Effect of Selected Polymers on Dissolution and Stabilization of Amorphous Form of Meloxicam

Abstract

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release. Conclusion:The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

Characterization of Novel Solid Dispersions of Moringa oleifera Leaf Powder Using Thermo-Analytical Techniques

“…The strong peaks suggest that the carrier is semi-crystalline or partially amorphous in structure. These results are in agreement with previous studies for PEG4000 (19.35° and 23.5° reported by Vasa et al [31] and Obaidat et al [32]. PEG6000 diffractogram exhibited two major, highly intense and defined diffraction peaks at 2𝜃 values of 19.29°, 23.65° and a few minor peaks at 2𝜃 = 15.37°, 22.32°, 26.16°, 27.38°, 28.85° and 36.59°, which are consistent with the data in previous reports (19.12° and 23.23°) [33], suggesting that PEG6000 is also semi-crystalline or partially amorphous.…”

Loading and evaluation of meloxicam and atorvastatin in carrageenan microspherical aerogels particles

“…De-aggregation of meloxicam and physical entrapment of the drug physically in the pores of the particle can be used to explain such results as previously reported by Obaidat et al (2017).…”

“…Aerogels can be produced from inorganic, organic, or organic-inorganic precursors, which gave them a flexible surface chemistry and allow them to be used in huge number of applications such as insulation, food technology, catalysis, environmental, and life sciences applications (Gurikov and Smirnova, 2017;Maleki, 2016;Maleki and Hüsing, 2018;Stergar and Maver, 2016;Ulker and Erkey, 2014). Being renewable, abundant, biodegradable, and biocompatible, polysaccharide-based aerogels have attracted increasingly attention in the field of tissue engineering and drug delivery (Barros et al, 2016;García-González et al, 2011;Martins et al, 2015;Obaidat et al, 2018).…”

Biocompatible Luminescent Nanosized Curcumin: Verified Parameters Affecting Stability and Bioavailability

“…Increasing the molecular weight of the stabilizer would increase its flexibility and elasticity, which in turn improves the ability of the stabilizer to surround and make a full inclusion of the newly synthesized curcumin nanoparticles inside it [26]. On the other hand, if the polymer length is too short, the nanoparticles would not be covered with the polymer layer completely, leading to their agglomeration.…”