{"entity": "journal", "iuid": "ee378960586c4feb90ac9df2d6f3b8f7", "timestamp": "2026-07-20T12:52:40.338Z", "links": {"self": {"href": "https://publications.scilifelab.se/journal/Eur%20J%20Pharm%20Sci.json"}, "display": {"href": "https://publications.scilifelab.se/journal/Eur%20J%20Pharm%20Sci"}}, "title": "Eur J Pharm Sci", "issn": "1879-0720", "issn-l": "0928-0987", "publications_count": 6, "publications": [{"entity": "publication", "iuid": "3ab0bc13f5cc43e99b0e24ac58f29f78", "links": {"self": {"href": "https://publications.scilifelab.se/publication/3ab0bc13f5cc43e99b0e24ac58f29f78.json"}, "display": {"href": "https://publications.scilifelab.se/publication/3ab0bc13f5cc43e99b0e24ac58f29f78"}}, "title": "Bioinspired mycobacterial lipid coating of porous particles for enhanced antimicrobial efficacy.", "authors": [{"family": "Campos Pacheco", "given": "Jes\u00fas E", "initials": "JE"}, {"family": "Davids", "given": "Camilla", "initials": "C"}, {"family": "Yalovenko", "given": "Tetiana", "initials": "T"}, {"family": "N\u00e4sstr\u00f6m", "given": "Elin", "initials": "E"}, {"family": "Ahnlund", "given": "Maria", "initials": "M"}, {"family": "Godaly", "given": "Gabriela", "initials": "G"}, {"family": "Valetti", "given": "Sabrina", "initials": "S"}], "type": "journal article", "published": "2025-10-01", "journal": {"title": "Eur J Pharm Sci", "issn": "1879-0720", "volume": "213", "pages": "107225", "issn-l": "0928-0987"}, "abstract": "The study aimed to investigate the unique lipid composition of Mycobacterium bovis BCG and its potential to enhance antimicrobial efficacy of lipid-coated mesoporous silica particles (MSPs). The bacterial lipids (BL) were extracted with petroleum ether and analyzed via LC-MS, revealing a complex mixture of phospholipids, including cardiolipin, phosphatidylcholine, phosphatidylethanolamine, and triacylglycerols. Lipid coating (using bacterial lipids and lung surfactant DPPC as the main component) was performed on MSPs via vesicle fusion approach and confirmed with ATR-FTIR spectroscopy. MSPs were loaded with clofazimine (CLZ), as a drug model for tuberculosis. The obtained BL-DPPC-coated CLZ-MSPs were more effective in inhibiting mycobacterial growth and killing intracellular mycobacteria compared to uncoated and DPPC-coated CLZ-MSPs. The bacterial lipids showed a good safety profile on M1-like and M2-like human primary macrophages without inducing a strong immune response or formation of foam cells. These findings suggest that the obtained bacterial lipid coatings can improve antimicrobial efficacy in treating both extracellular and intracellular mycobacteria infections directly in the lungs.", "doi": "10.1016/j.ejps.2025.107225", "pmid": "40780537", "labels": {"Swedish Metabolomics Centre": "Collaborative"}, "xrefs": [{"db": "pii", "key": "S0928-0987(25)00224-6"}], "notes": [], "created": "2025-11-18T12:03:29.035Z", "modified": "2025-11-18T12:03:29.055Z"}, {"entity": "publication", "iuid": "d75862d0095e4fce921c973775b9b75f", "links": {"self": {"href": "https://publications.scilifelab.se/publication/d75862d0095e4fce921c973775b9b75f.json"}, "display": {"href": "https://publications.scilifelab.se/publication/d75862d0095e4fce921c973775b9b75f"}}, "title": "Development of a canine artificial colonic mucus model for drug diffusion studies.", "authors": [{"family": "Barmpatsalou", "given": "V", "initials": "V"}, {"family": "Tjakra", "given": "M", "initials": "M"}, {"family": "Li", "given": "L", "initials": "L"}, {"family": "Dubbelboer", "given": "I R", "initials": "IR"}, {"family": "Karlsson", "given": "E", "initials": "E"}, {"family": "Pedersen Lomstein", "given": "B", "initials": "B"}, {"family": "Bergstr\u00f6m", "given": "C A S", "initials": "CAS"}], "type": "journal article", "published": "2024-03-01", "journal": {"title": "Eur J Pharm Sci", "issn": "1879-0720", "volume": "194", "pages": "106702", "issn-l": "0928-0987"}, "abstract": "Colonic mucus is a key factor in the colonic environment because it may affect drug absorption. Due to the similarity of human and canine gastrointestinal physiology, dogs are an established preclinical species for the assessment of controlled release formulations. Here we report the development of an artificial colonic mucus model to mimic the native canine one. In vitro models of the canine colonic environment can provide insights for early stages of drug development and contribute to the implementation of the 3Rs (refinement, reduction, and replacement) of animal usage in the drug development