Encapsulation of poorly soluble anti-cancer drugs in self-assembled nanoshell structure is a promising strategy for efficient delivery via intravenous administration. Stable dispersion of nanoparticles with an average size of 150 nm diameter and drug loading capacity of 60 wt. % was synthesized by using washless layer-by-layer (LbL) assembly to form camptothecin (CPT) cores coated with 8 bilayers of alternating heparin and block-copolymer of poly-L-lysine and polyethylene glycol (PEG). The outermost layer of nanoparticle was covered with PEG of 5 kDa and 20 kDa to resist serum protein adsorption and prolong systemic circulation due to sustained release kinetics. The advantage of LbL coated nanoparticle is to preserve active lactone form of CPT by initial 3.5 bilayers of the shell at acidic pH. Increasing active form of CPT was achieved by incorporation of bovine serum albumin (BSA) along with drug core as compared to the drug itself. In conclusion cytotoxicity activity of LbL coated CPT nanoparticles against CRL2303 glioblastoma cancer cells was found 20-25% higher than uncoated drug. IC50 of CPT was decreased from ca. ~146 nM to ~103 nM after encapsulation of drug using LbL coated nanoshell.

Enhanced cytotoxic activity of LbL coated camptothecin for cancer treatment

247th National Meeting (2014)

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