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Novel degradable polyphosphazene hydrogel beads for drug controlled release

机译:用于药物控制释放的新型可降解聚磷腈水凝胶珠

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Novel water-soluble polyphosphazene containing carboxylatophenamino groups (PCPAP) was synthesized by the substitution reaction of ethyl p-amino benzonate with poly(dichlorophosphazene), followed by alkali hydrolysis. Characterizations by IR, H-1-NMR, differential scanning calorimetry, and elemental analysis indicated that the reaction brought about an almost complete introduction of carboxylatophenamino to the polymer side chain. Calcium-crosslinked PCPAP hydrogel beads were accomplished with an extremely mild method. The erosion experiments were conducted in vitro in various pH environments. The erosion duration of the beads at pH 7.4 and 37degreesC was effectively extended by an increase in the concentration of the PCPAP or CaCl2 solution during the preparation process. Moreover, the bead erosion was sensitive to the pH. The sample dissolved 39.4% in a pH 8.0 buffer within 34 days but only 5.36% in a pH 5.0 buffer. Furthermore, PCPAP underwent degradation into macromolecular segments through the breaking of the backbone, and this could prevent accumulation in the body. These properties of PCPAP may be useful for controlled drug delivery, including intestine-specific oral delivery systems. (C) 2002 Wiley Periodicals, Inc. J Appl Polym Sci 87: 986-992, 2003. [References: 13]
机译:通过对氨基苯甲酸乙酯与聚二氯磷腈的取代反应,然后进行碱水解,合成了新型的含羧基苯乙氨基的水溶性聚磷腈(PCPAP)。通过IR,1 H-NMR,差示扫描量热法和元素分析的表征表明,该反应几乎完全将羧甲基苯酚引入聚合物侧链。钙交联的PCPAP水凝胶珠是通过一种非常温和的方法完成的。腐蚀实验是在各种pH环境中进行的。在制备过程中,PCPAP或CaCl2溶液浓度的增加有效地延长了珠在pH 7.4和37°C时的腐蚀持续时间。此外,珠粒侵蚀对pH敏感。样品在34天内在pH 8.0缓冲液中溶解了39.4%,但在pH 5.0缓冲液中仅溶解了5.36%。此外,PCPAP通过骨架的断裂而降解为大分子片段,这可以防止在体内的积累。 PCPAP的这些特性可用于受控的药物输送,包括肠道特异性口服输送系统。 (C)2002 Wiley Periodicals,Inc. J Appl Polym Sci 87:986-992,2003。[参考:13]

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