process. Our artificial colonic mucus could predict diffusion trends observed in native mucus and was successfully implemented in microscopic and macroscopic assays to study macromolecular permeation through the mucus. The traditional Transwell set up was optimized with the addition of a nylon filter to ensure homogenous representation of the mucus barrier in vitro. In conclusion, the canine artificial colonic mucus can be used to study drug permeation across the mucus and its flexibility allows its use in various set ups depending on the nature of the compound under investigation and equipment availability.", "doi": "10.1016/j.ejps.2024.106702", "pmid": "38218203", "labels": {"Integrated Microscopy Technologies Ume\u00e5": "Service", "Drug Discovery and Development": "Service"}, "xrefs": [{"db": "pii", "key": "S0928-0987(24)00013-7"}], "notes": [], "created": "2024-11-19T10:31:23.967Z", "modified": "2025-10-17T13:05:07.394Z"}, {"entity": "publication", "iuid": "1b3d6b5060314dd8b271175a1ef81d18", "links": {"self": {"href": "https://publications.scilifelab.se/publication/1b3d6b5060314dd8b271175a1ef81d18.json"}, "display": {"href": "https://publications.scilifelab.se/publication/1b3d6b5060314dd8b271175a1ef81d18"}}, "title": "Analysis of stabilization mechanisms in \u03b2-lactoglobulin-based amorphous solid dispersions by experimental and computational approaches.", "authors": [{"family": "Zhuo", "given": "Xuezhi", "initials": "X"}, {"family": "Foder\u00e0", "given": "Vito", "initials": "V"}, {"family": "Larsson", "given": "Per", "initials": "P"}, {"family": "Schaal", "given": "Zarah", "initials": "Z"}, {"family": "Bergstr\u00f6m", "given": "Christel A S", "initials": "CAS"}, {"family": "L\u00f6bmann", "given": "Korbinian", "initials": "K"}, {"family": "Kabedev", "given": "Aleksei", "initials": "A"}], "type": "journal article", "published": "2024-01-01", "journal": {"title": "Eur J Pharm Sci", "issn": "1879-0720", "volume": "192", "pages": "106639", "issn-l": "0928-0987"}, "abstract": "Our previous work shows that \u03b2-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for more than 12 months. The stability is probably due to hydrogen bond networks spread throughout the ASD, facilitated by the indomethacin which has both hydrogen donors and acceptors. To investigate the stabilization mechanisms further, here we tested five other drug molecules, including two without any hydrogen bond donors. A combination of experimental techniques (differential scanning calorimetry, X-ray power diffraction) and molecular dynamics simulations was used to find the maximum drug loadings for ASDs with furosemide, griseofulvin, ibuprofen, ketoconazole and rifaximin. This approach revealed the underlying stabilization factors and the capacity of computer simulations to predict ASD stability. We searched the ASD models for crystalline patterns, and analyzed diffusivity of the drug molecules and hydrogen bond formation. ASDs loaded with rifaximin and ketoconazole remained stable for at least 12 months, even at 90 % drug loading, whereas stable drug loadings for furosemide, griseofulvin and ibuprofen were at a maximum of 70, 50 and 40 %, respectively. Steric confinement and hydrogen bonding to the proteins were the most important stabilization mechanisms at low drug loadings (\u2264 40 %). Inter-drug hydrogen bond networks (including those with induced donors), ionic interactions, and a high Tg of the drug molecule were additional factors stabilizing the ASDs at drug loading greater than 40 %.", "doi": "10.1016/j.ejps.2023.106639", "pmid": "37967658", "labels": {"Bioinformatics Support for Computational Resources": "Service"}, "xrefs": [{"db": "pii", "key": "S0928-0987(23)00269-5"}], "notes": [], "created": "2024-11-25T10:12:53.188Z", "modified": "2024-11-25T10:12:53.193Z"}, {"entity": "publication", "iuid": "fb6cd985b2214826bf1603929fdb4a76", "links": {"self": {"href": "https://publications.scilifelab.se/publication/fb6cd985b2214826bf1603929fdb4a76.json"}, "display": {"href": "https://publications.scilifelab.se/publication/fb6cd985b2214826bf1603929fdb4a76"}}, "title": "Impact of N-methylation of the substance P 1-7 amide on anti-allodynic effect in mice after peripheral administration.", "authors": [{"family": "Skogh", "given": "Anna", "initials": "A"}, {"family": "Lesniak", "given": "Anna", "initials": "A"}, {"family": "Gaugaz", "given": "Fabienne