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Preparation and Antitumor Activity Evaluation of Folic Acid-Modified Phospholipid-Gambogic Acid Nanocrystals
Xiwen Zeng1, Sizhuo Liu1, Qianhui He1
1Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China.
Abstract:
Background: Liver cancer is a complex malignant tumor; gambogic acid (GA) has significant anti-cancer potential, but poor water solubility and low bioavailability limit its clinical application. In this paper, by integrating nanocrystal (NC) technology and an active targeting strategy, a new nanoagent-folic acid-modified phospholipid-gambogic acid nanocrystals (GA-NCs@FA)-was developed to improve the delivery efficiency and therapeutic effect of GA in the treatment of liver cancer. Methods: GA-NCs@FA was prepared by the CO2-assisted precipitation method and the thin-film hydration method. The in vitro anti-tumor activity of GA-NCs@FA was evaluated by cytotoxicity, as well as a scratch and uptake test. A HepG2 tumor-bearing nude mouse model was established to investigate the in vivo distribution and tumor targeting of GA. The in vivo anti-tumor activity was evaluated by the tumor inhibition rate, and the pathological changes of organs in each group were observed by H&E staining. Results: GA-NCs@FA significantly reduced HepG2 cell viability (IC50: 0.50 μg·mL-1) and migration ability (48 h healing rate: 11.50%) and enhanced intracellular fluorescence intensity. In vivo analysis showed that GA-NCs@FA significantly increased the accumulation of drugs in tumor tissues by active targeting and achieved a tumor growth inhibition rate of 70.9%. Histopathology confirmed that GA-NCs@FA induced the most obvious nuclear pyknosis and necrosis in tumor tissues while maintaining good biosafety. Conclusions: GA-NCs@FA significantly prolongs the systemic circulation time of the drug and enhances intratumoral accumulation; therefore, it is a method that can be considered for active targeting and treatment of liver cancer.
Insights
Researchers developed folic acid-conjugated gambogic acid nanocrystals (GA-NCs@FA) to enhance liver cancer treatment. This novel nanoagent improves drug delivery and exhibits significant anti-tumor activity, offering a promising strategy for targeting liver cancer effectively.
Area of Science:
- Nanotechnology
- Pharmacology
- Oncology
Background:
- Liver cancer presents complex treatment challenges.
- Gambogic acid (GA) shows anti-cancer potential but suffers from poor solubility and bioavailability.
- Developing novel drug delivery systems is crucial for effective GA application in liver cancer therapy.
Purpose of the Study:
- To develop a novel nanoagent, folic acid-modified phospholipid-gambogic acid nanocrystals (GA-NCs@FA), for improved liver cancer treatment.
- To enhance the delivery efficiency and therapeutic effect of gambogic acid (GA) through nanocrystal (NC) technology and active targeting.
- To evaluate the in vitro and in vivo efficacy and biosafety of the developed GA-NCs@FA nanoagent.
Main Methods:
- Preparation of GA-NCs@FA using CO2-assisted precipitation and thin-film hydration.
- In vitro assessment of anti-tumor activity via cytotoxicity, scratch, and uptake assays in HepG2 cells.
- In vivo evaluation in a HepG2 tumor-bearing nude mouse model, including biodistribution, tumor targeting, anti-tumor efficacy, and histopathological analysis.
Main Results:
- GA-NCs@FA demonstrated significant reduction in HepG2 cell viability (IC50: 0.50 μg·mL-1) and migration.
- Enhanced intracellular drug uptake was observed with GA-NCs@FA.
- In vivo studies showed increased drug accumulation in tumor tissues via active targeting, achieving a 70.9% tumor growth inhibition rate.
- Histopathology confirmed significant necrosis in tumor tissues with good biosafety.
Conclusions:
- GA-NCs@FA effectively prolongs drug circulation time and enhances intratumoral accumulation.
- The developed nanoagent shows significant potential for active targeting and treatment of liver cancer.
- This approach represents a viable strategy for improving gambogic acid's therapeutic efficacy in liver cancer.
