Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System of Clofazimine

RGUHS Journal of Pharmaceutical Sciences

article

Umeshkumar D Patel¹  Amolkumar A Kempwade¹  Vrushabh S Patil¹  Ravindra D Hiremath² 

[1] Department of Pharmaceutics, KLE College of Pharmacy;Department of Pharmaceutical Chemistry, KLE College of Pharmacy

关键词: SNEDDS;    Formulation;    Optimization;    Evaluation;    Clofazimine;    Oral.;   

DOI  :  10.26463/rjps.12_3_6

学科分类：药学、药理学、毒理学（综合）

来源: Rajiv Gandhi University of Health Sciences

【 摘 要 】

Aim: The present study aimed to formulate and evaluate Self-Nanoemulsifying Drug Delivery System (SNEDDS) for poorly water-soluble clofazimine.Methodology: Ethyl Acetate, Captex-300, and polyethylene glycol 400 (PEG-400) were utilized for the development of SNEDDS of clofazimine. Optimization of SNEDDS was carried out using 32 factorial design. Evaluation parameters such as dilution study by visual observation, self-emulsification time, percentage transmission, zeta potential, particle size, and polydispersity index (PDI) were performed for formulated SNEDDS. Formulated SNEDDS batches were studied for dissolution and stability.Results: The particle size of the formulation ranged between 288.9–918.2 nm. Zeta potential was found within the range of -1.10 to -8.25 which indicated the stability of the emulsion. Self-emulsification time of clofazimine formulations was found to be less than 1 min which confirmed its efficiency. Percentage transmission was seen at around 100% which confirmed the clarity and transparency of the nanoemulsion formulation. Dissolution of clofazimine from SNEEDS was very fast and achieved approximately 100% dissolution in 1 hour as that of the pure drug (<15%). Further stability study confirmed the stability of formulated SNEDDS.Conclusion: Present study demonstrated a systematic approach for the development of SNEDDS which can be very useful for delivering the drug orally for many emerging hydrophobic drugs with good therapeutic potential. Aim: The present study aimed to formulate and evaluate Self-Nanoemulsifying Drug Delivery System (SNEDDS) for poorly water-soluble clofazimine.Methodology: Ethyl Acetate, Captex-300, and polyethylene glycol 400 (PEG-400) were utilized for the development of SNEDDS of clofazimine. Optimization of SNEDDS was carried out using 32 factorial design. Evaluation parameters such as dilution study by visual observation, self-emulsification time, percentage transmission, zeta potential, particle size, and polydispersity index (PDI) were performed for formulated SNEDDS. Formulated SNEDDS batches were studied for dissolution and stability.Results: The particle size of the formulation ranged between 288.9–918.2 nm. Zeta potential was found within the range of -1.10 to -8.25 which indicated the stability of the emulsion. Self-emulsification time of clofazimine formulations was found to be less than 1 min which confirmed its efficiency. Percentage transmission was seen at around 100% which confirmed the clarity and transparency of the nanoemulsion formulation. Dissolution of clofazimine from SNEEDS was very fast and achieved approximately 100% dissolution in 1 hour as that of the pure drug (<15%). Further stability study confirmed the stability of formulated SNEDDS.Conclusion: Present study demonstrated a systematic approach for the development of SNEDDS which can be very useful for delivering the drug orally for many emerging hydrophobic drugs with good therapeutic potential.

【 授权许可】

CC BY