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Published on: February 9, 2019
Delivery of enzalutamide via nanoparticles for effectively inhibiting prostate cancer progression
Ze Gao1,2, Jun Huang3, Zhaoxiang Xie1
1Department of Urology, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou, China. huangh9@mail.sysy.edu.cn.
Abstract:
Androgen deprivation therapy has been used as a standard clinical treatment for prostate cancer, but the disease generally progresses to castration-resistant prostate cancer in a very short time. Enzalutamide (ENZ) is an emerging second-generation androgen receptor (AR) antagonist used for the treatment of patients with nonmetastatic castration-resistant prostate cancer (CRPC). However, due to the rapid onset of drug resistance, it provides only a modest increase in survival. Here, we propose a convenient and effective androgen receptor antagonist drug delivery strategy, that is, the use of a biocompatible nanoparticle (NP) drug delivery system for drug delivery to improve its bioavailability and therapeutic performance. Although the particle size of the phenylpropyl polymer (8P4) nanoparticles is small, it has a high drug-carrying capacity. ENZ-8P4 NPs can increase drug delivery efficiency, enhance drug cytotoxicity, and reduce the half-inhibitory concentration (IC50) of the drug. In addition, in vivo experiments confirmed that ENZ-8P4 preferentially accumulates in the tumor and significantly inhibits tumor growth. Hence, the 8P4 drug delivery system loaded with enzalutamide has excellent potential for the treatment of prostate cancer.
Insights
A novel nanoparticle drug delivery system using phenylpropyl polymer (8P4) nanoparticles loaded with enzalutamide (ENZ) shows promise for treating prostate cancer. This approach enhances drug delivery, improves efficacy, and inhibits tumor growth in vivo.
Area of Science:
- Oncology
- Nanomedicine
- Drug Delivery
Background:
- Androgen deprivation therapy is standard for prostate cancer but often leads to castration-resistant prostate cancer (CRPC).
- Enzalutamide (ENZ), an androgen receptor (AR) antagonist, treats nonmetastatic CRPC but drug resistance limits its survival benefit.
- Improved drug delivery systems are needed to overcome resistance and enhance therapeutic performance.
Purpose of the Study:
- To develop and evaluate a biocompatible nanoparticle (NP) drug delivery system for enzalutamide (ENZ).
- To enhance the bioavailability and therapeutic efficacy of ENZ for prostate cancer treatment.
- To investigate the anti-tumor effects of ENZ-loaded 8P4 NPs in vitro and in vivo.
Main Methods:
- Formulation of phenylpropyl polymer (8P4) nanoparticles with a high drug-carrying capacity for ENZ.
- In vitro assessment of ENZ-8P4 NPs for drug delivery efficiency, cytotoxicity, and IC50.
- In vivo studies to evaluate tumor accumulation and anti-tumor efficacy of ENZ-8P4 NPs.
Main Results:
- ENZ-8P4 NPs demonstrated increased drug delivery efficiency and enhanced cytotoxicity.
- A significant reduction in the half-inhibitory concentration (IC50) was observed for ENZ-8P4 NPs.
- In vivo experiments showed preferential accumulation of ENZ-8P4 NPs in tumors and significant tumor growth inhibition.
Conclusions:
- The 8P4 nanoparticle system effectively delivers enzalutamide, improving its therapeutic performance.
- ENZ-8P4 NPs show significant potential for the treatment of prostate cancer, including castration-resistant forms.
- This nanoparticle-based drug delivery strategy offers a promising approach to overcome drug resistance in prostate cancer therapy.
