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In Vitro and In Vivo Assessment of Darolutamide Encapsulated Lipid-Extruded PEGylated Liposomal Formulation
Ekta Pardhi1, Rahul Khemchandani2, Avinash Pawar1
1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana 500037, India.
ACS Applied Bio Materials
|April 8, 2026
Summary
PEGylated liposomes effectively delivered darolutamide (DALP) for non-metastatic castration-resistant prostate cancer (nmCRPC). This formulation enhanced drug efficacy, prolonged circulation time, and reduced toxicity, offering a promising nanocarrier approach for nmCRPC treatment.
Area of Science:
- Nanomedicine
- Pharmacology
- Oncology
Background:
- Darolutamide (DA) is a promising non-steroidal androgen receptor inhibitor for non-metastatic castration-resistant prostate cancer (nmCRPC).
- Poor aqueous solubility and high therapeutic doses limit darolutamide's clinical utility.
- PEGylated liposomes offer a potential solution for improving drug delivery and efficacy.
Purpose of the Study:
- To develop and characterize PEGylated liposomes encapsulating darolutamide (DALP).
- To evaluate the in vitro and in vivo performance of DALP for nmCRPC treatment.
- To assess the pharmacokinetic profile, anticancer efficacy, and safety of DALP.
Main Methods:
- Formulation of PEGylated liposomes encapsulating darolutamide (DALP).
- Characterization of particle size, polydispersity index, and zeta potential.
- In vitro release studies, cytotoxicity assays, apoptosis induction, cell invasion, and colony formation assays.
- In vivo pharmacokinetic, biodistribution, and acute toxicity studies.
Main Results:
- Optimized DALP showed favorable physicochemical properties (size, PDI, zeta potential) and high encapsulation efficiency (89.2%).
- DALP exhibited sustained drug release, enhanced antiproliferative activity (2.24-fold lower IC50), and increased apoptosis induction.
- Pharmacokinetic studies revealed prolonged plasma half-life (1.98-fold) and increased MRT (4.04-fold) with minimal off-target accumulation and confirmed safety.
Conclusions:
- PEGylated liposomal darolutamide (DALP) significantly improves the pharmacokinetic profile and therapeutic efficacy of darolutamide.
- DALP demonstrates enhanced anticancer activity and reduced systemic toxicity compared to free darolutamide.
- This nanocarrier strategy represents an advanced approach for treating non-metastatic castration-resistant prostate cancer.
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