Solubility improvement of curcumin by crystallization inhibition from polymeric surfactants in amorphous solid dispersions
To improve the solubility and maintain the amorphous state of BCS Ⅳ drug by preparing surfactant solid dispersions, solid dispersions of curcumin (CUR) with TPGS and HPMC were prepared by solvent method. The synthesized solid dispersions were characterized by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry and FTIR spectroscopy, whose aim is to elucidate morphology of the dispersed solid dispersion and the interactions occurring between CUR and carriers. The comprehensive solubilization mechanism of surfactants in vitro and the pharmaceutical properties of optimal formulations in vivo were revealed completely.
The results showed that TPGS as a carrier provides superior solubility and stability due to its stable hydrogen bonding strength and related crystal nuclei growth theory. At different pH values, TPGS significantly promoted the solubility and release rate of CUR in the whole gastrointestinal tract. In comparison with natural CUR, the cumulative release of solid dispersion is 3.7-fold, which could approximately reach 100% with assistance of surfactant. Thus, in consistent with the nature of CUR, solid dispersion with high solubility and stability significantly enhanced the gastric ulcer healed rate. Oral bioavailability of solid dispersion was increased 5-fold than pure CUR. Therefore, solid dispersion with novel applied surfactants is an effect strategy to improve pharmaceutical properties of CUR.
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Ziyue Xi, Yali Fei, Yuxin Wang, Qing Lin, Qidong Ke, Guotai Feng, Lu Xu, Solubility improvement of curcumin by crystallization inhibition from polymeric surfactants in amorphous solid dispersions, Journal of Drug Delivery Science and Technology, 2023, 104351, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2023.104351.
See also the interesting video on Vitamin E TPGS: