A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

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.

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

“…After fabrication of PLGA NSs loaded with GPS, there is no major shift in the characteristic peaks for all the constitutes of nanospheres ( Figure 5 ). FTIR spectrum of GPS-PLGA NSs displays peaks at 3425, 2998–2954-2854, 1758, 1168, and 1092 cm −1 for stretching of O-H, C-H, C=O, =C-O and C-O-C respectively and at 1457- 1397 - 1275 cm −1 for C-H bending lying at similar positions of PLGA peaks previously demonstrated in detail by Abdelkader et al 18 As it is shown in Figure 5 , the reduced peak intensity of O-H stretching at 3425 cm −1 after loading GPS might be attributed to partial adsorption of GPS molecules on PLGA surface. 42 Generally, some of the characteristic peaks of GPS summarized in Table 4 might be masked by the PLGA spectrum after encapsulation into its matrix.…”

“…PLGA is considered the most powerful factor significantly affecting the physical properties of GPS NSs including particle size and zeta potential in addition to % EE. 18 , 41 The higher viscosity of the internal phase at greater PLGA concentration provides more intact oil globules tightly entrapped GPS molecules preventing their diffusion out to the external aqueous phase 11 that produces GPS-PLGA NSs with significantly higher %EE ( Table 3 ). Generally, PLGA contents have a crucial effect on the total amount of GPS encapsulated into formulated NSs.…”

“…GPS-loaded PLGA NSs were prepared using the single emulsion solvent evaporation method as previously mentioned. 11 , 18 As demonstrated in Table 1 , different concentrations of PLGA (% w/v) dissolved in DCM were added to DMF containing GPS (60 mg). The organic phase with a volume ratio of DCM (1): DMF (1) was then vortexed for 1 minute to ensure complete homogeneity.…”

“…All in vitro release runs were performed in triplicate and the total percent cumulative release was expressed as a mean +SD. 18 …”

Targeting Cancer Cell Tight Junctions Enhances PLGA-Based Photothermal Sensitizers’ Performance In Vitro and In Vivo

“…Nanoparticles of poly-lactide-co-glycolide (PLGA) loaded with magnesium phthalocyanine were synthesized by the microemulsion "oil-in-water" method. The use of PLGA as a drug carrier, attracts the attention of researchers in modern biomedicine, since it provides a stable and controlled release of the compound, thereby reducing side effects [16][17][18][19][20]. PLGA degrades by hydrolysis of its ester linkages in the presence of water and the by-products, lactic acid and glycolic acid, are non-toxic, biocompatible, and rapidly metabolized in the human body.…”