How to design the surface of peptide-loaded nanoparticles for efficient oral bioavailability?

Malhaire, Hélène; Gimel, Jean-Christophe; Roger, Émilie; Benoı̂t, Jean-Pierre; Lagarce, Frédéric

doi:10.1016/j.addr.2016.03.011

Cited by 84 publications

(64 citation statements)

References 252 publications

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“…For instance, not only formation, kinetics and dynamic nature of the PC have been investigated in the last few years, but also strategies to either minimize its building-up or exploit its use for targeting purposes have been developed [4]. Nevertheless, the majority of studies on PC and colloidal stability of NPs are performed in blood or serum, thus only related to NPs administration by injection [3,5].…”

Section: The Learnt Lesson: Protein Corona Governs the Fate Of Nanopamentioning

confidence: 99%

“…Orally delivered NPs need to cross: 1) the harsh GI environment (i.e. low pH and digestive enzymes); 2) the mucus barrier and then 3) the intestinal enterocyte lining before reaching the bloodstream [5]. Scientists have focused so far on studying these three biological barriers only, without taking into consideration that NPs might completely change their physicochemical features even before reaching the mucosal and absorption sites in the gut.…”

Section: What About the Protein Corona In The Gut?mentioning

confidence: 99%

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Oral delivery of nanoparticles - let’s not forget about the protein corona

Berardi

Bombelli²

2019

Expert Opinion on Drug Delivery

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Section: The Learnt Lesson: Protein Corona Governs the Fate Of Nanopamentioning

confidence: 99%

Section: What About the Protein Corona In The Gut?mentioning

confidence: 99%

Oral delivery of nanoparticles - let’s not forget about the protein corona

Berardi

Bombelli²

2019

Expert Opinion on Drug Delivery

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“…It is acknowledged that polymeric nanoparticles can protect the loaded labile bio‐macromolecules from the harsh environment in the gastrointestinal tract (GIT). A myriad of polymeric materials were introduced to modify the charge, surface polarities, bioadhesive properties, and/or cellular interactions of the carriers with the purpose to enhance the oral absorption of intact nanoparticles . However, whether the nanocarriers can be absorbed intactly along with the cargo or the cargo is prematurely released in GIT prior to permeating across the intestinal membrane is yet inconclusive .…”

Section: Introductionmentioning

confidence: 99%

“…However, particle size may be the foundamental one due to the threshold size for absorption. [2a,c] Therefore, in this study, PCL nanoparticles with particle size of 50, 200, 600, and 2000 nm were prepared, respectively. ACQ probes, named as P2 or P4, were physically entrapped in the nanoparticles for bioimaging, facilitating visualization of in vivo translocation and cellular interaction of nanoparticles.…”

Section: Introductionmentioning

confidence: 99%

Bioimaging of Intact Polycaprolactone Nanoparticles Using Aggregation‐Caused Quenching Probes: Size‐Dependent Translocation via Oral Delivery

Xie

et al. 2018

Adv Healthcare Materials

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The limited information on biological fate impedes the development of more efficient polymeric nanoparticles for oral delivery of bio‐macromolecules. In this study, the in vivo fate as well as the trans‐epithelia transport of polycaprolactone (PCL) nanoparticles is explored by labeling with aggregation‐caused quenching probes, which is capable of identifying intact nanoparticles. Live imaging and confocal laser scan microscopy confirm size‐dependent absorption of PCL nanoparticles. In general, reducing particle size favors a faster and more oral absorption. Nanoparticles larger than 200 nm, such as 600 and 2000 nm, cannot be efficiently transported across the intestinal membrane. The absorbed nanoparticles (50 and 200 nm) mainly accumulate in the liver. Lymph may be the main absorption route for PCL nanoparticles, transporting 2.39 ± 1.81% and 0.98 ± 0.58% of administered 50 and 200 nm nanoparticles, respectively. Cellular uptake and transportation of PCL nanoparticles are also size dependent. Both enterocytes and M cells mediated transcytosis are involved in the transport of 50 nm PCL nanoparticles, while the M cell pathway is dominative for other nanoparticles. In conclusion, the study provides a valuable tool for bioimaging of intact polymeric nanoparticles as well as solid evidence supporting size‐dependent translocation of the nanoparticles via oral delivery.

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“…liposomes, noisomes, and polymeric nanoparticles was amongst the promising approaches attempted to overcome the obstacles facing oral protein delivery 4–6 . Moreover, several studies revealed that nanoparticles have an enormous impact on the oral bioavailability of biologic drugs including therapeutic proteins 3,4,7–9 . Polymeric nanocapsules (PNCs) comprise a core-shell structure in which proteins are confined and surrounded by a biodegradable polymer 10,11 .…”

Section: Introductionmentioning

confidence: 99%

Lysozyme and DNase I loaded poly (D, L lactide-co-caprolactone) nanocapsules as an oral delivery system

Abed

Chaw

Williams

et al. 2018

Sci Rep

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Clinical applications of oral protein therapy for the treatment of various chronic diseases are limited due to the harsh conditions encounter the proteins during their journey in the Gastrointestinal Tract. Although nanotechnology forms a platform for the development of oral protein formulations, obtaining physiochemically stable formulations able to deliver active proteins is still challenging because of harsh preparation conditions. This study proposes the use of poly (D, L-lactic-co-caprolactone)-based polymeric nanocapsules at different monomers’ ratios for protein loading and oral delivery. All formulations had a spherical shape and nano-scale size, and lysozyme encapsulation efficiency reached 80% and significantly affected by monomers’ ratio. Trehalose and physical state of lysozyme had a significant effect on its biological activity (P < 0.05). Less than 10% of the protein was released in simulated gastric fluid, and 73% was the highest recorded accumulative release percentage in simulated intestinal fluid (SIF) over 24 h. The higher caprolactone content, the higher encapsulation efficiency (EE) and the lower SIF release recorded. Therefore, the formulation factors were optimised and the obtained system was PEGylated wisely to attain EE 80%, 81% SIF release within 24 h, and 98% lysozyme biological activity. The optimum formulation was prepared to deliver DNase, and similar attributes were obtained.

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How to design the surface of peptide-loaded nanoparticles for efficient oral bioavailability?

Cited by 84 publications

References 252 publications

Oral delivery of nanoparticles - let’s not forget about the protein corona

Oral delivery of nanoparticles - let’s not forget about the protein corona

Bioimaging of Intact Polycaprolactone Nanoparticles Using Aggregation‐Caused Quenching Probes: Size‐Dependent Translocation via Oral Delivery

Lysozyme and DNase I loaded poly (D, L lactide-co-caprolactone) nanocapsules as an oral delivery system

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