Characterization of Celecoxib-Loaded Solid Lipid Nanoparticles Formulated with Tristearin and Softisan 100

Ea Fouad,Hn Alajami,Aeb Yassin

doi:10.4314/tjpr.v14i2.3

Abstract

Purpose: To prepare solid lipid nanoparticles employing softisan 100 (SOFTI) or tristearin (TS) as solid lipid carriers for celecoxib (CXB) to overcome its dissolution challenge.Methods: The solid lipid nanoparticles (SLN) of CXB were prepared by ultrasonic melt-emulsification technique. SLN was characterized using differential scanning calorimetry (DSC), Fourier transform infra spectroscopy (FTIR), as well as for entrapment efficiency, particle size, zeta potential and CXB release.Results: The SLN formulations exhibited high CXB entrapment efficiency (91.6 % for SOFTI and 94.6 % for TS) while mean particle size was 181.0 ± 4.6 and 346.3 ± 3.8 nm for SOFTI and TS, respectively. The DSC thermograms showed the disappearance of CXB peak due to its molecular distribution in the lipid nanoparticles while FTIR spectra revealed physical interaction of CXB with the tested lipids. The tendency of SOFTI to liberate CXB in 24 h was higher than that of TS (55.5 ± 1.07 vs 49.2 ± 2.94 %, p < 0.05). Drug release was by non-Fickian mechanism.Conclusion: Formulation of CXB in SLN using TS or SOFTI produces sustained drug release delivery that can overcome the dissolution limitation of the drug and thus, improve its therapeutic efficacy.Keywords: Celecoxib, Solid lipid nanoparticles, Tristearin, Softisan, Dissolution limitation, Sustained drug release

Highlights

Celecoxib (CXB) is a nonsteroidal antiinflammatory drug used for the treatment of osteoarthritis and rheumatoid arthritis
The mean physical parameters of the prepared solid lipid nanoparticles (SLN) containing CXB showed some differences between softisan 100 (SOFTI) and TS, The recorded mean particle size was significantly different (p < 0.05) with 181.0 ± 4.6 and 346.3 ± 3.8 nm for SOFTI and TS, respectively
These results reflect the effect of lipid structure on the prepared SLN, where TS is a mono acid (C18) triglyceride; SOFTI is a mixture of glycerides (C10C18)

Summary

Introduction

Celecoxib (CXB) is a nonsteroidal antiinflammatory drug used for the treatment of osteoarthritis and rheumatoid arthritis. It is a selective inhibitor for cyclooxygenase-2 (Cox-2), that is expressed during inflammation [1,2]. CXB does not cause gastropathy or GI bleeding [1]. CXB has a chemopreventive activity toward colon cancer [2], skin cancer induced by UV light [3] and breast cancer [4]. CXB has a half-life of 21 h with poor oral bioavailability of about 22-40 % from capsule formulations. The poor oral bioavailability of CXB was attributed to its poor solubility and poor dissolution rate [5]

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