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首页> 外文期刊>Journal of Applied Polymer Science >Chemical immobilization of retinoic acid within poly(epsilon-caprolactone) nanoparticles based on drug-polymer bioconjugates
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Chemical immobilization of retinoic acid within poly(epsilon-caprolactone) nanoparticles based on drug-polymer bioconjugates

机译：基于药物-聚合物生物共轭物的聚ε-己内酯纳米颗粒中视黄酸的化学固定

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摘要

All-trans-retinoic acid (RA) was chemically conjugated to biodegradable poly(epsilon-caprolactone) (PCL10; number-average M-w approximate to 1250) via an ester linkage. The conjugation was carried out using N,N-dicyclohexylcarbodiimide and 4-dimethyl aminopyridine as a coupling agent. The molar ratio of the drug to the polymer was 1.11 as determined by H-1-NMR analysis. DSC and WAXD results showed that the formation of crystalline structures of RA was effectively suppressed by conjugation with PCL. The RA-PCL conjugates were formulated into nanoparticles by a spontaneous phase-inversion technique. Morphological characteristics of the resultant nanoparticles and drug-loading efficiencies were compared with those of free RA-loaded nanoparticles. The drug-loading efficiency of RA-PCL conjugates was almost 100%, while that of free RA was only similar to12%. The majority of unconjugated RA was found to form undesirable free-drug crystals out of nanoparticles, as observed by TEM analysis. This study demonstrates that the conjugation approach of RA to PCL can be an effective means to immobilize and encapsulate RA within nanoparticles for pharmaceutical applications. (C) 2003 Wiley Periodicals, Inc. [References: 34]
机译：通过酯键将全反式维甲酸（RA）化学偶联至可生物降解的聚（ε-己内酯）（PCL10;数均M-w约为1250）。使用N，N-二环己基碳二亚胺和4-二甲基氨基吡啶作为偶联剂进行偶联。通过H-1-NMR分析测定，药物与聚合物的摩尔比为1.11。 DSC和WAXD结果表明，与PCL结合可有效抑制RA的晶体结构形成。通过自发相转化技术将RA-PCL共轭物配制成纳米颗粒。将所得纳米颗粒的形态特征和载药效率与游离RA载有的纳米颗粒进行了比较。 RA-PCL偶联物的载药率几乎为100％，而游离RA的载药率仅为12％。如通过TEM分析所观察到的，发现大多数未缀合的RA从纳米颗粒中形成不期望的游离药物晶体。这项研究表明，RA与PCL的缀合方法可以成为将RA固定和封装在纳米颗粒内的有效方法，以用于药物应用。 （C）2003 Wiley Periodicals，Inc. [参考：34]

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