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Formulation, Characterization, Optimization, and Pharmacokinetic Evaluation of Cilnidipine-Loaded Liquisolid Compacts with Improved Dissolution and Bioavailability

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Abstract

Purpose

Cilnidipine (BCS class II drug) is a calcium channel blocker used in the treatment of hypertension. Poor water solubility, unreliable oral absorption, and poor bioavailability make it a probable candidate for designing novel drug delivery. The objective of the present investigation was to formulate, optimize, and study in vitro and in vivo performance of cilnidipine-loaded liquisolid compacts.

Methods

Solid-state characterization was performed by FTIR, DSC, SEM, and XRD. Preliminary screening was performed to select non-volatile solvent, carrier, and coating material based on flowable liquid retention potential. Liquisolid compacts were optimized using 32 factorial designs and were studied for pre- and post-compression parameters, in vitro dissolution, dissolution validation, and pharmacokinetic and stability studies, whereas bioanalysis was carried out using HPLC–MS/Ms method.

Results

In the preformulation study, Transcutol HP was selected as the non-volatile solvent, and Neusilin US2 and Cab-o-sil were selected as the carrier and coating material, respectively, exhibiting compatibility with the drug. Liquisolid compacts were found to be compressible with the selected composition. In vitro studies indicated increased dissolution behaviour, whereas in vivo studies demonstrated improved bioavailability compared to the pure drug and marketed formulation.

Conclusion

In conclusion, formulated liquisolid compacts demonstrated increased dissolution and bioavailability making the formulation suitable for oral administration.

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Authors and Affiliations

  1. Babaria Institute of Pharmacy, Varnama. Gujarat Technological University, Vadodara, 391240, Gujarat, India

    Farhatjahan Shaikh & Deepti Jani

  2. Department of Pharmaceutics, Krishna School of Pharmacy & Research, Pallavi Patel Global University, Drs. Kiran &Krishna Edu. Campus, Vadodara, 391240, Gujarat, India

    Meenakshi Patel

  3. Department of Pharmaceutics, Srinath College of Pharmacy, Bajaj Nagar, Aurangabad, 431136, Maharashtra, India

    Santosh Shelke

  4. Department of Pharmaceutics, Faculty of Pharmacy, Parul Institute of Pharmacy, Parul University, Vadodara, 391760, Gujarat, India

    Vandana Patel & Gajanan Shinde

  5. Department of Pharmaceutics, Government College of Pharmacy, Ratnagiri,, Opp Govt. Polytechnic, Ratnagiri, 415612, Maharashtra, India

    Inayat Pathan

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  1. Farhatjahan Shaikh
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Correspondence to Santosh Shelke.

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Shaikh, F., Patel, M., Shelke, S. et al. Formulation, Characterization, Optimization, and Pharmacokinetic Evaluation of Cilnidipine-Loaded Liquisolid Compacts with Improved Dissolution and Bioavailability. J Pharm Innov 18, 404–425 (2023). https://doi.org/10.1007/s12247-022-09651-z

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