These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Stealth tanshinone IIA-loaded solid lipid nanoparticles: effects of poloxamer 188 coating on in vitro phagocytosis and in vivo pharmacokinetics in rats.
    Author: Zhang WL, Liu JP, Liu XX, Chen ZQ.
    Journal: Yao Xue Xue Bao; 2009 Dec; 44(12):1421-8. PubMed ID: 21348419.
    Abstract:
    Stealth tanshinone IIA-loaded solid lipid nanoparticles (TA-SSLNs) have been prepared and the influence of poloxamer 188 coating on in vitro phagocytosis and in vivo pharmacokinetics in rats were evaluated. TA-SSLNs have been prepared by a nanoprecipitation/solvent diffusion method. Poloxamer 188 was used as a stealth agent. The physicochemical parameters of TA-SSLNs were characterized in terms of particle size, zeta potential, transmission electron microscopy and stability. In vitro, phagocytosis was investigated by incubating TA-SSLNs and non-stealth tanshinone IIA-loaded solid lipid nanoparticles (TA-NSLNs) with murine macrophages. In vivo, pharmacokinetics of TA-SSLNs and TA-NSLNs after a single dose intravenous injection to rat has been studied. The control was tanshinone IIA solution (TA-SOL). The results showed that TA-SSLNs had an average diameter of (91.3 +/- 3.4) nm, zeta potential of (-19.7 +/- 1.6) mV, drug loading of (4.7 +/- 0.5) % and entrapment efficiency of (92.5 +/- 2.1) %. Phagocytosis studies showed significant differences between TA-SSLNs and TA-NSLNs and demonstrated that the poloxamer 188 coating could decrease the macrophage uptake. In vivo experiments showed that the plasma concentration data of TA-SSLNs, TA-NSLNs and TA-SOL were all fitted to a two-compartment model. Areas under curve (AUCs) of TA-NSLNs and TA-SSLNs were 1.28 and 3.70 times than that of TA-SOL, respectively. TA-SSLNs had generated a long circulating time in blood with a mean residence time (MRT) of 5.286 h, compared to 3.051 h of TA-NSLNs and 0.820 h of TA-SOL. Poloxamer 188 modification on solid lipid nanoparticles (SLNs) reduced opsonization by serum proteins and the macrophage uptake. AUC of tanshinone IIA increased as a function of SLNs. In addition, TA-SSLNs exhibited much longer circulation lifetimes for tanshinone IIA than TA-NSLNs. The pharmacokinetic behavior of the incorporated drug can be modified by changing the surface characteristics of SLNs with the use of poloxamer 188.
    [Abstract] [Full Text] [Related] [New Search]