Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study

Citation:
Kassem, M. A. A., A. N. ElMeshad, and A. R. Fares, "Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study", DRUG DELIVERY, vol. VOL. 25, issue NO. 1, pp. 132–142, 2018.

Abstract:

ABSTRACT
This study aims at preparing and optimizing lacidipine (LCDP) polymeric micelles using thin film hydration
technique in order to overcome LCDP solubility-limited oral bioavailability. A two-factor three-level
central composite face-centered design (CCFD) was employed to optimize the formulation variables to
obtain LCDP polymeric micelles of high entrapment efficiency and small and uniform particle size (PS).
Formulation variables were: Pluronic to drug ratio (A) and Pluronic P123 percentage (B). LCDP polymeric
micelles were assessed for entrapment efficiency (EE%), PS and polydispersity index (PDI). The
formula with the highest desirability (0.959) was chosen as the optimized formula. The values of the
formulation variables (A and B) in the optimized polymeric micelles formula were 45% and 80%,
respectively. Optimum LCDP polymeric micelles had entrapment efficiency of 99.23%, PS of 21.08nm
and PDI of 0.11. Optimum LCDP polymeric micelles formula was physically characterized using transmission
electron microscopy. LCDP polymeric micelles showed saturation solubility approximately 450
times that of raw LCDP in addition to significantly enhanced dissolution rate. Bioavailability study of
optimum LCDP polymeric micelles formula in rabbits revealed a 6.85-fold increase in LCDP bioavailability
compared to LCDP oral suspension.

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