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The solid dispersion of a novel curcumin analogue (CACN136) prepared using PVP/Mannitol composite carrier
Yumeng Wei1, Ke Gong2, Rongzhu Li3
1Central Nervous System Product Research and Development Key Laboratory of Sichuan Province, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan 646000, PR China.
Objective:
CACN136 is a novel curcumin analogue with antidepressant potential, but its poor aqueous solubility may restrict oral absorption. This study aimed to develop a rapidly dissolving solid dispersion of CACN136 (CACN136-SD) to further enhance its oral bioavailability and antidepressant efficacy.
Methods:
CACN136-SD was prepared using a solvent method with PVP and mannitol as composite carriers. Physicochemical characterization was performed through in vitro experiments, followed by pharmacokinetic and antidepressant behavioral evaluations.
Results:
CACN136-SD increased the apparent aqueous solubility of CACN136 approximately 20-fold. Cumulative dissolution at 10 min reached 95.69%, versus 6.64% for the active pharmaceutical ingredient (API). Differential scanning calorimetry and X-ray powder diffraction showed markedly reduced drug crystallinity, with CACN136 present predominantly in an amorphous or highly disordered state within the carrier matrix. Fourier-transform infrared spectroscopy showed changes in the local vibrational environment of CACN136 after incorporation into the matrix. The apparent terminal half-life of CACN136-SD was approximately 23 times that of the API, and its systemic exposure (AUC-t) was 8.95 times higher. In the chronic unpredictable mild stress (CUMS) model, CACN136-SD significantly alleviated depression-like behaviors and produced greater changes in serum and hippocampal 5-hydroxytryptamine (5-HT) and monoamine oxidase (MAO) levels than unformulated CACN136. Preliminary safety assessments detected no obvious cardiac, hepatic, or renal toxicity under the tested conditions.
Conclusion:
CACN136-SD improved the solubility, dissolution, and oral exposure of CACN136 and showed enhanced antidepressant-like activity associated with changes in monoamine-related markers. This solid dispersion represents a promising antidepressant candidate with potential for clinical translation.
