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Published on: September 8, 2017
Development and characterization of octreotide-modified curcumin plus docetaxel micelles for potential treatment of
Quan An1, Chen-Xiao Shi2, Hao Guo2
1Technology Research and Development Centre, Yunnan Baiyao Group Health Products Co., LTD , Kunming , China.
Abstract:
We prepared octreotide (OCT)-modified curcumin plus docetaxel micelles to enhance active targeting and inhibit tumor metastasis by destroying vasculogenic mimicry (VM) channels. Soluplus was applied as an amphiphilic material to form micelles via film dispersion. The cytotoxic effects, active cellular targeting, and inhibitory effects on metastasis were systematically evaluated in vitro using A549 cells, and in vivo antitumor effects were evaluated using xenograft tumor-bearing mice. In vitro assays indicated that the OCT-modified curcumin plus docetaxel micelles showed robust cytotoxicity on A549 cells and effectively inhibited VM channels and tumor metastasis. Studying the mechanism of action indicated that OCT-modified curcumin plus docetaxel micelles downregulated MMP-2 and HIF-1α. In vivo assays indicated that OCT-modified curcumin plus docetaxel micelles increased drug accumulation at tumor sites and showed obvious antitumor efficacy. The developed OCT-modified curcumin plus docetaxel micelles may offer a promising treatment strategy for non-small-cell lung cancer.
Insights
Octreotide-modified micelles loaded with curcumin and docetaxel effectively target non-small cell lung cancer cells. This novel drug delivery system inhibits tumor metastasis by disrupting vasculogenic mimicry channels.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Non-small cell lung cancer (NSCLC) poses a significant therapeutic challenge.
- Tumor metastasis and vasculogenic mimicry (VM) are critical factors in NSCLC progression.
- Developing targeted drug delivery systems is crucial for improving NSCLC treatment efficacy.
Purpose of the Study:
- To develop octreotide (OCT)-modified curcumin plus docetaxel micelles for enhanced active targeting of NSCLC.
- To evaluate the efficacy of these micelles in inhibiting tumor metastasis by destroying VM channels.
- To investigate the antitumor effects both in vitro and in vivo.
Main Methods:
- Micelles were formulated using Soluplus via film dispersion.
- In vitro studies involved A549 cells to assess cytotoxicity, cellular targeting, and VM inhibition.
- In vivo studies utilized xenograft tumor-bearing mice to evaluate antitumor efficacy and drug accumulation.
Main Results:
- OCT-modified micelles demonstrated robust cytotoxicity against A549 cells.
- Effective inhibition of VM channels and tumor metastasis was observed in vitro.
- Downregulation of MMP-2 and HIF-1α was identified as a mechanism of action.
- In vivo studies showed increased drug accumulation at tumor sites and significant antitumor efficacy.
Conclusions:
- OCT-modified curcumin plus docetaxel micelles represent a promising strategy for NSCLC treatment.
- This approach enhances active targeting and combats metastasis by inhibiting VM.
- The developed micelles offer a potential new therapeutic avenue for non-small-cell lung cancer.
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