Relationship Between the Enhancement Effects of Chemical Permeation Enhancers on the Lipoidal Transport Pathway Across Human Skin Under the Symmetric and Asymmetric Conditions In Vitro

Present investigation comprises the study of ex-vivo skin flux and in-vivo pharmacokinetics of Thiocolchicoside (THC) from transdermal films. The films were fabricated by solvent casting technique employing combination of hydrophilic and hydrophobic polymers. A flux of 18.08 µg/cm2h and 13.37µg/cm2h was achieved for optimized formulations containing 1, 8-cineole and oleic acid respectively as permeation enhancers. The observed flux values were higher when compared to passive control (8.66 µg/cm2h). Highest skin permeation was observed when 1,8-cineole was used as chemical permeation enhancer and it considerably (2-2.5 fold) improved the THC transport across the rat skin. In vivo studies were performed in rabbits and samples were analysed by LC-MS-MS. The mean area under the curve (AUC) values of transdermal film showed about 2.35 times statistically significant (p<0.05) improvement in bioavailability when compared with the oral administration of THC solution. The developed transdermal therapeutic systems using chemical permeation enhancers were suitable for drugs like THC in effective management of muscular pain.

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Transdermal Delivery of Acyclovir Sodium Via Carbopol Gels: Role of Chemical Permeation Enhancers

Letters in Drug Design & Discovery ◽

10.2174/157018011794839420 ◽

2011 ◽

Vol 8 (4) ◽

pp. 381-389 ◽

Cited By ~ 5

Author(s):

Raju Jukanti ◽

Ashok Mateti ◽

Suresh Bandari ◽

Prabhakar R Veerareddy

Keyword(s):

Transdermal Delivery ◽

Permeation Enhancers ◽

Chemical Permeation Enhancers ◽

Chemical Permeation

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Correction: Design, Synthesis of Novel Lipids as Chemical Permeation Enhancers and Development of Nanoparticle System for Transdermal Drug Delivery

PLoS ONE ◽

10.1371/journal.pone.0096964 ◽

2014 ◽

Vol 9 (4) ◽

pp. e96964

Author(s):

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Permeation Enhancers ◽

Design Synthesis ◽

Chemical Permeation Enhancers ◽

Nanoparticle System ◽

Chemical Permeation

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Influence of chemical permeation enhancers on transdermal permeation of alfuzosin: an investigation using response surface modeling

Drug Development and Industrial Pharmacy ◽

10.3109/03639045.2010.522192 ◽

2011 ◽

Vol 37 (4) ◽

pp. 465-474 ◽

Cited By ~ 16

Author(s):

Satyanarayan Pattnaik ◽

Kalpana Swain ◽

Amarendra Bindhani ◽

Subrata Mallick

Keyword(s):

Response Surface ◽

Surface Modeling ◽

Response Surface Modeling ◽

Permeation Enhancers ◽

Transdermal Permeation ◽

Chemical Permeation Enhancers ◽

Chemical Permeation

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Addressing the Issue of Tetrodotoxin Targeting

Marine Drugs ◽

10.3390/md16100352 ◽

2018 ◽

Vol 16 (10) ◽

pp. 352 ◽

Cited By ~ 9

Author(s):

Daria Melnikova ◽

Yuri Khotimchenko ◽

Timur Magarlamov

Keyword(s):

Medical Application ◽

Efficacy And Safety ◽

Analgesic Drug ◽

Permeation Enhancers ◽

Chemical Permeation Enhancers ◽

Main Emphasis ◽

Pain Models ◽

Attractive Candidate ◽

Nav Channels ◽

Chemical Permeation

This review is devoted to the medical application of tetrodotoxin (TTX), a potent non-protein specific blocker of voltage-gated sodium (NaV) channels. The selectivity of action, lack of affinity with the heart muscle NaV channels, and the inability to penetrate the blood–brain barrier make this toxin an attractive candidate for anesthetic and analgesic drug design. The efficacy of TTX was shown in neuropathic, acute and inflammatory pain models. The main emphasis of the review is on studies focused on the improvement of TTX efficacy and safety in conjunction with additional substances and drug delivery systems. A significant improvement in the effectiveness of the toxin was demonstrated when used in tandem with vasoconstrictors, local anesthetics and chemical permeation enhancers, with the best results obtained with the encapsulation of TTX in microparticles and liposomes conjugated to gold nanorods.

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Transdermal Nitroglycerin Delivery Using Acrylic Matrices: Design, Formulation, and In Vitro Characterization

ISRN Pharmaceutics ◽

10.1155/2014/493245 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 2

Author(s):

Houman Savoji ◽

Amir Mehdizadeh ◽

Ahmad Ramazani Saadat Abadi

Keyword(s):

Skin Permeation ◽

Peel Strength ◽

Adhesion Properties ◽

Pressure Sensitive Adhesives ◽

In Vitro Characterization ◽

Chemical Permeation Enhancers ◽

Transdermal Drug Delivery Systems ◽

Franz Diffusion Cells ◽

Chemical Permeation

Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux (Jss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest Jss. Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin.

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Transmucosal Absorption Enhancers in the Drug Delivery Field

Pharmaceutics ◽

10.3390/pharmaceutics11070339 ◽

2019 ◽

Vol 11 (7) ◽

pp. 339 ◽

Cited By ~ 7

Author(s):

Maher ◽

Casettari ◽

Illum

Keyword(s):

Drug Delivery ◽

Clinical Trials ◽

Drug Delivery Systems ◽

Permeation Enhancer ◽

Special Issue ◽

Permeation Enhancers ◽

Absorption Enhancers ◽

Chemical Permeation Enhancers ◽

Epithelial Barriers ◽

Chemical Permeation

Drug delivery systems that safely and consistently improve transport of poorly absorbed compounds across epithelial barriers are highly sought within the drug delivery field. The use of chemical permeation enhancers is one of the simplest and widely tested approaches to improve transmucosal permeability via oral, nasal, buccal, ocular and pulmonary routes. To date, only a small number of permeation enhancers have progressed to clinical trials, and only one product that includes a permeation enhancer has reached the pharmaceutical market. This editorial is an introduction to the special issue entitled Transmucosal Absorption Enhancers in the Drug Delivery Field (https://www.mdpi.com/journal/pharmaceutics/special_issues/transmucosal_absorption_enhancers). The guest editors outline the scope of the issue, reflect on the results and the conclusions of the 19 articles published in the issue and provide an outlook on the use of permeation enhancers in the drug delivery field.

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