Natural products as potential drug permeation enhancer in transdermal drug delivery system

Patil, U. K.; Saraogi, Richa

doi:10.1007/s00403-014-1445-y

Cited by 53 publications

(32 citation statements)

References 63 publications

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“…To solve this problem, numerous techniques have been used, such as the use of permeation enhancers (PEs) [3,4,5,6]. Essential oils (or volatile oils) are a type of natural permeation enhancers that can effectively promote the permeation of both hydrophilic and hydrophobic drugs [7,8,9]. Essential oils are biocompatible with commonly-used chemical synthetics PEs because they are safe, non-toxic, pharmacologically inert, non-irritating, hypo-allergenic and have a wide range of pharmacological functions, such as anti-inflammatory and anticancer applications [10,11,12,13].…”

Section: Introductionmentioning

confidence: 99%

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Dai

Yin

Wan

et al. 2016

IJMS

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Borneol is a natural permeation enhancer that is effective in drugs used in traditional clinical practices as well as in modern scientific research. However, its molecular mechanism is not fully understood. In this study, a mixed coarse-grained model of stratum corneum (SC) lipid bilayer comprised of Ceramide-N-sphingosine (CER NS) 24:0, cholesterol (CHOL) and free fatty acids (FFA) 24:0 (2:2:1) was used to examine the permeation enhancing mechanism of borneol on the model drug osthole. We found two different mechanisms that were dependent on concentrations levels of borneol. At low concentrations, the lipid system maintained a bilayer structure. The addition of borneol made the lipid bilayer loosen and improved drug permeation. The “pull” effect of borneol also improved drug permeation. However, for a strongly hydrophobic drug like osthole, the permeation enhancement of borneol was limited. When most borneol molecules permeated into bilayers and were located at the hydrophobic tail region, the spatial competition effect inhibited drug molecules from permeating deeper into the bilayer. At high concentrations, borneol led to the formation of water pores and long-lived reversed micelles. This improved the permeation of osthole and possibly other hydrophobic or hydrophilic drugs through the SC. Our simulation results were supported by Franz diffusion tests and transmission electron microscope (TEM) experiments.

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Section: Introductionmentioning

confidence: 99%

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Dai

Yin

Wan

et al. 2016

IJMS

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“…Immense amounts of research during the past two decades has led to the formulation of some different classes of penetration enhancers, including surfactants (for example, sorbitan trioleate), fatty acids/esters (for example, lauric acid), terpenes (for example, menthone), azone-like compounds (for example, azone), and solvents (for example, ethanol and dimethyl sulphoxide) (Table 1) [1,6,[12][13][14][15]. Fatty acids for the use of skin permeation enhancers: Fatty acids contain a aliphatic hydrocarbon chain and a terminal carboxylic acid group.…”

Section: Volume 2 | Issuementioning

confidence: 99%

“…The creation of transdermal drug delivery system (TDDS) has been one of the most sophisticated and innovative approaches of drug deliveries. The transdermal drug delivery system has attracted considerale attention because of its many potential advantages, including better patient compliance, avoidance of gastrointestinal disturbances, hepatic first-pass metabolism and sustained delivery of drugs to provide steady plasma profiles, particularly for drugs with short half-lives, reduction in systemic side effects and enhanced therapeutic efficacy [1][2][3][4][5][6].…”

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confidence: 99%

Review on Transdermal Drug Delivery Systems

Pang¹,

Han²

2014

Journal of Pharmaceutics and Drug Development

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ISSN: 2348-9782 During the past decades, intensive studies have focused on the technologies in drug delivery, and with the rapid developments and explorations in technologies, traditional drug delivery means are being replaced by the more effective and advanced ones. The creation of transdermal drug delivery system (TDDS) has been one of the most sophisticated and innovative approaches of drug deliveries. The transdermal drug delivery system has attracted considerale attention because of its many potential advantages, including better patient compliance, avoidance of gastrointestinal disturbances, hepatic first-pass metabolism and sustained delivery of drugs to provide steady plasma profiles, particularly for drugs with short half-lives, reduction in systemic side effects and enhanced therapeutic efficacy [1][2][3][4][5][6].Recently, transdermal drug delivery system (TDDS) has become a more and more important approach to administering drugs. Based on its advantages, which are not achievable by other modes of administration, many researchers are dedicated to the study of it, and have made great progress. Although the skin offers a painless interface for systemic drug delivery, it also presents limitations which are mainly caused by the stratum corneum. In this work, we state the increasingly impact of TDDS, discuss the limitations of it, and last but not least, we highlight the methods for overcoming these limitations by using permeation enhancers, microneedles, iontophoresis.Despite these advantages, most of the transdermal candidates have low permeability. The drugs administered across skin should have the three constraining characteristics: appropriate partition coefficient, low molecular mass (<500Da), and small required dose (upto milligrams) [3]. The limitations of transdermal drug delivery are caused by skin which protects against and is impermeable to foreign molecules. The human skin is consisted of two main layers: the layer of epidermis and the layer of dermis. Stratum corneum is the epidermis's outermost layer that composed of stratified keratinocytes, multiple lipid bilayers of ceramidas, fatty acids, cholesterol and cholesterol esters. Stratum corneum provides an extremely effective physical barrier for the control of drug penetration [2,[7][8][9][10]. Therefore, attempts to overcome this skin barrier is presently an important area of pharmaceutical and toxicological research. The techniques that weaken the barrier have included permeation enhancers , microneedles and iontophoresis [69][70][71][72][73][74][75][76][77][78][79][80][81][82][83][84]. Chemical permeation enhancersIn the last 50 years, a large number of chemical permeation enhancers (CPEs) which are defined as substances that interact with the major constituents of skin barrier, stratum corneum, to promote penetration of drugs into skin.The ideal enhancer should have the following conditions: 1. Non-pharmacological activities. 2. Nontoxic,. Rapid-acting with predictable and reproducible activity. 4. When removed from the skin...

