Preparation and evaluation of lidocaine hydrochloride-loaded TAT-conjugated polymeric liposomes for transdermal delivery

Wang, Yue; Su, Wenying; Li, Qin; Li, Changyi; Wang, Hanjie; Li, Yuchen; Cao, Yanjun; Chang, Jin; Zhang, Lianyun

doi:10.1016/j.ijpharm.2012.10.019

Cited by 63 publications

(36 citation statements)

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“…The confocal images can be obtained in the plane parallel to sample surface or in the plane perpendicular (Wu et al, 2009). This method has been widely used in assessing drug penetration or distribution in the skin layers following topical application of microparticles, nanoparticles and vesicular systems such as liposomes, niosomes etc (Desai et al, 2013;Khurana et al, 2013;Verma et al, 2013;Wang et al, 2013).…”

Section: Confocal Laser Scanning Microscopymentioning

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: Confocal Laser Scanning Microscopymentioning

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 EE and DL of the TAT-NLCs-LID and NLCs-LID were measured by gel filtration method using Sephadex G50 Column (GE Healthcare Bio-Sciences, Pittsburgh, PA) (Vitorino et al, 2013;Wang et al, 2013). The free LID was separated from the NLCs and the content of free drug was measured by using HPLC, performed on an Agilent 1100 series with a zorbax RP-select B column (Agilent Technologies, Santa Clara, CA) and the mobile phase was a mixture of 0.01 M sodium dihydrogen phosphate-methanol (25:75, v/v).…”

Section: Encapsulation Efficiency (Ee) and Drug Loading (Dl)mentioning

confidence: 99%

“…In vitro skin permeation studies were performed using Franz diffusion cells (Junyaprasert et al, 2008;Wang et al, 2013). Kunming mice were sacrificed by dislocation.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

“…Topical or transdermal administration of LA drugs has been an interesting area for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs (Negi et al, 2016). Compared to injection pathway, transdermal drug delivery (TDD) of LA agents has the following advantages: improved patient compliance; fewer side effects; continuous drug delivery; avoiding the hepatic first pass effect (Trotta et al, 2002;Wang et al, 2013). However, the main challenge in TDD is to overcome the barrier of the stratum corneum (the outermost layer of the skin) for most of the incoming substances (Alam et al, 2016;Vitorino et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

“…Recently, TAT has opened new avenues in the field of TTD to deliver various molecules such as ketoprofen, celecoxib, peptides and lidocaine (LID) hydrochloride across the skin (Shah et al, 2012;Wang et al, 2013;Ookubo et al, 2014). The results indicated that TAT has the potential to carry their payloads across the skin layers.…”

Section: Introductionmentioning

confidence: 99%

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Transcriptional transactivator peptide modified lidocaine-loaded nanoparticulate drug delivery system for topical anesthetic therapy

Wang¹,

Wang

Shi

2016

Drug Delivery

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Purpose: For the topical anesthetic, transcriptional transactivator peptide (TAT) modified lidocaine (LID) loaded nanostructured lipid carriers (TAT-NLCs-LID) were prepared and then used for improving transdermal delivery of local anesthetic drug. Methods: In this study, TAT was conjugated with Distearoyl phosphatidylethanolamine-(polyethylene glycol) 2000 -maleimide (DSPE-PEG 2000 -Mal) to obtain TAT-PEG 2000 -DSPE. TAT-NLCs-LID were successfully prepared and characterized by determination of their particle size, morphology, drug encapsulation efficiency and in vitro drug release behavior. The skin permeation of LID-LNPs was examined using a Franz diffusion cell mounted with depilated mouse skin in vitro and in vivo anesthesia effect was evaluated on mice. Results:The results showed that TAT-NLCs-LID have substantially small mean diameter (157.9 nm) and high encapsulation efficiency (81.8%). From the in vitro skin permeation results, transdermal flux of TAT-NLCs-LID was about several times higher than that of LID solution and NLCs-LID. In vivo anesthesia effect evaluation illustrated that TAT-NLCs-LID can enhance the transdermal delivery of LID by reducing the pain threshold in mice. Conclusion: These results indicate that the novel TAT containing drug delivery system is very useful for overcoming the barrier function of the skin and could deliver anesthetic through the skin. TAT-NLCs-LID could function as promising topical anesthetic system.

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