In vivo study of the mucus-permeating properties of PEG-coated nanoparticles following oral administration

Inchaurraga, Laura; Martín-Arbella, Nekane; Zabaleta, Virginia; Quincoces, Gemma; Peñuelas, Iván; Irache, Juan M.

doi:10.1016/j.ejpb.2014.12.021

Cited by 93 publications

(42 citation statements)

References 46 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Inchaurraga and coworkers investigated the effect of PEG molecular weight on orally administered NPs prepared from methyl vinyl ether-maleic anhydride copolymer (Gantrez® AN) [164]. In this study, the PEG coating was formed by incubation of the two polymers and desolvation, rather than covalent conjugation.…”

Section: Non-systemic Applications For Improved Delivery With Pegymentioning

confidence: 99%

“…Fluorescent images of the ileum suggested that the PEG containing particles were able to reach the villus cell surfaces, whereas the uncoated NP remained in the luminal mucus away from the tissue. They further suggested that the effect was more pronounced for NPs containing 2 kDa and 6 kDa PEG than 10 kDa PEG [164]. Maisel and coworkers investigated the effect of dense PEG coatings and NP size on both orally and rectally administered NPs [165].…”

Section: Non-systemic Applications For Improved Delivery With Pegymentioning

confidence: 99%

See 1 more Smart Citation

PEGylation as a strategy for improving nanoparticle-based drug and gene delivery

Suk

Kim

et al. 2016

Advanced Drug Delivery Reviews

3,169

2,076

View full text Add to dashboard Cite

Coating the surface of nanoparticles with polyethylene glycol (PEG), or “PEGylation”, is a commonly used approach for improving the efficiency of drug and gene delivery to target cells and tissues. Building from the success of PEGylating proteins to improve systemic circulation time and decrease immunogenicity, the impact of PEG coatings on the fate of systemically administered nanoparticle formulations has, and continues to be, widely studied. PEG coatings on nanoparticles shield the surface from aggregation, opsonization, and phagocytosis, prolonging systemic circulation time. Here, we briefly describe the history of the development of PEGylated nanoparticle formulations for systemic administration, including how factors such as PEG molecular weight, PEG surface density, nanoparticle core properties, and repeated administration impact circulation time. A less frequently discussed topic, we then describe how PEG coatings on nanoparticles have also been utilized for overcoming various biological barriers to efficient drug and gene delivery associated with other modes of administration, ranging from gastrointestinal to ocular. Finally, we describe both methods for PEGylating nanoparticles and methods for characterizing PEG surface density, a key factor in the effectiveness of the PEG surface coating for improving drug and gene delivery.

show abstract

Section: Non-systemic Applications For Improved Delivery With Pegymentioning

confidence: 99%

Section: Non-systemic Applications For Improved Delivery With Pegymentioning

confidence: 99%

PEGylation as a strategy for improving nanoparticle-based drug and gene delivery

Suk

Kim

et al. 2016

Advanced Drug Delivery Reviews

3,169

2,076

View full text Add to dashboard Cite

show abstract

“…Incorporation of paclitaxel into PEG‐coated nanoparticles increased the permeability of the drug compared to the commercial paclitaxel‐formulation. In a follow‐up study by Inchaurraga et al, 150 nm Gantrez AN‐nanoparticles exhibited a good mucopenetration when coated with 2 or 6 kDa PEG while the mucopenetration was less intense for nanoparticles coated with 10 kDa PEG, determined from the tissue distribution of nanoparticles in the gastrointestinal mucosa after oral administration in rats.…”

Section: Mucus Penetrationmentioning

confidence: 99%

“…This narrow threshold value is, however, likely to vary depending on the particle core material . For instance, Inchaurraga et al claimed that PEG‐coated 150 nm Gantrez AN‐nanoparticles with zeta potential of ≅44 mV were able to penetrate mucus. Cu and Saltzman compared the diffusion coefficients of 10% PEG‐coated PLGA nanoparticles to fully coated nanoparticles in CVM and discovered that when the surface coverage was low, increasing the molecular weight of PEG increased the diffusion.…”

Section: Mucus Penetrationmentioning

confidence: 99%

A Polymer Chemistry Point of View on Mucoadhesion and Mucopenetration

Schattling

Taipaleenmäki

Zhang

et al. 2017

Macromolecular Bioscience

View full text Add to dashboard Cite

Although oral is the preferred route of administration of pharmaceutical formulations, the long-standing challenge for medically active compounds to efficiently cross the mucus layer barrier limits its wider applicability. Efforts in nanomedicine to overcome this hurdle consider mucoadhesive and mucopenetrating drug carriers by selectively designing (macromolecular) building blocks. This review highlights and critically discusses recent strategies developed in this context including poly(ethylene glycol)-based modifications, cationic and thiolated polymers, as well as particles with high charge density, zeta-potential shifting ability, or mucolytic properties. The latest advances in ex vivo test platforms are also reviewed.

show abstract

“…For fluorescently labelled nanoparticles, a protocol previously described was used [27]. Thus, the animals received orally a single dose of 30 mg nanoparticles (LP-NP-Z) dispersed in 1 mL water.…”

Section: In Vivo Distribution Studymentioning

confidence: 99%