title: Nanosuspension for parenteral delivery of a p-terphenyl derivative: preparation, characteristics and pharmacokinetic studies.
abstract: Recently, nanosuspension technology has evolved into a mature drug delivery system, which can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. In this study, nanosuspensions of a p-terphenyl derivative (H2) were prepared by combining microfluidization and precipitation method and transformed into dry powder by lyophilization. The resultant nanosuspensions had a mean particle size of 201.7±5.87nm and a zeta potential of -21.07±0.57mV. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis verified that the crystalline state of H2 was not transformed when it was prepared to nanosuspensions. An increased saturation solubility (1.46ug/ml) and accelerated dissolution velocity were achieved. The percent drug release of bulk H2 and H2 nanosuspension dried powder was 7.16% and 93.5% at 120min point, respectively. The pharmacokinetic test in rats indicated that the area under plasma concentration-time curve (AUC0~∞) value of H2 nanosuspension (5.183mg/Lh) was about 5-fold higher than that of H2 solution (1.094mg/Lh). Additionally, the mean retention time (MRT) value of H2 nanosuspension (2.832h) was significantly longer than that of H2 solution (0.997h).
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Xiaona
authors.initials: X
authors.lastname: Tian
authors.forename: Han
authors.initials: H
authors.lastname: Li
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.forename: Guangpu
authors.initials: G
authors.lastname: Liu
authors.forename: Lejiao
authors.initials: L
authors.lastname: Jia
authors.forename: Dandan
authors.initials: D
authors.lastname: Zheng
authors.forename: Jingyi
authors.initials: J
authors.lastname: Shen
authors.forename: Yuemao
authors.initials: Y
authors.lastname: Shen
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D005612:Freeze Drying; D007263:Infusions, Parenteral; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D013535:Suspensions; D013730:Terphenyl Compounds / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013535:Suspensions; D013730:Terphenyl Compounds