POLY[(AMINO ACID ESTER)PHOSPHAZENES] AS SUBSTRATES FOR THE CONTROLLED-RELEASE OF SMALL MOLECULES
POLY[(AMINO ACID ESTER)PHOSPHAZENES] AS SUBSTRATES FOR THE CONTROLLED-RELEASE OF SMALL MOLECULES
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DOI：
10.1016/0142-9612(94)90205-4
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发表时间：
1994-06-01
期刊：
影响因子：
14
通讯作者：
SCOPELIANOS, AG
中科院分区：
文献类型：
--
作者：
ALLCOCK, HR;PUCHER, SR;SCOPELIANOS, AG
研究了三种不同的聚（氨基酸酯）磷腈，以研究它们作为药物递送载体的可能用途。这三种聚合物是聚[二（乙基甘草酸）磷腈]、聚[二（乙基白草酸）磷腈]和聚[二（苄基白草酸）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，这有助于比较聚合物的水解分解和小分子释放谱。该聚合物是用过量的适当氨基酸酯处理聚二氯磷腈合成的。然后将每种聚合物的四氢呋喃溶液与利尿剂乙酸或偶氮染料比布里希猩红彻底混合。将这些溶液制成的薄膜分别浸入25℃和37℃的水溶液（pH 7）中约1400小时。在这些实验中，通过紫外/可见光谱监测小分子的释放。测定了聚磷腈薄膜的分子量下降和质量损失。
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.