Pharmacokinetics, tissue distribution and bioavailability of nitrendipine solid lipid nanoparticles after intravenous and intraduodenal administration

Autor:	Vobalaboina Venkateswarlu, Kopparam Manjunath
Rok vydání:	2006
Předmět:	Male Duodenum Chemistry Pharmaceutical Biological Availability Pharmaceutical Science Pharmacology Excipients chemistry.chemical_compound Drug Stability Suspensions Nitrendipine Pharmacokinetics Phosphatidylcholine Solid lipid nanoparticle Electrochemistry medicine Animals Tissue Distribution Particle Size Rats Wistar Intubation Gastrointestinal Chemistry Trimyristin Poloxamer Calcium Channel Blockers Lipids Rats Bioavailability body regions Area Under Curve Injections Intravenous Tripalmitin Nanoparticles medicine.drug
Zdroj:	Journal of Drug Targeting. 14:632-645
ISSN:	1029-2330 1061-186X
DOI:	10.1080/10611860600888850
Popis:	The aim of this research was to study whether the bioavailability of nitrendipine (NDP) could be improved by administering nitrendipine solid lipid nanoparticles (SLN) duodenally to rats.Nitrendipine was incorporated into SLN prepared by hot homogenization followed by ultrasonication method. SLN were produced using various triglycerides (trimyristin, tripalmitin and tristearin), soy phosphatidylcholine 95%, poloxamer 188 and charge modifiers (dicetyl phosphate, DCP and stearylamine, SA). Particle size and charge measurements were made with a Malvern Zetasizer. Pharmacokinetics of nitrendipine SLNs (NDP-SLNs) after intravenous (i.v.) and intraduodenal (i.d.) administration to conscious male Wistar rats were studied. Tissue distribution studies of NDP-SLNs were carried out in Swiss albino mice after i.v. administration and compared to nitrendipine suspension (NDP-Susp).Average size and zeta potential of SLNs of different lipids, with and without charge modifiers ranged from 101.9 +/- 3.0 to 123.5 +/- 3.0 nm and - 35.1 +/- 0.5 to +34.6 +/- 2.3 mV, respectively. AUC(0-infinity) was increased (up to 4.51-folds) and clearance was decreased (up to 4.54-folds) after i.v. administration of NDP-SLNs with and without charge modifiers compared to NDP-Susp. Effective bioavailability of NDP-SLNs were 2.81-5.35-folds greater after i.d. administration in comparison with that of NDP-Susp. In tested organs, the AUC and MRT of NDP-SLNs were higher than those of NDP-Susp especially in brain, heart and reticuloendothelial cells containing organs.SLN are suitable drug delivery systems for the improvement of bioavailability of nitrendipine. Negatively and positively charged SLN were better taken up by the liver and brain, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::101337a3bb0eed3a1d3c72815ca66626 https://doi.org/10.1080/10611860600888850 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.