Transdermal delivery of peptide and protein drugs: An overview

Amsden, Brian G.; Goosen, Mattheus F. A.

doi:10.1002/aic.690410814

Cited by 73 publications

(44 citation statements)

References 147 publications

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“…Skin permeability to calcein, insulin, and BSA was increased by orders of magnitude. This result is significant, because skin is generally considered impermeable to macromolecules (13,19).…”

Section: Fabrication Of Hollow Microneedles Made Of Silicon Metal Amentioning

confidence: 99%

Microfabricated needles for transdermal delivery of macromolecules and nanoparticles: Fabrication methods and transport studies

McAllister

Wang

Davis

et al. 2003

Proc. Natl. Acad. Sci. U.S.A.

714

430

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Arrays of micrometer-scale needles could be used to deliver drugs, proteins, and particles across skin in a minimally invasive manner. We therefore developed microfabrication techniques for silicon, metal, and biodegradable polymer microneedle arrays having solid and hollow bores with tapered and beveled tips and feature sizes from 1 to 1,000 m. When solid microneedles were used, skin permeability was increased in vitro by orders of magnitude for macromolecules and particles up to 50 nm in radius. Intracellular delivery of molecules into viable cells was also achieved with high efficiency. Hollow microneedles permitted flow of microliter quantities into skin in vivo, including microinjection of insulin to reduce blood glucose levels in diabetic rats.transdermal drug delivery ͉ skin ͉ microelectromechanical systems ͉ solid microneedle ͉ hollow needle injection H ypodermic needles have provided the gold standard for drug delivery for over a century, but advances in biotechnology make their limitations increasingly apparent. As devices that transport molecules of nanometer dimensions, the millimeter and larger length scales of conventional needles are often unnecessary, and they cause pain and limit targeted delivery. We therefore sought to test the hypothesis that needles of micrometer dimensions can create transport pathways large enough for small drugs, macromolecules, nanoparticles, and fluid flow, but small enough to avoid pain and facilitate highly localized and even intracellular targeting.The microelectronics revolution has provided tools for highly precise, reproducible, and scalable methods to fabricate structures of micrometer dimensions (1). This lithography-based approach can produce large arrays of microneedles that can be inserted into cells, skin, or other tissues. The increased importance of macromolecular therapeutics, combined with the newly acquired power of microfabrication, has recently prompted interest in fabricating (2-6) and testing (7, 8) microneedles for drug delivery.In this study, we describe fabrication techniques used to make needles out of silicon, metal, polymer, and glass that have a range of geometries, can produce needles ranging from in-plane to normally protruding from substrates, and can be formed in large two-dimensional arrays. These methods mostly require just one or two fabrication steps or a single molding step and use technologies that are readily scalable for inexpensive mass production. We also demonstrate the ability of these microneedles to deliver molecules into cells and skin by using cell culture, cadaver skin, and hairless rats. MethodsFabrication of Silicon Microneedles. Solid microneedles were etched from silicon substrates as described previously (9). Briefly, chromium was sputter deposited and then lithographically patterned (e.g., 20 ϫ 20 arrays of 80-m-diameter dots with 150-m center-to-center spacing) onto 2-inch (5-cm), ͗100͘ oriented silicon wafers. Reactive ion etching (RIE; Plasma Therm, St. Petersburg, FL) was then carried out with 20 standard cm 3 ͞...

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Section: Fabrication Of Hollow Microneedles Made Of Silicon Metal Amentioning

confidence: 99%

Microfabricated needles for transdermal delivery of macromolecules and nanoparticles: Fabrication methods and transport studies

McAllister

Wang

Davis

et al. 2003

Proc. Natl. Acad. Sci. U.S.A.

714

430

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“…21 As known, the amount of sample detected in the receiving chamber represented the possibility of the sample to permeate through the skin barrier to circulation after transdermal application. 33 Then, the physical mixing of Tat with targeted peptide might be applicable for the development of the transdermal delivery system.…”

Section: Transdermal Absorption Through Rat Skinmentioning

confidence: 99%

Potent enhancement of GFP uptake into HT‐29 cells and rat skin permeation by coincubation with tat peptide

Lohcharoenkal

Manosaroi

Götz

et al. 2011

Journal of Pharmaceutical Sciences

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“…In the second case, verapamil diffuses across the viable epidermis and then is absorbed by the blood circulation. Although this is a hypothetical case designed purely for the purpose of this study, the result obtained for this case is expected to be useful since it has been shown that drug may be metabolized in the viable epidermis (Amsden and Goosen, 1995). In the figure, S a is the surface area h e of both the transdermal patch and microneedle arrays, L is the penetration depth of microneedles, H eff is the effective skin thickness (i.e., effective path length of molecules in tissue) that verapamil molecules can pass in the tissue from microneedle which depends on the needle geometry (Davidson et al, 2008).…”

Section: Modeling Strategymentioning

confidence: 99%

“…However, most of these models have studied the influence of skin metabolism for the full skin thickness (i.e., the stratum corneum and viable skin together). In fact, skin metabolism occurs primarily in the viable epidermis (Amsden and Goosen, 1995). In order to validate this fact we have carried out simulations of the common patch with two hypothetical cases.…”

Section: Introductionmentioning

confidence: 99%

Transdermal Drug Delivery by Microneedles: Does Skin Metabolism Matter?

Al-Qallaf¹,

Mori²,

Olatunji³

et al. 2009

International Journal of Chemical Reactor Engineering

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Microneedle arrays have been shown to increase skin permeability for the transdermal delivery of drugs with high molecular weights. Various theoretical studies have been proposed to predict the drug transport behaviour after drug injection using microneedles. However it is important for the optimal design of microneedle systems to consider the effects of biological factors such as skin metabolism and variations in pharmacokinetic parameters as well as to improve the enhancement of skin permeability. A mathematical model for microneedle systems is introduced and applied to simulate the verapamil transport with metabolism in the skin. A comparative analysis for a transdermal delivery of verapamil from microneedles is presented in this paper. The results indicate that the skin metabolism does not markedly affect the skin permeation after verapamil injection using microneedles.

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Transdermal delivery of peptide and protein drugs: An overview

Cited by 73 publications

References 147 publications

Microfabricated needles for transdermal delivery of macromolecules and nanoparticles: Fabrication methods and transport studies

Microfabricated needles for transdermal delivery of macromolecules and nanoparticles: Fabrication methods and transport studies

Potent enhancement of GFP uptake into HT‐29 cells and rat skin permeation by coincubation with tat peptide

Transdermal Drug Delivery by Microneedles: Does Skin Metabolism Matter?

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