Preparation of berberine micelles and its anti-skin damage in hyperglycemia mice

1. This study aimed to prepare and evaluate berberine micelles for improving the oral bioavailability and therapeutic effect against skin injury in hyperglycemic mice. Berberine micelles were fabricated using the film dispersion method with PLGA-PEG-PLGA and glycyrrhizic acid monoamine salt, followed by orthogonal optimization.2. The optimized berberine micelles exhibited a particle size of 112.55 ± 2.48 nm, polydispersity index of 0.217 ± 0.005, zeta potential of −31.60 ± 0.23 mV, encapsulation efficiency of 95.57 ± 1.36% (w/w), and drug loading capacity of 7.06 ± 0.25% (w/w). In vitro release of berberine from micelles was higher than that of free berberine across all tested media.3. Pharmacokinetic studies in rats showed that berberine micelles prolonged the half-life from 5.77 h to 12.19 h and extended the mean retention time from 20.74 h to 143.31 h, with a relative bioavailability 2.64‑fold greater than that of free berberine.4. In a streptozotocin‑induced hyperglycemic mouse skin injury model, the high‑dose berberine micelle group significantly accelerated wound closure compared to the free drug group on days 6 and 9, and histopathological analysis of skin, liver, spleen, and pancreas revealed superior tissue recovery. These findings suggest that berberine micelles effectively enhance the anti‑hyperglycemic and skin‑repairing efficacy of berberine.