The applications of Vitamin E TPGS in drug delivery.

doi:10.1016/J.EJPS.2013.02.006

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The applications of Vitamin E TPGS in drug delivery.

Journal Article•DOI•

The applications of Vitamin E TPGS in drug delivery.

Yuanyuan Guo¹, Jun Luo², Songwei Tan¹, Ben Oketch Otieno¹, Zhiping Zhang¹ - Show less +1 more•Institutions (2)

Huazhong University of Science and Technology¹, Zhejiang University²

13 May 2013-European Journal of Pharmaceutical Sciences (Eur J Pharm Sci)-Vol. 49, Iss: 2, pp 175-186

TL;DR: TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, adjuvant in vaccine systems, nutrition supplement, plasticizer of film, anticancer reagent and so on are discussed.

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About: This article is published in European Journal of Pharmaceutical Sciences.The article was published on 2013-05-13. It has received 437 citations till now. The article focuses on the topics: Drug delivery.

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Journal Article•DOI•

Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

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Wei Xu¹, Peixue Ling, Tianmin Zhang•Institutions (1)

Shandong University¹

27 Jun 2013-Journal of drug delivery

TL;DR: The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

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Abstract: Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

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424 citations

Cites background from "The applications of Vitamin E TPGS ..."

...Therefore, it has advantages over PEG and Vitamin E in application of various drug delivery device, including extending the half-life of the drug in plasma and enhancing the cellular uptake [169]....
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Journal Article•DOI•

Recent Advances in the Application of Vitamin E TPGS for Drug Delivery.

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Conglian Yang¹, Tingting Wu¹, Yan Qi¹, Zhiping Zhang¹•Institutions (1)

Huazhong University of Science and Technology¹

01 Jan 2018-Theranostics

TL;DR: The recent advances of TPGS in drug delivery including T PGS based prodrugs, nitric oxide donor and polymers, and unmodified TPGs based formulations are discussed, focused on enhancing delivery efficiency as well as the therapeutic effect of agents.

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Abstract: D-ɑ-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) has been approved by FDA as a safe adjuvant and widely used in drug delivery systems. The biological and physicochemical properties of TPGS provide multiple advantages for its applications in drug delivery like high biocompatibility, enhancement of drug solubility, improvement of drug permeation and selective antitumor activity. Notably, TPGS can inhibit the activity of ATP dependent P-glycoprotein and act as a potent excipient for overcoming multi-drug resistance (MDR) in tumor. In this review, we aim to discuss the recent advances of TPGS in drug delivery including TPGS based prodrugs, nitric oxide donor and polymers, and unmodified TPGS based formulations. These potential applications are focused on enhancing delivery efficiency as well as the therapeutic effect of agents, especially on overcoming MDR of tumors. It also demonstrates that the clinical translation of TPGS based nanomedicines is still faced with many challenges, which requires more detailed study on TPGS properties and based delivery system in the future.

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262 citations

Cites background or methods from "The applications of Vitamin E TPGS ..."

...In our previous reviews [5, 6], we discussed TPGS as a molecular biomaterial and its original application in drug delivery....
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...It has been widely used in fabricating nanodrugs or other formulations for many poorly water-soluble or permeable drugs, especially for biopharmaceutics classification system (BCS) class II and IV drugs [5, 6]....
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...TPGS can be functionalized as an excellent solubilizer, emulsifier, permeation and bioavailability enhancer of hydrophobic drugs [6]....
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Journal Article•DOI•

Vitamin E-based nanomedicines for anti-cancer drug delivery

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Nicolas Duhem¹, Fabienne Danhier¹, Véronique Préat¹•Institutions (1)

Université catholique de Louvain¹

28 May 2014-Journal of Controlled Release

TL;DR: This review aims to highlight the development of novel vitamin E conjugates for the vectorization of active pharmaceutical ingredients through nanotechnologies, and describes the biology and the metabolic functions of vitamin E.

