title: Budesonide/cyclodextrin complex-loaded lyophilized microparticles for intranasal application.
abstract: OBJECTIVE
  Lyophilized microparticles composed of budesonide (BDS), hydroxypropyl-β-cyclodextrin (HP-β-CD), and hydroxypropylmethylcellulose (HPMC) or sodium carboxymethylcellulose (CMC-Na) were developed for intranasal delivery and their characteristics were evaluated.
  
  
  METHODS
  The particle size and morphology were assessed by mean diameter measurement and scanning electron microscopy (SEM) image, respectively. The solid-state of products was tested by X-ray powder diffraction (XRPD), Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). In vitro drug release and cytotoxicity to the primary human nasal epithelial (HNE) cells were also evaluated.
  
  
  CONCLUSIONS
  Lyophilized microparticles exhibited vanishment of crystallinity of drug in XRPD analysis, the enfeeblement of carbonyl (C=O) stretching bands of carboxyl group in BDS in FT-IR spectra and the disappearance of endothermic peak of drug in the results of DSC study. Based on the results of solid-state studies, BDS was existed as an amorphous form in the lyophilized microparticles. CD complexation enhanced drug solubility and release rate, and HPMC or CMC-Na also improved drug dissolution rates. Cytotoxicity of developed microparticles to the HNE cells was measured and their safety to HNE cell was identified.
  
  
  CONCLUSIONS
  Developed microparticles can efficiently deliver insoluble drug, such as BDS, to the nasal epithelium and thus it may improve therapeutic efficacy in the respiratory tract.
authors.affiliation: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University , Seoul , Republic of Korea and.
authors.forename: Ji-Eon
authors.initials: JE
authors.lastname: Kim
authors.forename: Hyun-Jong
authors.initials: HJ
authors.lastname: Cho
authors.forename: Dae-Duk
authors.initials: DD
authors.lastname: Kim
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000281:Administration, Intranasal; D019819:Budesonide / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry* / Q000633:toxicity; D005612:Freeze Drying; D005938:Glucocorticoids / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000633:toxicity
chemical_list: D005079:Excipients; D005938:Glucocorticoids; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D019819:Budesonide
keywords: Budesonide; hydroxypropyl-β-cyclodextrin; intranasal delivery; lyophilized microparticle; solid-state study