Abstract
As nano-scale drug delivery systems, smart micelles that are sensitive to specific biological environment and allowed for target site-triggered drug release by reversible stabilization of micelle structure are attractive. In this work, a biocompatible and pH-sensitive copolymer is synthesized through bridging poly (2-methacryloyloxyethyl phosphorylcholine) (PMPC) block and poly (D, L-lactide) (PLA) block by a benzoyl imine linkage (Blink). Biomimetic micelles with excellent biocompatibility based on such PLA-Blink-PMPC copolymer are prepared as carriers for paclitaxel (PTX) delivery. Due to the rapid breakage of the benzoyl imine linkage under acidic condition, the micelle structure is disrupted with accelerated PTX release. Such pH-sensitive triggered drug release behavior in synchronization with acidic conditions at tumor site is helpful for improving the utilization of drug and facilitating antitumor efficacy. These micelles can be used as promising drug delivery systems due to their biocompatible and smart properties.
Highlights
Nano-polymeric drug carriers, such as micelles, have been extensively applied in cancer therapy for their significantly reduced side effects and improved therapeutic efficacy
A proper diameter of less than 200 nm can promote drug-loaded micelles to be passively accumulated into tumor tissue benefiting from the enhanced permeability and retention (EPR) effect, which indicates a potential for higher utilization ratio of drug and great convenience in chemotherapy [1,2,3]
Hydrophobic CPLA-OH was synthesized through ring-opening polymerization (ROP) of D, L-lactide monomer by using cinnamyl alcohol as initiator
Summary
Nano-polymeric drug carriers, such as micelles, have been extensively applied in cancer therapy for their significantly reduced side effects and improved therapeutic efficacy. In order to avoid recognizing by RES, biocompatible Poly (ethylene glycol) (PEG) based surface has been widely developed due to its compact associations with water molecules via hydrogen bond, which forms a hydrating layer and gives ‘stealth’ property to the micelles [7,8,9]. Poly (2-methacryloyloxyethyl phosphorylcholine) (PMPC) has been introduced into several nano-polymeric drug carriers as hydrophilic blocks and exhibited great performance [12,13,14,15]. Different from PEG, PMPC copolymer achieves high hydration by ionic solvation, which plays an important role in its non-fouling property [16, 17]. PMPC can be used as a promising block candidate for fabricating biomimetic drug delivery system [18,19,20]
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