A simple and general method for preparing antibody-PEG-PLGA sub-micron particles using electrospray technique: an in vitro study of targeted delivery of cisplatin to ovarian cancer cells.

Cisplatin-encapsulating maleimide-polyethylene glycol- Poly(d,l-lactic-co-glycolide) (cis-encapsulating mal-PEG-PLGA) particles were produced using the electrospray technique and bioconjugated with CD44 monoclonal antibody, targeting the counterpart receptor. The produced suspension of cis-encapsulating CD44-PEG-PLGA particles contains an antibody loading of 12.65-15.17 μg/mL and efficiently targets a CD44-overexpressed ovarian cancer cell line, such as CP70 and SKOV-3, within 6h of treatment, which was determined by Bradford assay, immunofluorescence analysis, and confocal laser scanning microscopic (CLSM) study. Most importantly, no tedious multi-step bioconjugation procedures are needed to synthesize mal-PEG-PLGA vehicles for antibody and drug loading, avoiding the undesirable hydrolysis of mal-PEG moiety and so successfully generating the cis-encapsulating mal-PEG-PLGA particles within one step. After conjugation of the CD44 antibody, the produced cis-encapsulating CD44-PEG-PLGA particles exhibited a better anti-proliferative ability against ovarian cancer cells compared to free form of cisplatin and PLGA particles without CD44 conjugation. Notably, the cis-encapsulating CD44-PEG-PLGA particles have approximately 10-14% greater the anti-proliferative ability against CP70 and SKOV-3 cells at a concentration of 1.25 μM, which falls within the concentrations used in chemotherapy. The proposed antibody-functionalization strategy represents an excellent platform for preparing particles with targeting ability in cancer therapy in vitro or in vivo.