SEDYAKINA Nataliya E. Nanosystem Ltd.

Surface-modified Biodegradable Nanoparticles for Targeted Drug Delivery

Co-authors GORSHKOVA Marina Y., MAKSIMENKO Olga O., GELPERINA Svetlana E.
Collaboration: A.V.Topchiev Institute of Petrochemical Synthesis RAS, Moscow, Russian Federation

Targeted drug delivery is suggests an affinity-based interaction of drug carriers with specific cells or tissues. Such drug delivery systems must be functionalized with a ligand that will bind specifically to receptors [1]. In this work the density of carboxyl groups on the surface of biodegradable nanoparticles was regulated to attach a model proteinacious ligand. PLGA/polyacid nanoparticles were prepared using two different methods: nanoprecipitation and high pressure emulsification - solvent evaporation technique. DIVEMA (copolymer of maleic anhydride and divinyl ether) was used as the polyacid. The effect of molecular weight of DIVEMA and the ratio of DIVEMA to PLGA (w/w) on the density of the carboxylic groups on the surface of the PLGA-DIVEMA nanoparticles was investigated. It was shown that the increase of the DIVEMA/PLGA (w/w) ratio from 1:10 to 1:1 led to the increase of the content of carboxylic groups from 1.5 to 10.8 mmol/g PLGA (nanoprecipitation). The model protein (insulin or human serum albumin (HSA)) was conjugated to carboxylic groups on the nanoparticles surface through a carbodiimide-meditated coupling reaction. The number of the functional groups on the nanoparticle surface was evaluated after each reaction step. The nanoparticles size, polydispersity (PD), and surface charge were measured using Zetasizer NanoZS (Malvern, GB). LITERATURE: [1]. McCARRON, P. A., MAROUF W. M., DONNELLY R. F., SCOTT C. Journal of Biomedical Materials Research Part A, 2008, 87A (4), 873 – 884.