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<p>This investigation was intended to prepare lipid-polymer hybrid nanoparticles (LPHNPs) that are laden with Gemcitabine hydrochloride (GEM) for the controlled delivery to treat Hepatocellular carcinoma (HCC). LPHNPs were developed by the solvent evaporation technique employing polycaprolactone (PCL) as the biodegradable polymeric core and a phospholipid shell comprised of soya phosphatidylcholine (SPC) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE). This study presents a cost-effective, simple method for functionalizing LPHNPs with the carbohydrate ligand D-galactose (GA) using stearyl amine (SA) as a linker. To examine the impact of three independent factors on the particle size, percent entrapment efficiency (% EE), and percent drug loading (% DL), a three-factor, three-level Box-Behnken design (BBD) was implemented with Design-Expert 13 software. The nanoparticles’ size range increased from 194.1 to 505.3&#xa0;nm when the polymer content increased. GEM’s percent drug release profile in the galactose functionalized gemcitabine-loaded lipid-polymer hybrid nanoparticles (GEM-LPHNPs-GA) suggests they are appropriate candidates for targeting the tumors microenvironment. In vitro drug release tests revealed a higher GEM release at pH 5.5 compared to the physiological pH of 7.4 for 48&#xa0;h. Fourier transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (<sup>1</sup>H-NMR) spectroscopy verified that the conjugate GA-SA imine bond formed. The cytotoxicity of GEM-LPHNPs-GA was significantly greater than that of GEM-LPHNPs or GEM alone, as evidenced by the MTT assay conducted on HepG2 cells. Throughout the incubation period, HepG2 cells exhibit a markedly higher absorption of dye-loaded LPHNPs-GA than LPHNPs. GEM-LPHNPs-GA is an efficacious formulation for the targeted administration of anti-cancer therapeutics.</p>

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Formulation and in vitro evaluation of lipid-polymer hybrid nanoparticles for targeted delivery of gemcitabine hydrochloride in the treatment of hepatocellular carcinoma

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • Swati Dubey,
  • Sanjeev Kumar Patel,
  • Chinmay Das,
  • Shalini Singh,
  • Geetika Sharma,
  • Chanakya Nath Kundu,
  • Sunita Minz

摘要

This investigation was intended to prepare lipid-polymer hybrid nanoparticles (LPHNPs) that are laden with Gemcitabine hydrochloride (GEM) for the controlled delivery to treat Hepatocellular carcinoma (HCC). LPHNPs were developed by the solvent evaporation technique employing polycaprolactone (PCL) as the biodegradable polymeric core and a phospholipid shell comprised of soya phosphatidylcholine (SPC) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE). This study presents a cost-effective, simple method for functionalizing LPHNPs with the carbohydrate ligand D-galactose (GA) using stearyl amine (SA) as a linker. To examine the impact of three independent factors on the particle size, percent entrapment efficiency (% EE), and percent drug loading (% DL), a three-factor, three-level Box-Behnken design (BBD) was implemented with Design-Expert 13 software. The nanoparticles’ size range increased from 194.1 to 505.3 nm when the polymer content increased. GEM’s percent drug release profile in the galactose functionalized gemcitabine-loaded lipid-polymer hybrid nanoparticles (GEM-LPHNPs-GA) suggests they are appropriate candidates for targeting the tumors microenvironment. In vitro drug release tests revealed a higher GEM release at pH 5.5 compared to the physiological pH of 7.4 for 48 h. Fourier transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy verified that the conjugate GA-SA imine bond formed. The cytotoxicity of GEM-LPHNPs-GA was significantly greater than that of GEM-LPHNPs or GEM alone, as evidenced by the MTT assay conducted on HepG2 cells. Throughout the incubation period, HepG2 cells exhibit a markedly higher absorption of dye-loaded LPHNPs-GA than LPHNPs. GEM-LPHNPs-GA is an efficacious formulation for the targeted administration of anti-cancer therapeutics.