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Among many nanotechnological applications, the therapeutical use of nanocarriers is of relevance. G-1, a G-protein estrogen receptor (GPER-1) selective agonist, was encapsulated in polymeric nanoparticles and liposomes modified for central nervous system applications. GPER-1 signals through the rapid estrogen pathway, which is linked with neuroprotection and anti-inflammatory phenomena. Polyssorbate-80-coated PLGA nanoparticles and anti-transferrin antibody labelled immunoliposomes were synthesized. The nanoparticles were obtained by the oil-in-water emulsion method followed by sonication. This synthesis was optimized in terms of surfactant (DMAB or DDAB), sonication regime, T-80 solution dispersion volume and size of stirrer on the size, polidispersity and zeta potential of the nanoparticles. Immunoliposomes containing either DPPC:CH:DSPE-PEG2000 or DOPC:CH:DSPE-PEG2000 at 4:1:0.2 molar proportions and DSPEPEG2000-Transferrin(mAb); were obtained by the lipid film hydration method followed by sonication. DMAB tends to produce more monodisperse and stable particles. Moreover, immunoliposomes obtained with DOPC are smaller than those with DPPC. In vitro experiments were performed with Neuro-2a and/or SHSY5Y cells. The results show that T-80-coated NPs do not possess cytotoxicity at low dilutions (324 μg/mL) and are internalized within 24 h. On the other hand, immunoliposomes did not reveal cytotoxicity and were internalized in neurons in less than 30 min. G-1 was encapsulated in both systems, in which PLGA nanoparticles revealed a much lower encapsulation efficiency (41,45 ± 4,05%) than immunoliposomes (97,17 ± 2,84%). These process optimizations may elucidate many aspects of nanocarrier synthesis. It is also believed that G-1-loaded nanocarriers may be efficient for the treatment of several central nervous system diseases more efficiently. Correspondence to: Listik E, Department of Pharmacology, Institute of Biomedical Sciences, Sao Paulo University, P.O. Box: 05508-000, Sao Paulo, Brazil, Tel/Fax: ++55-11-3091-7322; E-mail: eduardo.listik@usp.br

Development and optimization of G-1 polymeric nanoparticulated and liposomal systems for central nervous system applications