Terpene-Containing PEGylated Liposomes as Transdermal Carriers of a Hydrophilic Compound

Rangsimawong, Worranan; Opanasopit, Praneet; Rojanarata, Theerasak; Ngawhirunpat, Tanasait

doi:10.1248/bpb.b14-00535

Cited by 36 publications

(15 citation statements)

References 32 publications

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“…The polarity of the bilayer vesicles in the presence of PEGylated-lipids was more than that of the non-PEG modified liposomes. Thus, 15,20) For the niosome formulations, the %EE was 29 to 41%. The %EE of the niosomes was higher than that of the PEGylated niosomes (NIP1-4), suggesting that the PEG chain may make the niosome structure more rigid and decreased drug entrapment.…”

Section: Resultsmentioning

confidence: 99%

Skin Transport of Hydrophilic Compound-Loaded PEGylated Lipid Nanocarriers: Comparative Study of Liposomes, Niosomes, and Solid Lipid Nanoparticles

Rangsimawong

Opanasopit

Rojanarata

et al. 2016

Biological & Pharmaceutical Bulletin

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The effect of surface grafting with N-(carbonyl-methoxypolyethylene glycol-2000)-1,2-distearoyl-snglycero-3-phosphoethanolamine (PEG2000-DSPE) onto three types of lipid nanocarriers, liposomes, niosomes and solid lipid nanoparticles (SLNs) on the skin penetration of sodium fluorescein (NaFI) was investigated. Confocal laser scanning microscopy (CLSM) was used to visualize the penetration pathways. Fourier transform infrared spectroscopy (FT-IR) was used to determine the skin hydration. The results showed that the physicochemical properties of each nanocarrier were modified after PEG grafting. In the skin penetration study, PEG grafting increased the flux of NaFI-loaded PEGylated liposomes and significantly decreased the flux of NaFI-loaded PEGylated niosomes and NaFI-loaded PEGylated SLNs. The skin deposition study and CLSM images showed that the intact liposome vesicles permeated into the skin. The niosomes and SLNs had little or no vesicles in the skin, suggesting that NaFI may have been released from these nanocarriers before permeation. Additionally, the fluorescent CLSM images of the SLNs showed that NaFI deposited along the length of hair follicles inside the skin, indicating that the skin penetration route may be through the transfollicular pathway. For the PEGylated nanocarriers, the PEGylated liposomes had higher fluorescence intensities than the non-PEGylated liposomes, indicating higher NaFI concentrations. The PEGylated niosomes and PEGylated SLNs had lower fluorescence intensities than those of the non-PEG modified niosomes and SLNs. For FT-IR results, PEGylated liposomes increased the skin hydration, while the grafting PEG onto niosomes and SLN surfaces decreased the skin hydration. This study showed that the surface grafting of PEG onto various nanocarriers affected the skin transport of NaFI.Key words PEGylated nanocarrier; liposome; niosome; solid lipid nanoparticle; hydrophilic compound; skin penetration Transdermal routes provide a controlled and non-invasive method of drug delivery. The outermost layer of skin, the stratum corneum, is a major protective barrier against the ingress of xenobiotics and controls the rate of water loss from the body. Therefore, drug transports via simple vehicles are unable to achieve therapeutic drug concentrations. Many strategies for enhancing skin penetration have been developed, such as chemical penetration, supersaturated systems, vesicles or physical mechanisms. A few examples of these strategies include the use of prodrugs, iontophoresis, electroporation, and ultrasound. 1)Lipid-based nanocarriers are the most sought after devices for topical and transdermal delivery applications. These nanocarriers include liposomes, niosomes, ethosomes, transferosomes, solid lipid nanoparticles (SLNs) and nanostructure lipid carriers (NLCs) have been extensively studied for the transdermal delivery of drugs. Liposomes have the potential to be drug-carrier systems for transdermal delivery. They contain amphipathic phospholipids arranged in one or more concentric bilayers ...

