Prodrug Nano-Squalene Bioconjugate Drug Products

L. Benet, P. Couvreur
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Abstract

NSBs display extended blood circulation times, improved bioactivity, and reduced toxicity in multiple preclinical models. This technology platform has several applications with high drug loading that is supported by robust in-vitro and in-vivo data in animal models for a variety of indications. A. Pain – Squal Lenk The endogenous neuropeptide Leucine enkephalin (LENK) is conjugated to squalene. SQUAL – LENK formed with Squal NanoPro technology is an efficient approach to use the currently unusable LENK to act as an analgesic drug via peripheral opioid receptors (no addiction potential). Self-assembly into NSB’s; Slow release of peptide; Cmax at 45 min; Degraded over 10 hrs; Analgesic effect only in inflamed tissues; Exclusively acts on peripheral opioid receptors; Longer duration than morphine
前药纳米角鲨烯生物偶联药物产品
在多个临床前模型中,nsb表现出延长血液循环时间、提高生物活性和降低毒性。该技术平台具有高载药量的几种应用,在各种适应症的动物模型中得到了强大的体外和体内数据的支持。内源性神经肽亮氨酸脑啡肽(Lenk)与角鲨烯偶联。SQUAL - LENK由SQUAL NanoPro技术形成,是一种有效的方法,利用目前无法使用的LENK通过外周阿片受体(无成瘾潜力)作为镇痛药物。自组装成NSB;肽缓释;Cmax在45分钟;超过10小时退化;仅对炎症组织有镇痛作用;只作用于外周阿片受体;比吗啡持续时间更长
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