Synthesis of PVA capped naproxen conjugated MgO nanoparticles and its bioactivity screening

The prescribed use of non-steroidal anti-inflammatory drugs is associated with numerous life-threatening side effects. There is a great need to develop low-dose NSAID formulations to prevent the rate of adverse events while retaining the therapeutic efficacy. In this context, we prepared nanoformulated naproxen using MgO as a nanocarrier and PVA as coating agent and investigated its biological activity in comparison to free form naproxen sodium (NPRS) and standard anti-inflammatory drugs. MgO nanoparticles with a hydrodynamic size of approximately 140–484 nm were prepared and conjugated with NPRS and capped with hydrophilic polymer (PVA) successfully. Conjugation of NPRS with MgO nanoparticles was confirmed by UV–Visible, FTIR, XRD, DLS, LIBS techniques. The hydrodynamic size and surface charge of nanoformulated naproxen were found to be 161 nm and −8.85 mV, respectively. Nanoformulated naproxen showed maximal and sustained release (>95%) at pH 6.8 within 24 h. Investigation of thermal attributes showed that the nanoformulated naproxen was more stable at a higher temperature than free NPRS. In vivo anti-inflammatory, analgesic, and antipyretic activities of nanoformulated naproxen revealed that in all cases, the potency and efficacy of nanoformulated naproxen were found to be higher than NPRS. Moreover, nanoformulated naproxen was well tolerated up to 2000 mg/kg b.w with an LD50 of 2574.77 mg/kg. The ratio between the minimum effective dose (1 mg/kg) and LD50 indicated a broader therapeutic window. Since the concentration of NPRS in nanoformulated naproxen was only 43.2 ± 2%, our results indicated that conjugation to MgO nanocarrier boosts the biological activity of NPRS by approximately 2.3 times. In addition, nanoformulated naproxen is found to be biocompatible and hemocompatible. We conclude that the nanosizing of a drug offer much promise as a better alternative to standard anti-inflammatory drugs for the treatment of various diseases. [Display omitted]