RESUMO
In this study, chitosan low molecular weight (LCH) and chitosan medium molecular weight (MCH) were employed to encapsulate a yarrow extract rich in chlorogenic acid and dicaffeoylquinic acids (DCQAs) that showed antiproliferative activity against colon adenocarcinoma cells. The design of CH micro/nanoparticles to increase the extract colon delivery was carried out by using two different techniques: ionic gelation and spray drying. Ionic gelation nanoparticles obtained were smaller and presented higher yields values than spray-drying microparticles, but spray-drying microparticles showed the best performance in terms of encapsulation efficiency (EE) (> 94%), also allowing the inclusion of a higher quantity of extract. Spray-drying microparticles designed using LCH with an LCH:extract ratio of 6:1 (1.25 mg/mL) showed a mean diameter of 1.31 ± 0.21 µm and EE values > 93%, for all phenolic compounds studied. The release profile of phenolic compounds included in this formulation, at gastrointestinal pHs (2 and 7.4), showed for most of them a small initial release, followed by an increase at 1 h, with a constant release up to 3 h. Chlorogenic acid presented the higher release values at 3 h (56.91% at pH 2; 44.45% at pH 7.4). DCQAs release at 3 h ranged between 9.01- 40.73%, being higher for 1,5- and 3,4-DCQAs. After gastrointestinal digestion, 67.65% of chlorogenic and most DCQAs remained encapsulated. Therefore, spray-drying microparticles can be proposed as a promising vehicle to increase the colon delivery of yarrow phenolics compounds (mainly chlorogenic acid and DCQAs) previously described as potential agents against colorectal cancer.
Assuntos
Achillea , Proliferação de Células , Quitosana , Ácido Clorogênico , Neoplasias Colorretais , Nanopartículas , Tamanho da Partícula , Extratos Vegetais , Quitosana/química , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Achillea/química , Ácido Clorogênico/farmacologia , Ácido Clorogênico/administração & dosagem , Ácido Clorogênico/química , Nanopartículas/química , Proliferação de Células/efeitos dos fármacos , Neoplasias Colorretais/tratamento farmacológico , Linhagem Celular Tumoral , Ácido Quínico/análogos & derivados , Ácido Quínico/farmacologia , Ácido Quínico/química , Ácido Quínico/administração & dosagem , Liberação Controlada de Fármacos , Sistemas de Liberação de Medicamentos/métodos , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Colo/efeitos dos fármacos , Colo/metabolismo , Portadores de Fármacos/química , Peso MolecularRESUMO
Marjoram is a culinary herb that has been widely employed in folk medicine and presents a high content in phenolics. Thus, the aim of this project was to design formulations to encapsulate phenolic compounds from marjoram to allow their release in the colon. For this purpose, pectin was used as an encapsulating agent, applying two different encapsulation techniques (ionic gelation and spray-drying), followed by a CaCl2 bath. The ionic gelation technique showed a higher yield (77%) compared to spray-drying (31%), and the particles obtained were smaller (267 nm). However, the microparticles obtained by spray-drying presented a higher encapsulation efficiency (93%). Moreover, spray-dried microparticles protected a higher percentage of the encapsulated phenolics from the action of gastrointestinal pHs and enzymes. Hence, the results showed that spray-drying was a more appropriate technique than ionic gelation for the encapsulation of marjoram phenolics in order to protect them during the gastrointestinal step, facilitating their arrival in the colon. These microparticles would also be suitable for inclusion in food matrices for the development of phenolic colon delivery systems.