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211 citations

Journal Article•DOI•

Surface-Modified Nanocarriers for Nose-to-Brain Delivery: From Bioadhesion to Targeting

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Fabio Sonvico¹, Adryana Clementino¹, Francesca Buttini¹, Gaia Colombo², Silvia Pescina¹, Silvia Stanisçuaski Guterres³, Adriana Raffin Pohlmann³, Sara Nicoli¹ - Show less +4 more•Institutions (3)

University of Parma¹, University of Ferrara², Universidade Federal do Rio Grande do Sul³

15 Mar 2018-Pharmaceutics

TL;DR: In this review, nanomedicine delivery based on particle engineering exploiting surface electrostatic charges, mucoadhesive polymers, or chemical moieties targeting the nasal epithelium will be discussed and critically evaluated in relation to nose-to-brain delivery.

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Abstract: In the field of nasal drug delivery, nose-to-brain delivery is among the most fascinating applications, directly targeting the central nervous system, bypassing the blood brain barrier Its benefits include dose lowering and direct brain distribution of potent drugs, ultimately reducing systemic side effects Recently, nasal administration of insulin showed promising results in clinical trials for the treatment of Alzheimer’s disease Nanomedicines could further contribute to making nose-to-brain delivery a reality While not disregarding the need for devices enabling a formulation deposition in the nose’s upper part, surface modification of nanomedicines appears the key strategy to optimize drug delivery from the nasal cavity to the brain In this review, nanomedicine delivery based on particle engineering exploiting surface electrostatic charges, mucoadhesive polymers, or chemical moieties targeting the nasal epithelium will be discussed and critically evaluated in relation to nose-to-brain delivery

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192 citations

Cites methods from "The applications of Vitamin E TPGS ..."

..., diethylene glycol monoethyl ether, and Vitamin E TPGS were used to solubilize and enhance the absorption of the drugs through the nasal mucosa [135]....
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Journal Article•DOI•

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors.

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Agnese Gagliardi¹, Elena Giuliano¹, Eeda Venkateswararao², Massimo Fresta¹, Stefania Bulotta¹, Vibhudutta Awasthi², Donato Cosco¹ - Show less +3 more•Institutions (2)

Magna Græcia University¹, University of Oklahoma Health Sciences Center²

03 Feb 2021-Frontiers in Pharmacology

TL;DR: In this paper, the use of polymeric nanoparticles as drug delivery systems of anticancer compounds, their physico-chemical properties and their ability to be efficiently localized in specific tumor tissues have been described.

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Abstract: Advances in nanotechnology have favored the development of novel colloidal formulations able to modulate the pharmacological and biopharmaceutical properties of drugs. The peculiar physico-chemical and technological properties of nanomaterial-based therapeutics have allowed for several successful applications in the treatment of cancer. The size, shape, charge and patterning of nanoscale therapeutic molecules are parameters that need to be investigated and modulated in order to promote and optimize cell and tissue interaction. In this review, the use of polymeric nanoparticles as drug delivery systems of anticancer compounds, their physico-chemical properties and their ability to be efficiently localized in specific tumor tissues have been described. The nanoencapsulation of antitumor active compounds in polymeric systems is a promising approach to improve the efficacy of various tumor treatments.

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169 citations

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Heart-lung transplantation.

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Bartley P. Griffith¹•Institutions (1)

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TL;DR: A broad overview of the various grounds upon which this difference is likely based and discuss recent advances in each area: 1) criteria for the selection of candidates and donors, 2) methods for ex-vivo preservation of donor organs, 3) technical execution of the operative procedure, and 4) prevention of postoperative infection as discussed by the authors.

