Long circulating micelles of an amphiphilic random copolymer bearing cell outer membrane phosphorylcholine zwitterions

Fabrication of micelles from poly(butylene succinate) and poly(2‐methacryloyloxyethyl phosphorylcholine) copolymers as a potential drug carrier

“…Cationic amphiphilic copolymer micelles of poly(methacryloxyethyltrimethyl ammonium chloride‐ co ‐stearyl methacrylate), PDS55 (concentration 1 mg mL −1 ; size 117.2 ± 9.3 nm; zeta potential 14.6 ± 1.3 mV) and poly(lactic acid) (PLA) nanoparticles (concentration 1 mg mL −1 ; size 130.8 ± 5.8 nm; zeta potential −22.7 ± 1.1 mV) were prepared according to previous reports as reference samples.…”

“…Moreover, micelles demonstrate many superior features, including reduced side effects, improved drug tolerance and drug bioavailability . Nevertheless, one practical issue with conventional drug‐loaded polymeric micelles is that they can be recognized and entrapped by the monocyte phagocytic system (MPS) and then quickly eliminated following intravenous administration, resulting in short circulation lifetime and intolerable toxicity . Thus, the long circulation of micelles is an important prerequisite, which can ensure the encapsulated drug is delivered to the tumour site.…”

“…In previous studies, PC‐based polymers were found to exhibit excellent biocompatibility and resistance to protein adsorption and cell adhesion, which endow nanocarriers fabricated with these polymers a prolonged circulation time by escaping from the MPS . Gong and colleagues developed a series of amphiphilic random copolymers composed of 2‐methacryloyloxyethyl phosphorylcholine (MPC), stearyl methacrylate and trimethoxysilylpropyl methacrylate, and then prepared stable micelles with PC shells . In vivo studies in New Zealand rabbits demonstrated that the circulation half‐life of PMS55 micelles showed an ultra‐long circulation time (90.5 h) in the blood.…”

Effects of copolymer component on the properties of phosphorylcholine micelles

“…14 The hydrophilic phosphorylcholine groups in these polymers can stabilize their micelles in aqueous environment owing to the strong hydration through electrostatic interactions, 15 forming a mimetic cell outer membrane structure. 16 Poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) containing phosphorylcholine groups shows better anti-protein adsorption and non-bioadhesive properties than PEG. 14,17,18 Therefore, copolymer micelles composed of PMPC have been used to deliver poorly water soluble drugs.…”

“…The phosphorylcholine micelles exhibit excellent properties, eg, good biocompatibility, high drug-loading ability, excellent prolonged circulation and prominent tumor therapy effect. 16,[19][20][21][22][23][24] Zhao et al 16 investigated in detail the drug loading, in vitro phagocytic uptake, blood clearance and biodistribution in vivo of random copolymer phosphorylcholine micelles with different compositions. However, investigations on the relation between the component of phosphorylcholine micelles and their properties are far from enough.…”