Tocofersolan(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.
Various pharmacological properties of vitamin E.
1.1 Vitamin E TPGS, an amphiphilic polymer
E TPGS is a water-miscible form of vitamin E, which approved by the FDA and commonly used in drug delivery systems as a safe adjuvant. TPGS’s biological and physicochemical properties provide several advantages for its drug delivery applications such as high biocompatibility, drug solubility enhancement, drug permeation improvement, and selective antitumor activity .
1.2 Structure and properties
Vitamin E Tocofersolan(d-alpha-tocopheryl polyethylene glycol 1000 succinate or TPGS) is a water-soluble derivative of natural vitamin E, formed together with polyethylene glycol 1000 by esterification of d-alpha-tocopheryl polyethylene glycol succinate. Furthermore, TPGS is a macromolecule consisting of a lipophilic alkyl tail and a hydrophilic polar head which has amphiphilic properties (see Figure 2).
Chemical structure of Vitamin E Tocofersolan. The lipophile to hydrophile equilibrium of the TPGS is an unique amphiphilic structure. Consequently, it is a waxy solid with an air-stable melting point of about 41° C, ranging from yellow to light brown in color. In nature, it is bulky and has a broader surface area, so it is considered the ideal emulsifier and strong solubilizer . The chemical structure of TPGS used in many formulations/applications shown in Figure 2, such as: 1. Improving drug bioavailability, 2. Properties of surfactants which improve the solubilization of drugs poorly water soluble, 3. Stabilizer of amorphous drug forms 4. Inhibiting the efflux of P-glycoprotein which improves drug permeability, 5. Emulsion vehicle, 6. The active ingredient in self-emulsifying formulations, 7. Minimize drug damage to dermal tissues, 8. Carrier for wound care and therapy, 9. Vitamin E water-soluble source, 10. Fabrication nanosuspensions, 11. Self-microemulsifying and solid tablet/dispersion 12. Vaccine device Adjuvant, 13. Boost of nutrition, 14. Nano-particles formulation, 15. Micelles, 16. Liposomes, 17. Based prodrug.
TPGS-VE is an active solubilizer of various compounds that are water-soluble and insoluble in water, such as steroids, antibiotics, cyclosporins, taxanes, etc. TPGS vitamin E could function as a P-gp inhibitor with a higher capacity than other non-ionic surfactants, such as Tween 80, Pluronics and Cremophor EL, to inhibit P-gp activity .
Several studies indicated that the increased bioavailability was due to micelle formation improving solubility, while others showed that P-glycoprotein (P-gp) inhibition contributes to increased permeability support.
The applications of vitamin E TPGS in drug delivery .Polyethyeleneglycol (PEG).
The water-miscible type of vitamin E, TPGS, consists of a hydrophilic chain of PEG connected to the hydrophobic portion of vitamin E. According to a particular amphiphilic structure, it shows wonderful drug delivery capability.
Poor water solubility and/or poor permeability remain the great snag for maximum activity of therapeutic drugs. In drug delivery, TPGS can be used as a solubilizer, permeation enhancer, diffusion, and emulsifier as well as as a surface stabilizer. It has been commonly used for many poorly water-soluble or permeable drugs in the manufacture of nanodrugs or other formulations, mainly for class II and IV Biopharmaceutical Classification System (BCS) drugs .
Tocofersolan(TPGS) is a suitable candidate for safe new anti-malarial drug, This research has shown that TPGS therapy of malaria, survival rates in mice infected with two parasites have been significantly elevated. Similarly, the severity of Evans blue staining on the brains taken from mice treated with TPGS was lower than the remedy not received by mice.
TPGS-based polymers are extensively used in the drug delivery system, which can enhance the drug’s encapsulation efficiency, intracellular cell uptake and therapeutic efficacy in vitro and in vivo
7. Osteoartharitis
Osteoarthritis (OA) of the knee is a major reason of chronic, incompetence in elderly people, the pathogenesis of this disease until now not clear understood. Recent guide demonstrates that oxidative stress, the event wherein oxidant levels overtake those of antioxidative agents, is one of the motives factors of OA. ROS including oxidants that are generated under the physiological situation in the human body and controlled by cellular antioxidants, lead to functional and structural damage of cartilage cells.
For powder products, we usually send the products together with cartons or fiber drums.Our packaging methods are 1 kg/aluminum bag, 25 kg/box, and 25 kg/barrel. For some products that require special packaging during transportation, we will carry out more detailed packaging.
We support shipping by air, sea, FedEx, DHL, TNT, EMS, UPS, SF, and other carrier.
As a professional plant extract supplier, our quality inspection department is equipped with the most advanced testing and identification instruments, such as UPLC, HPLC, UV and TT (active ingredients) GC and GC-MS (solvent residue), ICP-MS ( Heavy metals), GC/LC-MS-MS (pesticide residues), HPTLC and IR (identification), ELIASA (ORAC value), PPSL (irradiation residues), microbial detection, etc.
To view our brochure or discuss a bulk order, contact us at information@sxrebecca.com.
FAQ
How do I make an order?
For Further Information, please contact: information@sxrebecca.com. We will connect you with one of our account managers who will be happy to assist you with your order.
When will my order ship?
Products in stock usually ship within 24-48 hours of your order being received and processed. If a product is not in stock, delivery time varies but is generally about 3-5 days, depending on exact order quantity.
What is your Return Policy?
Your satisfaction is very important to us. If there are any problems with the product you receive, please contact your account manager within 10 days of receiving of your order. Upon receipt and inspection, Shaanxi Rebecca will issue a credit, refund or replacement.
How can I pay for my order?
We accept T/T(Telegraphic Transfer)，L/C. etc.
_1735529080429.webp "Tocofersolan(TPGS)")
_1732783619322.webp)
_1730691017423.webp)