title: Optimization and characterization of dry powder of fanhuncaoin for inhalation based on selection of excipients.
abstract: In this study, dry powder formulations for inhalation of fanhuncaoin, a newly discovered antiinflammatorily active compound isolated from Chinese herb, were designed to optimize the composition and further explore the relationship between the composition, the physical properties and the aerosolization performance. Dry powders were prepared by spray-drying using leucine, chitosan, chitosan oligosaccharide and dipalmitoyl phosphatidylcholine (DPPC) as excipients. Following spray-drying, resultant powders were characterized using scanning electron microscopy, tapped density analysis, laser diffractometry, thermogravimetric analysis and differential scanning calorimetry. The aerosol behaviour of the powders was studied in a Twin Stage Impinger at an airflow rate of 60 l/min using a HandiHaler® inhaler device. Results revealed that the nature and the relative proportion of the excipients greatly influenced the physical characteristics of the powders and their aerodynamic behavior. Among the combinations tested, the composition ratio of fanhuncaoin/leucine/chitosan/chitosan oligosaccharide/DPPC of 10/45/33.75/11.25/0.4 (w/w/w/w/w) prepared in a total solid mass of 1% (w/v) formulation was found to be particularly optimal and exhibited a tapped density of 0.44 g/cm³, an aerodynamic diameter of 2.24 µm and an respirable fraction of 51.29%. In conclusion, optimization of the aerosolization properties of inhalation dry powders could be achieved by appropriately selecting the composition of the particles.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Liaoning, China.
authors.forename: Xiao-bo
authors.initials: XB
authors.lastname: Yang
authors.forename: Xiao-bo
authors.initials: XB
authors.lastname: Wang
authors.forename: Wei-san
authors.initials: WS
authors.lastname: Pan
authors.forename: Rong-gang
authors.initials: RG
authors.lastname: Xi
authors.forename: Yi-nan
authors.initials: YN
authors.lastname: Wang
authors.forename: Dan
authors.initials: D
authors.lastname: Liu
authors.forename: Yan
authors.initials: Y
authors.lastname: Shi
authors.forename: Shuang
authors.initials: S
authors.lastname: Jiang
mesh_terms: D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry; D000280:Administration, Inhalation; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000737:chemistry; D058995:Dry Powder Inhalers; D005079:Excipients / Q000737:chemistry*; D007930:Leucine / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D009844:Oligosaccharides / Q000737:chemistry; D010316:Particle Size; D011208:Powders; D012674:Senecio / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D004365:Drugs, Chinese Herbal; D005079:Excipients; D009844:Oligosaccharides; D011208:Powders; D015060:1,2-Dipalmitoylphosphatidylcholine; D048271:Chitosan; D007930:Leucine