دورية أكاديمية
Modeling percutaneous absorption for successful drug discovery and development.
| العنوان: | Modeling percutaneous absorption for successful drug discovery and development. |
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| المؤلفون: | Cheruvu HS; Therapeutics Research Centre, The University of Queensland Diamantina Institute, The University of Queensland , Woolloongabba, Australia., Liu X; Therapeutics Research Centre, The University of Queensland Diamantina Institute, The University of Queensland , Woolloongabba, Australia., Grice JE; Therapeutics Research Centre, The University of Queensland Diamantina Institute, The University of Queensland , Woolloongabba, Australia., Roberts MS; Therapeutics Research Centre, The University of Queensland Diamantina Institute, The University of Queensland , Woolloongabba, Australia.; University of South Australia School of Pharmacy and Medical Sciences, The Queen Elizabeth Hospital, Adelaide, Australia.; Therapeutics Research Centre, Basil Hetzel Institute for Translational Health Research, The Queen Elizabeth Hospital , Adelaide, Australia. |
| المصدر: | Expert opinion on drug discovery [Expert Opin Drug Discov] 2020 Oct; Vol. 15 (10), pp. 1181-1198. Date of Electronic Publication: 2020 Jun 25. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't; Review |
| اللغة: | English |
| بيانات الدورية: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101295755 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1746-045X (Electronic) Linking ISSN: 17460441 NLM ISO Abbreviation: Expert Opin Drug Discov Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2015- : Abingdon, Oxford : Taylor & Francis Original Publication: London : Informa Healthcare |
| مواضيع طبية MeSH: | Skin Absorption*, Drug Development/*methods , Drug Discovery/*methods, Animals ; Computer Simulation ; Drug Delivery Systems ; Drug Design ; Humans ; Models, Biological ; Permeability ; Skin/metabolism |
| مستخلص: | Introduction: Skin has been used as an administration route for local or systemic action since ancient times. The efficacy and toxicity of any product applied to the skin is determined by the chemical composition and physicochemical properties of the active(s) and excipients, which in turn govern their percutaneous absorption and effects. Areas Covered: This review addresses market trends, skin physiology, solute permeability, formulation properties and effects that are most relevant to a drug discovery scientist designing potentially active solutes for topical application. It also summarizes in silico model strategies, strengths, and limitations associated with the drug delivery design of topical products, with relevant examples. Expert Opinion: From a drug discovery perspective, many factors can determine the percutaneous absorption of an active solute. Current in silico models are limited by their dependence on data generated from the permeation of solutes across normal human skin from aqueous solutions. In practice, the choice of formulation, the pertinent skin physiology, and the solute properties, including its clearance, potency, and enhancement, also define dermal delivery. Consequently, there is an emerging trend of using in silico methods to inform effective drug design and development that are based on a combination of QSAR/QSPR with physiologically based pharmacokinetic and pharmacodynamic (PBPKPD) models. |
| فهرسة مساهمة: | Keywords: in silico modeling; Clearance; PBPKPD; QSAR/QSPR; exposure; percutaneous absorption; physicochemical properties; potency; skin irritancy; toxicity |
| تواريخ الأحداث: | Date Created: 20200626 Date Completed: 20210413 Latest Revision: 20210413 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1080/17460441.2020.1781085 |
| PMID: | 32584615 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher | تدمد: | 1746-045X |
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| DOI: | 10.1080/17460441.2020.1781085 |