Abstract
The purpose of this study is to design a flower-shaped lactose loaded curcumin solid lipid nanoparticles dry powder inhaler and characterize it to improve the solubility and dissolution rate of curcumin in lung. Curcumin solid lipid nanoparticles (Cur-SLNs) were prepared by solvent evaporation method, and then they were micronized by freeze-drying technology. Finally, Cur-SLN micropowder obtained by freeze-drying was mixed with flower-shaped lactose (FL) at a ratio of 2 : 1 and then passed through a 200-mesh sieve to obtain Cur-SLN-FL powder. Tween-80 was selected as the surfactant to inhibit the aggregation of drug solid lipid nanoparticles. Under the optimum conditions, the solid lipid nanoparticles (SLN) were relatively spherical, with an average particle size of 14.7 nm, narrow distribution, Zeta potential of −22.5 mV, encapsulation efficiency of 90.21%, and drug loading of 8.56%. According to the particle size, PI, Zeta potential, drug loading (LC%), encapsulation efficiency (EE%), morphology, and in vitro release characteristics, the prescription of solid lipid nanoparticles was screened. Dry powder inhaler (DPI) was characterized by differential scanning calorimetry, scanning electron microscopy, particle size, density, and in vitro release performance. Its cytotoxicity to mouse fibroblasts (L929) and human normal lung epithelial cells (BEAS-2B) in vitro was investigated, and its safety for pulmonary inhalation was preliminarily determined. FTIR analysis shows that the micronized Cur-SLN-FL has the same chemical structure as FL. FTIR and DSC analysis confirmed that the characteristic absorption peak of curcumin was not found in Cur-SLN-FL, showing similar structure to SLN and FL. In addition, curcumin was coated in solid lipid nanoparticles to make powder mist, which increased its drug loading, kept its aerodynamic particle size (4.03 ± 0.40) μm, and significantly improved its drug release performance in artificial lung fluid. In vitro cytotoxicity test results confirmed that Cur-SLN-FL was less toxic to BEAS-2B cells than L929 cells. Therefore, curcumin was prepared into solid lipid nanoparticles by emulsion evaporation-low temperature solidification method and then micronized and mixed with FL to prepare curcumin solid lipid nanoparticle powder mist loaded with flower-shaped lactose. The process is simple and feasible, and it has better safety performance for lung cells, which is expected to become a safe and effective delivery system for pulmonary inhalation drugs.
Highlights
In recent years, with the aggravation of environmental pollution, especially air pollution (PM2.5 particles), high smoking rate, and aging population, respiratory diseases caused by this are consuming more and more lives
Results show that Cur-solid lipid nanoparticles (SLN)-flower-shaped lactose (FL) has an average particle size (SMD) of 4.95 ± 0.57 μm and a median geometric particle size (De) of 7.66 ± 0.76 μm, and the optimal particle size for macrophage endocytosis is 1∼3 μm [22], so we prepared it for evaluation of particle size of powder mist agent by calculating aerodynamic particle size (Da); Da is calculated according to the following formula:
Means and standard deviations were calculated from three determinations. e results showed that the bulk density of Cur-SLN-FL composite dry powder was 0.16 ± 0.01 g/cm3 (Table 10), which indicated that the powder structure was loose, which was beneficial to the atomization and dispersion of lung inhalation
Summary
With the aggravation of environmental pollution, especially air pollution (PM2.5 particles), high smoking rate, and aging population, respiratory diseases caused by this are consuming more and more lives. Curcumin (Cur) is an important active polyphenol extracted from Curcuma, which can play a significant role in the treatment of COPD through anti-inflammation [3, 4]. Inhaled glucocorticoid combined with long-acting β2 receptor agonist can effectively reduce inflammation and improve lung function. E lactose in the dry powder composition cannot enter the bronchioles because of its particle size >5 μm, so how to desorb the drug becomes one of the important factors to improve the deposition rate of the effective parts of the drug. In this study, based on the optimization of SLN preparation process, a new Cur-SLN-FL loaded with FL was constructed, in order to achieve the targeting and long-term sustained-release effect of curcumin in lung. In this study, based on the optimization of SLN preparation process, a new Cur-SLN-FL loaded with FL was constructed, in order to achieve the targeting and long-term sustained-release effect of curcumin in lung. e cytotoxicity of Cur-SLN-FL in vitro was evaluated by mouse fibroblast (L929) cells and human normal lung epithelial cells (BEAS2B), respectively, in order to provide a safe and efficient intrapulmonary drug delivery method for the treatment of COPD
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