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Review
. 2017 Nov;24(1):1831-1842.
doi: 10.1080/10717544.2017.1406561.

Recent developments in d-α-tocopheryl polyethylene glycol-succinate-based nanomedicine for cancer therapy

Songwei Tan  1 , Chenming Zou  1 , Wei Zhang  1 , Mingxing Yin  2 , Xueqin Gao  1 , Qing Tang  1   3
Affiliations
Review

Recent developments in d-α-tocopheryl polyethylene glycol-succinate-based nanomedicine for cancer therapy

Songwei Tan et al. Drug Deliv. 2017 Nov.

Erratum in

Abstract

Cancer remains an obstacle to be surmounted by humans. As an FDA-approved biocompatible drug excipient, d-α-tocopheryl polyethylene glycol succinate (TPGS) has been widely applied in drug delivery system (DDS). Along with in-depth analyses of TPGS-based DDS, increasingly attractive results have revealed that TPGS is able to act not only as a simple drug carrier but also as an assistant molecule with various bio-functions to improve anticancer efficacy. In this review, recent advances in TPGS-based DDS are summarized. TPGS can inhibit P-glycoprotein, enhance drug absorption, induce mitochondrial-associated apoptosis or other apoptotic pathways, promote drug penetration and tumor accumulation, and even inhibit tumor metastasis. As a result, many formulations, by using original TPGS, TPGS-drug conjugates or TPGS copolymers, were prepared, and as expected, an enhanced therapeutic effect was achieved in different tumor models, especially in multidrug resistant and metastatic tumors. Although the mechanisms by which TPGS participates in such functions are not yet very clear, considering its effectiveness in tumor treatment, TPGS-based DDS appears to be one of the best candidates for future clinical applications.

Keywords: cancer; d-α-tocopheryl polyethylene glycol succinate (TPGS); drug delivery system; multidrug-resistant; nanomedicine.

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Conflict of interest statement

The authors report no conflicts of interest.

Figures

Figure 1.
Figure 1.
Scheme of potential bio-function of TPGS-based DDS for the treatment of cancer.
Figure 2.
Figure 2.
TPGS improves drug accumulation and penetration in tumors. (A) In vivo imaging, (B) Ex vivo imaging of excised tumors and (C) Intratumoral distributions of Did-loaded micelles in B16F10 tumor bearing mice. 1, Saline; 2, Did; 3, P84-TPGS mixed micelles; 4, F127 -TPGS mixed micelles; 5, F127 micelles (Cao et al., 2016).
Figure 3.
Figure 3.
Mixed micelle-based complex NPs for the co-delivery of chemo-drug and shRNA. (A) Schematic illustration of NP preparation. (B) Anticancer effects and body weight changes of different treatments in A549/T bearing nude mice. (C) In vivo biodistribution of different formulations of PTX or shSur in different formulation at 0.5, 4, 12, and 24 h in A549/T bearing nude mice (Shen et al., 2014a).
Figure 4.
Figure 4.
TNO3 and TPGS-S-S-PTX hybrid micelles. (A) In vivo tumor vascular permeability and blood perfusion presented by Representative MRI images in an S180 tumor model. (B) CLSM images for of micelle uptake and NO release in MCF-7/ADR cells. NO was detected by DAF-FM DA (green). Micelles were labeled by with RhB (red), and nuclei were stained by with DAPI (blue). Scale bar, 50 μm. (C) Representative immunofluorescentce images of blood vessels and tumor apoptosis of in MCF-7/ADR tumors. Blood vessels, nuclei and apoptotic cells were stained by α-CD31 antibody (red), DAPI (blue) and TUNEL (green), respectively (Yin et al., 2017b) (colour figure online).
Figure 5.
Figure 5.
Redox/pH dual-sensitive PBAE-g-TPGS hybrid micelles. (A) Scheme of the targeting delivery and overcoming MDR. (B) Rh123 retention in MCF-7/ADR cells. (C) Live images of MCF-7/ADR tumor-bearing mice that were i.v. administered Cy5 loaded micelles. (D) In vivo anticancer activities (Yin et al., 2017a).
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Grants and funding

This work was supported by National Natural Science Foundation of ChinaNational Natural Science Foundation of China (21204024 and 81273908) and Wuhan Science and Technology plan for youth (2016070204010151).