MUMBAI, India, Oct. 5 -- Intellectual Property India has published a patent application (202611102045 A) filed by Dr. Vijayakumar M. R. on August 24, 2026, for Gefitinib And Betulin-Loaded Asgpr-Targeted Liposomes Against Hepatocellular Carcinoma.
Inventors include Dr. Vijayakumar M. R.; and Amita Singh.
The application for the patent was published on October 02, 2026, under issue no. 40/2026.
Abstract: Hepatocellular carcinoma (HCC) is difficult to treat, and gefitinib monotherapy may offer limited therapeutic benefits. Combination or multimodal approaches are often required to achieve therapeutic efficacy in such cases. Betulin, a naturally occurring triterpene, is used in combination with gefitinib to enhance therapeutic efficacy against HCC, but its clinical translation is not possible due to poor bioavailability and lack of targeted delivery. Therefore, we developed non-targeted and Lf-grafted targeted liposomes of gefitinib (GEF-Lipo and GEF-Lf-Lipo) and betulin (BET-Lipo and BET-Lf-Lipo) by the ethanol injection method and subsequently characterized them. GEF-Lipo and GEF-Lf-Lipo were 113.7 ± 14.4 nm and 161.2 ± 10.0 nm, respectively. The vesicular sizes of the optimized BET-Lipo and BET-Lf-Lipo were 150.2 ± 10.0 nm and 181.6 ± 4.8 nm, respectively. The PDI values for GEF-Lipo and GEF-Lf-Lipo were found to be 0.307 ± 0.11 and 0.436 ± 0.12, respectively, and the PDI values for BET-Lipo and BET-Lf-Lipo were found to be 0.462 ± 0.04 and 0.399 ± 0.03, respectively. The zeta potentials of GEF-Lipo and GEF-Lf-Lipo were - 0.781 ± 0.34 mV and -5.28 ± 2.27 mV, respectively. The zeta potentials of BET-Lipo and BET-Lf-Lipo were -1.09 ± 0.06 mV and -9.6 ± 5.03 mV, respectively. %EE of GEF-Lipo, GEF-Lf-Lipo, BET-Lipo, and BET-Lf-Lipo were found to be 84.7 ± 1.22%, 90.08 ± 1.73%, 91.4 ± 2.63%, and 93.21 ± 1.88%, respectively. GEF-BET- Lf-Lipo showed significantly higher cytotoxicity than GEF-BET-Lipo and mixture of GEF-BET. The findings indicate that GEF-BET-Lf-Lipo could be an effective carrier in delivering GEF and BET to the target site, which is a promising approach to treat HCC. Furthermore, an in vivo study has been performed to assess the effectiveness of mixtures of GEF-BET, GEF-BET-Lipo, and ASGPR targeted GEF-BET-Lf-Lipo. Physiological parameters and HCC biomarker AFP were quantified. AFP levels were significantly increased in the cancer control versus normal control (p 0.0001) and were significantly reduced by treatment with pristine drugs, non- targeted liposomes, and targeted liposomes (p 0.0001), supporting the therapeutic effects of the formulations. Morphological changes in liver tissue were evaluated through histopathological examination and SEM. Western blotting and IHC showed that both GEF-BET-Lipo and GEF-BET-Lf-Lipo treatments significantly reduced pSTAT3 expression and increased the levels of the apoptotic marker caspase-3. Overall, the findings support the enhanced antitumor potential of GEF-BET-Lf-Lipo against HCC in animals.
Disclaimer: Curated by HT Syndication.
