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Updated: Dec 17, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Doxorubicin-loading core-shell pectin nanocell: A novel nanovehicle for anticancer agent delivery with multidrug
Jiabi Ouyang1, Mohui Yang1, Tian Gong1
1College of Pharmacy, Jinan University, Guangzhou, China.
Abstract:
Tumor is a prevalent great threat to public health worldwide and multidrug resistance (MDR) of tumor is a leading cause of chemotherapy failure. Nanomedicine has shown prospects in overcoming the problem. Doxorubicin (DOX), a broad-spectrum anticancer drug, showed limited efficacy due to MDR. Herein, a doxorubicin containing pectin nanocell (DOX-PEC-NC) of core-shell structure, a pectin nanoparticle encapsulated with liposome-like membrane was developed. The DOX-PEC-NC, spheroid in shape and sized around 150 nm, exerted better sustained release behavior than doxorubicin loading pectin nanoparticle (DOX-PEC-NP) or liposome (DOX-LIP). In vitro anticancer study showed marked accumulation of doxorubicin in different tumor cells as well as reversal of MDR in HepG2/ADR cells and MCF-7/ADR cells caused by treatment of DOX-PEC-NC. In H22 tumor-bearing mice, DOX-PEC-NC showed higher anticancer efficacy and lower toxicity than doxorubicin. DOX-PEC-NC can improve anticancer activity and reduce side effect of doxorubicin due to increased intracellular accumulation and reversal of MDR in tumor cells, which may be a promising nanoscale drug delivery vehicle for chemotherapeutic agents.
Insights
This study introduces a novel doxorubicin-loaded pectin nanocell (DOX-PEC-NC) to combat multidrug resistance (MDR) in cancer. The nanocell enhances drug delivery, reverses MDR, and improves anticancer efficacy with reduced toxicity.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Multidrug resistance (MDR) in tumors is a major obstacle to successful chemotherapy.
- Doxorubicin (DOX), a widely used anticancer drug, often faces efficacy limitations due to MDR.
- Nanomedicine offers potential solutions for overcoming drug resistance in cancer treatment.
Purpose of the Study:
- To develop and characterize a novel pectin nanocell encapsulating doxorubicin (DOX-PEC-NC) for improved cancer therapy.
- To evaluate the drug release profile, in vitro anticancer activity, and in vivo efficacy of DOX-PEC-NC.
- To investigate the potential of DOX-PEC-NC in reversing multidrug resistance (MDR) in cancer cells.
Main Methods:
- Fabrication of a core-shell structured pectin nanocell (DOX-PEC-NC) encapsulating doxorubicin.
- Assessment of sustained drug release behavior compared to conventional doxorubicin formulations.
- In vitro evaluation of cellular uptake and reversal of MDR in resistant cancer cell lines (HepG2/ADR, MCF-7/ADR).
- In vivo efficacy and toxicity studies in H22 tumor-bearing mice.
Main Results:
- DOX-PEC-NC exhibited a sustained release profile superior to doxorubicin-loaded pectin nanoparticles (DOX-PEC-NP) and liposomes (DOX-LIP).
- In vitro studies demonstrated enhanced intracellular accumulation of doxorubicin and significant reversal of MDR in HepG2/ADR and MCF-7/ADR cells.
- In vivo studies in H22 tumor-bearing mice showed that DOX-PEC-NC possessed higher anticancer efficacy and lower toxicity compared to free doxorubicin.
Conclusions:
- DOX-PEC-NC effectively enhances the anticancer activity of doxorubicin by increasing intracellular drug accumulation and reversing MDR.
- The developed nanocell formulation demonstrates potential as a promising nanoscale drug delivery vehicle for chemotherapeutic agents.
- DOX-PEC-NC offers a strategy to improve therapeutic outcomes and reduce side effects associated with doxorubicin chemotherapy.
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