Abstract：
:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility and wettability of both the crystalline forms were determined. It was found that surfactant can significantly improve the solubility of celastrol up to more than 104 times. Tween 80 and sodium dodecyl sulfate largely improved the wettability of the 2 crystals. Form I shows better wettability than form II in all the buffer solutions with polymers and surfactants. Compared with form II, form I exhibits higher solubility in carboxymethylcellulose and polyvinylpyrrolidone media but much lower solubility in tween 80 and sodium dodecyl sulfate solutions. An investigation of wettability and solubility mechanisms was fully explored, and a hypothesis was proposed to understand the abnormal solubility differences.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Zha J,Zhang Q,Li M,Wang JR,Mei Xdoi
10.1016/j.xphs.2018.07.008subject
Has Abstractpub_date
2018-11-01 00:00:00pages
2860-2868issue
11eissn
0022-3549issn
1520-6017pii
S0022-3549(18)30410-6journal_volume
107pub_type
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