IMPROVED DOSED DELIVERY OF HORMONES

激素和生物活性肽的数量迅速增加， 成为医学研究人员的研究对象。 这些药物不能口服 因此，研究它们的药理学作用非常重要。 作为长效注射剂的效果，首先在动物中，最终在人类中。 然而，肽类药物的成本如此之高， SBIR范围可以负担得起制备实验注射制剂的费用 只是在很小的范围内。 因此，BIOTEK建议开发一种 含肽微胶囊的小规模制备方法 基于无害的、可生物降解的聚乳酸-共-乙交酯（PLG） 过去的研究表明，大多数肽仍然具有生物活性， 在加载到PLG中、储存并在体内释放后。 的 方法依赖于BIOTEK开发的用于其他递送的方法 系统：将肽的水溶液喷涂到纯的 聚合物微球，然后用可生物降解的聚合物外涂 溶液 相对便宜的LHRH将被用作模型肽。 使用体外方法和体内方法将实现1-4周的释放， 大鼠研究将证实释放的生物活性。 第二阶段将寻求 将这项技术提供给NIH， 实验微胶囊，并将其应用于足够的肽 医疗和商业利益，以鼓励私营部门支持 第三阶段商业化。

A rapidly increasing number of hormones and bioactive peptides are becoming available to medical researchers. These drugs cannot be orally administered, so it is important to investigate their pharmacological effects as depot injections, first in animals and eventually in humans. The cost of peptide drugs is so high, however, that research programs of SBIR scope can afford to prepare experimental injectable formulations only on a very small scale. BIOTEK therefore proposed to develop a small scale preparative method for peptide-containing microcapsules based on harmless, biodegradable polylactide-co-glycolide (PLG) materials; past studies have shown that most peptides remain bioactive after being loaded into PLGs, stored, and released in vivo. The approach relies on a method developed by BIOTEK for other delivery systems: spray coating an aqueous solution of the peptide onto pure polymer microspheres and then overcoating with biodegradable polymer solution. Relatively inexpensive LHRH will be used as a model peptide. A 1-4 week release will be achieved using in vitro methods, and in vivo rat studies will confirm released bioactivity. Phase II will seek to make this technology available to NIH for custom preparation of experimental microcapsules and will apply it to a peptide of sufficient medical and commercial interest to encourage private sector support of Phase III commercialization.