transdermal permeation
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Author(s):  
Rania Moataz El-Dahmy ◽  
Ahmed Hassen Elshafeey ◽  
Nabaweya Abdelaziz Abd El Gawad ◽  
Omaima Naim El-Gazayerly ◽  
Ibrahim Elsayed

Author(s):  
Maria A. Vatmanidou ◽  
Konstantina Stathopoulou ◽  
Evangelos Gikas ◽  
Nektarios Aligiannis ◽  
Paraskevas P. Dallas ◽  
...  

Author(s):  
Katayoun Morteza-Semnani ◽  
Majid Saeedi ◽  
Jafar Akbari ◽  
Mohammad Eghbali ◽  
Amirhossein Babaei ◽  
...  

AbstractEssential oils have been proposed as promising non-toxic transdermal permeation enhancers. Their use is limited because of their low water solubility. The use of nanotechnology-based strategies is one of the ways to overcome this limitation. This study aimed to explore the transdermal permeation enhancing capability of cumin essential oil in nanoemulgel systems containing diclofenac sodium. Cumin essential oil nanoemulsion was produced by high-pressure homogenization technique. The formulation was optimized by changing HLB values in a range of 9.65–16.7 using different surfactant mixtures, namely, Tween 20, Tween 80, and Span 80. Preparations were characterized by polydispersity index, droplet size, and zeta potential. Nanoemulsion with concentrations of 2 and 4% essential oil was incorporated into 0.75% Carbopol gel matrix to make nanoemulgel formulation, and its permeation enhancing effect was performed through Franz diffusion cells. Antinociceptive activities of the formulations were measured in thermal (tail-flick) and chemical (formalin) models of nociception in mice. Characterization exhibited that at HLB value of 9.65, the smallest particle size (82.20 ± 5.82 nm) was formed. By increasing the essential oil percentage in the nanoemulgel from 1 to 2%, the permeation of diclofenac increased from 28.39 ± 1.23 to 34.75 ± 1.07 µg/cm2 at 24 h. The value of permeation from the simple gel (21.18 ± 2.51 µg/cm2) and the marketed product (22.97 ± 1.92 µg/cm2) was lower than the formulations containing essential oil. Nanoemulgel of diclofenac containing essential oil showed stronger antinociceptive effects in formalin and tail-flick tests than simple diclofenac gel and marketed formulation. In conclusion, the study proved that nanoemulgel formulation containing cumin essential oil could be considered as a promising skin enhancer to enhance the therapeutic effect of drugs. Graphical abstract


2021 ◽  
Vol 44 (1) ◽  
pp. 1-14
Author(s):  
Kishorkumar Sorathia ◽  
Mehul Patel ◽  
Tejal Soni ◽  
Vidur Vaghasiya ◽  
Jaydip Patel ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 682
Author(s):  
Mahmoud H. Teaima ◽  
Mohamed Azmi Ahmed Mohamed ◽  
Randa Tag Abd El Rehem ◽  
Saadia A. Tayel ◽  
Mohamed A. El-Nabarawi ◽  
...  

Bisoprolol hemifumarate (BH) is an antihypertensive drug that is used as first-line treatment for chronic hypertension and angina pectoris. Our study was performed to enhance the transdermal delivery of BH, a hydrophilic drug active with high molecular weight, through differently prepared hydrogels. The synergistic effect of permeation enhancers and iontophoresis was investigated via both ex vivo and in vivo permeation studies. Ex vivo iontophoretic permeation studies were performed by using male albino Wistar rat skin. Cellosolve® hydrogel (F7) showed a 1.5-fold increase in Q180, Jss, and FER compared to F5 (lacking permeation enhancer). BH pharmacokinetic data were studied in human volunteers, following transdermal delivery of F7, using Phoresor® Unit II iontophoresis device, compared to conventional oral tablets. F7 showed 1.9- and 2-fold higher values of Cmax and AUC0–40, respectively compared to Concor® tablets, as well as a smaller Tmax (2.00 ± 2.00 h). The relative bioavailability of F7 was found to be 201.44%, relative to Concor® tablets, demonstrating the significantly enhanced transdermal permeation of BH from the selected hydrogel by iontophoresis, in human volunteers. Finally, results showed the successful utility of permeation enhancers combined with iontophoresis in significantly enhanced transdermal permeation of BH, despite its large molecular weight and hydrophilic nature. Therefore, this strategy could be employed as a successful alternative route of administration to conventional oral tablets.


2021 ◽  
Vol 22 (4) ◽  
Author(s):  
Audrey N. Hernandes ◽  
Rodrigo Boscariol ◽  
Victor M. Balcão ◽  
Marta M. D. C. Vila

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 540
Author(s):  
Rodrigo Boscariol ◽  
Érika A. Caetano ◽  
Erica C. Silva ◽  
Thais J. Oliveira ◽  
Raquel M. Rosa-Castro ◽  
...  

In the present research work, we addressed the changes in skin by which deep eutectic solvents (DES) enhanced transdermal permeation of bioactive compounds and propose a rationale for this mechanism. Several studies showed that these unusual liquids were ideal solvents for transdermal delivery of biomolecules, but to date, no histological studies relating the action of DES to changes in the structure of the outer skin barrier have been reported. In the research effort described herein, we presented an in-depth analysis of the changes induced in the skin by choline geranate DES, a compound with proven capabilities of enhancing transdermal permeation without deleterious impacts on the cells. The results obtained showed that a low percentage of DES acted as a transient disruptor of the skin structure, facilitating the passage of bioactive compounds dissolved in it.


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