Biocompatible propylene glycol alginate-g-polytetrahydrofuran amphiphilic graft copolymers for highly effective drug carriers

The acylated propylene glycol alginate-g-polytetrahydrofuran amphiphilic graft copolymers (APGA-g-PTHF) with various grafting numbers (G(N)) of 3-23 per 1000 monosaccharide rings and PTHF (PTMG or PTMO) branches with different molecular weights (M-n,M-PTHF) of 600-3400 g/mol could be successfully synthesized via nucleophilic substitution of PTHF living chains carrying oxonium ions with the -OH side groups of APGA backbone. The nanophase separation, the hydrophobicity and the surface roughness were increased due to the less restricted movement of hydrophobic PTHF branches to the surface. APGA-g-PTHF graft copolymers behave low cytotoxicity and good anti-protein performance. Interestingly, APGA-g-PTHF amphiphilic graft copolymers could form homogeneous nanospheres (< 250 nm) via self-assembly in H2O/CH2Cl2 medium which could be used for drug (ibuprofen or curcumin) carriers having high drug loading efficiency (similar to 45%) and fast release behavior. The nanospheres carried curcumin behave very higher (10-fold) anticancer effect against HeLa cells than that of curcumin and thus reduce the harmful drug dosage. Moreover, the nanospheres carried drug might enter into HeLa cells and present pH-sensitive drug release. To the best of our knowledge, this is the first example of PGA based graft copolymers for highly effective nano-carriers and anti-protein surfaces, which would have a prospect in biomedical areas.

Automated summary

APGA-g-PTHF amphiphilic graft copolymers with nanophase separation, hydrophobicity, and increased surface roughness were successfully synthesized. These copolymers exhibited good anti-protein performance and could form homogeneous nanospheres for drug delivery with high drug loading efficiency and fast release behavior.