Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability

• Autori principali: Yihua Jiang (Autore), Yinxiang Cheng (Autore), Mengyuan Xia (Autore), Bingrui Zhang (Autore), Qiaoce Ding (Autore), Liye Lu (Autore), Jian-Rong Wang (Autore), Xuefeng Mei (Autore)
• Natura: Libro
• Pubblicazione: MDPI AG, 2022-11-01T00:00:00Z.
• Soggetti: article
• Accesso online: Connect to this object online.
• Notes: 10.3390/pharmaceutics14112478; 1999-4923
• Keywords: DHEA; cocrystallization; crystal structure; solubility; bioavailability; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 14, Iss 11, p 2478 (2022)

Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol (CAT), hydroquinone (HQ), resorcinol (RES), phloroglucinol (PG), 1,5-dihydroxy naphthalene (DHN), p-hydroxybenzoic acid (PHBA), gallic acid (GA), and 5-hydroxyisophthalic acid (5HIPA) were designed and synthesized. Some basic characterization tools, including powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and Fourier transform infrared spectroscopy, were also applied in our work for basic analyses of cocrystals. It is indicated that DHEA-GA exhibits its superiority in dissolution and pharmacokinetic behaviors. While the area under the curve values of DHEA-GA is improved at the ratio of 2.2, the corresponding bioavailability of DHEA is expected to be accordingly increased.