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Appraisal of Felodipine nanocrystals for solubility enhancement and pharmacodynamic parameters on cadmium chloride induced hypertension in rats.

Author(s):

Priyanka Maurya, Pawan Pandey, Samipta Singh, Alka Sonkar, Sonali Singh and Shubhini Saraf*  

Abstract:


Background and Objective: Felodipine (FDP), an antihypertensive drug possesses low water solubility and extensive first-pass metabolism leading to poor bioavailability. This impelled us to improve its solubility, bioavailability, and pharmacodynamic properties through the nanocrystal (NC) approach.

Methods: FDP-NC were prepared with Poloxamer F125 (PXM) by the antisolvent precipitation method. The experimental setup aimed at fine-tuning polymer concentration, the proportion of antisolvent to solvent, and the duration of ultrasonication for NC formulation.

Results: Optimized formulation was characterized for particle size, solubility, and PDI. Particle reduction of 74.96 times was achieved with a 9X solubility enhancement as equated to pure FDP. The morphology of NC was found to be crystalline through scanning electron microscopy observation. The formation of the crystal lattice in FDP-NC was further substantiated by the XRD and DSC results. Lowering of the heat of fusion of FDP-NC is a clear indication of size reduction. The stability studies showed no substantial change in physical parameters of the FDP-NC as assessed by particle size, zeta potential, and drug content.

Conclusion: The crystalline nature and improved solubility of FDP-NC improve the dissolution profile and pharmacodynamic data. The stability study data ensures that FDP-NC can be safely stored at 25℃. It is revealed that FDP-NC had a better release profile and improved pharmacodynamic effects as evident from better control over heart rate than FDP.

Keywords:

Antisolvent precipitation; Cadmium chloride; Felodipine; Heart rate variability; Heat of fusion, Crystallinity

Affiliation:

Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P. , Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P. , Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P. , Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P. , Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P. , Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, U.P.



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