title: Preparation and evaluation of stealth Tashinone IIA-loaded solid lipid nanoparticles: Influence of Poloxamer 188 coating on phagocytic uptake.
abstract: Stealth Tashinone IIA-loaded solid lipid nanoparticles (TA-SSLN) have been prepared by a nanoprecipitation/solvent diffusion method. Poloxamer 188 was used as a stealth agent. Nanoparticles were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The profile of Tashinone IIA release from TA-SSLN was studied. Phagocytosis was evaluated by incubating TA-SSLN and non-stealth Tashinone IIA-loaded solid lipid nanoparticles (TA-NSLN) with murine macrophages. Human serum was added to evaluate opsonization of serum proteins. Rhodamine B was incorporated into nanoparticles as a fluorescent marker to observe and compare the phagocytic uptake of two kinds of nanopreticles. The results showed that TA-SSLN had an average diameter of (92.4 +/- 5.2) nm, zeta potential of (-20.4 +/- 1.3) mV, drug loading of (4.6 +/- 0.2)% and entrapment efficiency of (93.3 +/- 2.1)%. In vitro release experiment confirmed a sustained release of TA-SSLN and showed that the release of Tashinone IIA from TA-SSLN was in accordance with the Weibull equation. Phagocytosis studies showed significant differences between TA-SSLN and TA-NSLN and demonstrated that the Poloxamer 188 coating could decrease the macrophages uptake.
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing, PR China.
authors.forename: Wenli
authors.initials: W
authors.lastname: Zhang
authors.forename: Jianping
authors.initials: J
authors.lastname: Liu
authors.forename: Suchun
authors.initials: S
authors.lastname: Li
authors.forename: Mengyuan
authors.initials: M
authors.lastname: Chen
authors.forename: Huan
authors.initials: H
authors.lastname: Liu
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008264:Macrophages / Q000378:metabolism; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010587:Phagocytosis; D010936:Plant Extracts / Q000008:administration & dosage; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D012235:Rhodamines / Q000737:chemistry / Q000378:metabolism; D012542:Scattering, Radiation
chemical_list: D001572:Benzofurans; D008055:Lipids; D010936:Plant Extracts; D012235:Rhodamines; C530742:tashinone IIA; D020442:Poloxamer; D011092:Polyethylene Glycols; C029773:rhodamine B