title: Lipid nanoparticles with no surfactant improve oral absorption rate of poorly water-soluble drug.
abstract: A pharmacokinetic study was performed in rats to evaluate the oral absorption ratios of nanoparticle suspensions containing the poorly water-soluble compound nifedipine (NI) and two different types of lipids, including hydrogenated soybean phosphatidylcholine and dipalmitoylphosphatidylglycerol. NI-lipid nanoparticle (LN) suspensions with a mean particle size of 48.0 nm and a zeta potential of -57.2 mV were prepared by co-grinding combined with a high-pressure homogenization process. The oral administration of NI-LN suspensions to rats led to a significant increase in the NI plasma concentration, and the area under the curve (AUC) value was found to be 108 min μg mL⁻¹, indicating a 4-fold increase relative to the NI suspensions. A comparison of the pharmacokinetic parameters of the NI-LN suspensions with those of the NI solution prepared using only the surfactant polysorbate 80 revealed that although the AUC and bioavailability (59%) values were almost identical, a rapid absorption rate was still observed in the NI-LN suspensions. These results therefore indicated that lipid nanoparticles prepared using only two types of phospholipid with a mean particle size of less than 50 nm could improve the absorption of the poorly water-soluble drug.
authors.affiliation: Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
authors.forename: Yuka
authors.initials: Y
authors.lastname: Funakoshi
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Iwao
authors.forename: Shuji
authors.initials: S
authors.lastname: Noguchi
authors.forename: Shigeru
authors.initials: S
authors.lastname: Itai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D008297:Male; D053758:Nanoparticles; D009543:Nifedipine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry*; D010715:Phosphatidylglycerols / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013025:Glycine max
chemical_list: D004337:Drug Carriers; D010713:Phosphatidylcholines; D010715:Phosphatidylglycerols; D011136:Polysorbates; D009543:Nifedipine; C030345:1,2-dipalmitoylphosphatidylglycerol