title: Encapsulation, pharmacokinetics and tissue distribution of interferon α-2b liposomes after intramuscular injection to rats.
abstract: The aim of the present study was to investigate the effect of liposome-encapsulation and liposome-size on the in vivo pharmacokinetics of interferon α-2b (IFNα-2b) following i.m. administration to rats, and whether there was any liver-targeting of these liposomes. Since liposomes of different sizes can be obtained by homogenization, the effect of homogenization on the IFNα-2b activity was also investigated. The pharmacokinetics of IFNα-2b solution (12.8 μg/kg) and IFNα-2b prepared in liposomes, including three mean sizes of 172 nm (12.2 μg/kg), 113 nm (44.2, 11.0, and 2.8 μg/kg, respectively), and 82 nm (13.1μg/kg), were studied after a single i.m. dose to rats. Compared to a solution of IFNα-2b. administration of liposomal IFNα-2b resulted in a significantly prolonged t(max), the apparent elimination half life (t(1/2β)) was 2.3 times longer, both AUC(0-∞) and MRT(0-∞) were also clearly enhanced and greater accumulation was obtained in the liver (p < 0.05). The AUC(0-∞) increased proportionally to the administered dose of IFNα-2b liposomes. Moreover, the size of liposomes ranging from 82 nm to 172 nm had no significant difference on the pharmacokinetic behavior in vivo (p > 0.05). In sum, compared with the free form, IFNα-2b encapsulated in liposomes can alter strikingly the pharmacokinetics properties following i.m. injection and if a liposomal size ranging from 82 nm to 172 nm was used, consistent pharmacokinetic behaviors of IFNα-2b was exhibited. The liposomal formulation apparently targeted the liver, offering a potential advantage for hepatitis B treatment.
authors: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, China.
authors: Hao
authors: H
authors: Li
authors: Li
authors: L
authors: Yang
authors: Gang
authors: G
authors: Cheng
authors: Hong-Yan
authors: HY
authors: Wei
authors: Qun
authors: Q
authors: Zeng
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D016503:Drug Delivery Systems; D006207:Half-Life; D007273:Injections, Intramuscular; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008081:Liposomes; D008099:Liver / Q000378:metabolism; D008297:Male; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D011994:Recombinant Proteins; D014018:Tissue Distribution
chemical_list: D000998:Antiviral Agents; D000077190:Interferon alpha-2; D016898:Interferon-alpha; D008081:Liposomes; D011994:Recombinant Proteins