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

IF 4.9 Q1 CHEMISTRY, MEDICINAL
Mohsin Kazi*, Ali Gaskari, Ahmad A. Shahba, Shoaib Ahmad, Mohammed S. Aldughaim and Muhammad Delwar Hussain*, 
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引用次数: 0

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.

Abstract Image

异丙酚:当前更新,挑战和改进自纳米乳化配方的策略
异丙酚通常用作静脉麻醉和镇静剂,需要严格的无菌处理以防止微生物污染。由于不安全的注射做法和重复使用一次性异丙酚小瓶,已经有令人震惊的血源性病原体传播报告。此外,麻醉诱导过程中的疼痛管理和确定正确的镇静剂量是静脉异丙酚的重大挑战。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使用。了解异丙酚如何起作用仍然很复杂。纳米技术的进步通过自纳米乳化给药系统(SNEDDS)显著提高了疏水药物的生物利用度。这些以脂质为基础的配方与胃肠道液体接触后产生纳米级乳剂,增强药物的溶解和吸收。例如,研究表明,与传统配方相比,SNEDDS可以将生物利用度提高2- 3倍,异丙酚等药物证明了这一点,异丙酚的水溶性差限制了其治疗效率。本综述深入研究了异丙酚的化学性质、药代动力学和药效学,评估了SNEDDS解决其配方挑战的潜力,并讨论了临床试验中有希望的候选药物。此外,它还研究了使用SNEDDS通过非静脉途径提高异丙酚生物利用度的潜力。这篇综述强调了sndds在提高异丙酚在传统麻醉中的治疗效果方面的潜力,为其应用开辟了新的途径。
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来源期刊
ACS Pharmacology and Translational Science
ACS Pharmacology and Translational Science Medicine-Pharmacology (medical)
CiteScore
10.00
自引率
3.30%
发文量
133
期刊介绍: ACS Pharmacology & Translational Science publishes high quality, innovative, and impactful research across the broad spectrum of biological sciences, covering basic and molecular sciences through to translational preclinical studies. Clinical studies that address novel mechanisms of action, and methodological papers that provide innovation, and advance translation, will also be considered. We give priority to studies that fully integrate basic pharmacological and/or biochemical findings into physiological processes that have translational potential in a broad range of biomedical disciplines. Therefore, studies that employ a complementary blend of in vitro and in vivo systems are of particular interest to the journal. Nonetheless, all innovative and impactful research that has an articulated translational relevance will be considered. ACS Pharmacology & Translational Science does not publish research on biological extracts that have unknown concentration or unknown chemical composition. Authors are encouraged to use the pre-submission inquiry mechanism to ensure relevance and appropriateness of research.
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