Mohsin Kazi*, Ali Gaskari, Ahmad A. Shahba, Shoaib Ahmad, Mohammed S. Aldughaim and Muhammad Delwar Hussain*,
{"title":"Propofol: Current Updates, Challenges, and Strategies for Improved Self-Nanoemulsifying Formulation","authors":"Mohsin Kazi*, Ali Gaskari, Ahmad A. Shahba, Shoaib Ahmad, Mohammed S. Aldughaim and Muhammad Delwar Hussain*, ","doi":"10.1021/acsptsci.4c0074510.1021/acsptsci.4c00745","DOIUrl":null,"url":null,"abstract":"<p >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.</p>","PeriodicalId":36426,"journal":{"name":"ACS Pharmacology and Translational Science","volume":"8 4","pages":"1013–1027 1013–1027"},"PeriodicalIF":4.9000,"publicationDate":"2025-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Pharmacology and Translational Science","FirstCategoryId":"1085","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acsptsci.4c00745","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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.
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.