Development of Chitosan/Mannitol Microparticles as Delivery System for the Oral Administration of a Spirulina Bioactive Peptide Extract

• Published in: Molecules (Basel, Switzerland) Switzerland), 2020-04, Vol.25 (9), p.2086
• Main Authors: Aquino, Rita P, Auriemma, Giulia, Conte, Giulio M, Esposito, Tiziana, Sommella, Eduardo, Campiglia, Pietro, Sansone, Francesca
• Format: Article
• Language: English
• Subjects: Administration, Oral; Algae; Algorithms; Bakeries; Biological activity; Biomass; Biomimetics; Blood pressure; Chitosan; Chitosan - chemistry; Drug Carriers - chemistry; Drug Compounding; Drug Delivery Systems; Drying; Efficiency; Encapsulation; Flow stability; Food; Intestine; Mannitol; Mannitol - chemistry; microencapsulation via spray drying; Models, Theoretical; Molecular weight; Morphology; nutraceutical products; Oral administration; Organoleptic properties; Particle Size; Peptides; Peptides - chemistry; Peptides - pharmacology; Permeability; Polymers; Proteins; Smell; Spirulina; Spirulina - chemistry; Spirulina extract; Spray drying; stability; technological properties; Vasodilation
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules25092086

contains several compounds showing nutritional and therapeutic benefits. Recently, a series of peptides able to reduce the blood pressure level and to enhance the endothelial vasorelaxation was isolated from the hydrolyzed highly water-soluble extract (HSE). However, HSE shows critical organoleptic characteristics also having poor intestinal permeability, limiting absorption when orally delivered. This research aims to overcome the critical issues through the encapsulation of HSE in Chitosan/Mannitol-(CM)-based microparticles by spray drying. The produced powders (CM-HSE) showed good process yield (≈70%) and encapsulation efficiency (≈100%) also having good derived flow properties as well as stability up to six months storage. The microparticles constituting the spray-dried powder resulted in an amorphous micrometric state (d ≈ 14 µm) able to retain dark colour and unpleasant smell of raw HSE. Moreover, the in vitro permeation study by Franz cell indicated that the engineered microparticles are able to enhance the permeation of HSE through an intestinal biomimetic barrier (551.13 μg/cm CM-HSE vs. 315.46 μg/cm HSE at 270 min).