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Section: Resultsmentioning

confidence: 99%

Skin Transport of Hydrophilic Compound-Loaded PEGylated Lipid Nanocarriers: Comparative Study of Liposomes, Niosomes, and Solid Lipid Nanoparticles

Rangsimawong

Opanasopit

Rojanarata

et al. 2016

Biological & Pharmaceutical Bulletin

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“…17 The drug entrapment efficiency of CL, PL, and PL-LI was 17.33%±1.13%, 21.76%±1.56%, and 29.60%±2.35%, respectively. According to the presence of PEG-lipids in the liposome formulation, the membrane bilayer became more polar and the efficiency of incorporation of the hydrophilic drug increased.…”

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“…16 In addition, our previous work reported that d-limonene containing PL provided a synergistic effect to enhance penetration of hydrophilic compounds into and through the skin. 17 Therefore, the aim of this study was to investigate the effect of low frequency SN (20 kHz) on the follicular pathway for transport of sodium fluorescein (NaFI)-loaded PL into porcine skin. PL containing d-limonene has been used as a carrier to enhance transdermal delivery of hydrophilic NaFI, with the transfollicular pathway as the major penetration pathway.…”

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Mechanistic study of decreased skin penetration using a combination of sonophoresis with sodium fluorescein-loaded PEGylated liposomes with D-limonene

Rangsimawong

Opanasopit

Rojanarata

et al. 2015

IJN

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The effect of low frequency sonophoresis (SN, 20 kHz) on the skin transport of sodium fluorescein (NaFI)-loaded liposomes was investigated. An in vitro skin penetration study in open and blocked hair follicles was performed, and confocal laser scanning microscopy and scanning electron microscopy were used to visualize the penetration pathways. The results showed that SN significantly increased the flux of NaFI solution, whereas it significantly decreased the flux of NaFI-loaded polyethylene glycol-coated (PEGylated) liposomes with D-limonene (PL-LI). SN did not significantly affect the flux of NaFI-loaded conventional liposomes and PEGylated liposomes. In the blocked follicles, the flux of NaFI-loaded PL-LI both with and without SN decreased, indicating that NaFI-loaded PL-LI penetrated the skin via the transfollicular pathway. A confocal laser scanning microscopy image showed that in the skin without SN, the fluorescence intensity of NaFI-loaded PL-LI was observed in the skin and along the length of hair inside the skin, whereas in the skin with applied SN, the fluorescence intensity was detected only on the top of hair outside the skin. From scanning electron microscopy images, SN dislocated the corneocytes and reduced the deposition of PL-LI around hair follicles. These results revealed that SN may partially plug hair follicle orifices and reduce percutaneous absorption through the follicular pathway.

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“…Os LCs são formados geralmente por fosfolipídios, com ou sem a adição de colesterol. Em 1992, CEVC e BLUME (1992) introduziram os lipossomas ultradeformáveis, usualmente chamados de Transfersomas® (IDEA AG, Munique, Alemanha).Lipossomas ultradeformáveis (UDL) são vesículas formadas por fosfolipídios e tensoativos, tais como surfactantes ou co-solventes que são capazes de enfraquecer as bicamadas lipídicas, diminuindo a tensão superficial, o que permite ao lipossoma mudar 23 a sua forma e, por conseguinte, levar a um aumento da deformabilidade das bicamadas que lhes permite por si só passar entre as células (ASCENSO et al, 2015) (Figura 9).Em virtude de sua natureza elástica e deformação, seu emprego como sistema de liberação transdérmica vem sendo recentemente estudado (CADDEO et al, 2015;LI et al, 2014c;RANGSIMAWONG et al, 2014;SAUVAGEOT et al, 2009;TYAGI et al, 2015). A eficácia dos UDLs tanto para sistemas de liberação dérmica e transdérmica tem mostrado resultados promissores encapsulando fármacos de diversos tamanhos moleculares e lipofilicidade diferentes, como por exemplo: lidocaína, tetracaína, hidrocortisona, dexametasona, o diclofenaco, o tamoxifeno, a testosterona (DUANGJIT et al, 2012;GHARIB et al, 2015;MAESTRELLI et al, 2010; SRISUK et al, 2012).…”

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Estudos fotofísicos e fotobiológicos de sistemas de liberação contendo o fármaco fotossensível cloro-ftalocianina de alumínio para aplicação em terapia fotodinâmica

