The applications of Vitamin E TPGS in drug delivery

Guo, Yuanyuan; Luo, Jun; Tan, Songwei; Otieno, Ben Oketch; Zhang, Zhiping

doi:10.1016/j.ejps.2013.02.006

Cited by 448 publications

(286 citation statements)

References 122 publications

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“…[18][19][20][21] Other than being an excellent emulsifier, TPGS itself has been reported to have anticancer efficacy because of its function as an inhibitor of P-glycoprotein to surmount multidrug resistance in tumor cells. [22][23][24] In this work, the TPGS-b-PCL copolymer was synthesized and characterized. The genistein-loaded NPs were prepared with a modified nanoprecipitation method instead of solvent extraction/evaporation method and characterized.…”

Section: Introductionmentioning

confidence: 99%

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Zhang¹,

Gan²,

Zeng³

et al. 2015

IJN

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Genistein is one of the most studied isoflavonoids with potential antitumor efficacy, but its poor water solubility limits its clinical application. Nanoparticles (NPs), especially biodegradable NPs, entrapping hydrophobic drugs have promising applications to improve the water solubility of hydrophobic drugs. In this work, TPGS- b -PCL copolymer was synthesized from ε-caprolactone initiated by d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) through ring-opening polymerization and characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, gel permeation chromatography, and thermogravimetric analysis. The genistein-loaded NPs were prepared by a modified nanoprecipitation method and characterized in the aspects of particle size, surface charge, morphology, drug loading and encapsulation efficiency, in vitro drug release, and physical state of the entrapped drug. The TPGS- b -PCL NPs were found to have higher cellular uptake efficiency than PCL NPs. MTT and colony formation experiments indicated that genistein-loaded TPGS- b -PCL NPs achieved the highest level of cytotoxicity and tumor cell growth inhibition compared with pristine genistein and genistein-loaded PCL NPs. Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS- b -PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice. In conclusion, the results suggested that genistein-loaded biodegradable TPGS- b -PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

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Section: Introductionmentioning

confidence: 99%

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Zhang¹,

Gan²,

Zeng³

et al. 2015

IJN

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“…In the present study, as shown above, the incorporation of nicotine in both lamellar and cubic phases enhanced the in vitro permeation and penetration in the skin. A possible explanation may be the action of Vitamin E-TPGS and IPM as penetration enhancers (Guo et al, 2013;Aggarwal, Goindi, Mehta, 2012;Engelbrecht et al, 2012). Indeed, it has been reported that Vitamin E acts as a permeation enhancer by intercalating within the lipid bilayer region of the SC, promoting changes of membrane permeability (Trivedi, Krill, Fort, 1995), while IPM acts as penetration enhancer by introducing phase separation and perturbing the multilamellar lipid assembly (Engelbrecht et al, 2012).…”

Section: Discussionmentioning

confidence: 99%

Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

Borgheti-Cardoso

Vicentini

Gratieri

et al. 2016

Braz. J. Pharm. Sci.

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Transdermal nicotine patches have been used in smoking cessation therapy, suggested for the treatment of skin disorders with eosinophilic infiltration and have been found to improve attention performance in patients with Alzheimer's disease and age-associated memory impairment. However, skin irritation with extended patch use is still a problem. The aim of this work was to develop a simple to prepare liquid crystalline system containing vitamin E TPGS that would be able to control nicotine delivery and reduce irritation and sensitization problems. The liquid crystalline phases were macroscopically characterized by visual analysis and examined microscopically under a polarized light microscope. Topical and transdermal delivery of nicotine were investigated in vitro using porcine ear skin mounted on a Franz diffusion cell. Nicotine skin permeation from the developed cubic phase followed zero-order kinetics (r = 0.993) and was significantly enhanced after 12 h when compared to the control formulation (nicotine solution) (p < 0.05) (138.86 ± 20.44 and 64.91 ± 4.06 μg/cm 2 , respectively). Cubic phase was also able to target viable skin layers in comparison to control solution (8.18 ± 1.89 and 2.63 ± 2.51 μg/cm 2 , respectively). Further studies to evaluate skin sensitization and irritation are now necessary.Uniterms: Nicotine/transdermal patches. Nicotine/controlled transdermal delivery. Liquid crystalline systems/development. Vitamin E TPGS. Skin irritation/control/in vitro study. Skin irritation/use of transdermal patches.Adesivos transdérmicos de nicotina são utilizados para cessação de fumar, tratamento de problemas de pele com infiltração de eosinófilos e para melhorar a atenção em pacientes com doença de Alzheimer e enfraquecimento da memória associada à idade. No entanto, a irritação da pele com o uso prolongado dos adesivos ainda é um problema. O objetivo deste trabalho foi desenvolver sistema líquido cristalino (SLC) de preparo simples contendo vitamina E TPGS capaz de controlar a liberação de nicotina e reduzir os problemas de irritação cutânea. Os SLCs foram caracterizados por análise visual e microscopia de luz polarizada. As administrações tópica e transdérmica de nicotina foram investigadas in vitro utilizando pele de orelha de porco em célula de difusão de Franz. A permeação da nicotina veiculada pela fase cúbica desenvolvida seguiu cinética de ordem zero (r = 0,993) e foi significativamente maior do que o controle (solução de nicotina) após 12 h (p < 0,05) (138,86 ± 20,44 e 64,91 ± 4,06 µg/cm 2 , respectivamente). A fase cúbica também promoveu aumento da penetração de nicotina nas camadas viáveis da pele quando comparado ao controle (8,18 ± 1,89 e 2,63 ± 2,51 µg/cm 2 , respectivamente). Estudos futuros para avaliar a sensibilização e irritação da pele são necessários.

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“…They are named as modulators and they exert effect by interacting membrane lipids and inhibiting P-glycoprotein (MDR protein) [22,23] . So cell membrane is the very important target of MDR modulators.…”

Section: Discussionmentioning

confidence: 99%

Exploring a natural MDR reversal agent: potential of medicinal food supplement Nerium oleander leaf distillate

Kars

Gündüz

Üney

et al. 2013

Asian Pacific Journal of Tropical Biomedicine

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The applications of Vitamin E TPGS in drug delivery

Cited by 448 publications

References 122 publications

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells

Liquid crystalline systems containing Vitamin E TPGS for the controlled transdermal nicotine delivery

Exploring a natural MDR reversal agent: potential of medicinal food supplement Nerium oleander leaf distillate

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