FORMULATION AND EVALUATION OF CLOPIDOGREL BISULFATE CAPSULE LOADED NANOPARTICLESAbstract
The present study aims to formulate and evaluate clopidogrel bisulfate capsule-loaded nanoparticles. Clopidogrel bisulfate nanoparticles were produced by the nano-precipitation method and emulsification solvent evaporation method using ethylcellulose polymer at different ratios and characterized for particle size drug entrapment efficiency dissolution testing scanning electron microscopy imaging (SEM) and compatibility studies (Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Optimized nanoparticles were filled into capsules with different concentrations of HPMC 4 KM and further evaluated. The prepared nanoparticles characterized and found to be the particle size was ranged from 100-2500 nm, and entrapment efficiency was ranged from 23.88 ± 0.20 % to 90.53 ± 0.31%. Amongst all formulations, F6 and F10 were considered for further optimization showed dissolution 53.20 ± 0.27 and 39.87 ± 0.12 % at the end of the first hour with entrapment efficiency 70% and 79%, respectively. SEM of clopidogrel bisulfate nanoparticles confirmed small particles without aggregation. The particle size of F6 and F10 obtained was 287.6 and 349.8 nm, respectively. Compatibility studies revealed that there is no chemical interaction between clopidogrel and excipients. The Poly-dispersity index narrowed down to 0.1-0.3. The Zeta potential of F6 and F10 were -40.4 mV and -37.8 mV, respectively. Nanoparticles containing capsules CF62 and CF102 showed floating time up to 12 h with drug release of 99.57 % and 97.052 %, respectively, and within the range of weight variation. Stability studies revealed prepared formulation is stable. The emulsification-solvent evaporation method was considered as an effective method for the preparation of nanoparticles due to its sustainability property and optimized in the form of capsules formulation.
Razia Sultana, Latha Kukati *, Naseeb Basha Shaik and Shailaja Thoudoju
Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Telangana, India.
14 December 2020
25 March 2021
01 October 2021
01 November 2021