Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase

Phenylketonuria (PKU) is a genetic metabolic disorder caused by an enzyme deficiency that leads to the accumulation of phenylalanine, which can cause neurotoxicity and several other problems. A potential alternative to the universal standard treatment based on a lifelong protein-restricted diet, is...

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Main Authors: Daniel Abella-López, Adrián López-Teijeiro, Tomás Pose-Boirazian, Natalia Barreiro-Piñeiro, José M. Martínez-Costas
Format: Article
Language:English
Published: Elsevier 2025-08-01
Series:Materials Today Bio
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Online Access:http://www.sciencedirect.com/science/article/pii/S2590006425005575
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author Daniel Abella-López
Adrián López-Teijeiro
Tomás Pose-Boirazian
Natalia Barreiro-Piñeiro
José M. Martínez-Costas
author_facet Daniel Abella-López
Adrián López-Teijeiro
Tomás Pose-Boirazian
Natalia Barreiro-Piñeiro
José M. Martínez-Costas
author_sort Daniel Abella-López
collection DOAJ
description Phenylketonuria (PKU) is a genetic metabolic disorder caused by an enzyme deficiency that leads to the accumulation of phenylalanine, which can cause neurotoxicity and several other problems. A potential alternative to the universal standard treatment based on a lifelong protein-restricted diet, is the development of oral replacement therapies using phenylalanine ammonia lyase from Anabaena variabilis (AvPAL). However, oral administration of polypeptides presents a major challenge due to gastrointestinal (GI) instability. To address this issue, the use of the IC-Tagging system as an advanced one step, in cellulo nanosphere (NS)-encapsulation strategy for protein stabilization and oral delivery is proposed. A highly active version of AvPAL was produced to which nanoencapsulation provides formidable thermostability, resistance to acidic pH, long-term storage stability and protection against proteolytic degradation. This latter characteristic, essential for oral delivery of polypeptides, is further enhanced by coating with chitosan the NS-encapsulated enzyme. Thus, a similarly nanoencapsulated and chitosan-coated luciferase displays sustained enzymatic activity through the entire GI transit when administered orally in mice, indicating the high protective capability of the system while maintaining the availability of the enzyme. Overall, these results highlight the potential and versatility for peptide-based oral delivery applications of this innovative methodology.
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spelling doaj-art-4f0ba098af2e4b3db3b65859cb4bec582025-08-20T03:21:55ZengElsevierMaterials Today Bio2590-00642025-08-013310198710.1016/j.mtbio.2025.101987Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferaseDaniel Abella-López0Adrián López-Teijeiro1Tomás Pose-Boirazian2Natalia Barreiro-Piñeiro3José M. Martínez-Costas4Department of Biochemistry and Molecular Biology and Center for Research in Biological Chemistry and Molecular Materials (CIQUS), University of Santiago de Compostela, C/ Jerónimo de la Fuente S/N, 15782, Santiago de Compostela, SpainDepartment of Biochemistry and Molecular Biology and Center for Research in Biological Chemistry and Molecular Materials (CIQUS), University of Santiago de Compostela, C/ Jerónimo de la Fuente S/N, 15782, Santiago de Compostela, SpainDepartment of Biochemistry and Molecular Biology and Center for Research in Biological Chemistry and Molecular Materials (CIQUS), University of Santiago de Compostela, C/ Jerónimo de la Fuente S/N, 15782, Santiago de Compostela, SpainDepartment of Biochemistry and Molecular Biology and Center for Research in Biological Chemistry and Molecular Materials (CIQUS), University of Santiago de Compostela, C/ Jerónimo de la Fuente S/N, 15782, Santiago de Compostela, SpainCorresponding author.; Department of Biochemistry and Molecular Biology and Center for Research in Biological Chemistry and Molecular Materials (CIQUS), University of Santiago de Compostela, C/ Jerónimo de la Fuente S/N, 15782, Santiago de Compostela, SpainPhenylketonuria (PKU) is a genetic metabolic disorder caused by an enzyme deficiency that leads to the accumulation of phenylalanine, which can cause neurotoxicity and several other problems. A potential alternative to the universal standard treatment based on a lifelong protein-restricted diet, is the development of oral replacement therapies using phenylalanine ammonia lyase from Anabaena variabilis (AvPAL). However, oral administration of polypeptides presents a major challenge due to gastrointestinal (GI) instability. To address this issue, the use of the IC-Tagging system as an advanced one step, in cellulo nanosphere (NS)-encapsulation strategy for protein stabilization and oral delivery is proposed. A highly active version of AvPAL was produced to which nanoencapsulation provides formidable thermostability, resistance to acidic pH, long-term storage stability and protection against proteolytic degradation. This latter characteristic, essential for oral delivery of polypeptides, is further enhanced by coating with chitosan the NS-encapsulated enzyme. Thus, a similarly nanoencapsulated and chitosan-coated luciferase displays sustained enzymatic activity through the entire GI transit when administered orally in mice, indicating the high protective capability of the system while maintaining the availability of the enzyme. Overall, these results highlight the potential and versatility for peptide-based oral delivery applications of this innovative methodology.http://www.sciencedirect.com/science/article/pii/S2590006425005575Oral peptide deliveryProtein stabilizationIC-TaggingPhenylketonuriaEnzyme replacement therapyAvPAL
spellingShingle Daniel Abella-López
Adrián López-Teijeiro
Tomás Pose-Boirazian
Natalia Barreiro-Piñeiro
José M. Martínez-Costas
Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
Materials Today Bio
Oral peptide delivery
Protein stabilization
IC-Tagging
Phenylketonuria
Enzyme replacement therapy
AvPAL
title Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
title_full Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
title_fullStr Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
title_full_unstemmed Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
title_short Nanoencapsulation platform for oral delivery of peptides: In vitro stabilization of AvPAL and formulation of a gastrointestinal-resistant luciferase
title_sort nanoencapsulation platform for oral delivery of peptides in vitro stabilization of avpal and formulation of a gastrointestinal resistant luciferase
topic Oral peptide delivery
Protein stabilization
IC-Tagging
Phenylketonuria
Enzyme replacement therapy
AvPAL
url http://www.sciencedirect.com/science/article/pii/S2590006425005575
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