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Abstract: The survival rate (average, 50%) of patients undergoing cardiopulmonary transplantation falls well below that expected for cardiac transplantation alone. We give a broad overview of the various grounds upon which this difference is likely based and discuss recent advances in each area: 1) criteria for the selection of candidates and donors, 2) methods for ex-vivo preservation of donor organs, 3) technical execution of the operative procedure, and 4) prevention of postoperative infection. In connection with the prevention of postoperative infection, we discuss the potential for the development of a chronic obliterative disease that, once established, has proved inexorable. Current efforts are focused on detection when the process is in an early, reversible stage, and on research into causation. (Texas Heart Institute Journal 1987; 14:364-368)

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Maria Laura Immordino¹, Franco Dosio, Luigi Cattel•Institutions (1)

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20 Oct 2006-International Journal of Nanomedicine

TL;DR: Stealth liposomes can be actively targeted with monoclonal antibodies or ligands and encapsulating active molecules, with high target efficiency and activity by synthetic modification of the terminal PEG molecule.

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Abstract: Among several promising new drug-delivery systems, liposomes represent an advanced technology to deliver active molecules to the site of action, and at present several formulations are in clinical use. Research on liposome technology has progressed from conventional vesicles ("first-generation liposomes") to "second-generation liposomes", in which long-circulating liposomes are obtained by modulating the lipid composition, size, and charge of the vesicle. Liposomes with modified surfaces have also been developed using several molecules, such as glycolipids or sialic acid. A significant step in the development of long-circulating liposomes came with inclusion of the synthetic polymer poly-(ethylene glycol) (PEG) in liposome composition. The presence of PEG on the surface of the liposomal carrier has been shown to extend blood-circulation time while reducing mononuclear phagocyte system uptake (stealth liposomes). This technology has resulted in a large number of liposome formulations encapsulating active molecules, with high target efficiency and activity. Further, by synthetic modification of the terminal PEG molecule, stealth liposomes can be actively targeted with monoclonal antibodies or ligands. This review focuses on stealth technology and summarizes pre-clinical and clinical data relating to the principal liposome formulations; it also discusses emerging trends of this promising technology.

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Solubilizing excipients in oral and injectable formulations.

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Robert G. Strickley

01 Feb 2004-Pharmaceutical Research

TL;DR: The chemical techniques to solubilize water-insoluble drugs for oral and injection administration include pH adjustment, cosolvents, complexation, microemulsions, self-emulsifying drug delivery systems, micelles, liposomes, and emulsions.

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Abstract: A review of commercially available oral and injectable solution formulations reveals that the solubilizing excipients include water-soluble organic solvents (polyethylene glycol 300, polyethylene glycol 400, ethanol, propylene glycol, glycerin, N-methyl-2-pyrrolidone, dimethylacetamide, and dimethylsulfoxide), non-ionic surfactants (Cremophor EL, Cremophor RH 40, Cremophor RH 60, d-alpha-tocopherol polyethylene glycol 1000 succinate, polysorbate 20, polysorbate 80, Solutol HS 15, sorbitan monooleate, poloxamer 407, Labrafil M-1944CS, Labrafil M-2125CS, Labrasol, Gellucire 44/14, Softigen 767, and mono- and di-fatty acid esters of PEG 300, 400, or 1750), water-insoluble lipids (castor oil, corn oil, cottonseed oil, olive oil, peanut oil, peppermint oil, safflower oil, sesame oil, soybean oil, hydrogenated vegetable oils, hydrogenated soybean oil, and medium-chain triglycerides of coconut oil and palm seed oil), organic liquids/semi-solids (beeswax, d-alpha-tocopherol, oleic acid, medium-chain mono- and diglycerides), various cyclodextrins (alpha-cyclodextrin, beta-cyclodextrin, hydroxypropyl-beta-cyclodextrin, and sulfobutylether-beta-cyclodextrin), and phospholipids (hydrogenated soy phosphatidylcholine, distearoylphosphatidylglycerol, L-alpha-dimyristoylphosphatidylcholine, L-alpha-dimyristoylphosphatidylglycerol). The chemical techniques to solubilize water-insoluble drugs for oral and injection administration include pH adjustment, cosolvents, complexation, microemulsions, self-emulsifying drug delivery systems, micelles, liposomes, and emulsions.

