Potential use of nanoparticles for transcutaneous vaccine delivery: effect of particle size and charge

Kohli, A.K.; Alpar, H. Oya

doi:10.1016/j.ijpharm.2003.10.038

Cited by 248 publications

(126 citation statements)

References 14 publications

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“…Vogt et al have showed that particles of 40 nm size have penetrated through the depth of 225 µm or in the region of epidermis or papillary dermis (Vogt et al, 2006). Kohli and Alpar (2004) have shown that the penetrability of nanoparticles across the skin depends not only on the size but also on the charge present on the surface of the particles. In general, most of the studies have demonstrated the penetrability of nanoparticles in the size range of <40 nm regardless of the surface charge across the SC via follicular as well as intercellular pathways.…”

Section: Drug Depot In Skinmentioning

confidence: 99%

Basic considerations in the dermatokinetics of topical formulations

Nair

Jacob

Al‐Dhubiab

et al. 2013

Braz. J. Pharm. Sci.

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Assessing the bioavailability of drug molecules at the site of action provides better insight into the efficiency of a dosage form. However, determining drug concentration in the skin layers following topical application of dermatological formulations is a great challenge. The protocols followed in oral formulations could not be applied for topical dosage forms. The regulatory agencies are considering several possible approaches such as tape stripping, microdialysis etc. On the other hand, the skin bioavailability assessment of xenobiotics is equally important for topical formulations in order to evaluate the toxicity. It is always possible that drug molecules applied on the skin surface may transport thorough the skin and reaches systemic circulation. Thus the real time measurement of molecules in the skin layer has become obligatory. In the last two decades, quite a few investigations have been carried out to assess the skin bioavailability and toxicity of topical/dermatological products. This review provides current understanding on the basics of dermatokinetics, drug depot formation, skin metabolism and clearance of drug molecules from the skin layers following application of topical formulations.Uniterms: Dermatological formulations/pharmacokinetics. Dermatological formulations/ toxicity. Dermatokinetics. Skin/metabolism. Microdialysis. Tape stripping.A avaliação da biodisponibilidade de moléculas de fármacos no sítio de ação oferece melhor compreensão sobre a eficiência da forma de dosagem. Entretanto, a determinação da concentração de fármaco nas camadas da pele em seguida à aplicação tópica de formulações dermatológicas é um grande desafio. Os protocolos seguidos para as formulações orais não podem ser aplicados para as formulações tópicas. As agências regulatórias consideram várias abordagens possíveis, tape stripping, microdiálise etc. Por outro lado, a avaliação da biodisponibilidade de xenobióticos na pele é igualmente importante para as formulações tópicas para se avaliar a toxicidade. É sempre possível que as moléculas de fármaco aplicadas na superfície da pele sejam transportadas através da pele e alcancem a circulação sistêmica. Assim, a medida em tempo real de moléculas na camada da pele tem se tornado obrigatória. Nas últimas duas décadas, realizaram-se poucas pesquisas para avaliar a biodisponibilidade da pele e a toxicidade de produtos tópicos/dermatológicos. Esta revisão fornece a compreensão atual com base na dermatocinética, formação de fármaco de depósito, metabolismo da pele e o clearance das moléculas de fármaco das camadas da pele em seguida à aplicação de formulações tópicas.Unitermos: Formulações dermatológicas/farmacocinética. Formulações dermatológicas/toxicidade. Dermatocinética Pele/metabolismo. Microdiálise. Tape stripping.

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Section: Drug Depot In Skinmentioning

confidence: 99%

Basic considerations in the dermatokinetics of topical formulations

Nair

Jacob

Al‐Dhubiab

et al. 2013

Braz. J. Pharm. Sci.

