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. 2022 Dec 21;28(1):69.
doi: 10.3390/molecules28010069.

Effect of Lipophilic Chains on the Antitumor Effect of a Dendritic Nano Drug Delivery System

Lijuan Ding  1 , Xiangtao Wang  1 , Ting Wang  1 , Bo Yu  1 , Meihua Han  1 , Yifei Guo  1   2   3
Affiliations

Effect of Lipophilic Chains on the Antitumor Effect of a Dendritic Nano Drug Delivery System

Lijuan Ding et al. Molecules. .

Abstract

Oligoethylene glycol dendron (G2) has been used in drug delivery due to its unique dendritic structure and excellent properties. In order to investigate the effects of lipophilic chains on drug delivery, the amphiphilic hybrid compound G2-C18 is synthesized, and celastrol (CSL) is selected to prepare "core-shell" structured CSL-G2-C18 nanoparticles (NPs) via the antisolvent precipitation method. Meanwhile, CSL-G2 NPs are prepared as the control. The two NPs show similar particle sizes and polydispersity indexes, while their morphologies exhibit dramatic differences. CSL-G2 NPs are solid spherical particles, while G2-C18 NPs are vesicles. The two NPs present ideal stability and similar release tendencies. The in vitro toxicity results show that the cell inhibition effect of CSL-loaded NPs is significantly enhanced when compared with free CSL, and the antitumor effect of CSL-G2-C18 NPs is stronger than that of CSL-G2 NPs. The IC50 value of CSL-G2 NPs and CSL-G2-C18 NPs is enhanced about 2.8-fold and 5-fold when compared with free CSL, respectively. The above results show that lipophilic chain-linking dendritic hybrid nanocarriers promote antitumor activity by affecting the morphology of NPs, which may aid in the selection of carrier designs.

Keywords: aliphatic chain; amphiphilic nanocarriers; antitumor activity; hybrid structure; morphology.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of nanocarriers G2 and G2-C18, CSL NPs cartoon illustration.
Figure 2
Figure 2
TEM images of G2 (a) (scale bar 500 nm), G2-C18 (b) (scale bar 500 nm), CSL-G2 NPs (c) (scale bar 200 nm), and CSL-G2-C18 NPs (d) (scale bar 500 nm).
Figure 3
Figure 3
Intensity ratio I384/I374 curves as a function of G2 and G2-C18 concentration.
Figure 4
Figure 4
DSC thermograms of CSL, nanocarriers, CSL-loaded NPs, and the physical mixture of CSL and nanocarriers: G2 series (a) and G2-C18 series (b).
Figure 5
Figure 5
XRD patterns of CSL, CSL-loaded NPs, and the physical mixture of CSL and nanocarriers: G2 series (a) and G2-C18 series (b).
Figure 6
Figure 6
Particle size and polydispersity index of CSL-loaded nanoparticles during storage at 4 °C: CSL-G2 NPs (a) and CSL-G2-C18 NPs (b), n = 3.
Figure 7
Figure 7
Particle size of the CSL-G2 NPs (a) and CSL-G2-C18 NPs (b) in glucose solution (5%) and plasma.
Figure 8
Figure 8
Cumulative release rate of CSL in 5% glucose solution at 37 °C over 144 h.
Figure 9
Figure 9
Cytotoxicity of CSL NPs to 4T1 cells after 48 h incubation (n = 5).
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