum of the amounts of drug that penetrate and permeate the skin (Barry, 2001;El Maghraby, Barry;Willi...

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Section: In Vitro Evaluation Of the Skin Permeation Of Drugsmentioning

confidence: 64%

mentioning

confidence: 65%

Section: Drug Transport Across the Skinmentioning

confidence: 99%

See 1 more Smart Citation

Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

209

135

View full text Add to dashboard Cite

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“…In another study, time to reach C max ranged from 18 to 66 h in children after patch application (25 lg/h) [104]. Transdermal pharmacokinetics is similar to those in adults [105][106][107].…”

Section: Transdermal Fentanylmentioning

confidence: 85%

Correction to: Pharmacokinetics of Fentanyl and Its Derivatives in Children: A Comprehensive Review

et al. 2017

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Fentanyl and its derivatives sufentanil, alfentanil, and remifentanil are potent opioids. A comprehensive review of the use of fentanyl and its derivatives in the pediatric population was performed using the National Library of Medicine PubMed. Studies were included if they contained original pharmacokinetic parameters or models using established routes of administration in patients younger than 18 years of age. Of 372 retrieved articles, 44 eligible pharmacokinetic studies contained data of 821 patients younger than 18 years of age, including more than 46 preterm infants, 64 full-term neonates, 115 infants/toddlers, 188 children, and 28 adolescents. Underlying diagnoses included congenital heart and pulmonary disease and abdominal disorders. Routes of drug administration were intravenous, epidural, oral-transmucosal, intranasal, and transdermal. Despite extensive use in daily clinical practice, few studies have been performed. Preterm and term infants have lower clearance and protein binding. Pharmacokinetics was not altered by chronic renal or hepatic disease. Analyses of the pooled individual patients' data revealed that clearance maturation relating to body weight could be best described by the Hill function for sufentanil (R 2 = 0.71, B max 876 mL/min, K 50 16.3 kg) and alfentanil (R 2 = 0.70, B max (fixed) 420 mL/min, K 50 28 kg). The allometric exponent for estimation of clearance of sufentanil was 0.99 and 0.75 for alfentanil clearance. Maturation of remifentanil clearance was described by linear regression to bodyweight (R 2 = 0.69). The allometric exponent for estimation of remifentanil clearance was 0.76. For fentanyl, linear regression showed only a weak correlation between clearance and bodyweight in preterm and term neonates (R 2 = 0.22) owing to a lack of data in older age groups. A large heterogeneity regarding study design, clinical setting, drug administration, laboratory assays, and pharmacokinetic estimation was observed between studies introducing bias into the analyses performed in this review. A limitation of this review is that pharmacokinetic data, based on different modes of administration, dosing schemes, and parameter estimation methods, were combined.The online version of the original article can be found under

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“…Dermal and transdermal delivery systems have proven to be effective in reducing dose frequency, long duration of activity, achieving target delivery, easily administrating and avoiding hepatic first pass metabolism. [1][2][3][4] The stratum corneum, or horny layer, is the outermost layer of the skin and has been identified as the main barrier of the most drug permeation. Various strategies have been employed in attempts to improve the efficacy of topical delivery of drugs, including iontophoresis, electroporation, occlusion and ultrasound.…”

Section: Introductionmentioning

confidence: 99%