Allcock H R, Pucher S R, Scopelianos A G
Department of Chemistry, Pennsylvania State University, University Park 16802.
Biomaterials. 1994 Jun;15(8):563-9. doi: 10.1016/0142-9612(94)90205-4.
Three different poly[(amino acid ester)phosphazenes] have been examined in order to investigate their possible use as drug delivery vehicles. The three polymers are poly[di(ethyl glycinato)phosphazene], poly[di(ethyl alanato)phosphazene] and poly[di(benzyl alanato)phosphazene]. These macromolecules either share the same amino acid residue or the same ester group, and this facilitated comparisons of the hydrolytic decomposition and the small molecule release profiles of the polymers. The polymers were synthesized by treatment of poly(dichlorophosphazene) with an excess of the appropriate amino acid ester. Tetrahydrofuran solutions of each polymer were then thoroughly mixed with ethacrynic acid, a diuretic, or Biebrich Scarlet, an azo dye. Films cast from these solutions were immersed in aqueous media (pH 7) at 25 degrees C and at 37 degrees C for approximately 1400 h. During these experiments, the release of the small molecules was monitored by UV/visible spectroscopy. The molecular weight decline and the mass loss of the polyphosphazene films were measured.
为了研究三种不同的聚[(氨基酸酯)磷腈]作为药物递送载体的潜在用途，对其进行了研究。这三种聚合物分别是聚[二(甘氨酸乙酯)磷腈]、聚[二(丙氨酸乙酯)磷腈]和聚[二(苄基丙氨酸酯)磷腈]。这些大分子要么具有相同的氨基酸残基，要么具有相同的酯基，这便于比较聚合物的水解分解和小分子释放情况。通过用过量的适当氨基酸酯处理聚(二氯磷腈)来合成聚合物。然后将每种聚合物的四氢呋喃溶液与利尿药依他尼酸或偶氮染料比布列希猩红充分混合。将从这些溶液中浇铸而成的薄膜在25℃和37℃下浸入pH值为7的水性介质中约1400小时。在这些实验过程中，通过紫外/可见光谱监测小分子的释放情况。测量了聚磷腈薄膜的分子量下降和质量损失。
