Pharmaceutical Applications of Vitamin E TPGS

2021 ◽  
Author(s):  
Adnan M. Jasim ◽  
Mohammed J. Jawad
Keyword(s):  
Drug Delivery ◽  
Vitamin E ◽  
Solid Dispersions ◽  
Nutritional Supplement ◽  
Water Soluble ◽  
Lymphatic Transport ◽  
Glycol Succinate ◽  
Vitamin E Tpgs ◽  
Low Concentrations ◽  
Dependent Inhibition

D-tocopheryl polyethylene glycol succinate (Vitamin E TPGS) has been approved as a safe pharmaceutical adjuvant by FDA, and several drug delivery systems (DDS) based on TPGS have been developed. 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, vaccine system adjuvant, nutritional supplement, film plasticizer, anticancer reagent, and so on, are discussed in this review. Consequenly, TPGS can inhibit ATP-dependent P-glycoprotein activity and act as a potent excipient that promotes the efficiency of delivery and the therapeutic effect of drugs. Inhibition of P-gp occurs through mitochondria-dependent inhibition of the P-gp pump. Many of the latest studies address the use of TPGS for many poorly water-soluble or permeable drugs in the manufacture of nanodrugs or other formulations. In addition, it has been reported that TPGS shows a robust improvement in chylomicron secretion at low concentrations and improves intestinal lymphatic transport, which would also boost the potential of drug absorption. It also indicates that there are still many problems facing clinical translation of TPGS-based nanomedicines, requiring a more deep evaluation of TPGS properties and a future-based delivery method.

scholarly journals Self-Microemulsifying Drug Delivery Systems: An Attractive Strategy for Enhanced Therapeutic Profile

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Samatha Akula ◽  
Aravind Kumar Gurram ◽  
Srinivas Reddy Devireddy
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Solid Dispersions ◽  
Oral Route ◽  
Delivery Systems ◽  
Water Soluble ◽  
Lymphatic Transport ◽  
Water Soluble Drugs ◽  
Solubilized Form

Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modification, and cocrystals exist, lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-microemulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present paper gives exhaustive information on the formulation design and characterization of SMEDDS along with the probable mechanisms by which the bioavailability can be improved with SMEDDS.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF NEVIRAPINE LOADED AMORPHOUS SOLID DISPERSIONS FOR SOLUBILITY ENHANCEMENT

2019 ◽  
pp. 176-182
Author(s):  
GAGANDEEP SINGH ◽  
NAVJOT SINGH ◽  
RANDEEP KUMAR ◽  
NEENA BEDI
Keyword(s):  
Vitamin E ◽  
Drug Release ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Glycol Succinate ◽  
Scanning Calorimetry ◽  
Compression Technique ◽  
Vitamin E Tpgs ◽  
Best Fitting

Objective: The present study entails the development of nevirapine (NVP)-loaded solid dispersions for improvement of solubility and in vitro profile. Methods: Solid dispersions were prepared through blending with a hydrophilic polymer and Vitamin E tocopherol polyethylene glycol succinate (TPGS) using the solvent evaporation method. The optimized formulations were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and morphological investigations by scanning electron microscopy. The optimized formulation was converted into fast dissolving tablets (FDTs) through direct compression technique and was characterized for pre- and post-compression parameters. Both amorphous dispersions and FDTs were evaluated for in vitro drug release. Results: NVP showed pH-dependent solubility in different pH media. Above 0.002% w/v Vitamin E TPGS, a linear relationship was observed between the NVP solubility and Vitamin E TPGS concentration. According to the study, the most suitable formulation was NVP:Vitamin E TPGS (1:0.75) in 30 ml solvent with a drug release of 82.96% in 2 h. The analysis of dissolution data of optimized formulation indicated the best fitting with the Higuchi model. FDTs exhibited faster drug release of about 50% in 5 min indicating desired attributes for the immediate dosage form. Conclusion: The present study vouches for better in vitro profile of NVP from solid dispersion based FDTs.

