Hydrophilic biodegradable microspheres of interferon-alpha and its pharmacokinetics in mice.
The goal of this research was to prepare a kind of hydrophilic sustained release microspheres of interferon-alpha (IFN-alpha), alginate-chitosan microspheres (ACM) of IFN, and investigate its pharmacokinetics in mice. Alginate microspheres of IFN-alpha were first prepared by an emulsion method and further incubated in chitosan to form IFN-ACM. The influences of isopropanol, bovine serum albumin (BSA), and pH adjustment by isoelectric point of IFN were studied. The optimized IFN-ACM was obtained with smooth and round morphology, size of 2.18 +/- 0.43 microm and entrapment efficiency of 40%. All the concentrations of IFN-alpha were determined by IFN assay kits. Finally the pharmacokinetics of IFN-ACM suspension was studied in ICR mice by intramuscular (I.M.) routes. Compared with IFN solution, C(max) of IFN-ACM reduced 2.3-fold, and time to achievement of maximum serum concentrations (T(max)) increased 4-fold. Meanwhile the area under the concentration-time curve (AUC) was the same as that of solution. The concentration-time profiles presented the prolonged serum levels of IFN from IFN-ACM.
Zheng
Cai-Hong
CH
Department of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Yu
He-Yong
HY
Gao
Jian-Qing
JQ
Sun
Xiao-Yi
XY
Liang
Wen-Quan
WQ
D000464:Alginates / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D002214:Capsules / Q000737:chemistry / Q000493:pharmacokinetics; D002417:Cattle; D048271:Chitosan / Q000737:chemistry / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D020723:Glucuronic Acid / Q000737:chemistry / Q000378:metabolism; D006603:Hexuronic Acids / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D016898:Interferon-alpha / Q000493:pharmacokinetics*; D051379:Mice; D008863:Microspheres; D010316:Particle Size; D013499:Surface Properties
D000464:Alginates; D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D016898:Interferon-alpha; D020723:Glucuronic Acid; D048271:Chitosan