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Characterization and in vitro evaluation of freeze-dried microparticles composed of granisetron-cyclodextrin complex and carboxymethylcellulose for intranasal delivery.
Cho, Hyun-Jong; Balakrishnan, Prabagar; Shim, Won-Sik; Chung, Suk-Jae; Shim, Chang-Koo; Kim, Dae-Duk.
Affiliation
  • Cho HJ; College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, San 56-1, Silim-Dong, Gwanak-gu, Seoul 151-742, South Korea.
Int J Pharm ; 400(1-2): 59-65, 2010 Nov 15.
Article in En | MEDLINE | ID: mdl-20801202
The aim of this study was to prepare microparticles (MPs) of granisetron (GRN) in combination with hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and sodium carboxymethylcellulose (CMC-Na) by the simple freeze-drying method for intranasal delivery. The composition of MPs was determined from the phase-solubility study of GRN in various CDs. Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD) analysis and differential scanning calorimetry (DSC) studies were performed to evaluate possible interactions between GRN and excipients. The results indicated the formation of inclusion complex between GRN and CD, and the conversion of drug into amorphous state. The in vitro release of GRN from MPs was determined in phosphate buffered saline (pH 6.4) at 37°C. Cytotoxicity of the MPs and in vitro permeation study were conducted by using primary human nasal epithelial (HNE) cells and their monolayer system cultured by air-liquid interface (ALI) method, respectively. The MPs showed significantly higher GRN release profile compared to pure GRN. Moreover, the prepared MPs showed significantly lower cytotoxicity and higher permeation profile than that of GRN powder (p<0.05). These results suggested that the MPs composed of GRN, HP-ß-CD and CMC-Na represent a simple and new GRN intranasal delivery system as an alternative to the oral and intravenous administration of GRN.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Serotonin Antagonists / Drug Carriers / Carboxymethylcellulose Sodium / Granisetron / Beta-Cyclodextrins / Nasal Mucosa Limits: Humans Language: En Journal: Int J Pharm Year: 2010 Document type: Article Affiliation country: Korea (South) Country of publication: Netherlands

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Serotonin Antagonists / Drug Carriers / Carboxymethylcellulose Sodium / Granisetron / Beta-Cyclodextrins / Nasal Mucosa Limits: Humans Language: En Journal: Int J Pharm Year: 2010 Document type: Article Affiliation country: Korea (South) Country of publication: Netherlands