Formulation and Evaluation of Solid Lipid Nanoparticle (SLN) Based Topical Gel of Etoricoxib

Roohi Kesharwani,Swati Singh,Dilip Patel,Anupam Sachan

doi:10.7324/japs.2016.601017

Abstract

The objective of present investigation was to prepare & evaluate solid lipid nanoparticle (SLN) based topical gel of non- steroidal anti-inflammatory drug (NSAID) etoricoxib for the treatment of arthritis which would attenuate the gastrointestinal related toxicities associated with oral administration. SLN were formulated by melt emulsification and solidification at low temperature method using stearic acid & tween 80. All the formulation were subjected to particle size, particle size distribution, zeta potential, scanning electron microscopy, crystallinity study by DSC and in-vitro release studies. It has been observed that, the high lipid concentration containing formulation have higher entrapment as compare to other two formulation. The SLN- dispersion shows 70.766% entrapment & zeta potential of the formulation were -25.6 which indicates the stability of formulation. The in vitro drug release rate of gel was evaluated using Modified franz diffusion cell containing dialysis membrane with phosphate buffer pH 7.4 as the receptor medium. The in-vitro release was carried out in comparison with a carbopol gel & hydroxypropylmethylcellulose (HPMC) gel. The permeability parameters steady-state flux (Jss) was significantly increased in SLN-F3C (carbopol) formulation as compared with SLN-F3HPMC (hydroxypropyl methylcellulose) formulation. It was concluded that the Etoricoxib loaded SLN based gel formulation containing carbopol was suitable for topical application and shows much better result of anti-inflammatory activity.

Highlights

Etoricoxib is a COX-2 selective inhibitor which selectively inhibits isoform 2 of the enzyme cyclooxygenase (COX-2) which reduces the generation of prostaglandins (PGs) from arachidonic acid (Takemoto et al, 2008)
The objective of present investigation was to prepare & evaluate solid lipid nanoparticle (SLN) based topical gel of non- steroidal anti-inflammatory drug (NSAID) etoricoxib for the treatment of arthritis which would attenuate the gastrointestinal related toxicities associated with oral administration
Etoricoxib was received as a gift sample from Unison Pharmaceuticals, Baddi, INDIA, Carbopol 934, HPMC were kindly provided by Guapha Pharmaceuticals, M.P., INDIA, Stearic acid, Isopropyl Myristate, Tween 80 & Glycerol were purchased from Fizmerk Chemicals, U.P., INDIA, Dialysis membrane was purchased from Hi Media Laboratories Pvt

Summary

Introduction

Etoricoxib is a COX-2 selective inhibitor which selectively inhibits isoform 2 of the enzyme cyclooxygenase (COX-2) which reduces the generation of prostaglandins (PGs) from arachidonic acid (Takemoto et al, 2008) It is a potent analgesic, antipyretic and anti-inflammatory agent has been approved for significantly reduces joint inflammation, pain intensity and the duration of morning stiffness and improved handgrip strength (Gonzalez et al, 1994). Solid lipid nanoparticles (SLN) introduced in 1991 represent an alternative carrier system to tradition colloidal carriers such as emulsions, liposomes and polymeric micro and nanoparticles. Nanoparticles made from solid lipids are attracting major attention as novel colloidal drug carrier for intravenous applications as they have been proposed as an alternative particulate carrier system. SLN offer unique properties such as small size, large surface area, high drug loading and the interaction of phases at the interface and are attractive for their potential to improve performance of pharmaceuticals (Ekambaram et al, 2012)

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Results

Conclusion