374473 Facile Access to Cation Functional Biodegradable Microparticles

Tuesday, November 18, 2014
Galleria Exhibit Hall (Hilton Atlanta)
Fang Feng1,2, Chao Deng3, Ru Cheng3, Fenghua Meng3 and Zhiyuan Zhong3, (1)Soochow University, Suzhou, China, (2)Suzhou University of Science and Technology, suzhou, China, (3)Soochow University, suzhou, China

Biodegradable polylactide(PLA), poly(lactic-co-glycolic acid)(PLGA) and poly(ε-carpolactone)(PCL) microparticles bearing a cationic surface have been investigated for mucoadhesive sustained release of therapeutic proteins, peptides, gene and vaccines. In the past years, different approaches have been developed to achieve a positively charged surface by either adsorbing cationic agents and surfactants or coating with polyelectrolyte, which is not very stable [1]. Here, we report on facile preparation of robust cationic biodegradable microparticles by treating poly(L-lactide-co-vinyl sulfone carbonate) (P(LLA-co-VSC)) microparticles with cationic mucoadhesive agents such as cysteamine and glycol chitosan.

P(LLA-co-VSC) random copolymers were synthesized by ring-opening copolymerization of L-lactic acid and vinyl sulfone carbonate (VSC) [2]. The microspheres based on P(LLA-co-VSC) were prepared by water-in-oil-in-water (W/O/W) emulsion process, followed by Michael-type conjugate addition with the thiol group of 2-mercaptoethylamine and the amine group of glycol chitosan, respectively. The results showed the P(LLA-co-VSC)3.57% microparticles had an  average size of  ca. 4 μm and a narrow particle size distribution. 1HNMR and XPS results displayed successful modification of microparticles with cationic agents under mild aqueous condition. SEM showed that cationic microparticles had a smooth surface morphorgy and a slightly increased particle size. Notably, the immobilization of glycol chitosan on the microspheres resulted in an increase of zeta potential to ca. +13 mV. The fluorescence images demonstrated obvious surface conjugation of amine-containing molecules. This gentle surface functionalization is important to maintain the bioactivity of proteins/peptides, gene and vaccines.


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