ABSORBABLE BIOPOLYMERS DERIVED FROM DIMER FATTY-ACIDS
ABSORBABLE BIOPOLYMERS DERIVED FROM DIMER FATTY-ACIDS
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DOI：
10.1002/pola.1993.080310523
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发表时间：
1993-04-01
影响因子：
--
通讯作者：
MANIAR, M
中科院分区：
文献类型：
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作者：
DOMB, AJ;MANIAR, M
以芥酸和癸二酸的非线性疏水二聚体（FAD）为原料，合成了一类新型的脂肪族共酐，该共酐具有理想的物理化学和机械性能，可用作药物载体。聚合物通过熔融缩合合成，得到分子量为250，000的成膜聚合物。通过1H-1-NMR和重量法测定共聚物的组成。体外降解研究表明，这些聚合物遵循一级动力学降解，在前10天内快速降解，残留物主要是FAD共聚单体。药物从聚合物中的释放也遵循与聚合物的降解过程相关的一级动力学。药物如卡铂、甲氨蝶呤、四环素和庆大霉素在体外释放超过2周，在某些情况下超过6周。在大鼠和家兔脑、肌肉和皮下进行的体内生物相容性试验证明了其毒理学惰性和生物降解性。第一：1 FAD的共聚物：SA被选为各种应用的载体，包括庆大霉素释放植入物，该植入物目前正在进行用于治疗骨髓炎的人体临床试验。
A new class of aliphatic copolyanhydrides was synthesized from nonlinear hydrophobic dimers (FAD) of erucic acid and sebacic acid which possessed the desired physico-chemical and mechanical properties for use as a carrier for drugs. The polymers were synthesized by melt condensation to yield film-forming polymers with molecular weights of 250,000. The copolymer composition was determined by H-1-NMR and gravimetric methods. In vitro degradation studies showed that these polymers degrade following a first-order kinetics with a rapid degradation in the first 10 days leaving a residue which is mostly the FAD comonomer. The drug release from the polymer also followed a first-order kinetics which correlates with the degradation process of the polymer. Drugs like carboplatin, methotrexate, tetracycline, and gentamicin were released in vitro for over 2 weeks and in some cases over 6 weeks. In vivo biocompatibility tests in rats and rabbits in the brain, muscle, and subcutaneously, demonstrated their toxicological inertness and biodegradability. The 1 : 1 copolymer of FAD : SA was selected as a carrier for various applications including a gentamicin-releasing implant which is now undergoing human clinical trials for the treatment of osteomyelitis.