Prodrug Nano-Squalene Bioconjugate Drug Products

L. Benet, P. Couvreur

Acta pharmaceutica Hungarica(2021)

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摘要
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
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