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Estudos fotofísicos e fotobiológicos de sistemas de liberação contendo o fármaco fotossensível cloro-ftalocianina de alumínio para aplicação em terapia fotodinâmica UNIVERSIDADE DE SÃO PAULO FACULDADE DE CIÊNCIAS FARMACÊUTICAS DE RIBEIRÃO PRETOEstudos fotofísicos e fotobiológicos de sistemas de liberação contendo o fármaco fotossensível cloro-ftalocianina de alumínio para aplicação em terapia fotodinâmica A terapia fotodinâmica (TFD) tem se apresentado nos últimos anos como uma alternativa para o tratamento de tumores cutâneos, viscerais e sistêmicos, demonstrando resultados promissores, tanto em estudos in vitro como in vivo. Trata-se de uma técnica simples e não invasiva. A terapia consiste na excitação de um fármaco fotossensibilizante por uma fonte de luz visível que depois de absorvida pela molécula, leva a produção espécies reativas de oxigênio (EROs) em presença do oxigênio molecular por uma sequencia de reações fotoquímicas. Nesse trabalho propõe-se a preparação, caracterização e detreminação da atividade fotodinâmica de uma nanoemulsão rica em colesterol e de lipossomas ultradeformáveis como novos sistemas formulations demonstrated that the incorporation was able to improve its photophysical characteristics. In in vitro studies, the drug delivery systems showed no cytotoxicity in the absence of light, but demonstrated increased in PcAlCl photodynamic activity up to 80% over the PcAlCl free when irradiated. All formulations showed characteristics, which cooperates with the use of these drug delivery systems for, increased the PcAlCl photodynamic activity for glioblastoma and melanoma treatment.Keywords: Glioblastoma, Melanoma, Liposome, LDE, Photodynamic therapy. 1 1. Introdução Gliomas e a barreira hematoencefálica (BHE)Gliomas malignos estão entre os tipos mais comuns de tumores cerebrais, ocorrendo em 5-7 a cada 100.000 indivíduos por ano (LARJAVAARA et al., 2007;SEHMER et al., 2014 et al., 2016). Esse tipo de patologia é sempre associado a um prognóstico ruim, podendo acometer qualquer parte do tecido cerebral e da medula espinhal, e a uma expectativa de vida muito curta entre 12 e 15 meses (ROBERTS et al., 2011;SCHNEIDER et al., 2016). Como opção mais utilizada de tratamento, adota-se ressecção cirúrgica, seguida por tratamento com radiação e quimioterapia com Temozolamida, que combinadas conferem um período médio de sobrevivência do paciente de até 14,6 meses (STUPP , MASON e VAN DEN BEUF, 2005;ZHANG et al., 2016). Contudo, às células do glioma tem apresentado resistência à radiação e a quimioterapia com base nos protocolos difundidos utilizados frequentemente (JOHANSSON et al., 2010). Além disso, a natureza das células tumorais do GBM e a existência de barreiras fisiológicas, especialmente a barreira hematoencefálica (BHE), o GBM continua sem cura. A falta da capacidade de permeação de fármacos na BHE faz com que o tratamento quimioterápico do glioblastoma seja limitado (LI et al., 2014c).A barreira hematoencefálica (BHE) é uma barreira celular que separa o sangue do tecido cerebral que regula a ...

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Terpene-Containing PEGylated Liposomes as Transdermal Carriers of a Hydrophilic Compound

Cited by 36 publications

References 32 publications

Skin Transport of Hydrophilic Compound-Loaded PEGylated Lipid Nanocarriers: Comparative Study of Liposomes, Niosomes, and Solid Lipid Nanoparticles

Skin Transport of Hydrophilic Compound-Loaded PEGylated Lipid Nanocarriers: Comparative Study of Liposomes, Niosomes, and Solid Lipid Nanoparticles

Mechanistic study of decreased skin penetration using a combination of sonophoresis with sodium fluorescein-loaded PEGylated liposomes with D-limonene

Estudos fotofísicos e fotobiológicos de sistemas de liberação contendo o fármaco fotossensível cloro-ftalocianina de alumínio para aplicação em terapia fotodinâmica

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