• Catiúscia P Oliveira, Willian A Prado, Vladimir Lavayen, Sabrina L Büttenbender, Aline Beckenkamp, Bruna S Martins, Diogo S Lüdtke, Leandra F Campo, Fabiano S Rodembusch, Andréia Buffon, Adalberto Pessoa, Silvia S Guterres, and Adriana R Pohlmann.
• Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil. catipadilha@yahoo.com.br.
• Pharm. Res. 2017 Feb 1; 34 (2): 438-452.

PurposeThis study was conducted a promising approach to surface functionalization developed for lipid-core nanocapsules and the merit to pursue new strategies to treat solid tumors.MethodsBromelain-functionalized multiple-wall lipid-core nanocapsules (Bro-MLNC-Zn) were produced by self-assembling following three steps of interfacial reactions. Physicochemical and structural characteristics, in vitro proteolytic activity (casein substrate) and antiproliferative activity (breast cancer cells, MCF-7) were determined.ResultsBro-MLNC-Zn had z-average diameter of 135 nm and zeta potential of +23 mV. The complex is formed by a Zn-N chemical bond and a chelate with hydroxyl and carboxyl groups. Bromelain complexed at the nanocapsule surface maintained its proteolytic activity and showed anti-proliferative effect against human breast cancer cells (MCF-7) (72.6 ± 1.2% at 1.250 μg mL-1 and 65.5 ± 5.5% at 0.625 μg mL-1). Comparing Bro-MLNC-Zn and bromelain solution, the former needed a dose 160-folds lower than the latter for a similar effect. Tripan blue dye assay corroborated the results.ConclusionsThe surface functionalization approach produced an innovative formulation having a much higher anti-proliferative effect than the bromelain solution, even though both in vitro proteolytic activity were similar, opening up a great opportunity for further studies in nanomedicine.

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