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Microparticles will probably play a promising role in the future of chemotherapy. These polymeric delivery systems are capable of maximizing the therapeutic activity while reducing side effects of anti-cancer agents. Usnic acid (UA) is a secondary metabolite produced by lichens, which exhibits an anti-tumour activity. In this study, PLGA-microspheres containing usnic acid from Cladonia substellata were prepared by the double emulsion method, with or without PEG as stabilizer. The morphology of the microspheres was examined by optical and scanning electron microscopy. The in vitro kinetic profile of usnic acid loaded-microspheres was carried out by dissolution testing. The usnic acid content was analysed by HPLC. The cytotoxicity of free and encapsulated usnic acid was evaluated against HEp-2 cells using the MTT method. The anti-tumour assay was performed in mice against Sarcoma-180 tumour (UA 15 mg kg(-1) weight body/day) during 7 days. Animals were then sacrificed and tumour and organs were excised for histopathological analysis. Microspheres presented a smooth spherical surface with a mean diameter of 7.02 +/- 2.72 microm. The usnic acid encapsulation efficiency was approximately 100% (UA 10 mg 460 mg(-1) microspheres). A maximum release of 92% was achieved at the fifth day. The IC50 values for free and encapsulated usnic acid were 12 and 14 microg ml(-1), respectively. The encapsulation of usnic acid into microspheres promoted an increase of 21% in the tumour inhibition as compared with the free usnic acid treatment. In summary, usnic acid was efficiently encapsulated into PLGA-microspheres and the microencapsulation improved its anti-tumour activity.

Cupuassu is a fruitful species from the Amazon basin with great economical potential, due to the multiple uses of its pulp and seeds in the food and cosmetic industries. This fruit generates large amounts of solid waste, which, despite of its high content of bioactive compounds, is discarded in the environment. Therefore, with the aim of reusing these wastes and adding economic value, we investigated the nutritional potential of the seed by-product resulting from industrial cupuassu oil extraction. The by-product was submitted to green extraction, and its contents of bioactive compounds were quantified by HPLC. The extract had a total polyphenol content (16.9 ± 1.8 mg/g DM ) and an antioxidant activity, ABTS + (151.0 ± 5.5 mg/100 g) and DPPH . (85.4 ± 1.7 mmol/L). HPLC analysis of the extract identified epicatechin and glycosylated quercetin as the major flavonoids. This by-product shows great potential for being used as a source of the ingredients of high nutritional value, especially dietary fiber and polyphenols. Practical Application:The by-product feature potential for its reutilization in different biotechnological processes.

Cupuassu (Theobroma grandiflorum Schum.) is a popular Amazonian fruit because of its intense aroma and nutritional value, whose lipid fraction is alternatively used in cosmetics. To preserve active principles and ensure their controlled release, extract was microencapsulated by spray drying. Influence of spray-drying conditions on microencapsulation of cupuassu seed by-product extract was investigated according to a 3-Box Behnken factorial design, selecting inlet temperature, maltodextrin concentration and feed flowrate as independent variables, and total polyphenol and flavonoid contents, antiradical power, yields of drying and microencapsulation as responses. Fitting the results by second-order equations and modelling by Response Surface Methodology allowed predicting optimum conditions. Epicatechin and glycosylated quercetin were the major microencapsulated flavonoids. Microparticles showed satisfactory antiradical power and stability at 5 °C or under simulated gastrointestinal conditions, thus they may be used to formulate new foods or pharmaceuticals.

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