ABSTRACT
Curcumin is widely known for its antibacterial, antioxidant and anti inflammatory effects and has been reported to possess anticancerous activity as well. However, its medical application is limited because of poor bioavailability and rapid metabolism. In this study, we encapsulated curcumin in solid lipid nanoparticles and studied its anticancerous effect in Dalton’s Ascites Lymphoma (DAL) mice model. The physicochemical characteristics of curcumin solid lipid nanoparticles (CUR-SLN) were assessed and the anticancer efficacy was determined by in vivo studies. The curcumin solid lipid nanoparticles were synthesized by solvent emulsification evaporation method with particle size less than 100 nm. Antitumor effect of nanocurcumin (50 mg/kg) and curcumin (100 mg/kg) was evaluated in Dalton’s Ascites Lymphoma bearing mice. Pathological and immunohistochemical parameters were studied. Mean survival time and percentage increase in lifespan were assessed. Nanocurcumin group showed more significant influence in reducing tumor volume and weight, inducing apoptosis, reducing angiogenesis and invasion restoring antioxidant parameters and increased mean survival time. Curcumin and nanocurcumin inhibited the activation of nuclear factor-kappa B (Nf-kB), and thereby proved the pathway by which it induced anti-angiogenic and anti-invasive property.
ABSTRACT
Objective: To prepare naringenin-loaded solid lipid nanoparticles (NRG-SLN) lyophilized powder, and investigate its physicochemical properties and release characteristics, then to investigate the pharmacokinetic characteristics in rats after pulmonary delivery. Methods: NRG-SLN were prepared by solvent emulsification-evaporation method, the formulation was optimized by orthogonal design, with encapsulation efficiency as reference, and the measurements of particle size, morphology, Zeta potential, the polydispersity index (PDI) and in vitro drug release behavior were performed. To screen the best lyoprotectants in appearance, color, and redispersibility as indexes the differential scanning calorimetry (DSC) was used to analyze its material phase of the drug in nanoparticles. The study on pulmonary pharmacokinetics in rats was carried out by pulmonary instillation. Results: The NRG-SLN assumed a spherical shape with an even distribution of diameter and particle size of (97.69±2.84) nm, the PDI was 0.207±0.010, Zeta potential was (-26.20±0.45) mV, entrapment efficiency was (81.09±1.37)%, and drug loading was (8.30±0.04)% (n=3). Mannitol (5%) was the best protective agent for lyophilized powder of NRG-SLNs. The characterization indicated that the drug to amorphous state dispersed in a lipid. In vitro dissolution experiments showed NRG-SLN compared with pure drugs had obviously sustained release. After pulmonary administration to rats, the pharmacokinetic parameters of NRG-SLN and solution were as follows: Cmax (163.00±23.05) and (269.00±35.34) ng/mL, AUC0-t (929.32±190.28) and (3 390.23±533.68) ng∙h/mL, t1/2 (5.13±0.23) and (18.93±7.90) h, MRT (7.19±0.44) and (23.29±9.27) h. Conclusion: The technique of preparing NRG-SLN by solvent emulsification-evaporation has small particle size, high entrapment efficiency, and good stability, and the process is simple. Compared with the naringenin solution, the SLN show the sustained-release characteristics and can significantly improve the bioavailability after pulmonary administration.
ABSTRACT
Objective: To optimize the formulation of curcumin-catanionic nanoparticles lipid carriers (Cur-CNLC) by central composite design-response surface methodology (CCD-RSM). Methods: Cur-CNLC were prepared by film dispersion-ultrasonic emulsifying method. A four factor, five-level central composite design was employed, with the solid lipid quality (X1), liquid lipid quality (X2), lecithin quality (X3), and mixed surfactant concentration (X4) as the independent variables. The dependent variables were the entrapment efficiency (Y1) and drug loading (Y2). The data were simulated using multi-linear equation and second-order polynomial equation, the possibly optimal formulation was predicted by response surface method. Results: The entrapment efficiency, drug loading, average particle size, polydispersity, and Zeta potential of the Cur-CNLCs prepared under the optimized conditions were (94.38 ± 2.67)%, (6.93 ± 0.39)%, (235.9 ± 9.6) nm, 0.272 ± 0.017, and (-28.40 ± 0.35) mV, respectively. The bias between the measured values and the predicted ones is less than 5%. Conclusion: The CCD-RSM is effective and suitable for optimizing the formulation of Cur-CNLC.
ABSTRACT
Objective: To prepare lyophilized powder of baicalein solid lipid nanoparticles (BA-SLNs) and investigate its physicochemical properties and release characteristics. Methods: Ba-loaded SLN was prepared by solvent emulsification-evaporation method, the formulation was optimized by orthogonal design, with encapsulation efficiency (EE) as reference, the measurement of particle size, morphology, Zeta potential, the polydispersity index (PDI), and in vitro drug release behavior. The lyophilized powder of appearance, color, redispersibility as indexes, the differential scanning calorimetry (DSC), X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) were used to analyze its material phase of the drug in nanoparticles. Results: The Ba-SLNs assumed a spherical shape with an even distribution of diameter and particle size was (82.64 ± 6.78) nm, the PDI was 0.242 ± 0.013, Zeta potential was (-25.7 ± 0.5) mV, EE was (81.3 ± 1.2)%, and drug loading was (7.16 ± 0.14)% (n = 3). The 5% mannitol was the best protective agent for lyophilized powder of Ba-SLNs. Through the characterization indicated that the drug to amorphous state dispersed in a lipid. In vitro dissolution experiments showed Ba-SLNs compared with pure drugs had obviously sustained release. Conclusion: The technique of preparing Ba-SLN by solvent emulsification-evaporation has small particle size, high EE, and good stability, and the process is simple.