Preparation and Evaluation of Tapentadol Hydrochloride Solid Lipid Nanoparticles

Abstract

Tapentadol Hydrochloride is a centrally acting opioid analgesic used for the treatment of musculoskeletal pain. The aim of the present study is to release the drug at a controlled rate by formulating solid lipid nanoparticles using Hot Homogenization method. In the present study SLN’s are prepared by using Glycerol Monostearate and Stearic acid as lipids and Poloxamer-188 as stabilizer in different ratios in order to get the optimized formulation. The solid lipids and drug were evaluated for drug interactions by using FTIR, DSC, and surface morphology by SEM in order to select the effective formulation. The prepared formulations (F1-F12) were evaluated for Particle size, Zeta potential, %Entrapment efficiency, in vitro drug release studies and stability studies. The FTIR spectra revealed that there is no significant interaction between the drug and lipids. SEM images revealed that the particles are spherical in shape with smooth surface. The particle size was found as 101.9 nm, Zeta potential was found as -18.1mV, % Entrapment Efficiency (%EE) was found as 88.7±0.36 and the % drug release was found as 97.8±0.60 in 10 hours following first order release kinetics and Higuchi model. The Tapentadol Hcl loaded SLN’s of F3 formulation shows more effective when compared to all the other formulations. All the results shows that the Tapentadol Hcl SLN’s can be effectively used for treating severe pain by controlling the rate of release at the targeted site.

Keywords: Tapentadol Hydrochloride, Glycerol Monostearate, Stearic acid, Poloxamer-188, Hot Homogenoisation method.