Action of skin penetration enhancers?the Lipid Protein Partitioning theory

1988 ◽  
Vol 10 (6) ◽  
pp. 281-293 ◽  
Author(s):  
B. W. BARRY
2009 ◽  
Vol 6 (3) ◽  
pp. 274-279 ◽  
Author(s):  
Ashu Mittal ◽  
U. Sara ◽  
Asgar Ali ◽  
Mohd. Aqil

ChemInform ◽  
2007 ◽  
Vol 38 (34) ◽  
Author(s):  
Manisha Iyer ◽  
Tao Zheng ◽  
A. J Hopfinger ◽  
Yufeng J. Tseng

2007 ◽  
Vol 12 (23-24) ◽  
pp. 1061-1067 ◽  
Author(s):  
Mohammed Aqil ◽  
Abdul Ahad ◽  
Yasmin Sultana ◽  
Asgar Ali

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Monika Kopečná ◽  
Miloslav Macháček ◽  
Anna Nováčková ◽  
Georgios Paraskevopoulos ◽  
Jaroslav Roh ◽  
...  

Abstract Skin penetration/permeation enhancers are compounds that improve (trans)dermal drug delivery. We designed hybrid terpene-amino acid enhancers by conjugating natural terpenes (citronellol, geraniol, nerol, farnesol, linalool, perillyl alcohol, menthol, borneol, carveol) or cinnamyl alcohol with 6-(dimethylamino)hexanoic acid through a biodegradable ester linker. The compounds were screened for their ability to increase the delivery of theophylline and hydrocortisone through and into human skin ex vivo. The citronellyl, bornyl and cinnamyl esters showed exceptional permeation-enhancing properties (enhancement ratios up to 82) while having low cellular toxicities. The barrier function of enhancer-treated skin (assessed by transepidermal water loss and electrical impedance) recovered within 24 h. Infrared spectroscopy suggested that these esters fluidized the stratum corneum lipids. Furthermore, the citronellyl ester increased the epidermal concentration of topically applied cidofovir, which is a potent antiviral and anticancer drug, by 15-fold. In conclusion, citronellyl 6-(dimethylamino)hexanoate is an outstanding enhancer with an advantageous combination of properties, which may improve the delivery of drugs that have a limited ability to cross biological barriers.


2019 ◽  
Vol 25 (4) ◽  
pp. 455-466 ◽  
Author(s):  
Francisco Arriagada ◽  
Javier Morales

The first limiting barrier for the transport in the skin is the stratum corneum; different strategies have been developed to overcome this barrier, including chemical enhancers. However, these penetration enhancers have limitations, including toxic adverse effects. In this context, research into nanomaterials has provided new tools to increase the residence time of drugs by generating a reservoir, increasing the specificity of drugs and reducing their adverse effects, and improving the penetration of drugs that are difficult to formulate. Silica nanoparticles have been proposed as suitable nanocarriers for skin delivery. Unfortunately, the mechanisms involved in the interaction, transport and fate of silica nanoparticles in the skin have not been fully investigated. This paper reviews significant findings about the interaction between silica-based nanocarriers and the skin. First, this review focuses on the properties and functions of the skin, the skin penetration properties of silica nanoparticles, their synthesis strategies and their toxicity. Finally, advances and evidence on the application of silica nanocarriers in skin drug delivery are provided, in which the use of nanoparticles increases the stability and solubility of the bioactive compound, enhancing its performance, act as penetrator enhancer and improving controlled release. Thus, improving the treatment of some skin disorders.


2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.


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