Lipid-coated mesoporous silica nanoparticles of hydroxycamptothecin for sustained release and cancer therapy

Lipids with galactosylceramide-coated mesoporous silica nanoparticles were formulated in this study as a new strategy for the delivery of the poorly-soluble anticancer drug, hydroxycamptothecine. To improve drug loading, the mesoporous silica nanoparticle formulations and one of its preparation step-removal of cetyltrimethylammonium bromide were optimized under different conditions. The optimization produced uniform MSN with a hexagonal pore structure, surface area of 1131.48 m2·g-1, and HCPT drug loading of up to 29.94%. The surface of HCPT loaded with MSN was lipid-coated (HCPT-GC-LMSN) using a simple lipid film hydration method, optimized using the central composite design-response surface methodology, and then galactoseceramide was added to the lipid. The prepared HCPT-GC-LMSN was characterized using transmission electron microscopy, and particle size measurement indicated successful coating with an approximately 25 nm-thick lipid membrane. The in vitro cumulative release of HCPT-GC-LMSN was 48.82% within 36 h under a simulated tumor environment, showing sustained release properties. The cell-counting kit, (CCK)-8 cell viability test showed that HCPT-GC-LMSN had stronger inhibitory effects on hepatocellular carcinoma cells with a half-maximal inhibitory value of 7.13 μg/mL after 72 h, which was 2.97 times that than of HCPT. This formulated lipid with galactosylceramide-coated MSN could provide an effective strategy for delivering poorly-soluble anticancer drugs.