HO-1-u-1 model for screening sublingual drug delivery—Influence of pH, osmolarity and permeation enhancer

HO-1-u-1 (Ueda-1) is a human tumor cell line established from human sublingual squamous cell carcinoma. In previous study, HO-1-u-1 cell line was grown on cell culture inserts and utilized as in vitro model for screening sublingual drug delivery. The aim of current study was to further investigate t...

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Bibliographic Details
Published in:International journal of pharmaceutics 2009-03, Vol.370 (1), p.68-74
Main Authors: Wang, Yanfeng, Zuo, Zhong, Chow, Moses S.S.
Format: Article
Language:English
Subjects:
Adjuvants, Pharmaceutic - chemistry
Administration, Sublingual
Adrenergic beta-Antagonists - pharmacokinetics
Animals
Atenolol - pharmacokinetics
Biological and medical sciences
Biological Transport
Cardiovascular system
Cell Line, Tumor
Chromatography, High Pressure Liquid
Diffusion
Drug Evaluation, Preclinical - methods
Enhancer
General pharmacology
Glycodeoxycholic Acid - chemistry
HO-1-u-1
Humans
Hydrogen-Ion Concentration
In Vitro Techniques
Male
Medical sciences
Metoprolol - pharmacokinetics
Models, Biological
Mouth Mucosa - metabolism
Osmolar Concentration
Osmolarity
Permeability
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Propranolol - pharmacokinetics
Sublingual delivery
Sus scrofa
β-Blocker
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Description
Summary:HO-1-u-1 (Ueda-1) is a human tumor cell line established from human sublingual squamous cell carcinoma. In previous study, HO-1-u-1 cell line was grown on cell culture inserts and utilized as in vitro model for screening sublingual drug delivery. The aim of current study was to further investigate the effects of pH, osmolarity and permeation enhancer, sodium glycodeoxycholate (GDC) on the permeability of three β-blockers with different lipophilicities. The cytotoxicity was evaluated by MTS/PES assay. The permeability studies were carried out using the cell culture model and compared with that obtained from fresh porcine sublingual mucosa. The results showed the enhancement effects caused by pH, osmolarity and GDC were highly lipophilicity-dependent and in the order atenolol > metoprolol > propranolol. The apparent permeability coefficients ( P app) of all the three β-blockers were significantly increased by increasing pH. However, less enhancing effects were observed by non-physiological osmolarity or the presence of GDC in permeability study using both cell culture and porcine sublingual mucosa. The present results suggested that the HO-1-u-1 cell culture model maybe a useful and effective in vitro model for evaluating the enhancement effects and mechanism in sublingual drug delivery.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2008.11.010