Abstract
Purpose: To design, formulate and characterize sustained-release formulations of dexketoprofen trometamol (DT) nanoparticles (NPs)Methods: Dexketoprofen trometamol (DT)-loaded poly(lactic-co-glycolic acid) (PLGA) NPs were produced by double emulsion-solvent evaporation method. The NPs were variously characterized for drug loading and release, particle profile, as well as by thermal analysis, x-ray difraction (XRD), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance analysis (1H-NMR). Furthermore, the NPs were evaluated for cytotoxicity against NIH-3T3 cells by 3-(4,5-dimethylthiazol-2- Yl)-2,5-diphenyltetrazolium bromide (MTT) assay.Results: The DT-loaded NPs demonstrated nanostructural characteristics and extended drug release. Particle size was in the range of 243 and 295 nm which remained unchanged in drug stability testing in simulated gastrointestinal media. Encapsulation efficiency ranged from 49 – 64 % for all the formulations. Higuchi and Korsmeyer-Peppas were the best-fit release kinetic models for the NPs containing 5 and 10 % DT, respectively. The NPs with 10 % DT presented no significant cytotoxicty at the doses and periods studied.Conclusion: Stable and non-toxic DT NPs with potential for sustained and controlled release of the drug have been successfully developed.Keywords: Dexketoprofen trometamol, Poly-lactic-co-glycolic acid (PLGA), Nanoparticles, Release kinetics, Stability
Highlights
The ability to manage and treat pain continues to be one of the most common clinical objectives of practitioners
The poly(lactic-co-glycolic acid) (PLGA) NPs were subjected to NMR analysis (1H-NMR)
All data obtained from six independent experiments were expressed as the mean diameter and standard deviation (SD) values
Summary
The ability to manage and treat pain continues to be one of the most common clinical objectives of practitioners. Pain has a very important effect on the biological, psychological, sociological and economic dispositions of a patient [1]. Nonsteroidal anti-inflammatory drugs (NSAIDs), skeletal muscle relaxants and opioid analgesics are among the most prescribed drugs for pain [2]. The NSAIDs block a group of physiological proteins called cyclooxygenase (COX) which are invoved in the production of prostaglandins and thromboxanes responsible for pain and inflammation [3]. Ketoprofen, a member of the arylpropionate group of NSAIDs has well-defined analgesic and anti-inflammatory effects. Racemic ketoprofen is used as an analgesic and anti-inflammatory agent, and it is one of the most potent inhibitors of prostaglandin synthesis in vitro [4]. İt is a rapidlyacting analgesic agent in the treatment of painful musculoskeletal disorders such as back pain and osteoarthritis [5]
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