Z", "initials": "FZ"}, {"family": "Svensson", "given": "Richard", "initials": "R"}, {"family": "Lindeberg", "given": "Gunnar", "initials": "G"}, {"family": "Fransson", "given": "Rebecca", "initials": "R"}, {"family": "Nyberg", "given": "Fred", "initials": "F"}, {"family": "Hallberg", "given": "Mathias", "initials": "M"}, {"family": "Sandstr\u00f6m", "given": "Anja", "initials": "A"}], "type": "journal article", "published": "2017-09-05", "journal": {"volume": "109", "issn": "1879-0720", "issue": null, "pages": "533-540", "title": "Eur J Pharm Sci", "issn-l": "0928-0987"}, "abstract": "Substance P 1-7 (SP1-7, Arg(1)-Pro(2)-Lys(3)-Pro(4)-Gln(5)-Gln(6)-Phe(7)) is the major bioactive metabolite formed after proteolytic degradation of the tachykinin substance P (SP). This heptapeptide often opposes the effects of the mother peptide. Hence, SP1-7 is having anti-inflammatory, anti-nociceptive and anti-hyperalgesic effects in experimental models. Despite all encouraging properties of SP1-7 its exact mode of action has not yet been elucidated which has hampered further development of this heptapeptide in drug discovery. Contrary to SP that mediates its biological activity via the NK-1 receptor, the N-terminal fragment SP1-7 acts through an unknown target that is distinct from all known opioid and tachykinin receptors. The SP1-7 amide 1 (Arg(1)-Pro(2)-Lys(3)-Pro(4)-Gln(5)-Gln(6)-Phe(7)-NH2) was previously shown to be superior to the endogenous SP1-7 in all experimental pain models where the two compounds were compared. Herein, we report that N-methylation scan of the backbone of the SP1-7 amide (1) results in peptides that are significantly less prone to undergo proteolysis in plasma from both mouse and human. However, with the two exceptions of the [MeLys(3)]SP1-7 amide (3) and the [MeGln(5)]SP1-7 amide (4), the peptides with a methyl group attached to the backbone are devoid of significant anti-allodynic effects after peripheral administration in the spared nerve injury (SNI) mouse model of neuropathic pain. It is suggested that the N-methylation does not allow these peptides to form the accurate bioactive conformations or interactions required for efficient binding to the macromolecular target. The importance of intact N-terminal Arg(1) and C-terminal Phe(7), anticipated to serve as address and message residues, respectively, for achieving the anti-allodynic effect is emphasized. Notably, the three heptapeptides: the SP1-7 amide (1), the [MeLys(3)]SP1-7 amide (3) amide and the [MeGln(5)]SP1-7 amide (4) are all considerably more effective in the SNI mouse model than gabapentin that is widely used in the clinic for treatment of neuropathic pain.", "doi": "10.1016/j.ejps.2017.09.007", "pmid": "28887235", "labels": {"Chemical Biology Consortium Sweden": "Collaborative", "Drug Discovery and Development": "Service"}, "xrefs": [{"db": "pii", "key": "S0928-0987(17)30497-9"}], "notes": [], "created": "2017-10-24T12:16:43.310Z", "modified": "2025-10-17T13:05:08.746Z"}, {"entity": "publication", "iuid": "07677b1e93c84aba875182cf118ebb28", "links": {"self": {"href": "https://publications.scilifelab.se/publication/07677b1e93c84aba875182cf118ebb28.json"}, "display": {"href": "https://publications.scilifelab.se/publication/07677b1e93c84aba875182cf118ebb28"}}, "title": "Importance of N- and C-terminal residues of substance P 1-7 for alleviating allodynia in mice after peripheral administration.", "authors": [{"family": "Skogh", "given": "Anna", "initials": "A"}, {"family": "Lesniak", "given": "Anna", "initials": "A"}, {"family": "Gaugaz", "given": "Fabienne Z", "initials": "FZ"}, {"family": "Svensson", "given": "Richard", "initials": "R"}, {"family": "Lindeberg", "given": "Gunnar", "initials": "G"}, {"family": "Fransson", "given": "Rebecca", "initials": "R"}, {"family": "Nyberg", "given": "Fred", "initials": "F"}, {"family": "Hallberg", "given": "Mathias", "initials": "M"}, {"family": "Sandstr\u00f6m", "given": "Anja", "initials": "A"}], "type": "journal article", "published": "2017-08-30", "journal": {"volume": "106", "issn": "1879-0720", "issue": null, "pages": "345-351", "title": "Eur J Pharm Sci", "issn-l": "0928-0987"}, "abstract": "The heptapeptide SP1-7 (1, Arg(1)-Pro(2)-Lys(3)-Pro(4)-Gln(5)-Gln(6)-Phe(7)) is the major bioactive metabolite formed after proteolytic processing of the neuropeptide substance P (SP, Arg(1)-Pro(2)-Lys(3)-Pro(4)-Gln(5)-Gln(6)-Phe(7)-Phe(8)-Gly(9)-Leu(10)-Met(11)-NH2). The heptapeptide 1 frequently exhibits opposite effects to those induced by SP, such as exerting antinociception, or attenuating thermal hyperalgesia and mechanical allodynia. The heptapeptide