The cutaneous absorption parameters of xenobiotics are crucial for the development of drugs and cosmetics, as well as for assessing environmental and occupational chemical risks. Despite the great variability in the design of experimental conditions due to uncertain international guidelines, datasets like HuskinDB have been created to report skin absorption endpoints. This review updates available skin permeability data by rigorously compiling research published between 2012 and 2021. Inclusion and exclusion criteria have been selected to build the most harmonized and reusable dataset possible. The Generative Topographic Mapping method was applied to the present dataset and compared to HuskinDB to monitor the progress in skin permeability research and locate chemotypes of particular concern. The open-source dataset (SkinPiX) includes steady-state flux, maximum flux, lag time and permeability coefficient results for the substances tested, as well as relevant information on experimental parameters that can impact the data. It can be used to extract subsets of data for comparisons and to build predictive models.
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http://dx.doi.org/10.1038/s41597-024-03026-4 | DOI Listing |
Comput Biol Chem
January 2025
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea; Elicure, 12, Gyeongyeol-ro 17 beon-gil, Seo-gu, Gwangju, Republic of Korea. Electronic address:
This study aimed to profile metabolites from five Trichoderma strains and assess their cytotoxic and pharmacological activities, particularly targeting oral squamous cell carcinoma (OSCC). UHPLC-TOF-MS analysis revealed the presence of 25 compounds, including heptelidic acid, viridiol isomers, and sorbicillinol from the different Trichoderma extracts. Pharmacokinetic analysis showed moderate permeability and low interaction with P-glycoprotein, suggesting good drug absorption with minimal interference in cellular uptake.
View Article and Find Full Text PDFPharmaceutics
January 2025
Department of Pharmaceutical Sciences, Università degli Studi di Milano, via G: Colombo, 71, 20133 Milano, Italy.
Background/objectives: The objective of this paper is to design a novel film-forming system (FFS) based on Eudragit E PO (EuE) polymeric solutions, differing in volatile solvents (i.e., isopropanol and ethanol) and plasticizers (i.
View Article and Find Full Text PDFPharmaceutics
January 2025
Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, 70125 Bari, Italy.
: Since 2008, following clinical studies conducted on children that revealed the ability of the β-adrenergic antagonist propranolol to inhibit capillary growth in infantile hemangiomas (IHs), its oral administration has become the first-line treatment for IHs. Although oral propranolol therapy at a dosage of 3 mg/kg/die is effective, it can cause systemic adverse reactions. This therapy is not necessarily applicable to all patients.
View Article and Find Full Text PDFPharmaceutics
December 2024
Faculty of Pharmaceutical Sciences, Josai International University, 1 Gumyo, Togane 283-8555, Chiba, Japan.
: Laurocapram (Azone) attracted attention 40 years ago as a compound with the highest skin-penetration-enhancing effect at that time; however, its development was shelved due to strong skin irritation. We had already prepared and tested an ante-enhancer (IL-Azone), an ionic liquid (IL) with a similar structure to Azone, consisting of ε-caprolactam and myristic acid, as an enhancer candidate that maintains the high skin-penetration-enhancing effect of Azone with low skin irritation. In the present study, fatty acids with different carbon numbers (caprylic acid: C8, capric acid: C10, lauric acid: C12, myristic acid: C14, and oleic acid: C18:1) were selected and used with ε-caprolactam to prepare various IL-Azones in the search for a more effective IL-Azone.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Faculty of Chemical Engineering and Biotechnology, National University of Science and Technology POLITEHNICA of Bucharest, Polizu No 1, 011061 Bucharest, Romania.
The study aims to investigate an improved version of lipid nanocarriers (NLCs) (formulated with functional coconut butter and marula oil) by designing hyaluronic acid (HA) decorated NLC co-loaded with dual UVA (butyl methoxy dibenzoyl methane, BMDBM), UVB absorbers (ethyl-hexyl-salicylate, EHS) and a Raspberry rich polyphenols fraction (RPRF) for development of more natural NLC-based to-pical formulations. : Quality and quantitative attributes of classic- and HA-NLC have been assigned based on particle size, electrokinetic potential, encapsulation efficiency, spectroscopic characteristics, and high-resolution mass spectrometry. To establish the performance profile of antioxidant activity, release of active substances, sun blocking action, and photostability, in vitro studies were conducted.
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