Recent insights in the use of nanocarriers for the oral delivery of bioactive proteins and peptides

Batista, Patrícia; Castro, Pedro M.; Madureira, Ana Raquel; Sarmento, Bruno; Pintado, Manuela

doi:10.1016/j.peptides.2018.01.002

Cited by 78 publications

(36 citation statements)

References 117 publications

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“…Therefore, similarly to other nutrients and food bioactives, the incorporation of peptides into carriers has been demonstrated to increase their stability and bioavailability [ 207 ]. These systems show multiple mechanisms of action such as mucoadhesion, permeation enhancement across absorptive epithelium and TJs, high total surface area, targeted delivery, and affinity to specific intestinal cells [ 208 ]. Effective delivery systems must protect bioactive peptides from adverse conditions (variations of pH and temperature, enzymatic activity, etc.)…”

Section: Bioavailability Of Food Peptidesmentioning

confidence: 99%

“…The core-to-wall ratio influences the encapsulation efficiency; thus, it decreases when the core concentration increases [ 257 ]. However, controversial results from studies encapsulating different protein hydrolyzates/peptides indicate that in addition to the influence exerted by the core-to-wall ratio, the nature and molecular composition of the encapsulated material, and the type of the wall material, another factor to take into account is the encapsulation technique [ 208 ]. The most relevant techniques applied for the encapsulation of food protein hydrolyzates and peptides include film hydration, spray drying, coacervation, and ionotropic gelation ( Table 3 ).…”

Section: Bioavailability Of Food Peptidesmentioning

confidence: 99%

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Current Evidence on the Bioavailability of Food Bioactive Peptides

2020

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Food protein-derived bioactive peptides are recognized as valuable ingredients of functional foods and/or nutraceuticals to promote health and reduce the risk of chronic diseases. However, although peptides have been demonstrated to exert multiple benefits by biochemical assays, cell culture, and animal models, the ability to translate the new findings into practical or commercial uses remains delayed. This fact is mainly due to the lack of correlation of in vitro findings with in vivo functions of peptides because of their low bioavailability. Once ingested, peptides need to resist the action of digestive enzymes during their transit through the gastrointestinal tract and cross the intestinal epithelial barrier to reach the target organs in an intact and active form to exert their health-promoting properties. Thus, for a better understanding of the in vivo physiological effects of food bioactive peptides, extensive research studies on their gastrointestinal stability and transport are needed. This review summarizes the most current evidence on those factors affecting the digestive and absorptive processes of food bioactive peptides, the recently designed models mimicking the gastrointestinal environment, as well as the novel strategies developed and currently applied to enhance the absorption and bioavailability of peptides.

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Section: Bioavailability Of Food Peptidesmentioning

confidence: 99%

Section: Bioavailability Of Food Peptidesmentioning

confidence: 99%

Current Evidence on the Bioavailability of Food Bioactive Peptides

2020

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“…Today, developments are pursued considering "old" drug molecules and all APIs from the new generation including poorly soluble molecules and various biomolecules, i.e., peptides, proteins, nucleic acids. Drug delivery performances of polymer nanoparticles have been explored using almost all routes of administration [Cappel and Kreuter, 1991, Vauthier and Couvreur, 1991, Vauthier et al, 2003a, Mesiha et al, 2005, Ludwig et al, 2006, Alonso and Csaba, 2012, Fonte et al, 2015, Jonagam, 2017, Batista et al, 2018, Gedawy et al, 2018. Whatever the route of administration, the success of the delivery method greatly depends on the passage through different barriers separing the site of administration from the target site [Alonso and Csaba, 2012, Duncan and Richardson, 2012, Blanco et al, 2015, Ross et al, 2015, Lundquist and Arturson, 2016, Anchordoquy et al, 2017, Dai et al, 2018.…”

Section: Designing Nanoparticles Controlling Their In Vivo Drug Delivmentioning

confidence: 99%

“…Many questions about the mechanism, the safety and effectiveness of delivery methods that uses nanotechnologies such as polymer nanoparticles are yet unanswered [Card and Magnuson, 2011, Fonte et al 2015, Aguirre et al, 2016, Griffin et al, 2016, Lundquist and Artursson, 2016, Moraz et al, 2016, Gedawy et al, 2018. In the meanwhile, the approach initiated by Patrick coworkers in 1988 [Damgé et al, 1988] on the oral delivery of insulin with PACA nanoparticles has also been extended to many other therapeutic peptides and the use of other types of polymer nanoparticles [Couvreur and Puisieux, 1993, Vranckx et al, 1996, Damgé et al, 1997, Couvreur and Vauthier, 2006, Fonte et al, 2015, Batista et al, 2018, Kafka et al, 2011. The success of the approach raises debate.…”

Section: Oral Delivery Of Peptidesmentioning

confidence: 99%

A journey through the emergence of nanomedicines with poly(alkylcyanoacrylate) based nanoparticles

Vauthier

2019

Journal of Drug Targeting

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Starting in the late 1970s, the pioneering work of Patrick Couvreur gave birth to the first biodegradable nanoparticles composed of a biodegradable synthetic polymer. These nanoparticles, made of poly(alkylcyanoacrylate) (PACA), were the first synthetic polymer based nanoparticulate drug carriers undergoing a phase III clinical trial so far. Analyzing the journey from the birth of PACA nanoparticles to their clinical evaluation, the paper highlights their remarkable adaptability to bypass various drug delivery challenges found on the way. At present, PACA nanoparticles includes a wide range of nanoparticles that can associate drugs of different chemical nature and be administered in vivo by different routes. The most recent technologies giving the nanoparticles customized functions could also be implemented on this family of nanoparticles. Through different examples, the paper discusses the seminal role of the PACA nanoparticles' family in the development of nanomedicines.

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“…Consequently, biopharmaceuticals, including hormones, enzymes and immunomodulators, play an important role through the controlling of various functions, therefore they are useful in clinical practice to treat or prevent human disorders pathophysiological processes [4]. These days various macromolecules are intensively examined and more than thirty have been accepted by the Food and Drug Administration (FDA) for commercialization [5].…”

Section: Introductionmentioning

confidence: 99%

Review of recently used techniques and materials to improve the efficiency of orally administered proteins/peptides

et al. 2019

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Objectives The main objective of present review is to explore and evaluate the effectiveness of recently developed methods to improve the bioavailability of orally administered biopharmaceutical drugs. Methods A systematic search of sciencedirect, tandfonline and Google Scholar databases based on various sets of keywords was performed. All results were evaluated based on their abstracts, and irrelevant studies were neglected during further evaluation. Results At present, biopharmaceuticals are used as injectable therapies as they are not absorbed adequately from the different routes of drug administration, particularly the oral one. Their insufficient absorption is attributed to their high molecular weight, degradation by proteolytic enzymes, high hydrophilicity and rigidity of the absorptive tissues. From industrial aspect incorporation of enzyme inhibitors (EIs) and permeation enhancers (PEs) and mucoadhesive polymers into conventional dosage forms may be the easiest way of formulation of orally administered macromolecular drugs, but the effectiveness of protection and absorption enhancement here is the most questionable. Conjugation may be problematic from regulatory aspect. Encapsulation into lipid-based vesicles sufficiently protects the incorporated macromolecule and improves intestinal uptake but have considerable stability issues. In contrast, polymeric nanocarriers may provide good stability but provides lower internalization efficacy in comparison with the lipid-based carriers. Conclusion It can be concluded that the combination of the advantages of mucoadhesive polymeric and lid-based carriers in hybrid lipid/polymer nanoparticles may result in improved absorption and might represent a potential means for the oral administration of therapeutic proteins in the near future.

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Recent insights in the use of nanocarriers for the oral delivery of bioactive proteins and peptides

Cited by 78 publications

References 117 publications

Current Evidence on the Bioavailability of Food Bioactive Peptides

Current Evidence on the Bioavailability of Food Bioactive Peptides

A journey through the emergence of nanomedicines with poly(alkylcyanoacrylate) based nanoparticles

Review of recently used techniques and materials to improve the efficiency of orally administered proteins/peptides

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