Abstract
In this study, a series of diblock glycopolymers, poly(6-O-methacryloyl-d-galactopyranose)-b-poly(6-cholesteryloxyhexyl methacrylate) (PMAgala-b-PMAChols), with cholesterol/galactose grafts were prepared through a sequential reversible addition-fragmentation chain transfer (RAFT) polymerization and deprotection process. The glycopolymers could self-assemble into aggregates with various morphologies depending on cholesterol/galactose-containing block weight ratios, as determined by transmission electronic microscopy (TEM) and dynamic laser light scattering (DLS). In addition, the lectin (Ricinus communis agglutinin II, RCA120) recognition and bovine serum albumin (BSA) adsorption of the PMAgala-b-PMAChol aggregates were evaluated. The SK-Hep-1 tumor cell inhibition properties of the PMAgala-b-PMAChol/doxorubicin (DOX) complex aggregates were further examined in vitro. Results indicate that the PMAgala-b-PMAChol aggregates with various morphologies showed different interaction/recognition features with RCA120 and BSA. Spherical aggregates (d ≈ 92 nm) possessed the highest RCA120 recognition ability and lowest BSA protein adsorption. In addition, the DOX-loaded spherical complex aggregates exhibited a better tumor cell inhibition property than those of nanofibrous complex aggregates. The morphology-variable aggregates derived from the amphiphilic glycopolymers may serve as multifunctional biomaterials with biomolecular recognition and drug delivery features.
Highlights
Synthetic glycopolymers with saccharide grafts have attracted increasing attentions due to their interesting self-assembly behavior [1] and biological functions, which guarantee their applications as advanced biomaterials such as gene/drug carriers, immunodiagnostic reagents, and bio-targeting materials [2,3,4]
Diblock copolymer poly(6-O-methacryloyl-D-galactopyranose)-b-poly(6-cholesteryloxyhexyl methacrylate) (PMAgala-b-PMAChol) amphiphiles were synthesized by sequential reversible addition-fragmentation chain transfer (RAFT) polymerization and successive trifluoroacetic acid (TFA)-mediated deprotection
Thereafter, the as-prepared PMAIpGP and PMAIpGP-b-PMAChols were deprotected at room temperature in mixed trifluoroacetic acid (TFA) and dichloromethane (DCM) (1/2, v/v) for 32 h, and water-soluble PMAgala and PMAgala-b-PMAChol block copolymer amphiphiles were achieved with good yields through repeated precipitation in anhydrous cold methanol and drying under vacuum
Summary
Synthetic glycopolymers with saccharide grafts have attracted increasing attentions due to their interesting self-assembly behavior [1] and biological functions, which guarantee their applications as advanced biomaterials such as gene/drug carriers, immunodiagnostic reagents, and bio-targeting materials [2,3,4]. We prepared block copolymer amphiphiles with pendant cholesterol mesogens They could self-assemble into micro/nanoparticles with well-ordered cholesterol mesogens in the cores of cylinder micelles, solid spheres, and bowl-shaped aggregates, and in the membranes of hollow nanotubes, ellipsoidal vesicles and so forth. [44,45,46,47,48] as an essential component of plasma membranes, cholesterol plays important roles in cell membrane formation, adhesion, and signal transduction, regulating lipid bilayer interaction [49] and intracellular trafficking of nanoparticles [50,51] This brings the cholesterol-based amphiphiles new potential applications in biomedical engineering [52,53,54]. Employing the PMAgala-b-PMAChol aggregates as potential drug carriers, the DOX loading capacity, the morphology of the PMAgala-b-PMAChol/DOX complex aggregates, and related DOX delivery properties in human hepatocarcinoma SK-Hep-1 cells were investigated and discussed
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