AI Article Synopsis
- Monoclonal antibodies for cancer often don't work well in receptor-positive patients because the bound receptors are rapidly internalized, causing treatment failure.
- High doses of prochlorperazine (PCZ) can prevent this endocytosis, improving the effectiveness of antibodies, but may lead to neurological side effects.
- PEGylated liposomal formulations of PCZ (LPCZ) show promise by encapsulating the drug effectively, reducing its brain uptake, and maintaining its ability to inhibit receptor internalization, suggesting LPCZ could enhance mAb therapy in cancer treatment.
Article Abstract
Anti-cancer monoclonal antibodies often fail to provide therapeutic benefit in receptor-positive patients due to rapid endocytosis of antibody-bound cell surface receptors. High dose co-administration of prochlorperazine (PCZ) inhibits endocytosis and sensitises tumours to mAbs by inhibiting dynamin II but can also introduce neurological side effects. We examined the potential to use PEGylated liposomal formulations of PCZ (LPCZ) to retain the anti-cancer effects of PCZ, but limit brain uptake. Uncharged liposomes showed complete drug encapsulation and pH-dependent drug release, but cationic liposomes showed limited drug encapsulation and lacked pH-dependent drug release. Uncharged LPCZ showed comparable inhibition of EGFR internalisation to free PCZ in KJD cells. After IV administration to rats, LPCZ reduced the plasma clearance and brain uptake of PCZ compared to IV PCZ. The results suggest that LPCZ may offer some benefit over PCZ as an adjunct therapy in cancer patients receiving mAb treatment.
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| http://dx.doi.org/10.1016/j.nano.2024.102733 | DOI Listing |
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