scholarly journals Drug Delivery Innovations for Enhancing the Anticancer Potential of Vitamin E Isoforms and Their Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-16 ◽  
Author(s):  
Christiana M. Neophytou ◽  
Andreas I. Constantinou
Keyword(s):  
Drug Delivery ◽  
Vitamin E ◽  
Drug Delivery Systems ◽  
Single Agent ◽  
Delivery Systems ◽  
Chemotherapeutic Agents ◽  
Alpha Tocopherol ◽  
Glycol Succinate ◽  
Anticancer Properties ◽  
Vitamin E Tpgs

Vitamin E isoforms have been extensively studied for their anticancer properties. Novel drug delivery systems (DDS) that include liposomes, nanoparticles, and micelles are actively being developed to improve Vitamin E delivery. Furthermore, several drug delivery systems that incorporate Vitamin E isoforms have been synthesized in order to increase the bioavailability of chemotherapeutic agents or to provide a synergistic effect. D-alpha-tocopheryl polyethylene glycol succinate (Vitamin E TPGS or TPGS) is a synthetic derivative of natural alpha-tocopherol which is gaining increasing interest in the development of drug delivery systems and has also shown promising anticancer effect as a single agent. This review provides a summary of the properties and anticancer effects of the most potent Vitamin E isoforms and an overview of the various formulations developed to improve their efficacy, with an emphasis on the use of TPGS in drug delivery approaches.

Targeting vitamin E TPGS–cantharidin conjugate nanoparticles for colorectal cancer therapy

RSC Advances ◽  
2015 ◽  
Vol 5 (66) ◽  
pp. 53846-53856 ◽  
Author(s):  
Shihou Sheng ◽  
Tao Zhang ◽  
Shijie Li ◽  
Jun Wei ◽  
Guangjun Xu ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Delivery ◽  
Vitamin E ◽  
Chinese Medicine ◽  
Side Effects ◽  
Cancer Therapy ◽  
Traditional Chinese Medicine ◽  
Drug Efficacy ◽  
Vitamin E Tpgs ◽  
Colorectal Cancer Cells

A traditional Chinese medicine cantharidin which was previously found to be effective on colorectal cancer cells was translated into nanoparticles for drug delivery to reduce its side effects and enhance its drug efficacy.

Vitamin E TPGS as a molecular biomaterial for drug delivery

Biomaterials ◽  
2012 ◽  
Vol 33 (19) ◽  
pp. 4889-4906 ◽  
Author(s):  
Zhiping Zhang ◽  
Songwei Tan ◽  
Si-Shen Feng
Keyword(s):  
Drug Delivery ◽  
Vitamin E ◽  
Vitamin E Tpgs

scholarly journals Dissolution study of Spironolactone by using solid dispersion technique

2012 ◽  
Vol 4 (2) ◽  
pp. 42-47
Author(s):  
Irwin Dewan ◽  
SM Ashraful Islam ◽  
Mohammad Shahriar
Keyword(s):  
Drug Delivery ◽  
Solid Dispersion ◽  
Release Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dispersion Technique

The main objective of the current study was to formulate poorly water soluble drug Spirinolactone by using solid dispersion technique in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. Solid dispersions were prepared using two methods; solvent method and fusion method. Solid dispersion was prepared by using polymers, such as Hydroxy propylymethyl cellulose (HPMC 6cp), Hydroxy propyl cellulose (HPC), Sodium carboxymethylcellulose (Na-CMC), Povidone K12, Povidone K30, Poloxamer 407. Solid dispersions containing Spironolactone with HPC (96.81%), HPMC 6cp (93.05%), Poloxamer 407 (90.84%) and Na-CMC (89.93%) provided higher release rate than the release rate of solid dispersion containing only Spironolactone (35.27%), and Spironolactone with Povidone K12 (76.17%), Povidone K30 (67.92%). So the present study revealed that the solid dispersion may be an ideal means of drug delivery system for poorly water soluble drugs. Further study in this field was required to establish these drug delivery systems so that in future it can be used effectively in commercial basis.DOI: http://dx.doi.org/10.3329/sjps.v4i2.7776S. J. Pharm. Sci. 4(2) 2011: 42-47

Vitamin E TPGS as a Molecular Biomaterial for Drug Delivery

2014 ◽  
pp. 939-981
Author(s):  
Zhiping Zhang ◽  
Songwei Tan ◽  
Si-Shen Feng
Keyword(s):  
Drug Delivery ◽  
Vitamin E ◽  
Vitamin E Tpgs
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