Novel chemical permeation enhancers for transdermal drug delivery

Chen, Yang; Quan, Peng; Liu, Xiaochang; Wang, Manli; Fang, Liang

doi:10.1016/j.ajps.2014.01.001

Cited by 98 publications

(76 citation statements)

References 72 publications

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“…To improve skin penetrability, physical/chemical enhancers such as electricity, ultrasound, microneedles, dimethyl sulfoxide (DMSO), urea, azone, pyrrolidones, alcohols, oils, and fatty acids are often used. [18,21,40,41] Although effective, concomitant irritation at the site of application and toxicity has impeded clinical utility of chemical penetration enhancers. [40] In this study, we present CAGE as a novel transdermal delivery material that can significantly improve penetration of proteins through the skin.…”

Section: Discussionmentioning

confidence: 99%

“…[18,21,40,41] Although effective, concomitant irritation at the site of application and toxicity has impeded clinical utility of chemical penetration enhancers. [40] In this study, we present CAGE as a novel transdermal delivery material that can significantly improve penetration of proteins through the skin. Specifically, CAGE retains the structure of proteins such as insulin while enhancing its permeability across the skin to significantly reduce blood glucose levels in rats.…”

Section: Discussionmentioning

confidence: 99%

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Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Banerjee

Ibsen

Iwao

et al. 2017

Adv Healthcare Materials

163

155

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Transdermal delivery of peptides and other biological macromolecules is limited due to skin's inherent low permeability. Here, the authors report the use of a deep eutectic solvent, choline and geranate (CAGE), to enhance topical delivery of proteins such as bovine serum albumin (BSA, molecular weight: ≈66 kDa), ovalbumin (OVA, molecular weight: ≈45 kDa) and insulin (INS, molecular weight: 5.8 kDa). CAGE enhances permeation of BSA, OVA, and insulin into porcine skin ex vivo, penetrating deep into the epidermis and dermis. Studies using tritium-labeled BSA and fluorescein isothiocyanate labeled insulin show significantly enhanced delivery of proteins into and across porcine skin, penetrating the skin in a time-dependent manner. Fourier transform IR spectra of porcine stratum corneum (SC) samples before and after incubation in CAGE show a reduction in peak area attributed to SC lipid content, suggesting lipid extraction from the SC. Circular dichroism confirms that CAGE does not affect insulin's secondary conformation. In vivo studies in rats show that topical application of 10 U insulin dispersed in CAGE (25 U kg −1 insulin dose) leads to a highly significant 40% drop in blood glucose levels in 4 h that is relatively sustained for 12 h. Taken together, these studies demonstrate that CAGE is a promising vehicle for transdermal delivery of therapeutic proteins; specifically, as a noninvasive delivery alternative to injectable insulin for the treatment of diabetes.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Banerjee

Ibsen

Iwao

et al. 2017

Adv Healthcare Materials

163

155

View full text Add to dashboard Cite

show abstract

“…Then the cap (donor chamber) was placed and fixed on that to avoid evaporation. The cell was placed in a shaker-incubator (Heidolph Incubator 1000, Heidolph Co., Germany) with a temperature of 32℃ for three hours (3,21). The cap was taken away every 15 minutes and the lotion was rubbed evenly by a swab to help the active ingredient penetration.…”

Section: Permeation Testmentioning

confidence: 99%

“…Development of transdermal products is restricted by the low permeability of the skin. To overcome this problem, numerous chemicals have been employed as skin permeation enhancers (3). Several groups of enhancers have been introduced including certain peptides, hydrophobic nanoparticles, surfactants, and solvents (3,4).…”

Section: Introductionmentioning

confidence: 99%

“…To overcome this problem, numerous chemicals have been employed as skin permeation enhancers (3). Several groups of enhancers have been introduced including certain peptides, hydrophobic nanoparticles, surfactants, and solvents (3,4). In the present study, 12 conventional hydrophilic and hydrophobic solvents, which have been widely investigated in the present literature, were selected to explore their effect on skin permeation of HA as well as AHA.…”

Section: Introductionmentioning

confidence: 99%

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Effects of Skin Penetration Enhancers in Topical Antiaging Products Containing α-HydroxyAcids and Hyaluronic Acid

Shokri

Javar²,

Ghadermazi³

2014

Avicenna J Med Biochem

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Background: Transdermal drug delivery has several advantages and has been vastly investigated over the last decades. Chemical enhancers improve the quantity of drug penetration through the skin. Objectives: In this study, some conventional solvents and surfactants were used as enhancers to promote dermal penetration of α-hydroxyacids (AHA) and hyaluronic acid (HA). Materials and Methods: A total of 42 different formulations containing AHA or HA as the active ingredient and a solvent or surfactant as the enhancer were prepared. The experiments for determination of transdermal absorption of AHA or HA for each formulation were performed using a diffusion cell and a slice of chicken skin as model at 32℃. After 1.5 or 12 hours, samples from the medium were collected and analyzed for AHA or HA concentration. Results: After 1.5 and 12 hours, the maximum permeated amount of AHA were 89.8 and 342.5 mg, respectively, which related to the formulations with liquid paraffin. After 1.5 and 12 hours, the maximum permeated amount of HA were 57.3 and 70.6 mg, respectively, which related to the formulations with glycerol. Conclusions:The most effective enhancer for AHA and HA were liquid paraffin and glycerol, respectively. The most effective surfactant for both AHA and HA was Tween 80. The effects of the enhancers were increased by prolonging the exposure time.

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Smart Skin‐Adhesive Patches: From Design to Biomedical Applications

Wong

Deen

Bates

et al. 2023

Adv Funct Materials

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With the advancement of medical and digital technologies, smart skin adhesive patches have emerged as a key player for complex medical purposes. In particular, skin adhesive patches with integrated electronics have created an excellent platform for monitoring health conditions and intelligent medication. However, the efficient design of the adhesive patches is still challenging as it requires a strong combination of network structure, adhesion, physical properties, and biocompatibility. To design an assimilated device, one must have a deep knowledge of various skin adhesive patches. This article provides a comprehensive review of the recent advances in skin-adhesive patches, including hydrogel-based adhesive patches, transdermal patches, and electronic skin (E-skin) patches, for various biomedical applications such as wound healing, drug delivery, biosensing, and health monitoring. Furthermore, the key challenges, implementable strategies, and future designs that can potentially provide researchers in designing innovative multipurpose smart skin patches are discussed. These advanced approaches are promising for managing the health and fitness of patients who require regular medical care.

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Novel chemical permeation enhancers for transdermal drug delivery

Cited by 98 publications

References 72 publications

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

Effects of Skin Penetration Enhancers in Topical Antiaging Products Containing α-HydroxyAcids and Hyaluronic Acid

Smart Skin‐Adhesive Patches: From Design to Biomedical Applications

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