Lipid carriers for delivery of celecoxib: In vitro, in vivo assessment of nanomedicine in rheumatoid arthritis

Abstract

Celecoxib loaded tristearin lipid nanoparticles (CEL‐TS‐LN) formulation was prepared by micro emulsion technique. The prepared CEL‐TS‐LN formulations were characterized by photon correlation spectroscopy (PCS), Zeta potential, transmission electron microscopy (TEM), in vitro release kinetics, In vivo toxicity and pharmacokinetics; and Freund's adjuvant‐induced arthritic studies were conducted. The mean diameter of the CEL‐TS‐LN was about 188 nm; the particles had spherical morphology and an amorphous nature. In vitro drug release study of CEL‐TS‐LN revealed sustained drug release of 62% for 36 hrs; and the drug release was found to follow zero order and Fickian diffusion mechanism. The biochemical and haematology reports of in vivo toxicity studies revealed that CEL‐TS‐LN does not exhibit any toxic symptoms on vital organs and could be safe. With 88% percent inhibition of edema, serum biochemical parameters of CEL‐TS‐LN treated animal groups showed significant difference (p < 0.05) compared to arthritic control (without treatment). In conclusion, the results clearly suggested that CEL‐TS‐LN facilitated sustained release enhanced bioavailability and improved therapeutic efficiency of the encapsulated celecoxib drug.Practical applications: In this paper we stress the importance of solid lipid nanoparticles for oral delivery. We also discuss the feasibility of large scale production of celecoxib loaded tristearin lipid nanoparticles (CEL‐TS‐LN) by micro emulsion technique for industrial application. Celecoxib (CEL) has been recommended as oral use for the treatment of rheumatoid arthritis (RA). Low oral bioavailability and long term oral administration of CEL produces severe gastrointestinal side effects. CEL‐TS‐LN holds promise for safe, improved bioavailability and enhanced therapeutic efficiency in the treatment of RA.Successfully incorporated celecoxib into tristearin solid lipid Nanoparticles (CEL‐TS‐LN).The optimized CEL‐TS‐LN preparation was exhibited spherical morphology, amorphous nature, maximum entrapment efficiency and sustained release of celecoxib. CEL‐TS‐LN does not exhibit any toxic symptoms, enhanced bioavailability and therapeutic efficiency in In Vivo.