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

2000年至2002年，合成了一种基于Val-Pro-Gly-Val-Gly(VPGVG)重复序列的具有自组装性质的聚合物。这种聚合物聚(VPGVG)具有完全可逆的自组装和解聚特性。基于上述VPGVG序列和可被环AMP依赖的蛋白激酶磷酸化的Arg-Gly-Tyr-Ser-Leu-Gly(RGYSLG)序列或可将Asp残基转化为Asp残基的Gly-Ser-Asn-His-Gly(GSNHG)序列，合成了两种随机共聚物，但由于副产物的意外形成，这些合成均未成功。2003年，我们通过改变合成路线，再次尝试了上述无规共聚物的合成，得到了两种无规共聚物的定量产率。每一种共聚物都具有不完全可逆的自组装和解聚特性。聚(VPGVG)自组装时凝聚的微滴尺寸为1~2μm，药物从微球中释放得到控制。上述两种无规共聚物微粒的药物释放情况正在研究中。

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