Formulation and Characterization of Anthocyanins-Loaded Nanoparticles.

BACKGROUND: Açaí berry, from the Euterpe oleracea Mart. Palm, has been described as the most important fruit in the Brazilian Amazon. Several studies have reported that anthocyanins (ACNs), one of the components of the açaí, have enormous potential for pharmaceuticals applications. However, the bioavailability of anthocyanins is relatively low compared to that of other flavonoids. Then, in the present work, anthocyanins-loaded nanoparticles have been developed to overcome their poor bioavailability. METHODS: A two-level factorial design with three factors was considered to evaluate the effect of EUDRAGIT ® L100, polyethylene glycol 2000 (PEG 2000) and polysorbate 80 on encapsulation efficiency (EE) of anthocyanins. Also, major parameters of nanoparticles were assessed by using mainly SEM microscopy and Dynamic light scattering. RESULTS: PEG 2000 was the only individual factor that has statistical significance (95% confidence level). The process yields (PY) were found in between 67% and 92%; the particle size and morphology analysis showed two distribution size, one for NPs and another for the agglomerates. CONCLUSION: The pH-sensitive polymer together with the hydrophilic polymer showed to be suitable as ACNs delivery system. The delayed release profile of ACNs, observed for all formulations, can enhance their poor bioavailability. Nevertheless, ACNs bioavailability in vivo remains to be studied.

Self-assembly in aqueous solution of amphiphilic graft copolymers from oxidized carboxymethylcellulose.

A series of oxidized carboxymethylcellulose-graft-poly(ethylene glycol)-dodecylamine (OCMC-g-PEG-DDA) was prepared by using an appositely prepared PEG with terminal amino groups and different amounts of DDA. The nanoaggregates formed in aqueous solution were characterized by surface tension measurements, fluorescence spectroscopy, dynamic light scattering (DLS) and scanning electron microscopies (SEM and TEM). The micelles showed narrow hydrodynamic size distributions and diameters varying from 163 to 193nm depending on the ratio of DDA to PEG chains. The DDA content in the graft copolymers also affected the core-shell interfacial compactness.

Design of indomethacin-loaded nanoparticles: effect of polymer matrix and surfactant.

Despite recent advances in nonsteroidal anti-inflammatory drug (NSAID) formulations, the design of targeted delivery systems to improve the efficacy and reduce side effects of NSAIDs continues to be a focus of much research. Enteric nanoparticles have been recognized as a potential system to reduce gastrointestinal irritations caused by NSAIDs. The aim of this study was to evaluate the effect of EUDRAGIT® L100, polyethylene glycol, and polysorbate 80 on encapsulation efficiency of indomethacin within enteric nanoparticles. Formulations were developed based on a multilevel factorial design (three factors, two levels). The amount of polyethylene glycol was shown to be the factor that had the greatest influence on the encapsulation efficiency (evaluated response) at 95% confidence level. Some properties of nanoparticles like process yield, drug-polymer interaction, particle morphology, and in vitro dissolution profile, which could affect biological performance, have also been evaluated.