Synthesis and in vitro evaluation of melatonin entrapped PLA nanoparticles: An oxidative stress and T‐cell response using golden hamster

Abstract

This study was carried out to evaluate the effects of melatonin entrapped PLA nanoparticles (Mel-NPs) and pure Mel on impact of reactive oxygen species (ROS), blastogenic responses (%SR) in terms of proliferation of splenocytes. ROS have been proposed to play an important role in balancing the pro- and antioxidant homeostasis during different physiological condition of organism. Melatonin has been suggested as an effective free radical scavenger that may have an important role during this process. Mel-NPs were prepared by using emulsification (o/w) nanoprecipitation method and their physicochemical characterizations were studied for evaluation of particle size and encapsulation efficiency by using SEM, TEM, particle size analyzer, DSC and FTIR. The TEM micrograph showed excellent findings regarding size, shape, encapsulation efficiency and difference between pure PLA nanoparticles and Mel-NPs. The SEM micrographs of Mel-NPs showed spherical shape, smooth surfaces and the homogeneous particle size distribution. In TEM micrograph, the average diameter of Mel-NPs was found to be 36 ± 8 nm with ∼78% (w/w) of entrapment efficiency. The size of pure PLA nanoparticles was found to be larger as compared to Mel-NPs which confirm that the drug supports the reduction of the size of Mel-NPs. In in vitro study, we observed that Mel-NPs significantly reduce the level of ROS in splenocytes and increased the level %SR at 96 h of splenocytes culture as compared to the culture with pure Mel. Thus our results propose high clinical value for improvement of depressed immunity by Mel-NPs.

Application of a validated HPLC-PDA method for the determination of melatonin content and its release from poly(lactic acid) nanoparticles

“…Recently, other authors have also obtained PLGA nanoparticles containing MLT and the drug quantitation was carried out by spectrophotometry at 279 nm [38] . In another work, PLA nanoparticles as MLT carriers were obtained by a nanoprecipitation method and the encapsulation efficiency as well as MLT release profile were assessed by UV-spectrophotometry [37] . However, considering the sensitivity, in some situations spectrophotometric methods are not so convenient as HPLC methods.…”

“…Analytical determination of MLT in pharmaceutical formulations is also limited [32] , [33] , [34] . It has been cited for spectrophotometric analysis for evaluation of MLT in nanoparticles [35] , [36] , [37] , [38] . However, the higher sensitivity of the HPLC method over UV-spectrophotometry is important for the determination of the drug release profile from nanoparticles, since the amount of drug released over the time is low.…”

PolyRad – Protection Against Free Radical Damage

“…∞ is the fractional drug release at time t, τ is the lag time, b is the fractional drug burst release, k is a kinetic constant that measures the drug release rate characteristic of the drug/polymer system, and n is the release exponent which characterizes the drug release mechanism [52][53][54][55][56][57][58] .…”

Melatonin-Loaded Nanocarriers: New Horizons for Therapeutic Applications

“…The effect of pure melatonin was compared with melatonin entrapped PLA NPs on the reactive oxygen species (ROS), and blastogenic responses in the proliferation of splenocytes obtained from adult golden hamster [127]. The melatonin-loaded PLA NPs was generated by emulsification/nanoprecipitation method, and their physicochemical properties showed good results regarding shape, size, EE (diameter of 36 ± 8 nm with ~78% entrapment efficiency), smooth surfaces, and homogeneous distribution of particle size.…”