Anti-inflammatory activity and percutaneous absorption of quercetin and its polymethoxylated compound and glycosides: the relationships to chemical structures.

The potential of quercetin-related compounds for topical application has not previously been systematically investigated. To better elucidate relationships of the structure and activity with skin permeation, some quercetin compounds were used as permeants, including aglycone, a polymethoxylated compound (quercetin 3,5,7,3',4'-pentamethylether, QM), and seven glycosides. Quercetin and the glycoside with glucopyranuronic acid (Q4) at a dose of 30 μM completely inhibited superoxide anion activated neutrophils.

Combined strategies of apomorphine diester prodrugs and nanostructured lipid carriers for efficient brain targeting.

Our aim is to develop nanostructured lipid carriers (NLCs) for loading the apomorphine diester prodrugs, diacetyl apomorphine (DAA) and diisobutyryl apomorphine (DIA), into the brain. NLCs were prepared using sesame oil/cetyl palmitate as the lipid matrices. Experiments were performed with the objective of evaluating the physicochemical characteristics, drug release, safety and brain-targeting efficacy of the NLCs.

Enhancement of transdermal apomorphine delivery with a diester prodrug strategy.

Diester prodrugs of apomorphine, diacetyl apomorphine (DAA), and diisobutyryl apomorphine (DIA) were synthesized, and their partition coefficients, capacity factor (log K'), enzymatic hydrolysis, and in vitro permeation across nude mouse skin were characterized. The lipophilicity of the diesters was between that of apomorphine HCl and the apomorphine base. The prodrugs were chemically stable, but enzymatically unstable in esterase medium, skin homogenate, and human plasma.