PEGylated polymers for medicine: from conjugation to self-assembled systems

Hydroxyethyl starch–10-hydroxy camptothecin conjugate: synthesis, pharmacokinetics, cytotoxicity and pharmacodynamics research

“…It has been reported that the substitution on 20-OH group of 10-HCPT can substantially reduce the tendency for lactone ring opening and increase the solubility, and a variety of conjugates that link 10-HCPT via 20-OH group have been performed, including PEG-camptothecin conjugate, polyglutamate-camptothecin conjugate, PEG-SN38 conjugate and PAMAM-camptothecin conjugate, some of them have entered into the phase of clinical research (Bhatt et al, 2003;Cheng et al, 2004;Fleming et al, 2004;Samor et al, 2008;Joralemon et al, 2010;Tong & Cheng, 2010). Except improving the solubility and stability of 10-HCPT, polymer conjugate can also prolong circulation time through avoiding rapid clearance by the renal and reticuloendothelial systems (RES), decrease side effects, passive target tumor tissues via the enhanced permeability and retention (EPR) effect and improve bioavailability (Li & Wallace, 2008;Maeda et al, 2009;Torchilin, 2011).…”

Gelatinase-stimuli strategy enhances the tumor delivery and therapeutic efficacy of docetaxel-loaded poly(ethylene glycol)-poly(ε-caprolactone) nanoparticles

“…28 PEGylation prolongs blood circulation, increases tumor accumulation, reduces serum protein adherence and creates a stealth surface to avoid the uptake by the reticuloendothelial systems (RES). PEGylated nanoparticles are also preferable with good biocompatibility, biodegradability, low antigenicity, and immunogenicity.…”

The Development of Targeted Drug Delivery Systems for Rheumatoid Arthritis Treatment

“…Liu & Frechet, 1999). Mono-and di-hydroxyl terminated poly(ethylene glycol) (PEG) have proven to be the most versatile polymers for increasing the stability, solubility, and pharmacokinetic properties of associated therapeutics, with several PEG-drug conjugates on the market for a number of indications (Joralemon et al, 2010). Only recently has this research translated to the development of macromolecular therapeutics for the treatment of rheumatoid arthritis, as discussed further in Section 4.…”

“…Although conventional liposomes suffer from rapid uptake by the reticuloendothelial system, incorporation of PEG into the bilayer yields so called "stealth" liposomes with enhanced circulation times. Starting with the anticancer compound Doxil (Gabizon, 2001), several PEG-modified liposomes with encapsulated therapeutics have reached commercialization (Joralemon, et al, 2010). As a consequence, liposomal use has been widely studied as a potential carrier system for drug delivery for rheumatoid arthritis (Foong & Green, 1993;Konigsberg et al, 1999;Monkkonen et al, 1994;Shaw et al, 1979) .…”