Abstract
The aim of this study was to determine the effect of lipid ratio of stearic acid and oleic acid on the physical characteristics as well as the entrapment efficiency of diethylammonium diclofenac with Nanostructure Lipid Carrier (NLC) system. Diethylammonium diclofenac (DETA) is Non-Steroid Anti-Inflamatory Drugs (NSAIDs) that has been widely used in the treatment of osteoarthritis and rheumatoid arthritis. In the formulation of NLC-DETA, three different lipid ratios were used, which the ratio of stearic acid:oleic acid were 60:40, 70:30, and 80:20, respectively. In this NLC system, DETA served as the active drug, stearic acid as solid lipid, oleic acid as liquid lipid, and Tween 80 as surfactant components. NLC were characterized for organoleptic characteristics, pH, viscosity, particle morphology, particle size and polydispersity index (PI), profiles of Fourier Transform Infra-Red (FTIR) and Differential Thermal Analysis (DTA), and drug entrapment efficiency. The particle shape and morphology were determined by Transmission Electron Microscopy (TEM). The results showed that the different ratios of oleic acid lipids and stearic acid had no significant effects on the viscosity and entrapment efficiency of NLC-DETA. On the other hand, it affected the pH of all formulas, which were significantly different. Increasing the amount of liquid lipid in the formulations reduced the size of NLC-DETA particles.
Highlights
Non-Steroid Anti-Inflamatory Drugs (NSAIDs) can be classified based on the drug’s selectivity to inhibit cyclooxygenase (COX) enzymes
It can be concluded that the different ratios of oleic acid and stearic acid, which were 60:40, 70:30, 80:20, respectively, did not affect the sample viscosity
For samples particle size and Polydispersity Index (PDI), the differences were occurred for formula with lipid ratio of 80:20 to 60:40 and 70:30
Summary
Non-Steroid Anti-Inflamatory Drugs (NSAIDs) can be classified based on the drug’s selectivity to inhibit cyclooxygenase (COX) enzymes. The ion pair formation between anions and cations of alkilamonium diclofenac may increase skin permeability and drug solubility in non-aqueous carrier (Fini et al, 2012). An analgesic such as DETA is intended to give rapid and long term effect. Other study reported that the meloxicamloaded NLC (MLX) was used for topical application using monostearin and alpha-tocopherol as lipid matrix These lipids was combined at six different ratios of solid and liquid lipid matrix, which were 70:30, 75:25, 80:20, 85:15, 90:10, and 95:5, respectively. We further evaluated which lipid ratio that was able to produce good characterization and entrapment efficiency of DETA-NLC
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