Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy
Amorphous solid dispersion (ASD) technology is popularly used for enhancing the solubility of poorly water-soluble drugs. Drug molecules in ASDs can be dispersed in the form of either amorphous (AASD) or molecular (MASD) forms. The boundary between AASDs and MASDs (A–M boundary) is defined as the dr...
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MDPI AG
2025-05-01
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| author | Shixin Fan Wenling Zheng Shizhao Ren Wangchuan Xiao Fenghua Chen Rongrong Xue |
| author_facet | Shixin Fan Wenling Zheng Shizhao Ren Wangchuan Xiao Fenghua Chen Rongrong Xue |
| author_sort | Shixin Fan |
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| description | Amorphous solid dispersion (ASD) technology is popularly used for enhancing the solubility of poorly water-soluble drugs. Drug molecules in ASDs can be dispersed in the form of either amorphous (AASD) or molecular (MASD) forms. The boundary between AASDs and MASDs (A–M boundary) is defined as the drug concentration at which the existence of MASDs obviously influences the physicochemical properties of ASDs. In this work, fluorescence spectroscopy based on the aggregation-caused quenching (ACQ) phenomenon was used to determine the A–M boundary of curcumin (CUR) ASDs prepared via neat ball milling. The relationship between the fluorescence intensity and the loading of CUR in the sample is consistent with the Stern–Volmer equation. For the CUR ASDs with PVP, the samples with CUR loading below 10% show significantly increased fluorescence and have a higher solubility (~178 μg·mL<sup>−1</sup>), suggesting the A–M boundary is around 10%. Similar A–M boundaries around 10% were also observed for CUR ASDs with PVPVA, Soluplus, HPMC, and HPMCAS. It is of great significance to define the A–M boundary of ASDs for guiding pharmaceutical ASD formulas by balancing drug loading, stability, and solubility. |
| format | Article |
| id | doaj-art-ff0fec18dfd345d49b32dfc25b293fb0 |
| institution | Kabale University |
| issn | 2073-4352 |
| language | English |
| publishDate | 2025-05-01 |
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| series | Crystals |
| spelling | doaj-art-ff0fec18dfd345d49b32dfc25b293fb02025-08-20T03:27:28ZengMDPI AGCrystals2073-43522025-05-0115651210.3390/cryst15060512Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence SpectroscopyShixin Fan0Wenling Zheng1Shizhao Ren2Wangchuan Xiao3Fenghua Chen4Rongrong Xue5College of Material Engineering, Fujian Agriculture and Forestry University, Fuzhou 350100, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaSchool of Resources and Chemical Engineering, Sanming University, Sanming 365004, ChinaAmorphous solid dispersion (ASD) technology is popularly used for enhancing the solubility of poorly water-soluble drugs. Drug molecules in ASDs can be dispersed in the form of either amorphous (AASD) or molecular (MASD) forms. The boundary between AASDs and MASDs (A–M boundary) is defined as the drug concentration at which the existence of MASDs obviously influences the physicochemical properties of ASDs. In this work, fluorescence spectroscopy based on the aggregation-caused quenching (ACQ) phenomenon was used to determine the A–M boundary of curcumin (CUR) ASDs prepared via neat ball milling. The relationship between the fluorescence intensity and the loading of CUR in the sample is consistent with the Stern–Volmer equation. For the CUR ASDs with PVP, the samples with CUR loading below 10% show significantly increased fluorescence and have a higher solubility (~178 μg·mL<sup>−1</sup>), suggesting the A–M boundary is around 10%. Similar A–M boundaries around 10% were also observed for CUR ASDs with PVPVA, Soluplus, HPMC, and HPMCAS. It is of great significance to define the A–M boundary of ASDs for guiding pharmaceutical ASD formulas by balancing drug loading, stability, and solubility.https://www.mdpi.com/2073-4352/15/6/512amorphous solid dispersionsboundaryfluorescencesolubilityaggregation-caused quenchingcurcumin |
| spellingShingle | Shixin Fan Wenling Zheng Shizhao Ren Wangchuan Xiao Fenghua Chen Rongrong Xue Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy Crystals amorphous solid dispersions boundary fluorescence solubility aggregation-caused quenching curcumin |
| title | Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy |
| title_full | Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy |
| title_fullStr | Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy |
| title_full_unstemmed | Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy |
| title_short | Boundary Between Amorphously and Molecularly Dispersed Curcumin of Its Amorphous Solid Dispersions Determined by Fluorescence Spectroscopy |
| title_sort | boundary between amorphously and molecularly dispersed curcumin of its amorphous solid dispersions determined by fluorescence spectroscopy |
| topic | amorphous solid dispersions boundary fluorescence solubility aggregation-caused quenching curcumin |
| url | https://www.mdpi.com/2073-4352/15/6/512 |
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