Modes of action of terpene penetration enhancers in human skin; Differential scanning calorimetry, small-angle X-ray diffraction and enhancer uptake studies

It was aimed to develop the matrix type polysaccharide-based transdermal films of nifedipine (NFD) to provide its long term plasma concentration. The mechanical tests were carried out on gel formulations which were utilised in the fabrication of transdermal films to determine the type of polymer (pectin, sodium alginate) and plasticizer (propylene glycol, glycerine) as well as their concentrations. The mechanical strength, elasticity, bioadhesiveness and the drug release characteristics of optimised films containing NFD were evaluated. Permeation of NFD from the films with/without adding an enhancer (nerolidol) was followed through excised rat skin using Franz diffusion cells. Results showed that the gels composed of either pectin or sodium alginate were appropriate for the fabrication of transdermal films of NFD, and the addition of propylene glycol improved mechanical strength, flexibility, and bioadhesiveness of the films. Permeation data showed that nerolidol was an effective permeation enhancer for the polysaccharide-based transdermal films of NFD.Key words nifedipine; transdermal film; sodium alginate; pectin; texture analysis; nerolidol Transdermal delivery possesses many advantages over conventional drug administration routes, including avoidance of intestinal and/or hepatic first pass metabolism, reduction in side effects and better patient compliance. Polymers are crucial components for the formulation of transdermal delivery systems. There are some critical parameters for the optimisation of transdermal therapeutic systems including physical or chemical stability of the formulation, compatibility with skin, adhesion to skin, the release characteristics of drug from the vehicle and its permeation through the skin. Therefore, the choice of polymers and plasticizers used in transdermal systems have strong impact on drug release, permeability, elasticity, and wearing properties of transdermal formulations. 1,2)Natural polysaccharides such as sodium alginate, chitosan, pectin, guar gum, gellan gum have been widely evaluated as a polymer in the optimisation of transdermal systems due to their non-toxic, biocompatible and potentially biodegradable properties.3,4) Sodium alginate is a mixture of polyuronic acids composed of residues of D-mannuronic acid and L-guluronic acid, which is used in design of controlled drug delivery formulations.5) It has also been used to formulate transdermal films. 6,7)Despite all the advantages of transdermal drug delivery, stratum corneum, the outermost layer of the skin, provides the greatest resistance to entrance of drugs to the systemic blood stream. In order to achieve therapeutic drug concentration following transdermal administration, penetration enhancers which reduce the barrier characteristics of stratum corneum reversibly are added into transdermal formulations. 8,9)Terpenes appear to have good skin penetration characteristics for transdermal systems due to their low cutaneous irritancies, good toxicological profiles.8) Moreover, this interaction with the stratum cor...

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“…13,14) Different types of terpenes have been shown to be effective penetration enhancers for both hydrophilic 15,16) and lipophilic drugs.…”

Section: )mentioning

confidence: 99%

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Bektaş

Cevher

Güngör

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…6) In addition, assessments to understand the mechanism of action of CPEs are carried out by differential scanning calorimetry (DSC), Fourier transform (FT)-IR, ESR, or X-ray diffractometry (XRD). [7][8][9][10] Although these techniques can observe changes in the SC structure, they require specialist manipulation techniques and are labor intensive, time consuming, and costly. High-throughput screening (HTS) techniques have been introduced using electrical resistance-based methods.…”

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confidence: 99%

Potential of Stratum Corneum Lipid Liposomes for Screening of Chemical Skin Penetration Enhancers

Sakdiset

Todo

Sugibayashi

2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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The evaluation of effective skin chemical penetration enhancers (CPEs) is a crucial process in the development of transdermal and dermal formulations with the capacity to overcome the stratum corneum barrier. In the present study, we aimed to investigate the potential of stratum corneum lipid liposomes (SCLLs) as an alternative tool for the screening of various types and concentrations of CPEs. SCLLs were prepared using a thin-film hydration technique, and two types of fluorescent probes ( Key words stratum corneum lipid liposome; chemical skin penetration enhancer; liposome; high-throughput screening Skin has been recognized as an application site of therapeutic drugs for several decades. However, only small numbers of drugs are available nowadays intended for systemic absorption through the skin. The stratum corneum (SC), the outermost layer of the skin, provides a strong barrier to protect against extraneous molecules from entering the body, and thus limits the skin penetration of drugs. The structure of the SC consists of keratin-rich corneocytes embedded in an intercellular lipid matrix.

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“…The use of penetration enhancer is a valuable and important factor for achieving therapeutic plasma levels for many drugs. Terpenes have been used to increase the skin permeation of a large number of compounds and they reported to increase the drug diffusivity in stratum corneum and also drug partitioning into stratum corneum by disrupting the intercellular lipid bi-layers 15 . The intensity of their effects depends mainly on the lipophilicity of the drug and vehicle used 16 .…”

Section: Discussionmentioning

confidence: 99%

Anti-inflammatory and Analgesic Effects of Ketoprofen in Palm Oil Esters Nanoemulsion

et al. 2010

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Modes of action of terpene penetration enhancers in human skin; Differential scanning calorimetry, small-angle X-ray diffraction and enhancer uptake studies

Cited by 203 publications

References 36 publications

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Potential of Stratum Corneum Lipid Liposomes for Screening of Chemical Skin Penetration Enhancers

Anti-inflammatory and Analgesic Effects of Ketoprofen in Palm Oil Esters Nanoemulsion

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