Aiming to contribute to drug pre-formulation, new eutectic mixtures were developed. Thymol, coumarin, or quaternary ammonium chlorides as excipients, were combined with the active pharmaceutical ingredients (APIs) acetylsalicylic acid, acetaminophen, ibuprofen, ketoprofen, or lidocaine. Their solid-liquid equilibrium (SLE) binary phase diagrams were measured to study eventual phase separation between the compounds, preventing manufacturing problems, and to study the molecular interactions between the APIs and ionic or non-ionic excipients. The Conductor-like Screening Model for Real Solvents (COSMO-RS) capability to predict the SLE of mixtures containing non-ionic excipients was further evaluated. COSMO-RS gives a good quantitative description of the experimental SLE being a tool with great potential in the screening of eutectic systems containing APIs and non-ionic excipients. While thymol presents strong interactions with the APIs, and consequently negative deviations to thermodynamic ideality, systems containing coumarin follow a quasi-ideal behavior. Regarding the ionic excipients, both choline chloride and the tetraalkylammonium chlorides are unable to establish relevant interactions with the APIs, and no significant negative deviations to ideality are observed. The liquefaction of the APIs here studied is favored by using non-ionic excipients, such as thymol, due to the strong interactions it can establish with the APIs.
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http://dx.doi.org/10.1016/j.ejps.2020.105583 | DOI Listing |
Pharmaceuticals (Basel)
November 2024
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.
: Drugs exhibiting poor aqueous solubility present a challenge to efficient delivery to the site of action. Spanlastics (a nano, surfactant-based drug delivery system) have emerged as a powerful tool to improve solubility, bioavailability, and delivery to the site of action. This study aimed to better understand factors affecting the physicochemical properties of spanlastics, quantify their effects, and use them to enhance the bioavailability of famotidine (FMT), a model histamine H2 receptor antagonist (BCS class IV).
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Division of Clinical Geriatrics, Centre for Alzheimer Research, Department of Neurobiology, Care Sciences and Society, Karolinska Institutet, 141 57 Stockholm, Sweden.
Choline-acetyltransferase (ChAT) is the key cholinergic enzyme responsible for the biosynthesis of acetylcholine (ACh), a crucial signaling molecule with both canonical neurotransmitter function and auto- and paracrine signaling activity in non-neuronal cells, such as lymphocytes and astroglia. Cholinergic dysfunction is linked to both neurodegenerative and inflammatory diseases. In this study, we investigated a serendipitous observation, namely that the catalytic rate of human recombinant ChAT (rhChAT) protein greatly differed in buffered solution in the presence and absence of Triton X-100 (TX100).
View Article and Find Full Text PDFJ Chromatogr A
February 2025
Thermofisher Scientific (China) Co. Ltd. Building A, No.2517 Jinke Road, Pudong District, Shanghai 201203, China. Electronic address:
Polysorbates (PS), as non-ionic surfactants, contribute significantly to the stability of proteins in formulations. However, their lack of chromophore groups makes them difficult to detect with high sensitivity and simplicity. The charged aerosol detector (CAD) is an emerging and universal detector that can provide highly sensitive response signals to non-volatile or semi-volatile substances, such as esters, acids, oxidized aldehydes, and contaminant ions in PS.
View Article and Find Full Text PDFJ Oleo Sci
January 2025
Center of Excellence for Advanced Materials Research, King Abdulaziz University.
In the present study, the mixed micellization behavior of gemini surfactant-1, 5-bis (N-hexadecyl- N, N-dimethylammonium) pentane dibromide (G5) with non-ionic surfactant triton X-100 (TX-100) was investigated in the micellar phase by utilizing the conductometric technique. The deviation of ideal critical micelle concentration (cmc*) from experimental critical micelle concentration (cmc) has been estimated using well-known Clint's theory of mixed micelles. The regular solution approximation was used to determine the interaction parameter (β) and found to be negative.
View Article and Find Full Text PDFInt J Pharm
January 2025
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, India. Electronic address:
Poloxamer 407 is a versatile excipient that enhances drug solubilization and prolongs drug release. Poloxamers are non-ionic tri-block copolymers composed of a central hydrophobic chain of polyoxypropylene flanked by two hydrophilic chains of polyoxyethylene. Various researchers have utilized Poloxamer 407 in topical and transdermal drug delivery systems, and it has also been reported to enhance skin permeability.
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