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author:

Fan, Shixin (Fan, Shixin.) [1] | Zheng, Wenling (Zheng, Wenling.) [2] | Ren, Shizhao (Ren, Shizhao.) [3] | Xiao, Wangchuan (Xiao, Wangchuan.) [4] | Chen, Fenghua (Chen, Fenghua.) [5] | Xue, Rongrong (Xue, Rongrong.) [6]

Indexed by:

EI Scopus SCIE

Abstract:

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 (similar to 178 mu g.mL(-1)), 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.

Keyword:

aggregation-caused quenching amorphous solid dispersions boundary curcumin fluorescence solubility

Community:

  • [ 1 ] [Fan, Shixin]Fujian Agr & Forestry Univ, Coll Mat Engn, Fuzhou 350100, Peoples R China
  • [ 2 ] [Fan, Shixin]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 3 ] [Zheng, Wenling]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 4 ] [Ren, Shizhao]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 5 ] [Xiao, Wangchuan]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 6 ] [Chen, Fenghua]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 7 ] [Xue, Rongrong]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China
  • [ 8 ] [Fan, Shixin]Sanming Univ, Sanming Inst Fluorochem Ind, Sanming 365004, Peoples R China
  • [ 9 ] [Xiao, Wangchuan]Sanming Univ, Sanming Inst Fluorochem Ind, Sanming 365004, Peoples R China
  • [ 10 ] [Zheng, Wenling]Fuzhou Univ, Sch Chem Engn, Fuzhou 350116, Peoples R China

Reprint 's Address:

  • [Chen, Fenghua]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China;;[Xue, Rongrong]Sanming Univ, Sch Resources & Chem Engn, Sanming 365004, Peoples R China

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Source :

CRYSTALS

Year: 2025

Issue: 6

Volume: 15

2 . 4 0 0

JCR@2023

Cited Count:

WoS CC Cited Count:

SCOPUS Cited Count:

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 1

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