E. Ron et al., CONTROLLED-RELEASE OF POLYPEPTIDES FROM POLYANHYDRIDES, Proceedings of the National Academy of Sciences of the United Statesof America, 90(9), 1993, pp. 4176-4180
The effects of both polymer hydrophobicity and addition of stabilizers
on the release and integrity of polymer-encapsulated proteins were st
udied. By using very hydrophobic poly[1,3-bis(p-carboxyhydroxy)hexane
anhydride] with sucrose as an excipient, both recombinant bovine somat
otropin and zinc insulin were released intact over 3 weeks. The releas
ed proteins appeared to maintain their integrity as judged by acidic r
everse-phase HPLC, size-exclusion HPLC, radioimmunoassay, and conforma
tion-sensitive immunoassays. Our results also suggest how polymer hydr
ophobicity can be used to enhance protein stability.