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Published on: June 13, 2014
ROS-responsive dimeric prodrug-based nanomedicine targeted therapy for gastric cancer
Jiachi Ma1, Yuzhong Chen1, Wanqing Liang2
1Department of Oncological Surgery, The First Affiliated Hospital of Bengbu Medical College, Bengbu, People's Republic of China.
Abstract:
Gastric cancer (GC) remains a major public health problem. Ursolic acid (UA) is reported to be effective in inhibiting GC; however, its low solubility and poor biocompatibility have greatly hindered its clinical application. Herein, an innovative reactive oxygen species (ROS)-sensitive UA dimeric prodrug is developed by coupling two UA molecules via a ROS-cleavable linkage, which can self-assemble into stable nanoparticles in the presence of surfactant. This new UA-based delivery system comprises the following major components: (I) dimeric prodrug inner core that can achieve high drug-loading (55%, w/w) and undergo rapid and selective conversion into intact drug molecules in response to ROS; (II) a polyethylene glycol (PEG) shell to improve colloid stability and extend blood circulation, and (III) surface-modified internalizing RGD (iRGD) to increase tumor targeting. Enhancement of the antitumor effect of this delivery system was demonstrated against GC tumors in vitro and in vivo. This novel approach offers the potential for clinical applications of UA.
Insights
This study developed a novel ursolic acid (UA) nanoparticle delivery system that is sensitive to reactive oxygen species (ROS). This system enhances UA
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Gastric cancer (GC) poses a significant global health challenge.
- Ursolic acid (UA) shows promise for inhibiting GC but faces limitations due to poor solubility and biocompatibility.
- Overcoming these limitations is crucial for effective GC treatment.
Purpose of the Study:
- To develop an innovative reactive oxygen species (ROS)-sensitive UA dimeric prodrug delivery system.
- To enhance the anti-gastric cancer efficacy of ursolic acid.
- To improve the clinical applicability of UA for cancer therapy.
Main Methods:
- Synthesized a dimeric UA prodrug linked via a ROS-cleavable bond.
- Formulated nanoparticles with a polyethylene glycol (PEG) shell and RGD peptide surface modification.
- Evaluated drug loading, stability, ROS-triggered drug release, and anti-tumor effects in vitro and in vivo.
Main Results:
- Achieved high drug loading (55% w/w) in the dimeric prodrug nanoparticles.
- Demonstrated rapid and selective conversion of the prodrug to UA in response to ROS.
- Showcased enhanced anti-tumor efficacy against gastric cancer in vitro and in vivo models.
- Confirmed improved colloid stability and extended blood circulation due to the PEG shell.
- Observed increased tumor targeting via RGD surface modification.
Conclusions:
- The developed ROS-sensitive UA dimeric prodrug nanoparticles offer a promising strategy for gastric cancer treatment.
- This novel delivery system effectively overcomes UA's solubility and biocompatibility issues.
- The approach holds potential for advancing UA's clinical application in oncology.
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