Abstracts Book - IMRC 2018

• SB6-O033
PREPARATION AND CHARACTERIZATION OF CONTROLLED DRUG
DELIVERY SYSTEM OF POLYMERIC NANOPARTICLES [poly(D,Llactide-co-glycolide)/poly(L-γ-glutamic
acid)], CONJUGATED TO
FOLIC ACID FOR TARGETED DELIVERY OF DOXORUBICIN
Laura Jaimes Aguirre 1 , Enrique Morales Avila 1 , Blanca E. Ocampo García 2 , Luis A. Medina 3
1 Universidad Autónoma del Estado de México, Pharmacy, Mexico. 2 Instituto Nacional de
Investigaciones Nucleares (ININ), Radiactive Materials, Mexico. 3 Universidad Nacional
Autónoma de México, Instituto de Física, Mexico.
Polymeric nanoparticles have an alternative to conventional cancer therapy,
since they allow to increase the selectivity of the treatment, minimizing
undesirable side effects on healthy tissues. PLGA and γ-PGA are polymers used
to obtain nanoparticles in drug delivery. Folic acid (FA) conjugates have shown
improved drug delivery to tumour cells by interaction with over-expressed folate
receptors. Thus, the aim of this study was to obtain and characterize a PLGA/ γ-
PGA-based nanoparticle system, functionalized with FA to delivery and release
of doxorubicin (DOX), as a model antineoplastic agent. In this research, PLGA
nanoparticles were obtained by emulsification-solvent evaporation technique.
The superficial modification with γ-PGA displayed a band at 208 nm, whilst FA
conjugation showed two bands at 280 nm and 248 nm, by UV-Vis spectrocopy.
Changes in signals in the range of 1250 cm -1 y 1780 cm -1 by FT-IR spectroscopy
demonstrated the successful modifications made to nanoparticles. TEM/SEM
micrographs exhibited quasi-spherical nanoparticles, with cumulus of polymeric
material. After modifications, particle size (DLS) remained lower than 600 nm,
and it was observed a change in zeta potential - 10.28 ± 1.37 mV a 14.2 ± 2.69
mV. DOX encapsulation efficiency was of 47.97 ± 1.8 %, with a loading efficiency
of 0.33 ± 0.012 %. Release profile of DOX-PLGA/γ-PGA-FA nanoparticles
responded to acidic conditions (pH 5.3), showing a release percentage of 55.42
± 0.6 %. Finally, DOX-PLGA/γ-PGA-FA were evaluated on HeLa cells, displaying a
viability decrease of 60 %, approximately, after 72 h of exposure. Cellular uptake
was attributed to FA receptor-mediated endocytosis. Based on these results, it
was concluded that PLGA/γ-PGA-FA nanoparticles are a potential carrier for
transport and delivery of drugs, such as DOX, through molecular recognition of
folate receptors over-expressed in some types of cancer, making it a suitable
candidate for further therapeutic applications.