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gPTX-IL (glycosylated paclitaxel-loaded immunoliposome) is an experimental targeted drug delivery system developed by researchers at Okayama University and collaborating institutions. It consists of liposomes encapsulating 7-alpha-glucosyloxyacetylpaclitaxel (gPTX), a water-soluble glucose-conjugated derivative of paclitaxel, which are further functionalized with targeting monoclonal antibodies on their surface. Two primary formulations of gPTX-IL have been evaluated in preclinical studies: one conjugated with trastuzumab to target HER2-overexpressing cancers (such as breast and colorectal cancers), and another conjugated with an anti-CD44 antibody to target CD44-positive ovarian cancer cells. By utilizing a novel remote loading method with a solubility gradient, gPTX is efficiently encapsulated into the aqueous core of the liposomes. Preclinical in vitro and in vivo evaluations have demonstrated that gPTX-IL formulations exhibit enhanced tumor-targeting efficiency, rapid cellular internalization, and potent antitumor efficacy with significantly reduced systemic toxicity compared to free paclitaxel or non-targeted liposomes.
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