Penetration Enhancement of Transdermal Delivery-Current Permutations and Limitations

Purdon, Carryn H.; Azzi, Chad G; Zhang, Jin; Smith, Eric W.; Maibach, Howard I.

doi:10.1615/critrevtherdrugcarriersyst.v21.i2.20

Cited by 65 publications

(43 citation statements)

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“…Diferentes estratégias têm sido testadas com o objetivo de romper a barreira imposta pela camada córnea e aumentar a passagem de fármacos através da pele, incluindo o emprego de sistemas nanoestruturados lipídicos. 43,44 O aumento da superfície de contato do fármaco com os corneócitos, o efeito oclusivo provocado sobre a pele, a rápida e constante liberação do fármaco e a ação do surfactante sobre a permeabilidade parecem estar envolvidos no aumento da permeação cutânea de fármacos a partir destes nanocarreadores. 45,46 Assim, buscando obter formulações destinadas à administração tópica cutânea, a encapsulação do resveratrol em sistemas nanoestruturados lipídicos foi realizada usando o método de difusão do solvente a quente para a preparação das suspensões coloidais.…”

Section: Resultsunclassified

Preparação e caracterização de suspensões coloidais de nanocarreadores lipídicos contendo resveratrol destinados à administração cutânea

Nemen¹,

Lemos‐Senna²

2011

Quím. Nova

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CUTANEOUS ADMINISTRATION. Solid lipid nanoparticles (SLN), nanoemulsions (NE), and microemulsions (ME) were prepared by the hot solvent diffusion method, using tristearin or castor oil as oily phase, and soy lecithin and Solutol HS 15 as surfactants. Mean particle sizes ranged from 20 to 215 nm and negative zeta potentials were obtained for all nanocarriers. A HPLC method used to determine resveratrol was specific, linear, exact and precise. The entrapment efficiency was high for all formulations. However, resveratrol content was significantly varied among the lipid nanocarriers. Lipid nanocarrier containing hydrogels exhibiting pseudoplastic behavior were obtained after incorporation of hydroxyethylcellulose in the colloidal dispersions.Keywords: resveratrol; lipid-based nanocarriers; hydrogels. INTRODUÇÃOO resveratrol (3,4,5-tri-hidroxiestilbeno) (Figura 1) é uma fitoalexina presente numa grande variedade de espécies vegetais, incluindo amoras, amendoins e uvas, e, portanto, é um constituinte da dieta humana. Este composto, tal como outros membros da família do estilbeno, é produzido nos vegetais em resposta ao ataque de patógenos, à radiação ultravioleta e à exposição ao ozônio. A Vitis vinifera, ou a uva, sintetiza o resveratrol como meio de proteção às infecções fún-gicas, sendo, portanto, encontrado em altas concentrações no vinho. 1,2 Vários estudos têm destacado e comprovado os benefícios do resveratrol à saúde. Esta substância tem demonstrado propriedades quimiopreventivas, 3-8 antioxidante, 9,10 antiplaquetária, 11 antifúngica, 12 anti-inflamatória, 13 cardioprotetora, 14,15 entre outras. O resveratrol age como efetor biológico pleiotrópico que regula as três fases do processo da carcinogênese, ou seja, início, promoção e progressão do tumor. 1 Uma vez absorvidos, os agentes quimiopreventivos podem agir por diferentes mecanismos, seja pela inibição da ativação metabólica de compostos carcinogênicos, estímulo da detoxificação de metabólitos reativos, prevenção da sua interação com o DNA da célula e supressão da progressão do tumor. Experimentos in vitro, ex vivo e in vivo têm demonstrado que além de atuar nos mecanismos quimiopreventivos descritos acima, o resveratrol também possui potencial quimioterapêutico. De fato, o resveratrol suprime o crescimento de várias linhagens de células cancerosas, em parte pela inibição da DNA polimerase e ribonucleotídeo redutase ou pela indução da suspensão do ciclo celular ou apoptose. 16 Os efeitos anticarcinogênicos provocados pelo resveratrol também parecem estar associados à sua atividade antioxidante, visto que ele tem demonstrado inibir a ciclo-oxigenase, hidroperoxidase, proteína quinase C, fosforilação da Bcl-2, proteína quinase B (PKB ou Akt), quinase de adesão focal, NF-κB, metaloprotease de matriz tipo 9, e reguladores do ciclo celular. 17 O resveratrol também inibe a oxidação da LDL, por modular a atividade do metabolismo de lipídeos e lipoproteínas, 2,18 suprime a angiogênese 18 e apresenta atividade estrogênica devido a sua semelhança estrutural com o ag...

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Section: Resultsunclassified

Preparação e caracterização de suspensões coloidais de nanocarreadores lipídicos contendo resveratrol destinados à administração cutânea

Nemen¹,

Lemos‐Senna²

2011

Quím. Nova

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“…Several approaches have been explored that provide additional driving force in the form of electrical (iontophoresis) [48] or ultrasound (sonophoresis) [49] energies, structural perturbation of SC (e.g., electroporation, thermal microporation, microneedles), [50] penetration enhancers, [51,52] or a combination of these strategies.…”

Section: Approaches For Transdermal Deliverymentioning

confidence: 99%

Non Invasive Delivery of Protein and Peptide Drugs: A Review

Lakshmi

Prasanthi

Veeresh

2017

Asian J Pharm Clin Res

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The most common and improved bioavailable route for protein and peptide drugs is injectable route. These drugs are generally preferred to give in invasive route to get high bioavailability though possessing disadvantages and the major one is patient non-compliance. Hence, various non-invasive route of administration has been under research for these drugs to fetch more advantages. Although bioavailability is a major problem with non-invasive route such as oral, nasal, ocular, transdermal, rectal, colon, and vaginal route, these routes have been preferred compared to existing invasive one. Many researches have been conducted in this area, but achieving success is significantly challenging. The nasal delivery has been successfully exploited for vaccines compare to all other non-invasive drug delivery system. Currently, only molecule to reach market is oral cyclosporine. The present review aims to discuss the potential non-invasive routes of protein and peptide drug delivery. The factors which will affect drug permeation, and the bioavailability of proteins administered through these routes is also emphasized.

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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%

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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Penetration Enhancement of Transdermal Delivery-Current Permutations and Limitations

Cited by 65 publications

References 0 publications

Preparação e caracterização de suspensões coloidais de nanocarreadores lipídicos contendo resveratrol destinados à administração cutânea

Preparação e caracterização de suspensões coloidais de nanocarreadores lipídicos contendo resveratrol destinados à administração cutânea

Non Invasive Delivery of Protein and Peptide Drugs: A Review

Review on Transdermal Drug Delivery Systems

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