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1,383 citations

"The applications of Vitamin E TPGS ..." refers methods in this paper

...To 151 solubilize water-insoluble drugs for oral and parenteral administration, there are many techniques 152 such as pH adjustment, cosolvents, complexation, microemulsions, self-emulsifying DDSs, 153 micelles, liposomes, and emulsions (Kuentz, 2011; Strickley, 2004)....
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Journal Article•DOI•

Vitamin E TPGS as a molecular biomaterial for drug delivery

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Zhiping Zhang¹, Songwei Tan¹, Si-Shen Feng²•Institutions (2)

Huazhong University of Science and Technology¹, National University of Singapore²

01 Jun 2012-Biomaterials

TL;DR: TPGS has an amphiphilic structure of lipophilic alkyl tail and hydrophilic polar head with a relatively low critical micelle concentration (CMC) of 0.02% w/w, which make it to be an ideal molecular biomaterial in developing various drug delivery systems, including prodrugs, micelles, liposomes and nanoparticles.

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501 citations

"The applications of Vitamin E TPGS ..." refers background or methods in this paper

...Many drugs or functional 441 elements like docetaxel, paclitaxel, doxorubicin, curcumin, supraparamagnetic iron oxide and 442 quantum dots can be encapsulated in TPGS-PLA nanoparticles with high encapsulation efficiency, 443 improved cellular uptake and cell cytotoxicity and long-circulation property (Zhang et al., 2012)....
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...TPGS was 111 found to enhance the cytotoxicity of doxorubicin, vinblastine, paclitaxel and colchicine in the 112 human MDR1 cDNA (G185) cells which were 27-135 fold more resistant to these drugs than the 113 parental NIH3T3 cells....
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...…441 elements like docetaxel, paclitaxel, doxorubicin, curcumin, supraparamagnetic iron oxide and 442 quantum dots can be encapsulated in TPGS-PLA nanoparticles with high encapsulation efficiency, 443 improved cellular uptake and cell cytotoxicity and long-circulation property (Zhang et al., 2012)....
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...87 2.1 P-gp inhibitor and inhibition mechanism 88 P-gp is an ATP-dependent drug efflux pump, also known as multidrug resistance protein 1 (MDR1) 89 or ATP-binding cassette sub-family B member 1 (ABCB1)....
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...The addition of TPGS as a surfactant and stabilizer to 409 liposomes or lipid based formulations may bring some advantages to these systems, such as 410 improved cytotoxicity and overcoming MDR (Zhang et al., 2012)....
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Journal Article•DOI•

Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers.

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Bhagwant D. Rege¹, Joseph P. Y. Kao², James E. Polli¹•Institutions (2)

University of Maryland, Baltimore¹, University of Maryland Biotechnology Institute²

01 Sep 2002-European Journal of Pharmaceutical Sciences

TL;DR: The results suggest that surfactants can inhibit multiple transporters but that changes in membrane fluidity may not be a generalized mechanism to reduce transporter activity.

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471 citations

"The applications of Vitamin E TPGS ..." refers background in this paper

...It seems that TPGS can inhibit the P-gp activity without affecting the membrane 125 fluidity (Rege et al., 2002; Yamagata et al., 2007)....
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...Surfactant/ Micelle structure Nanocrystal SEDDS SMEDDS Paclitaxel/Cyclosporine Epirubicin/Raloxifene Verapamil/Quercetin Amprenavir/Talinolol Colchicine/Vancomycin P-gp inhibition mechanism/ Solubility enhancer/ Oral absorption enhancer P-gp inhibition from Caco-2 monolayer model; influence of ATPase activity without membrane fluidity changement (Rege et al., 2002); inhibitor for CYP-mediated metabolism (Christiansen et al....
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...…enhancer/ Oral absorption enhancer P-gp inhibition from Caco-2 monolayer model; influence of ATPase activity without membrane fluidity changement (Rege et al., 2002); inhibitor for CYP-mediated metabolism (Christiansen et al., 2011); Inhibitor of P-gp and MRP2 (Hanke et al., 2010); increased AUC…...
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