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Updated: Aug 4, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Doxorubicin-Loaded Liposome with the Function of "Killing Two Birds with One Stone" against Glioma
Juan Cen1, Xiaoying Dai1, Han Zhao1
1School of Pharmacy, Key Laboratory of Natural Medicine and Immune Engineering, Henan University, Kaifeng 475004, PR China.
Abstract:
The blood-brain barrier (BBB) continues to be one of the main clinical obstacles in the treatment of glioma. Current chemotherapies always bring many different side effects, some even permanent. To date, nanomaterial-based vehicles have shown great potential in treating glioma. Herein, we developed a dual targeting liposomal delivery vector loaded with the anticancer drug doxorubicin (DOX) to treat glioma. SS31, a small peptide, has shown dual targeting effects of penetrating the BBB and specifically targeting mitochondria. In this study, a new liposomal delivery system, LS-DOX, was prepared by modifying DOX-loaded liposomes with SS31 for the treatment of in situ glioma. The liposomes demonstrated a high drug encapsulation rate and drug-loading capacity, satisfactory biocompatibility, high glioma accumulation ability, and good stability in vitro. Experimental results showed that the liposomes could effectively cross the BBB and target gliomas, and mitochondria-targeting of SS31 enhances cell uptake. In addition, the liposomes showed a good therapeutic effect on nude mice with glioma in situ with no obvious toxicity and side effects. Therefore, the present research will provide a novel alternative and reference for the effective treatment of glioma.
Insights
This study introduces a novel dual-targeting liposomal delivery system for treating glioma. The system effectively crosses the blood-brain barrier and targets tumors, offering a promising, low-toxicity alternative for glioma treatment.
Area of Science:
- Nanomedicine
- Neuro-oncology
- Drug Delivery Systems
Background:
- The blood-brain barrier (BBB) presents a significant challenge in glioma treatment.
- Conventional chemotherapy for glioma often results in severe side effects.
- Nanomaterial-based drug delivery vehicles show promise for improved glioma therapy.
Purpose of the Study:
- To develop and evaluate a dual-targeting liposomal delivery system (LS-DOX) for treating glioma.
- To utilize the peptide SS31 for enhanced BBB penetration and mitochondria-specific targeting.
- To assess the efficacy and safety of LS-DOX in an in situ glioma model.
Main Methods:
- Preparation of doxorubicin (DOX)-loaded liposomes modified with SS31 peptide.
- In vitro characterization of liposomes for drug encapsulation, loading capacity, biocompatibility, and stability.
- Evaluation of BBB crossing and glioma targeting capabilities.
- Assessment of therapeutic efficacy and toxicity in nude mice with in situ glioma.
Main Results:
- LS-DOX exhibited high drug encapsulation and loading capacity with good in vitro stability and biocompatibility.
- The liposomes effectively crossed the BBB and accumulated in gliomas.
- SS31-mediated mitochondria targeting enhanced cellular uptake.
- LS-DOX demonstrated significant therapeutic effects in vivo with no obvious toxicity.
Conclusions:
- The developed dual-targeting liposomal system (LS-DOX) is effective for glioma treatment.
- This nanomedicine approach offers a promising, safe, and efficient strategy for overcoming BBB limitations in glioma therapy.
- LS-DOX provides a novel alternative for clinical glioma treatment and a valuable reference for future research.
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