Efficiency of high molecular weight backbone degradable HPMA copolymer-prostaglandin E1 conjugate in promotion of bone formation in ovariectomized rats.

Abstract:

:Multiblock, high molecular weight, linear, backbone degradable HPMA copolymer-prostaglandin E1 (PGE1) conjugate has been synthesized by RAFT polymerization mediated by a new bifunctional chain transfer agent (CTA), which contains an enzymatically degradable oligopeptide sequence flanked by two dithiobenzoate groups, followed by postpolymerization aminolysis and thiol-ene chain extension. The multiblock conjugate contains Asp8 as the bone targeting moiety and enzymatically degradable bonds in the polymer backbone; in vivo degradation produces cleavage products that are below the renal threshold. Using an ovariectomized (OVX) rat model, the accumulation in bone and efficacy to promote bone formation was evaluated; low molecular weight conjugates served as control. The results indicated a higher accumulation in bone, greater enhancement of bone density, and higher plasma osteocalcin levels for the backbone degradable conjugate.

journal_name

Biomaterials

journal_title

Biomaterials

authors

Pan H,Sima M,Miller SC,Kopečková P,Yang J,Kopeček J

doi

10.1016/j.biomaterials.2013.05.003

subject

Has Abstract

pub_date

2013-09-01 00:00:00

pages

6528-38

issue

27

eissn

0142-9612

issn

1878-5905

pii

S0142-9612(13)00557-7

journal_volume

34

pub_type

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