Transdermal penetration enhancers: Applications, limitations, and potential

Finnin, Barrie C.; Morgan, Timothy M.

doi:10.1021/js990154g

Cited by 229 publications

(145 citation statements)

References 39 publications

Supporting

Mentioning

137

Contrasting

Unclassified

Order By: Relevance

“…Finnin and Morgan [21] indicated that molecules with a Mw of <500 Da can penetrate across the skin because of their small molecular volumes. Se-L-M fits this criterion (Mw 196.1 Da).…”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

View full text Add to dashboard Cite

Aim: To investigate the in vitro and in vivo percutaneous absorption of seleno-L-methionine (Se-L-M), an ultraviolet (UV)-protecting agent, from aqueous solutions. Methods: Aqueous solutions of Se-L-M were prepared in pH 4, 8, and 10.8 buffers. The pH 8 buffer contained 30% glycerol, propylene glycol (PG) and polyethylene glycol (PEG) 400. The in vitro skin permeation of Se-L-M via porcine skin and nude mouse skin was measured and compared using Franz diffusion cells. The in vivo skin tolerance study was performed, which examined transepidermal water loss (TEWL), skin pH and erythema. Results: In the excised porcine skin, the flux was 0.1, 11.4 and 8.2 μg· cm -2 ·h -1 for the pH 4, 8, and 10.8 buffers, respectively. A linear correlation between the flux and skin deposition was determined. According to permeation across skin with different treatments (stripping, delipidation, and ethanol treatments), it was determined that the intracellular route comprised the predominant pathway for Se-L-M permeation from pH 8 buffer. Aqueous solutions of seleno-DL-methionine (Se-DL-M), selenium sulfide and selenium-containing quantum dot nanoparticles were also used as donor systems. The DL form showed a lower flux (7.0 vs 11.4 μg· cm -2 ·h -1 ) and skin uptake (23.4 vs 47.3 μg/g) as compared to the L form, indicating stereoselective permeation of this compound. There was no or only negligible permeation of selenium sulfide and quantum dots into and across the skin. With in vivo topical application for 4 and 8 h, the skin deposition of Se-L-M was about 7 μg/g, and values were comparable to each other. The topical application of Se-L-M for up to 5 d did not caused apparent skin irritation. However, slight inflammation of the dermis was noted according to the histopathological examination. Conclusion: Se-L-M was readily absorbed by the skin in both the in vitro and in vivo experiments. The established profiles of Se-L-M skin absorption will be helpful in developing topical products of this compound.Keywords: seleno-L-methionine; selenium; percutaneous absorption; topical delivery; skin [5] . In humans, a low selenium status is associated with up to a 4-fold increased risk of developing skin cancer [6] . Topical selenium compounds also increase the minimum dose of UV radiation required to cause skin reddening and protect against skin damage caused by UVB [7,8] . Seleno-L-methionine (Se-L-M), the major component of dietary selenium, represents an organic form of selenium which may provide enhanced protection of the skin [9] . Se-L-M also decreases the oxidative stress of neurodegenerative diseases, rheumatoid arthritis, and HIV/AIDS [10,11] . Most ingested selenium, whether in organic or inorganic form, is converted by liver metabolism [3] . In addition, selenium toxicity can produce gastrointestinal problems [12] . Delivery of pharmacologically active compounds via the skin is an attractive alternative to oral dosing for numerous reasons including stable plasma concentrations, bypass of firstpass effects, and reduction of some si...

show abstract

“…Finnin and Morgan [21] indicated that molecules with a Mw of <500 Da can penetrate across the skin because of their small molecular volumes. Se-L-M fits this criterion (Mw 196.1 Da).…”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

Lin

Fang²,

Al‐Suwayeh

et al. 2011

Acta Pharmacol Sin

View full text Add to dashboard Cite

show abstract

“…Evaluations of transdermal patches: [31][32][33][34][35][36][37][38][39] The evaluation methods for transdermal dosage form can be classified into following types: 1) Physicochemical evaluation 2) In-vitro evaluation 3) In-vivo evaluation 4) Stability studies 1) Physicochemical evaluation Thickness…”

Section: • Laser Radiationmentioning

confidence: 99%

A Comprehensive Review on: Transdermal drug delivery systems.

Kharat¹,

Bathe²

2016

Int J of Biomed & Adv Res

View full text Add to dashboard Cite

Transdermal drug delivery system was introduced to overcome the difficulties of drug delivery through oral route. Despite their relatively higher costs, transdermal delivery systems have proved advantageous for delivery of selected drugs, such as estrogens, testosterone, clonidine and nitro-glycerine. Transdermal delivery provides a leading edge over injectable and oral routes by increasing patient compliance and avoiding first pass metabolism respectively. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive methods of drug delivery. Skin is an effective medium from which absorption of the drug takes place and enters into systematic circulation over a period of time. The present article reviews the selection of drug candidates and polymers suitable to be formulated as transdermal system, advantages, disadvantages of formulation design and the methods of evaluation.

show abstract

“…New technologies to overcome the skin barrier function are constantly being developed. Recently, biomaterials have emerged as novel penetration enhancers for enhanced transdermal delivery (Finnin & Morgan, 1999). Particularly, some of them exhibit excellent enhancing ability towards the transdermal absorption of macromolecules, which is often circumscribed by conventional chemical enhancers (Chen et al, 2006;Hsu & Mitragotri, 2011).…”

Section: Introductionmentioning

confidence: 99%

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

2013

View full text Add to dashboard Cite

The highly organized structure of the stratum corneum provides an effective barrier to the drug delivery into or across the skin. To overcome this barrier function, penetration enhancers are always used in the transdermal and dermal drug delivery systems. However, the conventional chemical enhancers are often limited by their inability to delivery large and hydrophilic molecules, and few to date have been routinely incorporated into the transdermal formulations due to their incompatibility and local irritation issues. Therefore, there has been a search for the compounds that exhibit broad enhancing activity for more drugs without producing much irritation. More recently, the use of biomaterials has emerged as a novel method to increase the skin permeability. In this paper, we present an overview of the investigations on the feasibility and application of biomaterials as penetration enhancers for transdermal or dermal drug delivery systems.

show abstract

Transdermal penetration enhancers: Applications, limitations, and potential

Cited by 229 publications

References 39 publications

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

In vitro and in vivo percutaneous absorption of seleno-L-methionine, an antioxidant agent, and other selenium species

A Comprehensive Review on: Transdermal drug delivery systems.

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

Contact Info

Product

Resources

About