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Wang M.-T.,Key Laboratory of Drug Targeting and Drug Delivery System | Jin Y.,Key Laboratory of Drug Targeting and Drug Delivery System | Yang Y.-X.,University of Sichuan | Zhao C.-Y.,Key Laboratory of Drug Targeting and Drug Delivery System | And 7 more authors.
International Journal of Nanomedicine | Year: 2010

We aimed to evaluate whether the enhancement of the liver accumulation and anti-inflammatory activity of dexamethasone acetate (DXMA) could be achieved by incorporating it into nanostructured lipid carrier (NLCs). DXMA-NLCs were prepared using a film dispersion-ultrasonication method and characterized in terms of particle size, PDI, zeta potential, differential scanning calorimetry, drug loading capacity, encapsulation efficiency, and in vitro release. The biodistribution and pharmacokinetics of DXMA-NLCs in mice were significantly different from those of the DXMA solution (DXMA-sol). The peak concentration of DXMA-NLCs was obtained half an hour after intravenous administration. More than 55.62% of the total administrated dose was present in the liver. An increase of 2.57 fold in the area under the curve was achieved when compared with that of DXMA-sol. DXMA-NLCs exhibited a significant anti-inflammatory and hepatoprotective effect on carrageenan-induced rats and carbon tetrachloride-induced mice compared with DXMA-sol. However, the effect was not in proportion to the dosage. The intermediate and low dosages presented better effects than DXMA-sol. All results indicate that NLCs, as a novel carrier for DXMA, has potential for the treatment of liver diseases, increasing the cure efficiency and decreasing the side effects on other tissues. © 2010 Wang et al, publisher and licensee Dove Medical Press Ltd.


Zheng Y.,University of Sichuan | Zheng Y.,Key Laboratory of Drug Targeting and Drug Delivery System | Zheng Y.,Ohio State University | Song X.,West China Hospital | And 13 more authors.
Journal of Biotechnology | Year: 2010

To develop a receptor-mediated intracellular delivery system that can transport therapeutic proteins to specific tumor cells, folate-poly(ethylene glycol)-grafted-trimethylchitosan (folate-PEG-g-TMC) was synthesized. Nano-scaled spherical polyelectrolyte complexes between the folate-PEG-g-TMC and fluorescein isothiocyanate conjugated bovine serum albumin (FITC-BSA) were prepared under suitable weight ratio of copolymer to FITC-BSA by ionic interaction between the positively charged copolymers and the negatively charged FITC-BSA. Intracellular uptake of FITC-BSA was specifically enhanced in SKOV3 cells (folate receptor over-expressing cell line) through folate receptor-mediated endocytosis compared with A549 cells (folate receptor deficient cell line). Folate-PEG-g-TMC shows promise for intracellular transport of negatively charged therapeutic proteins into folate receptor over-expressing tumor cells. © 2009 Elsevier B.V.


Chen Q.,Chengdu University of Technology | Chen Q.,University of Sichuan | Chen Q.,Chongqing Medical University | Chen Q.,Key Laboratory of Drug Targeting and Drug Delivery System | And 7 more authors.
Journal of Pharmaceutical and Biomedical Analysis | Year: 2011

A simple and sensitive high performance liquid chromatography method with fluorescence detection (HPLC-FD) was described for the determination of aesculin (AL) at low concentrations in rabbit plasma and ocular tissues. After deproteinization by methanol using pazufloxacin mesilate (PM) as an internal standard (I.S.), supernatants were evaporated to dryness at 40 °C under a gentle stream of nitrogen. The residue was reconstituted in mobile phase and a volume of 20 μL was injected into the HPLC for analysis. Analytes were separated on an Ultimate XB-C18 column (250. mm × 4.6. mm i.d., 5 μm particle size) and protected by a ODS guard column (10. mm × 4.0. mm i.d., 5 μm particle size), using acetonitrile-0.1% triethylamine in water (adjusted to pH 3.0 using phosphoric acid) (12:88, v/v) as mobile phase with a flow rate of 1.0. mL/min. The wavelengths of fluorescence detector (FD) were set at 344. nm for excitation and 466. nm for emission. The lower limit of quantitation (LOQ) for AL was 0.80. ng/mL for plasma and vitreous body, 1.59. ng/mL for aqueous humor, and 6.55. ng/g for iris and 1.66. ng/g for retina. The method was used in the study of AL concentrations in plasma and ocular tissues after topical administration of AL eye drops. © 2011.


Huang Z.,University of Sichuan | Wu C.,University of Sichuan | Shang Z.,University of Sichuan | Deng Y.,University of Sichuan | Deng Y.,Key Laboratory of Drug Targeting and Drug Delivery System
Chinese Journal of Organic Chemistry | Year: 2012

A novel process for synthesis of 1,2,6,7-tetrahydro-8H-indeno[5,4-6]furan- 8-one, a key intermediate for preparation of ramelteon, a MT1 and MT2 melatonin receptor selective agonist, was developed. The key intermediate 3-(2,3-dihydro-benzofuran-5-yl)propanoic acid was synthesized by condensation of p-bromophenol with bromoacetaldehyde diethyl acetal in the presence of K2CO3 and Friedel-Crafts reaction to give 5-bromobenzofuran, which was subsequently subjected to Heck coupling reaction with methyl acrylate in the presence of palladium acetate, then catalytic hydrogenation and hydrolysis in one pot reaction. Subsequently, 1,2,6,7-tetrahydro-8H-indeno[5, 4-b]furan-8-one was synthesized from 3-(2,3-dihydrobenzo-furan-5-yl)propanoic acid through bromination, Friedel-Crafts acylation and catalytic hydrogenolysis debromination. The overall yield was about 49.9%. The structures of intermediates and final product were determined by 1H NMR, 13C NMR and HRMS techniques. This method has the advantages of easily available starting materials, simply conducted procedures, relatively high yield and easy purification, and is more suitable for scale-up production.


Huang Z.,University of Sichuan | Sang Z.,University of Sichuan | Cao H.,University of Sichuan | Chao R.,University of Sichuan | And 2 more authors.
Chinese Journal of Organic Chemistry | Year: 2014

The ester bond and amide bond of linezolid were selectively hydrolyzed by using LiOH to afford N-[(2R)-3-[[3-fluoro-4-(4-morpholino)phenyl] amino]-2-hydroxypropyl] acetamide (2) and (2S)-1-amino-3-[[3-fluoro-4-(4-morpholino)-phenyl]-amino]-2-propanol (4) with 78.3% and 86.6% yields respectively, which were the partially hydrolyzed impurity and fully hydrolyzed impurity of the injection of linezolid. The terminal amino group of compound 4 was then protected with tert-butyloxycarbonyl and subjected to N, O-diacetylation. Subsequently, N-[(2S)-3-amino-2-hydroxypropyl]-N-[3-fluoro-4-(4-morpholino)phenyl] acetamide (3) hydrochloride was synthesized by removal of O-acetyl with ammonia/methanol and then deprotection tert-butoxycarbonyl using saturated solution of hydrogen chloride in ether with 62.3% overall yield. © 2014 Chinese Chemical Society & SIOC, CAS.

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