Formulation, Characterization and Stability Assessment of a Food‐Derived Tripeptide, Leucine‐Lysine‐Proline Loaded Chitosan Nanoparticles

• Autores: Minna K. Danish, Giuliana Vozza, Hugh J. Byrne, J.M. Frias, Sinéad M. Ryan
• Localización: Journal of food science, ISSN 0022-1147, Vol. 82, Nº 9, 2017, págs. 2094-2104
• Idioma: inglés
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• Resumen

  • The chicken‐ or fish‐derived tripeptide, leucine‐lysine‐proline (LKP), inhibits the angiotensin converting enzyme and may be used as an alternative treatment for prehypertension. However, it has low permeation across the small intestine. The formulation of LKP into a nanoparticle (NP) has the potential to address this issue. LKP‐loaded NPs were produced using an ionotropic gelation technique, using chitosan (CL113). Following optimization of unloaded NPs, a mixture amount design was constructed using variable concentration of CL113 and tripolyphosphate at a fixed LKP concentration. Resultant particle sizes ranged from 120 to 271 nm, zeta potential values from 29 to 37 mV, and polydispersity values from 0.3 to 0.6. A ratio of 6:1 (CL113:TPP) produced the best encapsulation of approximately 65%. Accelerated studies of the loaded NPs indicated stability under normal storage conditions (room temperature). Cytotoxicity assessment showed no significant loss of cell viability and in vitrorelease studies indicated an initial burst followed by a slower and sustained release. This paper lays the basis for the formulation of a food origin peptide with potential antihypertensive bioactivity. An oral nanoparticle‐based delivery system is proposed. This approach has the potential to produce formulations with food‐based ingredients. The present work shows that the formulation matches the preclinical physicochemical characteristics required for oral delivery.