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“…The nano-size of NLCs allowed the particles to be in close contact with the outer layer skin cells to increase the fluidity of the skin and then compelled the nanoparticles into the deeper skin layer. 46 The components composing the NLCs were reported to have a permeation ability which could facilitate the penetration of nanoparticles into the deeper skin layer. 47 The sustained release of NLCs also contributed to the enhancement of the permeation of capsaicin.…”

mentioning

confidence: 99%

Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation

Wang¹,

Gao²,

Niu³

et al. 2017

IJN

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Capsaicin has been used in clinical applications for the treatment of pain disorders and inflammatory diseases. Given the strong pungency and high oil/water partition coefficient of capsaicin, capsaicin-loaded nanolipoidal carriers (NLCs) were designed to increase permeation and achieve the analgesic, anti-inflammatory effect with lower skin irritation. Capsaicin-loaded NLCs were prepared and later optimized by the Box–Behnken design. The physicochemical characterizations, morphology, and encapsulation of the capsaicin-loaded NLCs were subsequently confirmed. Capsaicin-loaded NLCs and capsaicin-loaded NLCs gel exhibited sustained release and no cytotoxicity properties. Also, they could significantly enhance the penetration amount, permeation flux, and skin retention amounts of capsaicin due to the application of NLCs. To study the topical permeation mechanism of capsaicin, 3,3′-dioctadecyloxacarbocyanine perchlorate (Dio) was used as a fluorescent dye. Dio-loaded NLCs and Dio-loaded NLCs gel could effectively deliver Dio up to a skin depth of 260 and 210 μm, respectively, primarily through the appendage route on the basis of version skin sections compared with Dio solution, which only delivered Dio up to 150 μm. In vivo therapeutic experiments demonstrated that capsaicin-loaded NLCs and capsaicin-loaded NLCs gel could improve the pain threshold in a dose-dependent manner and inhibit inflammation, primarily by reducing the prostaglandin E2 levels in the tissue compared with capsaicin cream and capsaicin solution. Meanwhile, skin irritation was reduced, indicating that application of NLCs could decrease the irritation caused by capsaicin. Overall, NLCs may be a potential carrier for topical delivery of capsaicin for useful pain and inflammation therapy.

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“…11,12 Because cells are so densely packed inside the hydrophobic SC, passage of charged, hydrophilic, and large drug molecules is extremely limited. 13 Nevertheless, hydrophilic pharmaceutical compounds can enter the skin through hair follicles and tight junctions, which are skin barrier regulators in the viable epidermis.…”

Section: Hsiao Et Almentioning

confidence: 99%

Enhancing the in vivo transdermal delivery of gold nanoparticles using poly(ethylene glycol) and its oleylamine conjugate

Hsiao

Peng

Tang

et al. 2016

IJN

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In this study, we investigated the effect of (ethylene glycol) (PEG) and PEG–oleylamine (OAm) functionalization on the skin permeation property of gold nanoparticles (GNS) in vivo. Chemisorption of polymers onto GNS was verified by a red shift in the ultraviolet–visible spectrum as well as by a change in the nanoparticle surface charge. The physicochemical properties of pristine and functionalized nanoparticles were analyzed by ultraviolet–visible spectroscopy, zeta potential analyzer, and transmission electron microscopy. Transmission electron microscopy revealed that the interparticle distance between nanoparticles increased after GNS functionalization. Comparing the skin permeation profile of pristine and functionalized GNS, the follicular deposition of GNS increased twofold after PEG–OAm functionalization. Moreover, PEG- and PEG–OAm-functionalized nanoparticles were able to overcome the skin barrier and deposit in the deeper subcutaneous adipose tissue. These findings demonstrate the potential of PEG- and PEG–OAm-functionalized GNS in serving a multitude of applications in transdermal pharmaceuticals.

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Potential use of nanoparticles for transcutaneous vaccine delivery: effect of particle size and charge

Cited by 248 publications

References 14 publications

Basic considerations in the dermatokinetics of topical formulations

Basic considerations in the dermatokinetics of topical formulations

Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation

Enhancing the in vivo transdermal delivery of gold nanoparticles using poly(ethylene glycol) and its oleylamine conjugate

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