Abstract

The synthesis of a redox-based chemical delivery system for dopamine (DA-CDS) was modified to yield a crystalline final product that had an improved stability profile during storage. Oxidation was the primary degradation process observed in crystalline DA-CDS samples, while hydration was a major degradation process in amorphous samples. Amorphous samples showed significant appearance of the 5,6-water addition product during storage. The crystalline DA-CDS was soluble in aqueous hydroxypropyl-β-cyclodextrin (HP-β-CyD). Lyophilized samples of the drug-HP-β-CyD complex had decreased stability compared to pure crystalline DA-CDS samples, which was attributed to the known hygroscopic properties of HP-β-CyD. In-vivo distribution was examined after intraperitoneal administration of a prototype aqueous formulation containing HP-β-CyD. Results indicate that the drug can reach target sites in the central nervous system after intraperitoneal dosing.

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