SP1-7 amide (2, Arg(1)-Pro(2)-Lys(3)-Pro(4)-Gln(5)-Gln(6)-Phe(7)-NH2) is often more efficacious than 1 in experimental pain models. We have now assessed the anti-allodynic outcome after systemic administration of 2 and a series of Ala-substituted and truncated analogues of 2, in the spared nerve injury (SNI) mice model and the results obtained were correlated with in vitro plasma stability and permeability measurements. It is herein demonstrated that an intact Arg(1) in SP1-7 amide analogues is fundamental for retaining a potent in vivo effect, while Lys(3) of 2 is less important. A displacement with Ala(1) or truncation rendered the peptide analogues either inactive or with a significantly attenuated in vivo activity. Thus, the pentapeptide SP3-7 amide (7, t1/2=11.1 min) proven to be the major metabolite of 2, demonstrated an in vivo effect itself although considerably less significant than 2 in the SNI model. Intraperitoneal administration of 2 in a low dose furnished the most powerful anti-allodynic effect in the SNI model of all the analogous evaluated, despite a fast proteolysis of 2 in plasma (t1/2=6.4 min). It is concluded that not only the C-terminal residue, that we previously demonstrated, but also the N-terminal with its basic side chain, are important for achieving effective pain relief. This information is of value for the further design process aimed at identifying more drug-like SP1-7 amide related peptidomimetics with pronounced anti-allodynic effects.", "doi": "10.1016/j.ejps.2017.06.004", "pmid": "28587787", "labels": {"Drug Discovery and Development": "Collaborative"}, "xrefs": [{"db": "pii", "key": "S0928-0987(17)30336-6"}], "notes": [], "created": "2017-10-24T12:41:03.996Z", "modified": "2025-10-17T13:05:08.767Z"}, {"entity": "publication", "iuid": "08b74c12de1a465ab2aaa3b32739bc07", "links": {"self": {"href": "https://publications.scilifelab.se/publication/08b74c12de1a465ab2aaa3b32739bc07.json"}, "display": {"href": "https://publications.scilifelab.se/publication/08b74c12de1a465ab2aaa3b32739bc07"}}, "title": "Supersaturation of poorly soluble drugs induced by mesoporous magnesium carbonate.", "authors": [{"family": "Zhang", "given": "Peng", "initials": "P"}, {"family": "Zard\u00e1n G\u00f3mez de la Torre", "given": "Teresa", "initials": "T"}, {"family": "Welch", "given": "Ken", "initials": "K"}, {"family": "Bergstr\u00f6m", "given": "Christel", "initials": "C"}, {"family": "Str\u00f8mme", "given": "Maria", "initials": "M"}], "type": "journal article", "published": "2016-10-10", "journal": {"volume": "93", "issn": "1879-0720", "issue": null, "pages": "468-474", "title": "Eur J Pharm Sci", "issn-l": "0928-0987"}, "abstract": "This work investigates whether the solubility of poorly soluble compounds can be improved by using mesoporous magnesium carbonate (MMC) as the drug delivery system. A solvent evaporation method was used to load structurally diverse model drugs (celecoxib, cinnarizine and griseofulvin) into the pores of MMC. The drug-loaded carrier system was then characterized in terms of porosity, crystallinity, and release profiles by a variety of experimental techniques, including X-ray diffraction, nitrogen adsorption analysis, differential scanning calorimetry, infrared spectroscopy, UV absorption spectroscopy, and thermogravimetric analysis. All three drugs were in a non-crystalline state after loading into the pores of MMC. The concentrations of the drugs in solution over time (a measure of the release rates from loaded MMC) were higher than the corresponding concentrations (dissolution rates) of equal amounts of the crystalline drugs. The release rates were five (celecoxib), three (cinnarizine) and two times (griseofulvin) higher than the dissolution rates of their crystalline counterparts. Supersaturation release profiles were also observed; the areas under the concentration-time curves (0-240min) were 25- (celecoxib), 5- (cinnarizine) and 2-fold (griseofulvin) greater than those of the crystalline drugs. Hence, MMC shows promise as a general drug delivery vehicle for increasing the bioavailability of compounds with dissolution rate- or solubility-limited absorption.", "doi": "10.1016/j.ejps.2016.08.059", "pmid": "27590126", "labels": {"BioMaterial Interactions (BioMat)": "Service"}, "xrefs": [{"db": "pii", "key": "S0928-0987(16)30347-5"}], "notes": [], "created": "2017-05-03T13:02:31.449Z", "modified": "2017-06-12T11:40:02.980Z"}], "created": "2017-05-09T09:12:01.169Z", "modified": "2020-11-27T13:14:07.892Z"}