TY - JOUR
T1 - PEGylation as a strategy for improving nanoparticle-based drug and gene delivery
AU - Suk, Jung Soo
AU - Xu, Qingguo
AU - Kim, Namho
AU - Hanes, Justin
AU - Ensign, Laura M.
N1 - Funding Information:
This work was supported by National Institutes of Health grants U19AI133127 (J.H., L.M.E.), R01HL127413 (J.H., J.S.S.), R33AI094519 (J.H., L.M.E.), and R01EB020147 (J.H.); the Johns Hopkins University Center for AIDS Research P30AI094189 (L.M.E.); the 2015 Burroughs Wellcome Fund Preterm Birth Initiative (L.M.E); the Raymond Kwok Family Research Fund, USA (J.H. and Q.X.); and the Cystic Fibrosis Foundation (J.H., J.S.S.).
Publisher Copyright:
© 2015 Elsevier B.V.
PY - 2016/4/1
Y1 - 2016/4/1
N2 - 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.
AB - 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.
KW - Enhanced permeability and retention (EPR) effect
KW - Liposomes
KW - Mononuclear phagocyte system (MPS)
KW - Mucosal delivery
KW - Stealth coatings
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U2 - 10.1016/j.addr.2015.09.012
DO - 10.1016/j.addr.2015.09.012
M3 - Review article
C2 - 26456916
AN - SCOPUS:84960201366
SN - 0169-409X
VL - 99
SP - 28
EP - 51
JO - Advanced Drug Delivery Reviews
JF - Advanced Drug Delivery Reviews
ER -