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“…This technique can be useful for applications that contain peptides and small proteins. Physical methods that temporarily improve skin permeability such as electroporation and ultrasound are used, representing perspectives in the application of drugs of low or high molecular weight (Patil, Saraogi, 2014). However, not much studying has been done about the use of CryoLaser as a method of biophysical permeation.…”

Section: Introductionmentioning

confidence: 99%

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

Andréo

Rufino

Ubaldo

et al. 2016

Braz. J. Pharm. Sci.

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Aiming to alter and/or improve permeation of active compounds in the skin, many strategies have been developed, including biophysical methods. One of the physical absorption techniques, currently known as Cryo Laser Phoresis (CLP), consists of an apparatus that emits radiation on polar or nonpolar molecules of the active substance, resulting in faster penetration when in comparison to the standard topical application. The goal of this work was to evaluate the efficacy of a method that proposes to increase cutaneous permeation of diclofenac sodium by using CLP technique. The influence on permeation was evaluated ex vivo, using Franz cell and human skin obtained from cosmetic surgery. The results were evaluated using statistical methods and data exploratory analysis: clusters, k-means and Principal Component Analysis. The results showed a larger increase in the concentration of diclofenac sodium in the dermis with the use of laser. In all samples (with or without laser application) it was observed that skin surface showed an amount of diclofenac sodium and that there was no active passage to the receptor liquid, suggesting that diclofenac sodium was not absorbed. These results indicate that CLP, when used under the conditions described in this study, is able to increase diclofenac sodium penetration and its retention into deeper layers. Uniterms:Cryo Laser Phoresis/dematologic use. Cutaneous permeation. Diclofenac sodium/cutaneous permeation. Franz cell.No sentido de alterar e/ou melhorar a penetração de substâncias na pele, diversas estratégias têm sido desenvolvidas, variando desde a aplicação de novos veículos e ativos encapsulados, até equipamentos que atuam por métodos biofísicos. Uma das técnicas de absorção física, atualmente conhecida como Crio Laser Forese (CLF), consiste em um aparato que emite radiação sobre moléculas polares ou apolares da substância ativa, tornando sua penetração mais rápida, se comparada à administração tópica comum. O objetivo deste trabalho foi avaliar a eficácia de um método que propõe aumentar a permeação cutânea do diclofenaco de sódio incorporado a um gel, por meio do uso da CLF. A influência sobre a permeação foi avaliada ex vivo, utilizando célula de Franz e pele humana obtida de cirurgia plástica. Os resultados foram balizados mediante aplicação de métodos estatísticos e análise exploratória de dados: clusters, k-means e Análise por Componentes Principais. Os resultados demonstraram aumento na concentração do diclofenaco de sódio na derme com o uso do laser. Em todas as amostras (com ou sem aplicação de laser), observou-se, uma quantidade de diclofenaco de sódio na superfície da pele e que não houve passagem de ativo para o líquido do receptor, sugerindo que o diclofenaco de sódio não foi absorvido. Estes resultados indicam que CLF usada sob as condições descritas neste estudo é capaz de aumentar a penetração do diclofenaco de sódio e sua retenção em camadas mais profundas da pele Unitermos: Crio Laser Forese/uso em dermatologia. Permeação cutânea. Diclofenaco de sódio/perme...

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Natural products as potential drug permeation enhancer in transdermal drug delivery system

Cited by 53 publications

References 63 publications

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes

Review on Transdermal Drug Delivery Systems

Performance evaluation of Cryo Laser Phoresis technique as biophysical method to promote diclofenac sodium cutaneous perfusion

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