Laboratory of Physiology, Department for Sustainable Development and Ecological Transition, University of Piemonte Orientale, UPO, 13100 Vercelli, Italy.
Noivita S.r.l.s., Spin Off of University of Piemonte Orientale, Via Solaroli 17, 28100 Novara, Italy.
Int J Mol Sci. 2024 Aug 21;25(16):9079. doi: 10.3390/ijms25169079.
Palmitoylethanolamide (PEA) is a highly lipophilic molecule with low solubility, making absorption difficult. Recent techniques like micronisation, ultra-micronisation and combining PEA with solvents have improved their bioavailability and stability. Our study analysed particle size differences and absorption kinetics using specific solvents (PEAΩ and PEA DynoΩ) over time (0.5 h-6 h) in a dose-dependent manner (200 mg-1800 mg). The results showed that PEAΩ and PEA DynoΩ achieved 82-63% absorption at 3 h, compared to 30-60% for micronised, ultra-micronised PEA and a commercial product, highlighting the optimal dose range of 300 mg-600 mg. In addition, a 3D model of the peripheral nerve was utilised to explain the efficacy after gut passage and support the most effective dose (300 mg or 600 mg) achieved at the gut level. PEAΩ and PEA DynoΩ, which are associated with better intestinal bioavailability compared to PEA-micronised, PEA ultra-micronised and a commercial product, have allowed not only a reduction in the inflammatory context but also an improvement of peripheral nerve well-being by increasing specific markers like MPZ (26-36% vs. 8-15%), p75 (25-32% vs. 13-16%) and NRG1 (22-29.5% vs. 11-14%). These results highlight the potential of advanced PEA formulations to overcome solubility challenges and maintain in vitro efficacy, modulating peripheral nerve well-being.
棕榈酰乙醇酰胺（PEA）是一种具有低水溶性的高度亲脂性分子，这使得其吸收变得困难。最近的技术，如微粉化、超微粉化以及将 PEA 与溶剂结合，已经提高了它们的生物利用度和稳定性。我们的研究分析了使用特定溶剂（PEAΩ和 PEA DynoΩ）在不同时间点（0.5 h-6 h）、不同剂量（200 mg-1800 mg）下的粒径差异和吸收动力学。结果表明，PEAΩ和 PEA DynoΩ 在 3 h 时达到 82-63%的吸收，而微粉化、超微粉化 PEA 和商业产品的吸收仅为 30-60%，这突出了 300 mg-600 mg 的最佳剂量范围。此外，我们还利用外周神经的 3D 模型来解释肠道通过后的疗效，并支持在肠道水平上达到最佳效果的剂量（300 mg 或 600 mg）。与微粉化 PEA、超微粉化 PEA 和商业产品相比，PEAΩ和 PEA DynoΩ 与更好的肠道生物利用度相关，不仅降低了炎症环境，还通过增加特定标志物（如 MPZ（26-36%对 8-15%）、p75（25-32%对 13-16%）和 NRG1（22-29.5%对 11-14%））改善了外周神经的健康状况。这些结果突出了先进的 PEA 配方的潜力，它们可以克服溶解度挑战并保持体外疗效，从而调节外周神经的健康。
