Encapsulation of Bromelain in Combined Sodium Alginate and Amino Acid Carriers: Experimental Design of Simplex-Centroid Mixtures for Digestibility Evaluation

• Published in: Molecules (Basel, Switzerland) Vol. 27; no. 19; p. 6364
• Main Authors: Ricardo, Philipi Cavalcante, Serudo, Ricardo Lima, Ţălu, Ştefan, Lamarão, Carlos Victor, da Fonseca Filho, Henrique Duarte, de Araújo Bezerra, Jaqueline, Sanches, Edgar Aparecido, Campelo, Pedro Henrique
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 27-09-2022; MDPI
• Subjects: alginate; Alginates - chemistry; Alginic acid; Amino Acids; Analgesics; Analysis; Bioavailability; bromelain; Bromelains; Centroids; Controlled release; Coronaviruses; COVID-19; Delayed-Action Preparations; Denaturation; Design of experiments; Digestibility; Digestion; Encapsulation; Enzymatic activity; Enzymes; Excipients; Experimental design; gastric digestion; Health aspects; Hydrogels; In vitro methods and tests; Inflammation; Intestine; Laboratories; Mixtures; Moisture content; Oral administration; Protein denaturation; Proteins; Research Design; Sodium; Sodium alginate; Software; Stabilizers (agents); Statistical analysis; Viscosity; Brazil; Japan; Romania; alginate; encapsulation; controlled release; gastric digestion; bioavailability; bromelain
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27196364

Bromelain has potential as an analgesic, an anti-inflammatory, and in cancer treatments. Despite its therapeutic effects, this protein undergoes denaturation when administered orally. Microencapsulation processes have shown potential in protein protection and as controlled release systems. Thus, this paper aimed to develop encapsulating systems using sodium alginate as a carrier material and positively charged amino acids as stabilizing agents for the controlled release of bromelain in in vitro tests. The systems were produced from the experimental design of centroid simplex mixtures. Characterizations were performed by FTIR showing that bromelain was encapsulated in all systems. XRD analyses showed that the systems are semi-crystalline solids and through SEM analysis the morphology of the formed systems followed a pattern of rough microparticles. The application of statistical analysis showed that the systems presented behavior that can be evaluated by quadratic and special cubic models, with a p-value < 0.05. The interaction between amino acids and bromelain/alginate was evaluated, and free bromelain showed a reduction of 74.0% in protein content and 23.6% in enzymatic activity at the end of gastric digestion. Furthermore, a reduction of 91.6% of protein content and 65.9% of enzymatic activity was observed at the end of intestinal digestion. The Lis system showed better interaction due to the increased stability of bromelain in terms of the amount of proteins (above 63% until the end of the intestinal phase) and the enzymatic activity of 89.3%. Thus, this study proposes the development of pH-controlled release systems aiming at increasing the stability and bioavailability of bromelain in intestinal systems.