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Mechanisms of Drug ...
Mechanisms of Drug Solubility Enhancement Induced by β-Lactoglobulin-Based Amorphous Solid Dispersions
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- Zhuo, Xuezhi (author)
- Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
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- Sener, Zeyneb (author)
- Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
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- Kabedev, Aleksei (author)
- Uppsala universitet,Institutionen för farmaci
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- Zhao, Min (author)
- China Med Univ, China Med Univ Queens Univ Belfast Joint Coll CQC, Shenyang 110000, Peoples R China.;Queens Univ Belfast, Sch Pharm, Belfast BT9 7BL, Antrim, North Ireland.
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- Arnous, Anis (author)
- Zerion Pharm AS, Blokken 11, DK-3460 Birkerod, Denmark.
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- Leng, Donglei (author)
- Zerion Pharm AS, Blokken 11, DK-3460 Birkerod, Denmark.
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- Fodera, Vito (author)
- Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
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- Löbmann, Korbinian (author)
- Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.;Zerion Pharm AS, Blokken 11, DK-3460 Birkerod, Denmark.
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Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark Institutionen för farmaci (creator_code:org_t)
- American Chemical Society (ACS), 2023
- 2023
- English.
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In: Molecular Pharmaceutics. - : American Chemical Society (ACS). - 1543-8384 .- 1543-8392. ; 20:10, s. 5206-5213
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Protein-based amorphous solid dispersions (ASDs) have emerged as a promising approach for enhancing solubility in comparison to crystalline drugs. The dissolution behavior of protein-based amorphous solid dispersions (ASDs) was investigated in various pH media. ASDs of four poorly soluble model drugs with acidic ( furosemide and indomethacin), basic (carvedilol), and neutral (celecoxib) properties were prepared by spray drying at 30 wt % drug loading with the protein ss-lactoglobulin (BLG). The effect of spray-dried BLG (SD-BLG) solubility and protein binding ability with dissolved drugs in solution were investigated to retrieve the mechanisms governing the improvement of drug solubility from the BLG-based ASDs. Powder dissolution results showed that all ASDs obtained a higher maximum concentration (C-max) compared to the respective pure crystalline drugs. It was found that the solubility increase of the drugs from the ASDs was to a large extent dependent on the solubility of the pure SD-BLG at the investigated pH values (low solubility at pH near the isoelectric point (pI) of BLG). Furthermore, drug-protein interactions in a solution were observed, in particular at pH values where the drugs were neutral. These drug-protein interactions also resulted, to some extent, in the stabilization of the drug in supersaturation.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- amorphous solid dispersion
- ss-lactoglobulin
- dissolution
- supersaturation
- binding ability
Publication and Content Type
- ref (subject category)
- art (subject category)
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