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Purpose <p>The study developed and optimized a lyophilized dry emulsion (LDE) of Nicardipine Hydrochloride (NHCl) using a pseudo-ternary phase diagram (PTPD) and a Box–Behnken design (BBD) to enhance aqueous solubility and to obtain a free-flowing, compressible powder suited for solid dosage form development.</p> Methods <p>A PTPD was constructed using caprylic capric (CC), Smix (Tween 80 and Transcutol HP<sup>®</sup>, 1:1), and a water phase (WP) containing 5% w/v maltodextrin as a cryoprotectant and 2% sodium alginate as a matrix former to define the emulsifying region. A BBD with CC, Smix, WP, temperature, and vacuum as independent variables was used to generate formulations. The solubility responses of these formulations were analyzed by Analysis of Variance (ANOVA) and response surface methodology (RSM) to identify an optimized batch. The optimized LDE (OLDE) was prepared under the predicted conditions and evaluated for zeta potential, solubility, flow properties, X-ray diffraction (XRD), Scanning Electron Microscope (SEM), and Differential Scanning Calorimetry (DSC).</p> Results <p>The PTPD identified an emulsification region, and BBD analysis revealed Smix, CC, and WP as key factors influencing solubility. The OLDE exhibited a solubility of 1.698 ± 0.010&#xa0;mg/mL, higher than the pure NHCl. It showed good flow properties-Angle of repose 29.85°, Hausner ratio (HR) 1.15, Carr’s index (CI) 13.09% and a zeta potential of − 26.2 mV, indicating emulsion stability. XRD, SEM, and DSC analyses confirmed reduced crystallinity and formation of amorphous matrix.</p> Conclusion <p>A PTPD-guided and BBD-OLDE successfully enhanced the aqueous solubility and flow properties of NHCl. The OLDE of NHCl exhibited good physicochemical and solid-state characteristics, supporting promising platform for the NHCl solid oral dosage forms.</p>

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Box–Behnken Design Optimization of Nicardipine Hydrochloride Lyophilized Dry Emulsion

  • 期刊论文

  • 发表日期：

    2026年4月18日

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  • Rahul Yuvraj Pagar,
  • Avinash Balasaheb Gangurde

摘要

Purpose

The study developed and optimized a lyophilized dry emulsion (LDE) of Nicardipine Hydrochloride (NHCl) using a pseudo-ternary phase diagram (PTPD) and a Box–Behnken design (BBD) to enhance aqueous solubility and to obtain a free-flowing, compressible powder suited for solid dosage form development.

Methods

A PTPD was constructed using caprylic capric (CC), Smix (Tween 80 and Transcutol HP®, 1:1), and a water phase (WP) containing 5% w/v maltodextrin as a cryoprotectant and 2% sodium alginate as a matrix former to define the emulsifying region. A BBD with CC, Smix, WP, temperature, and vacuum as independent variables was used to generate formulations. The solubility responses of these formulations were analyzed by Analysis of Variance (ANOVA) and response surface methodology (RSM) to identify an optimized batch. The optimized LDE (OLDE) was prepared under the predicted conditions and evaluated for zeta potential, solubility, flow properties, X-ray diffraction (XRD), Scanning Electron Microscope (SEM), and Differential Scanning Calorimetry (DSC).

Results

The PTPD identified an emulsification region, and BBD analysis revealed Smix, CC, and WP as key factors influencing solubility. The OLDE exhibited a solubility of 1.698 ± 0.010 mg/mL, higher than the pure NHCl. It showed good flow properties-Angle of repose 29.85°, Hausner ratio (HR) 1.15, Carr’s index (CI) 13.09% and a zeta potential of − 26.2 mV, indicating emulsion stability. XRD, SEM, and DSC analyses confirmed reduced crystallinity and formation of amorphous matrix.

Conclusion

A PTPD-guided and BBD-OLDE successfully enhanced the aqueous solubility and flow properties of NHCl. The OLDE of NHCl exhibited good physicochemical and solid-state characteristics, supporting promising platform for the NHCl solid oral dosage forms.