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Application of vitamin E polyethylene glycol succinate


    Vitamin E polyethylene glycol succinate (TPGS) is a water-soluble derivative of vitamin E, which is formed by the reaction of the carboxyl group of vitamin E succinate with the hydroxyl group of polyethylene glycol. Because it contains both vitamin E ester groups and polyethylene glycol hydrophilic long chain, it has good surfactant properties and water solubility, which can significantly increase the absorption of insoluble drugs in the gastrointestinal tract and improve bioavailability. In foreign countries, vitamin E polyethylene glycol succinate has been widely used in preparation research, as a solvent, absorption enhancer, emulsifier, plasticizer and water insoluble or fat soluble drug delivery system carrier, such as solid dispersion, eye delivery carrier, nasal delivery carrier. In recent years, many studies have found that in addition to being used as pharmaceutical excipients,TPGS has many unique properties, such as being an absorption enhancer and multi-drug resistance reversal agent, etc. TPGS can also be applied to precursor drugs, micelles, liposomes,TPGS copolymer carriers to improve the solubility, permeability and stability of the preparations. Thus, slow, controlled release and targeted action can be achieved to promote drug absorption.

    Weigh 5.6 grams of natural vitamin E succinate with 90% purity, 20 grams of polyethylene glycol 600 with a molecular weight of 600, 0.8 grams of concentrated sulfuric acid with a mass percentage of 98%, and put them into a three-neck bottle, stirring at 100℃ for 2 hours, and cooling to room temperature after the reaction. The reaction product was transferred to a round-bottom flask, and then 150ml of ethyl acetate was added to the round-bottom flask to obtain the mixture. The mixture was transferred to a separating funnel and extracted three times with saturated salt water to collect the organic phase. The organic phase was steamed to obtain 8.3 g of TPGS. The purity of the product was 90.1%, the conversion rate of vitamin E succinate was 89.2%, and the yield of TPGS was 79.2%.

    1. Reduce the particle size of antitumor drugs
      Only liposomes with a particle size of 100 to 200nm can deliver drugs to specific targets and increase drug concentration in the liver. The particle size of antitumor drugs modified with vitamin E PEGsuccinate is reduced, which may be due to the fact that vitamin E pegsuccinate possesses both hydrophilic and oleophilic groups, which are uniformly distributed around the surface of liposomes after connecting to them, reducing their surface tension and forming smaller and more stable blisters. Studies have shown that the modification of vitamin E polyethylene glycol succinate can reduce the size of nanoparticles carrying anti-tumor drugs, promote drug uptake into tumor cells through cells, and then play a killing role on tumor cells.
    2. Increase the drug load and improve the stability of nanoparticles
      Mixed micelles have a more compact structure than ordinary micelles, which can provide a better hydrophobic microenvironment and allow for the encapsulation and stabilization of hydrophobic agents in their cores, thereby enhancing the bioavailability of these agents and extending cycle times. Mixed micelles can passively accumulate at the tumor site through vascular leakage due to enhanced permeability and retention. In addition, the mixed micelles also enhanced cytotoxicity and increased the blood circulation time of chemotherapy drugs. Vitamin E polyethylene glycol succinate is similar to conventional surfactants in that it has both hydrophobic and hydrophilic parts. More importantly, its hydrophobic alkyl head (tocopherol succinate) and hydrophilic polar tail are bulky and have a large surface area. Nanoparticles loaded with antitumor drugs prepared with vitamin E polyethylene glycol succinate showed narrow diameter particle distribution and high emulsification efficiency.

    It can also significantly improve drug encapsulation efficiency, increase nanoparticle cell uptake and cancer cell mortality. The main reason for the large drug loading of nanoparticles after the use of vitamin E PEGsuccinate may be attributed to the high partition coefficient and retention time in the organic phase, which is beneficial to the solidification of nanoparticles, especially the emulsification of vitamin E pegsuccinate catalyzes this process. As an excellent emulsifier, vitamin E polyethylene glycol succinate can be arranged at the oil-water interface to improve the integrity and stability of nanoparticles by reducing their surface free energy at low concentrations, thereby preventing the diffusion of encapsulated drugs from the nanoparticles.

    3 Increase the Zeta potential
    The targeting of nanoparticles is related to the surface charge and hydrophobic properties of the particles, and the negatively charged particles on the surface are easily taken up by the liver. The particle size and the properties of the surface of the nanoparticles determine which opsonins are adsorbed and the degree of adsorption, as well as the pathway and mechanism of phagocytosis. The Zeta potential of the particles treated with vitamin E PEGsuccinate is negative, because vitamin E pegsuccinate has the role of liver cell specific recognition and the carrier charge is also negative, and vitamin E pegsuccinate modified liposome has liver targeting, which can improve the active targeting effect of nanoparticles on liver. So that anti-tumor drugs can better play their anti-liver cancer role. The surface of tumor cells has more negative charge than that of normal cells, and nanoparticles with positive surface charge or near neutral surface are more easily taken up by tumor cells. It has been shown that the Zeta potential of nanoparticles treated with vitamin E polyethylene glycol succinate is greater than that of untreated particles, thus making them more easily taken up by tumor cells.

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