Suppr超能文献

丙泊酚:当前进展、挑战及改进自纳米乳化制剂的策略

Propofol: Current Updates, Challenges, and Strategies for Improved Self-Nanoemulsifying Formulation.

作者信息

Kazi Mohsin, Gaskari Ali, Shahba Ahmad A, Ahmad Shoaib, Aldughaim Mohammed S, Hussain Muhammad Delwar

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

ACS Pharmacol Transl Sci. 2025 Mar 17;8(4):1013-1027. doi: 10.1021/acsptsci.4c00745. eCollection 2025 Apr 11.

Abstract

Propofol, commonly used as an intravenous (IV) anesthetic and sedative, requires strict aseptic handling to prevent microbial contamination. There have been alarming reports of bloodborne pathogen transmission due to unsafe injection practices and the reuse of single-use propofol vials. Additionally, managing pain during anesthesia induction and determining the correct dose for sedation pose significant challenges with IV propofol. Despite its effectiveness, propofol's limited water solubility and poor oral bioavailability restrict its use outside of anesthesia. Understanding how propofol works remains complex. Advances in nanotechnology have significantly improved the bioavailability of hydrophobic drugs through self-nanoemulsifying drug delivery systems (SNEDDS). These lipid-based formulations create nanoscale emulsions upon contact with gastrointestinal fluids, enhancing drug solubilization and absorption. For instance, studies have shown that SNEDDS can improve bioavailability by 2- to 3-fold compared to traditional formulations, as demonstrated with drugs such as propofol, whose poor water solubility limits its therapeutic efficiency. This review delves into propofol's chemical properties, pharmacokinetics, and pharmacodynamics, evaluating the potential of SNEDDS to address its formulation challenges and discussing promising candidates in clinical trials. Furthermore, it examines the potential of using SNEDDS to improve propofol's bioavailability through nonintravenous routes. This review highlights the potential of SNEDDS to enhance propofol's therapeutic effectiveness beyond its traditional use in anesthesia, opening new avenues for its application.

摘要

丙泊酚通常用作静脉麻醉剂和镇静剂,需要严格无菌操作以防止微生物污染。有令人担忧的报告称,由于不安全的注射操作和一次性丙泊酚小瓶的重复使用,导致了血源性病原体传播。此外,在麻醉诱导期间控制疼痛以及确定正确的镇静剂量对静脉注射丙泊酚来说是重大挑战。尽管丙泊酚有效,但其有限的水溶性和较差的口服生物利用度限制了其在麻醉以外的应用。了解丙泊酚的作用机制仍然很复杂。纳米技术的进步通过自纳米乳化药物递送系统(SNEDDS)显著提高了疏水性药物的生物利用度。这些基于脂质的制剂在与胃肠液接触时会形成纳米级乳液,增强药物的溶解和吸收。例如,研究表明,与传统制剂相比,SNEDDS可使生物利用度提高2至3倍,丙泊酚等药物就证明了这一点,其水溶性差限制了其治疗效果。本综述深入探讨了丙泊酚的化学性质、药代动力学和药效学,评估了SNEDDS应对其制剂挑战的潜力,并讨论了临床试验中有前景的候选药物。此外,它还研究了使用SNEDDS通过非静脉途径提高丙泊酚生物利用度的潜力。本综述强调了SNEDDS在提高丙泊酚在麻醉传统用途之外的治疗效果方面的潜力,为其应用开辟了新途径。

相似文献

7
Pain management for women in labour: an overview of systematic reviews.分娩期女性的疼痛管理:系统评价综述
Cochrane Database Syst Rev. 2012 Mar 14;2012(3):CD009234. doi: 10.1002/14651858.CD009234.pub2.
8
The abuse potential of propofol.丙泊酚的滥用潜力。
Clin Toxicol (Phila). 2010 Mar;48(3):165-70. doi: 10.3109/15563651003757954.

本文引用的文献

3
Propofol-Related Infusion Syndrome: A Clinical Review.丙泊酚输注综合征:临床综述
Cureus. 2022 Oct 17;14(10):e30383. doi: 10.7759/cureus.30383. eCollection 2022 Oct.
10
Effects of propofol on the development of cancer in humans.丙泊酚对人类癌症发展的影响。
Cell Prolif. 2020 Aug;53(8):e12867. doi: 10.1111/cpr.12867. Epub 2020 Jun 29.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验