Oxaprozin-Loaded Lipid Nanoparticles towards Overcoming NSAIDs Side-Effects

Abstract

The inflammatory process is the innate immune response for the presence of pathogens, toxic molecules, tissue injuries or any other harmful conditions. The inflammation process is characterized for redness, pain, swelling, heat and disturbance of function and comprises inducers, sensors, mediators and effectors components from cellular and humoral origin.

Applying nanotechnology to increase the rumen protection of amino acids in dairy cows

“…characterization of nanoparticle formulations. Three types of lipid nanoparticles were produced in this study: solid lipid nanoparticles (SLN) -NP composed of lipids that are solid at body temperature 35 , nanostructured lipid carriers (NLC) -NP composed of a mixture of lipids that are solid and liquid at body temperature 36 and multiple lipid nanoparticles (MLN) -NP composed of a mixture of solid and liquid lipids that contain large water vacuoles 37 . NP formulations with all the proposed lipid and surfactant combinations were produced, except when using poly(vinyl) alcohol, where the formulations solidified and were thus discarded.…”

“…2B,C) might be explained by the presence of liquid lipids in their lipid matrix, specifically Miglyol 812. The use of both liquid and solid lipids decreases the crystallinity of the lipid matrix and potentially increases substance entrapment while reducing expulsion due to a shift in the lipid form 36 . However, the ruminal conditions appear to destabilize the liquid-solid lipid matrix, exposing it to microbial digestion.…”

“…production of nanoparticle formulations. Three types of lipid nanoparticles were produced using an organic solvent-free emulsification-sonication method: SLN 35 , NLC 36 and MLN 37 . The proposed nanoparticles were selected for their properties.…”

“…The higher values observed for the NLC than the SLN might be attributed to the presence of liquid lipids in the NP matrix that confers a less crystalline structure with more cavities and defects in which the encapsulated molecules can be trapped 52,53 . This structure may also reduce the effects of shifts in lipids (changes that occur in the lipid structure over time and lead to a more stable polymorphic structure) that may cause the encapsulated molecules to be expelled 36 . SLN are composed of only solid lipids and form a crystalline structure of hydrophobic molecules, resulting in fewer locations for molecule entrapment 53 and thus a lower %Lys.…”

Oxaprozin prodrug as safer nonsteroidal anti‐inflammatory drug: Synthesis and pharmacological evaluation

“…On another hand, chronic oral use of oxaprozin potentially leads to GI perforation owing local irritation of the carboxylic acid group and ion trapping mechanism from the lumen to mucosa . Due to inappropriate masking of the carboxylic acid group of NSAID moieties, many attempts were not successful in overcoming the NSAID based GI complications …”