Studies On Dry Powder Inhalation Of Curcumin Loaded Solid Lipid Nanoparticles

Curcumin low solubility in water, and the effects of poor oral absorption, resulting in its low bioavailability affect its clinical efficacy, so in recent years researchers from curcumin improve the water solubility and bioavailability start by being contained within the liposomes, solid lipid nanoparticles, in situ gel, slow release carrier, in order to improve its clinical efficacy. The purpose of this study is to develop curcumin SLN dry powder inhaler, and a preliminary evaluation of its physicochemical properties and stability.Pseudo-ternary phase diagram of microemulsion formed after the impact of the three factors(emulsifier, co-emulsifier and Km) were investigated to determine the optimal formulation of the microemulsion. On this basis, the heat is dispersed in cold water microemulsion phase dispersion preparation of solid lipid nanoparticles suspension. After univariate preliminary screening(different emulsifiers and different lipid and the amount of cold water temperature and the heat dispersed phase microemulsion injection temperature), encapsulation efficiency index orthogonal design prescriptions and verify its encapsulation efficiency particle size distribution and polydispersity index. 65 ? determined by the stearate, polysorbate 80, anhydrous ethanol, Km = 1: 4 best prepared microemulsion. Optimal conditions of solid lipid nanoparticles curcumin dosage of 50 mg, stearic acid in an amount of 0.5g, cold water with a temperature of 2 ?, microemulsion holding temperature is 65 ?, the resulting solid lipid nanoparticles encapsulation efficiency to 87.73%, 7.72% drug loading, particle size 156.9 ± 2.2nm, more dispersion coefficient was 0.480, the average Zeta potential-24.8m V[1].Then separately spray drying and freeze-dried to obtain a solid lipid nanoparticle curcumin powder, powder properties of the two after reconstitution and after the effective part of the Vitro deposition rate of screening performed single factor of this product formulation(lactose- and the proportion of single-dose dry powder per capsule of load), and verify that the average particle size optimized, moisture, content uniformity, deposition rate and effective part in vitro emptying rate. Effective part in vitro deposition rate of spray-dried and freeze-dried powder was 29.98% and 15.69%, respectively. Optimized single dose dry powder formulation of Cur-SLN- lactose(1: 1) mixture of 50 mg, 10 mg lactose third component filled in No. 4 capsules. The prepared powder average particle size of 3.35?m, 4.57% moisture, content uniformity qualified, effective part in vitro deposition rate was 28.73 percent, emptying rate was 95.17%.Establishing analytical methods Cur-SLN-DPI in curcumin. The powder properties of the product(particle size and distribution, solubility, hygroscopicity and moisture sorption, mobility and water) the nature and quality of the preparation(content uniformity, in vitro emptying rate and effective part of the deposition rate, etc.) based on the review, based on its long-term, accelerated and stress testing, a preliminary evaluation of the stability of the product. Cur-SLN-DPI optimize the process to obtain the dry powder of an average particle size 3.35?m, critical relative humidity of about 70%, the average angle of repose 24.03 °, a water content of 4.57%, 95.17% emptying rate, the effective part of the deposition rate of 28.73%. The product of pure light and high temperature stability for 10 days at a relative humidity of 75%, a decrease of the effective part of drug deposited amount of about 5%, 5 days a capsule placed in RH92.5% softened condition and weight gain of more than 5% therefore, this product should be stored in airtight and dry container. Accelerated test results show that the product is not stable enough for the hot and humid; good long-term stability test place in September.DPI we prepared with good atomization performance, the indicators meet the "Chinese Pharmacopoeia" 2010 edition appendix require dry powder inhaler, prescription through exploration and technology, the resulting dry powder inhaler can meet the region deposited on the alveolar epithelium requirements, and it can maintain a certain nanoparticle encapsulation efficiency, in order to achieve sustained release in the lungs. Process validation results show that the product formulation process is stable and reliable quality. Therefore speculated This product meets the requirements of inhalation.