The College of Pharmacy / University of Baghdad discussed the PhD dissertation entitled “Preparation and In Vitro and In Vivo Evaluation of Repaglinide-Loaded Nanomicelles as Fast Dissolving Film”, by the student Zainab Ahmed Sadeq and the supervisor, Assistant Professor Dr. Lubna Abdalkarim Sabri, at the Pharmaceutics Department.
The study aimed to prepare and optimize Repaglinide-loaded nanomicelles to improve the dissolution characteristics and oral bioavailability of Repaglinide, a poorly water-soluble drug classified as a Biopharmaceutical Classification System (BCS) class II drug.
The study involved the preparation of Repaglinide-loaded nanomicelles using the thin-film hydration method. A Box-Behnken experimental design was employed to optimize the formulation by investigating the effects of the amount of Soluplus®, Poloxamer 338, hydration volume, and stirring speed on particle size, polydispersity index, and entrapment efficiency. The optimized formulation was evaluated for its drug release profile, morphology, and compatibility with the formulation excipients. In addition, the optimized micelles were incorporated into a fast-dissolving film and evaluated.
The results showed that the optimized Repaglinide-loaded micelles had a particle size of 61.25 nm, a polydispersity index of 0.085, and an entrapment efficiency of 87%. Moreover, the optimized formulation demonstrated a significant improvement in the in-vitro dissolution rate compared with pure Repaglinide. In addition, pharmacokinetic evaluation in rats demonstrated enhanced systemic exposure following administration of the optimized Repaglinide-loaded micelles, in which the formulation achieved a Cmax of 77.6 ± 0.2 ng/mL, a Tmax of 0.5 ± 0.05 hours, and an AUC0–6 of 230.38 ± 4.3 ng·h/mL, compared with a Cmax of 24 ± 0.6 ng/mL, a Tmax of 1 ± 0.3 hours, and an AUC0–6 of 88.63 ± 2.1 ng·h/mL for the oral Repaglinide suspension.
The study concluded that nanomicelles enhanced the dissolution and bioavailability of Repaglinide and showed promising potential as an oral fast-dissolving film dosage form. Further stability, preclinical, and clinical studies were recommended to evaluate its safety and efficacy.
