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<p>Hypertension is the foremost reason for death among patients with heart disease, stroke, and chronic kidney disease. Cilnidipine (CLN), a fourth–generation dihydropyridine calcium channel blocker, shows promising results for cardiovascular diseases, but its bioavailability (6–30%) negatively impacts its effectiveness. The synthesis of cilnidipine encapsulated Nanostructured Lipid Carriers was achieved through high–pressure homogenization and 3<sup>3</sup> Box–Behnken Design was utilized for optimization. The physicochemical characterization evaluated the entrapment efficiency (%EE), size of the particle, its zeta potential, thermal behavior, crystallinity, and chemical interactions. The optimized formulation presented 190.21 ± 21.63&#xa0;nm (mean particle size), 0.27 ± 0.12 (PDI), -29.25 ± 0.31 mV (Zeta), and 79.35% ± 3.13% (Entrapment efficiency). Analysis using DSC and XRD confirmed the transition of the drug’s crystalline form to an amorphous form within the nanostructured lipid carriers (NLCs), potentially improving its solubility and bioavailability. Fourier–transform infrared spectroscopy (FTIR) affirmed compatibility between Cilnidipine and formulation excipients. The studies of <i>in–vitro</i> release showed an initial surge in release, followed by a gradual slow drug release from NLCs, exhibiting a dual–release pattern. This study aims to develop, optimize, and evaluate CLN–NLCs to boost the oral bioavailability of CLN, thereby improving its therapeutic effectiveness and patient compliance.</p>

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Innovative Nanostructured Lipid Scaffolds for Cilnidipine: Design and Optimization to Elevate the Therapeutic Potential in Hypertensive Therapy

  • 期刊论文

  • 发表日期：

    2025年4月5日

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  • Yogesh Mali,
  • Rarchita Sharma,
  • Yogeeta Agrawal,
  • Kiran Patil

摘要

Hypertension is the foremost reason for death among patients with heart disease, stroke, and chronic kidney disease. Cilnidipine (CLN), a fourth–generation dihydropyridine calcium channel blocker, shows promising results for cardiovascular diseases, but its bioavailability (6–30%) negatively impacts its effectiveness. The synthesis of cilnidipine encapsulated Nanostructured Lipid Carriers was achieved through high–pressure homogenization and 33 Box–Behnken Design was utilized for optimization. The physicochemical characterization evaluated the entrapment efficiency (%EE), size of the particle, its zeta potential, thermal behavior, crystallinity, and chemical interactions. The optimized formulation presented 190.21 ± 21.63 nm (mean particle size), 0.27 ± 0.12 (PDI), -29.25 ± 0.31 mV (Zeta), and 79.35% ± 3.13% (Entrapment efficiency). Analysis using DSC and XRD confirmed the transition of the drug’s crystalline form to an amorphous form within the nanostructured lipid carriers (NLCs), potentially improving its solubility and bioavailability. Fourier–transform infrared spectroscopy (FTIR) affirmed compatibility between Cilnidipine and formulation excipients. The studies of in–vitro release showed an initial surge in release, followed by a gradual slow drug release from NLCs, exhibiting a dual–release pattern. This study aims to develop, optimize, and evaluate CLN–NLCs to boost the oral bioavailability of CLN, thereby improving its therapeutic effectiveness and patient compliance.