Chitosan-graft-poly(lactic acid) (CS-

g

-PLA) copolymer was synthesized through emulsion self-assembly in a water-in-oil (W/O) microemulsion. The water phase was composed of CS aqueous solution

while the oil phase was made up of PLA in chloroform. The W/O microemulsion was fabricated in the presence of surfactant span-80 and the self-assembly was performed between PLA and CS under the effect of

N

-(3-dimethylaminopropyl)-

N

′-ethylcarbodiimide hydrochloride (EDC·HCl). FTIR and

1

H-NMR analysis indicated PLA was grafted onto the backbone of CS

via

the reaction between the carboxyl groups in PLA and the amino groups in CS.

1

H-NMR characterization further revealed the grafting content of PLA was 16%. The obtained CS-

g

-PLA could self-assemble to form micelles

their size distributed in the range of 125−375 nm with average diameter of 142 nm. The present design integrates the favorable biological properties of CS and the excellent mechanical properties of PLA

which makes CS-

g

-PLA copolymer a promising candidate as a carrier for targeted bioactive molecules delivery.