title: Construction and in vitro/in vivo evaluation of 17-allylamino-17-demethoxygeldanamycin (17AAG)-loaded PEGylated nanostructured lipid carriers.
abstract: In this study, the PEGylated nanostructured lipid carriers (PEG-NLC) were constructed for the intravenous delivery of 17-allylamino-17-demethoxygeldanamycin (17AAG). 17AAG-PEG-NLC was successfully prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature using a mixture of glycerol monostearate and PEG2000-stearate as solid lipids, and medium-chain triglyceride as the liquid lipid. The results revealed that the morphology of the NLC was spheroidal. The particle size, zeta potential and entrapment efficiency for 17AAG-PEG-NLC were observed as 189.4 nm, -20.2 mV and 83.42%, respectively. X-ray diffraction analysis revealed that 17AAG existed as amorphous structures in the nanoparticles. In the in vitro release study, the 17AAG from 17AAG-PEG-NLC exhibited a biphasic release pattern with burst release initially and sustained release afterwards. In addition, 17AAG-PEG-NLC showed a significantly higher in vitro antitumor efficacy and longer retention time in vivo than 17AAG solution. These results indicated that 17AAG-PEG-NLC may offer a promising alternative to the current 17AAG formulations for the treatment of solid tumors.
authors: a Department of Pharmacy Intravenous Admixture Service , the Second Affiliated Hospital of Harbin Medical University.
authors: Zhiyong
authors: Z
authors: Wang
authors: b Department of Pharmacy Intravenous Admixture Service , the First Affiliated Hospital of Harbin Medical University , and.
authors: Jinhua
authors: J
authors: Wang
authors: c Department of Biology Pharmacy , Heilongjiang Vocational College of Biology Science and Technology , Harbin , Heilongjiang , P.R. China.
authors: Songling
authors: S
authors: Yang
authors: b Department of Pharmacy Intravenous Admixture Service , the First Affiliated Hospital of Harbin Medical University , and.
authors: Shuying
authors: S
authors: Hou
mesh_terms: D061605:Administration, Intravenous; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016227:Benzoquinones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D065546:Drug Liberation; D004655:Emulsions; D005990:Glycerol / Q000737:chemistry; D006801:Humans; D047029:Lactams, Macrocyclic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008055:Lipids / Q000737:chemistry; D061986:MCF-7 Cells; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013228:Stearates / Q000737:chemistry; D014280:Triglycerides / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D000903:Antibiotics, Antineoplastic; D016227:Benzoquinones; D004337:Drug Carriers; D004655:Emulsions; D047029:Lactams, Macrocyclic; D008055:Lipids; D013228:Stearates; D014280:Triglycerides; D011092:Polyethylene Glycols; C112765:tanespimycin; D005990:Glycerol
keywords: Antitumor; in vitro drug release; nanostructured lipid carriers