Study on Design o fDrug Delivery System Using Assembly-deassemby Mechanicsm of Drug-inclusion Carrier

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In 2000 to 2002, a polymer based on the repeating pentapeptide sequence Val-Pro-Gly-Val-Gly(VPGVG) which possesses the property of self-assembly was synthesized. This polymer, poly(VPGVG), was characteristic of completely reversible self-assembly and deassembly. The syntheses of two random copolymers based on the VPGVG sequence described above and a peptide sequence Arg-Gly-Tyr-Ser-Leu-Gly(RGYSLG) which can be phosphorylated by cyclic AMP-dependent protein kinase or a peptide sequence Gly-Ser-Asn-His-Gly(GSNHG) in which Asp residue can be converted to Asp residue were performed but these syntheses were unsuccessful because of the unexpected formation of by-products. In 2003, we tried again the syntheses of the above random copolymers by changing the synthetic scheme and quantitative yields of two random copolymers were obtained. Each of these copolymers was characteristic of incompletely reversible self-assembly and deassembly. The size of coacervate droplets of poly(VPGVG) in self-assembly was 1〜2 μm and the release of drug from microparticles of poly(VPGVG) was controlled. The release of drugs from microparticles of two random copolymers described above is under investigation