Chemistry Routes for Copolymer Synthesis Containing PEG for Targeting, Imaging, and Drug Delivery Purposes

Abstract

Polyethylene glycol (PEG) is one of the most frequently used polymers for coating nanocarriers to enhance their biocompatibility, hydrophilicity, stability, and biodegradability. PEG is now considered to be among the best biocompatible polymers. It offers sterical hindrance against other nanoparticles and blood components such as opsonin, preventing their macrophage phagocytosis and resulting in a prolonged circulation time in blood stream, consequently a ‘stealth character’ in vivo. Therefore, PEG has a very promising future for the development of current therapeutics and biomedical applications. Moreover, the vast number of molecules that PEG can conjugate with might enhance its ability to have an optimistic perspective for the future. This review will present an update on the chemistry used in the modern conjugation methods for a variety of PEG conjugates, such methods include, but are not limited to, the synthesis of targeting PEG conjugates (i.e., Peptides, Folate, Biotin, Mannose etc.), imaging PEG conjugates (i.e., Coumarin, Near Infrared dyes etc.) and delivery PEG conjugates (i.e., doxorubicin, paclitaxel, and other hydrophobic low molecular weight drugs). Furthermore, the type of nanoparticles carrying those conjugates, along with their biomedical uses, will be briefly discussed.

Effects of polyethylene glycol on the surface of nanoparticles for targeted drug delivery

“…Some strategies need to be taken to solve these problems. (1) Improvement of the equipment feature for measuring PEG density on NPs surface, to optimize and standardize existing methods 182 ; (2) Further study the relationship between the MW, the surface density of PEG, and the biophysical and chemical characteristics of NPs;…”

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“…36 PEGylation is considered one of the best methods to stealth DDS of immunological responses. [51][52][53] In addition, it has been shown that PEGs increase the solubility, size, molecular mass, and pharmacokinetic and pharmacodynamic properties of drugs. [54][55][56] For example, Zhang et al encapsulated paclitaxel (PTX) into PEGylated polyphosphoester-based nanocarriers, increasing the aqueous drug solubility from <2.0 µg/mL to 4.8 mg/mL.…”

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“…This miRNA was encapsulated into chondroitin sulphate-functionalized nanoparticles (SP-OA-CS). These glycosylated nanoparticles are capable of active targeting towards LSECs through the mannose receptors and hyaluronan receptors [38, 39]. These nanoparticles were able to efficiently target and transfect isolated murine LSECs in vitro with a model EGFP plasmid and reduce their migration.…”