PEGylation of PLA nanoparticles to improve mucus-penetration and colloidal stability for oral delivery systems

• Surface properties of PLA nanoparticles can be tuned to be used in oral drug delivery.
• To let the oral administration of PLA nanoparticles since by themselves it is limited.
• PEGylation is a strategy to ensure rapid Nps transport through the mucus.
• Dense PEG coating modulates bioadhesive properties of PLA nanoparticles.

Poly(lactic acid) (PLA) nanoparticles are one of the most studied systems for drug delivery due to their biodegradability and biocompatibility. However, oral administration, which is a non-invasive and convenient route, is limited by PLA hydrophobicity as well as low chemical and colloidal stability in the gastrointestinal track. These drawbacks can be overcome by coating the PLA nanoparticle surface with hydrophilic polymers, such as polyethylene glycol, and controlling the coverage density. This type of modification is being extensively explored for oral drug delivery. The challenges associated with the delivery of these nanoparticles depend greatly on the surface properties, such as hydrophobicity, charge and particle size. This review highlights nanoparticle design considerations for overcoming physiological hurdles (i.e. chemical and enzymatic barriers) for the oral administration of drugs.

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