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GLG-PT-IL is an immunoliposomal formulation designed for targeted cancer therapy. It consists of liposomes encapsulating 7-alpha-glucosyloxyacetylpaclitaxel (7-GLG-PT, a water-soluble glycosylated derivative of paclitaxel) and conjugated with the anti-HER2 monoclonal antibody trastuzumab on the liposome surface. The glycosylation of paclitaxel at the 7-OH position with glucose improves its water solubility, allowing for highly efficient encapsulation into the inner aqueous core of liposomes via remote loading. Trastuzumab on the surface of the liposomes mediates specific binding and receptor-mediated endocytosis into HER2-overexpressing cancer cells, such as SK-BR-3 breast cancer cells and HT-29 colon cancer cells. Once internalized, the formulation releases the paclitaxel prodrug, which stabilizes microtubules and inhibits cell division, leading to rapid cell growth suppression and tumor regression with reduced systemic toxicity compared to free paclitaxel.
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