Introduction: Berberine is an isoquinoline alkaloid with multiple therapeutic effects. Its salt, berberine chloride (BCL), has recently been explored for its effectiveness in diabetes. However, BCL exhibits poor water solubility and low permeability, which limits its oral bioavailability. The aim of this study was to optimize and evaluate a nanostructured lipid carrier (NLC)-based transdermal gel formulation of BCL. Methods: BCL-loaded NLCs were fabricated by high-speed homogenization followed by ultrasonication. The formulation was optimized using a three-level, three-factor Box-Behnken Design, with the concentration of surfactant, the ratio of solid to liquid lipid, and the total lipid concentration as independent variables. Entrapment efficiency (%) and flux (μg/cm²/h) were selected as dependent variables. Particle size, polydispersity index, entrapment efficiency, zeta potential, and permeation were all evaluated for the optimized formulation. After optimization, a gel formulation for transdermal application was developed and evaluated. Results: The optimized formulation showed a particle size of 665.5 ± 5.23 nm, zeta potential of - 46.6 mV, and entrapment efficiency of 71.18 ± 1.89%. In vitro release studies revealed prolonged and high drug release from the NLC-based gel (78.73 ± 0.46%) compared to the conventional gel (46.08 ± 0.39%) formulation of BCL. The NLC-based gel demonstrated higher permeation (28.53 ± 1.17 μg/cm²/h) of BCL through mouse skin compared with the conventional gel formulation (9.31 ± 0.26 μg/cm²/h). The gel formulation was stable at 30°C/70% relative humidity after 3 months of storage. Animal studies using female Swiss mice exhibited a significant reduction in hyperglycemia after transdermal application of the NLC-based gel of BCL (101 ± 5 mg/dL) compared to the conventional gel formulation (143 ± 6 mg/dL). Discussion: This study successfully optimized and evaluated BCL-NLC for transdermal drug delivery. Sustained drug release was observed due to the entrapment of BCL within the NLC matrix. The components of NLCs enhanced the permeation of BCL through the mice skin compared to the conventional gel formulation. The developed NLC formulation exhibited improved anti-hyperglycemic activity due to enhanced skin permeation in vivo. Conclusion: The developed NLC gel of BCL holds potential as an efficient therapeutic approach for the management of diabetes.
Khan et al. (Tue,) studied this question.
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