Abstract
Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.
Highlights
Statins are classified according to their solubility into lipophilic such as atorvastatin, lovastatin and simvastatin or hydrophilic-like pravastatin and fluvastatin
We study the effect of encapsulating atorvastatin calcium (At-Ca) into PLGA NPs and compare it with free At-Ca and placebo NPs
The influences of these two independent factors were screened on the mean particle size, polydispersity index (PDI), zeta potential, entrapment efficiency and In vitro release pattern of At-Ca NPs
Summary
Statins are classified according to their solubility into lipophilic such as atorvastatin, lovastatin and simvastatin or hydrophilic-like pravastatin and fluvastatin. They are divided into two generations depending on their originality: naturally occurring (simvastatin and pravastatin) or chemically synthetized (e.g., atorvastatin and rosuvastatin) agents. L-mevalonate pathway has several biofunctions beside cholesterol production, e.g., enhancing cellular proliferation and migration, controlling formation of myelin sheath and dynamicity of filamentous network of cellular proteins. This ensures that statins have some auxiliary pharmacological effects known as “pleiotropic effects” [2]
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