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

Yang, Conglian; Wang, Tingting; Qi, Yan; Zhang, Zhiping

doi:10.7150/thno.22711

Cited by 302 publications

(184 citation statements)

References 153 publications

Supporting

Mentioning

181

Contrasting

Unclassified

Order By: Relevance

“…19,20 TPGS has been approved as a safe and effective solublizer and stabilizer for water-insoluble and unstable drug. 21 TPGS is also a P-glycoprotein (P-gp) inhibitor and widely used as an absorption enhancer for improving the oral absorption of insoluble drug. [22][23][24] Our previous research showed that D-α-tocopheryl polyethylene glycol 1000 succinate micelle (TP-PMs) had significantly increased the oral bioavailability of curcumin (Cur); however, the improved transport efficiency of Cur across epithelium by TP-PMs is still limited.…”

Section: Introductionmentioning

confidence: 99%

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

Wang¹,

Wang²,

Liu³

et al. 2018

IJN

View full text Add to dashboard Cite

IntroductionPolymeric micelles (PMs) hold promise for improving solubility and oral absorption of poorly soluble drugs. Unfortunately, the oral absorption of PMs is also limited by intestinal epithelium. To improve the oral delivery efficiency of micelles, transporter-mediated micelles could enhance the transport efficiency across the epithelial barrier, and they have attracted more attention.MethodsPeptide transporter 1 (PepT1)-mediated micelles (Val-PMs/Phe-PMs) were designed by grafting valine (or phenylalanine) onto the surface of curcumin (Cur)-loaded-D-α-tocopheryl polyethylene glycol 1000 succinate micelles (TP-PMs). The oral absorption mechanism and oral bioavailability were further investigated in vitro and in vivo.ResultsThe cellular study showed that Val-PMs/Phe-PMs had a high PepT1 affinity, resulting in a higher drug uptake and transcellular transport than TP-PMs. In rats, Val-PMs/Phe-PMs exhibited higher intestinal accumulation in the apical side of the intestinal epithelium than TP-PMs, promoting drug diffusion across epithelial barrier. The oral bioavailability of Cur was significantly improved by Val-PMs/Phe-PMs, which was about 10.50- and 3.40-fold greater than that of Cur-Sol and TP-PMs, respectively.ConclusionPepT-1-mediated micelles, using PepT1 as a target on intestinal epithelium, have unique functions with intestine and prove promising for oral delivery of poorly water-soluble drugs.

show abstract

Section: Introductionmentioning

confidence: 99%

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

Wang¹,

Wang²,

Liu³

et al. 2018

IJN

View full text Add to dashboard Cite

show abstract

“…TPGS can also be used as precursor drugs, micelles, and liposomes to improve the solubility, permeability, and stability of the preparation; thus, achieving sustained, controlled release and targeting effects. 27,49 In this study, we used TPGS as a pore-forming agent to improve the performance of PLGA nanoparticles. The advantages of PLGA/TPGS nanoparticles are that both PLGA and TPGS are FDA-approved materials with good biocompatibility.…”

Section: Discussionmentioning

confidence: 99%

<p>Co-Delivery of Docetaxel and Salinomycin to Target Both Breast Cancer Cells and Stem Cells by PLGA/TPGS Nanoparticles</p>

Gao¹,

Liu²,

Xie³

et al. 2019

IJN

View full text Add to dashboard Cite

Conventional chemotherapy is hampered by the presence of breast cancer stem cells (BCSCs). It is crucial to eradicating both the bulky breast cancer cells and BCSCs, using a combination of conventional chemotherapy and anti-CSCs drugs. However, the synergistic ratio of drug combinations cannot be easily maintained in vivo. In our previous studies, we demonstrated that the simultaneous delivery of two drugs via nanoliposomes could maintain the synergistic drug ratio for 12 h in vivo. However, nanoliposomes have the disadvantage of quick drug release, which makes it difficult to maintain the synergistic drug ratio for a long time. Herein, we developed a co-delivery system for docetaxel (DTX)-a first-line chemotherapy drug for breast cancer-and salinomycin (SAL)-an anti-BCSCs drug-in rigid nanoparticles constituted of polylactide-co-glycolide/D-alpha-tocopherol polyethylene glycol 1000 succinate (PLGA/TPGS). Methods: Nanoparticles loaded with SAL and DTX at the optimized ratio (NSD) were prepared by the nanoprecipitation method. The characterization, cellular uptake, and cytotoxicity of nanoparticles were investigated in vitro, and the pharmacokinetics, tissue distribution, antitumor and anti-CSCs activity of nanoparticles were evaluated in vivo. Results: We demonstrated that a SAL/DTX molar ratio of 1:1 was synergistic in MCF-7 cells and MCF-7-MS. Moreover, the enhanced internalization of nanoparticles was observed in MCF-7 cells and MCF-7-MS. Furthermore, the cytotoxicity of NSD against both MCF-7 cells and MCF-7-MS was stronger than the cytotoxicity of any single treatment in vitro. Significantly, NSD could prolong the circulation time and maintain the synergistic ratio of SAL to DTX in vivo for 24 h, thus exhibiting superior tumor targeting and anti-tumor activity compared to other treatments. Conclusion: Co-encapsulation of SAL and DTX in PLGA/TPGS nanoparticles could maintain the synergistic ratio of drugs in vivo in a better manner; thus, providing a promising strategy for synergistic inhibition of breast cancer.

show abstract

“…Acetone was chosen as the anti-solvent being generally recognized as safe, 23 green, 24 and easily removable by nebulization, while TPGS is a widely used surfactant in pharmaceutics, drug delivery and powders for inhalation. 25,26 At 20 °C and in absence of surfactant, water/acetone ratios of 1:3.7 and 1:5 (v/v) resulted in low precipitation yields (5% and 22%, respectively) ( Table 1, entries 1 and 2), while the use of a 1:10 water/acetone solution afforded a good precipitation (yield up to 60%) and the formation of particles with an average diameter of 5 µm and a 1 µm-subpopulation (22.4%) ( Table 1, entry 3). Higher or lower temperatures resulted in an increase of the average size (Table 1, entries 4 and 5).…”

Section: Preliminary Batch Screeningmentioning

confidence: 99%

In-Flow Flash Nanoprecipitation of Size-Controlled D-Leucine Nanoparticles for Spray-Drying Formulations

Cerra¹,

Gabriele²,

Ricci³

et al. 2019

Preprint

View full text Add to dashboard Cite

We report the development of a novel flow-based method for the flash nanoprecipitation of size-controlled D-leucine nanoparticles for spray-drying formulations. Preliminary experiments were conducted in batch to define best flowable conditions that were then optimized considering nanoparticle size and distribution using a mesofluidic flow system. The method was applied to the streamilined preparation of D-leucine nanoparticles readily nebulized by mini and nano spray-dryer devices and characterized by SEM spectroscopy. Finally, the D-leucine atomized powder was used as glidant in dry powder for inhalation with micronized budesonide, a poorly water-soluble and low flowable anti-asthma drug.

show abstract

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

Cited by 302 publications

References 153 publications

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

Apically targeted oral micelles exhibit highly efficient intestinal uptake and oral absorption

<p>Co-Delivery of Docetaxel and Salinomycin to Target Both Breast Cancer Cells and Stem Cells by PLGA/TPGS Nanoparticles</p>

In-Flow Flash Nanoprecipitation of Size-Controlled D-Leucine Nanoparticles for Spray-Drying Formulations

Contact Info

Product

Resources

About