BRANCHED COPOLYMER AS PEPTIDE DRUG DELIVERY SYSTEM

描述（由申请人提供）：本SBIR I期项目将开发一种新型支化共聚物，作为药理学应用的肽药物递送载体。该载体是一种高度结构化的共聚物，可与肽类药物在水介质中形成胶束状结构。这种类型的分子结构的稳定性将使包封的肽药物的早期降解最小化，并减少来自过早药物释放的有害副作用。聚合物/药物胶束将表现出均匀的尺寸和药物负载水平，以及可预测的、良好控制的药物释放速率。 I期计划的总体目标是开发基于所提出的用于药理学应用的共聚物的药物递送系统，特别是用于递送肽类药物。具体的技术目标是：1.高分子药物载体的合成与表征。2.聚合物/药物包封工艺的优化和药物释放速率的研究。将使用具有商业意义的模型肽药物进行包封研究。将研究聚合物/药物制剂的药物释放速率。3.聚合物生物相容性的测定。将使用体外细胞毒性试验研究合成聚合物的潜在细胞毒性。 蛋白质和肽药物递送的潜在市场是非常重要的。这些药物中的许多具有稳定性问题和不期望的副作用。利用这种提出的新的药物递送系统，以较低剂量更有效的药物递送是可能的。这将减少不良副作用，并使有效的药物治疗疾病的治疗。新的药物输送系统几乎对医学的每一个分支都产生了影响。受控药物输送是一个价值200亿美元的行业，而且正在迅速增长。

DESCRIPTION (provided by applicant): This SBIR Phase I project will develop a novel branched copolymer as a peptide drug delivery carrier for pharmacological application. The carrier is a highly-structured copolymer that can form micelle-like structures with the peptide drug in aqueous media. The stability of this type of molecular structure will minimize early degradation of the encapsulated peptide drug and decrease harmful side-effects from premature drug release. The polymer/drug micelles will exhibit uniform size and drug loading level, and a predictable, well-controlled drug release rate. The overall objective in the Phase I program is to develop a drug delivery system based on the proposed copolymer for pharmacological applications, especially for delivery of peptide drugs. The specific technical aims are: 1. Synthesis and characterization of the polymer drug carrier. 2. Optimization of the polymer/drug encapsulation process and investigation of the drug release rate. A commercially significant model peptide drug will be used for the encapsulation study. The drug release rate from the polymer/drug formulation will be investigated. 3. Determination of the polymer biocompatibility. The potential cytotoxicity of the synthesized polymer will be investigated using in vitro cytotoxicity assays. Potential markets for protein and peptide drug delivery are highly significant. Many of these drugs have stability problems and undesirable side effects. With this proposed new drug delivery system, more efficient drug delivery with lower dosage is possible. This will reduce untoward side effects and enable efficient drug therapy for disease treatment. New drug delivery systems have had an impact on nearly every branch of medicine. Controlled drug delivery is a $20 billion industry and rising rapidly.