PharmaceuticsSep 26, 2026

Using PSMA-Targeted Liposomes to Deliver Treatment into Prostate Cancer Cells

mRNA Technology Weekly Brief ↗PubMed ↗DOI ↗OA ↗

Updated Sep 27, 2026

Abstract

Talazoparib-loaded liposomes targeting prostate-specific membrane antigen (PSMA) showed preferential accumulation at tumor sites in mouse models.

The developed liposomes exhibited excellent stability and specific binding to PSMA-expressing prostate cancer cells in laboratory tests.
In mouse studies, these PSMA-targeted liposomes accumulated preferentially at tumor sites compared to other tissues.
Talazoparib, a PARP inhibitor, has limited solubility and cytotoxicity, impacting its effectiveness in prostate cancer treatment.
Combining Talazoparib-loaded liposomes with BI 2536 may enhance their antitumor activity in prostate cancer models.
Further research with larger control groups is necessary to confirm the therapeutic efficacy of this combination approach.

Simplified

Background: Prostate cancer (PCa) remains a significant health challenge, requiring innovative treatments. Here, we evaluated the efficacy of Talazoparib-loaded liposomes incorporating a targeting moiety, in combination with BI 2536, in PCa. This study develops lipid nanoparticles (LIPOs) targeting prostate-specific membrane antigen (PSMA) for better drug delivery. Methods: Two new PSMA-targeting agents, DUPA-DSPE and DUPA-PEG-DSPE, were created and incorporated into LIPOs via thin-film hydration. LIPOs' size and morphology were characterized using Dynamic light scattering, and structural analysis was done via TEM imaging. In vitro cytotoxicity and cell viability were assessed using an MTT assay, while in vivo radioactivity was evaluated by PET imaging, and radioactive activity was quantified using a γ-counter. Results: These LIPOs demonstrated excellent stability and specific binding to PSMA-expressing prostate cancer cells in vitro. In vivo, mouse model studies showed that PSMA-targeted LIPOs accumulated preferentially at tumor sites. Talazoparib, a PARP inhibitor with low solubility and cytotoxicity, has limited use in PCa. Conclusions: These findings provide proof-of-concept evidence that PSMA-targeted DUPA-PEG LIPOs can facilitate Talazoparib delivery and, particularly in combination with BI 2536, may enhance antitumor activity in PCa models. Further studies with expanded control groups and larger cohorts are warranted to validate the therapeutic efficacy of this combination strategy and support its further development for PCa treatment.

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Using PSMA-Targeted Liposomes to Deliver Treatment into Prostate Cancer Cells

Abstract

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