pH-responsive stealth micelles composed of cholesterol-modified PLA as a nano-carrier for controlled drug release

Present research is a preliminary report on the novel ph-responsive micelles based on an amphiphilic brush copolymer p(pegma)-b-p(dmaema-co-cpla- ma) used as the promising drug carrier. the copolymer was synthesized using cholesteryl poly(l-lactic acid) methacrylate (cplama), poly(ethylene glycol) mono- methyl ether methacrylate (pegma) and 2-(dimethyl- amino)ethyl methacrylate (dmaema) with appropriate hydrophobic/hydrophilic ratios via atom transfer radical polymerization. the copolymer compositions were determined by 1h nmr. the synthesized copolymer self-assembled into nano-scale micelles capable of encap- sulating hydrophobic model drug naproxen in their hydrophobic cores in aqueous solutions. ph sensitivity andself-assembly behaviors of copolymer were studied by uv–vis transmittance, fluorescence spectroscopy, trans- mission electron microscopy (tem) and dynamic light scattering. the results showed that the copolymer had high ph responsivity with a phase transition ph around ph 6.2. the critical micelle concentrations at ph 6.5 were found about 2.4 mg l-1. the stable and small micelles were obtained at ph 5.5–6.5. upon increasing ph higher than 7, the single micelles further assembled into the micellar aggregates. tem images of copolymer micelles showed that the micelles are spherical in shape with the mean diameter of 152 nm at ph 6.2. in vitro release study of naproxen-loaded micelles with about 44 % loading efficiency and 8 % loading capacity was performed using dialysis method in phosphate-buffered solution at 37 °c.release study implied that the proposed brush copolymercould produce stable nano-carriers with controllable drugrelease at the target sites (ph 5.5–7).