International Journal of Drug Delivery Technology
Volume 14, Issue 3

Design, Formulation, and Optimization of Nicardipine-Loaded Gastroretentive Floating Microspheres: In-vitro, Ex-vivo and In-vivo Characterization

Sepuri Vijayalaxmi1*, Abbaraju Krishna Sailaja2

1University College of Technology, Department of Pharmaceutics, Osmania University, Hyderabad, Telangana, India.

2Department of Pharmaceutics, RBVRR Women’s College of Pharmacy, Osmania University, Hyderabad, India. 

Received: 07th March, 2024; Revised: 04th May, 2024; Accepted: 15thJuly, 2024; Available Online: 25th September, 2024 

ABSTRACT

Nicardipine hydrochloride is highly soluble at low pH values. The objective of this investigation was to design, manufacture, and refine the drug’s floating microspheres to increase its bioavailability and prolong its period of residence in the gastrointestinal tract. To optimize the Box-Behken and prepare the floating microspheres, solvent evaporation was employed. The formulation F5 was discovered to be the best as anticipated by the design expert software’s point prediction. Evaluations of pre- and post- compressional parameters were conducted. Utilizing several kinetic models, the drug release pathways were examined. The drugs and excipients did not interact, according to the FTIR/DSC investigations. According to the radiological approach, F5 showed good in-vitro buoyancy. The gastroretentive property of microspheres is revealed by X-ray pictures obtained at 2, 8, and 12 hours for the buoyancy investigation. F5 (235.04%) demonstrated a high relative bioavailability over oral tablets, according to the in-vivo pharmacokinetic investigation. In comparison to the marketed formulation group, the F5-treated group experienced a considerably larger percent decline in BP values (20.00 ± 6.00 and 13.00 ± 4.00%, respectively) at 36 and 48 hours of the in-vivo pharmacodynamic testing. For 90 days, the F5 formulation was maintained at 5 ± 2 and 25 ± 2°C, indicating the stability of nicardipine microspheres.

Keywords: Nicardipine, Optimization, Floating Microspheres, Ethylcellulose, Experiment design. International Journal of Drug Delivery Technology (2024); DOI: 10.25258/ijddt.14.3.57

How to cite this article: Vijayalaxmi S, Sailaja AK. Design, Formulation, and Optimization of Nicardipine-Loaded Gastroretentive Floating Microspheres: In-vitro, Ex-vivo and In-vivo Characterization. International Journal of Drug Delivery Technology. 2024;14(3):1652-1660.

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