Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.


:In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) medium as a dissolution medium confirmed that the DOX release from CSO-SA micelles was successfully delayed by the core modification of CSO-SA micelles with stearic acid (SA). The cell viability assay against A549 cells indicated the 50% inhibition concentration (IC(50)) of blank CSO-SA micelles and the core modified CSO-SA micelles was 369 +/- 27 microg/mL and 234 +/- 9 microg/mL, respectively. The entrapment of DOX by CSO-SA micelles could decrease the IC(50) of DOX from 3.5 to 1.9 microg/mL, and a further reduction to 0.7 microg/mL could result by the core modification of CSO-SA micelles. The fluorescence image observations of DOX and DOX concentration measurements inside A549 cells demonstrated that the DOX concentration inside cells was increased by the entrapment of CSO-SA micelles, and further enhanced by the core modification of CSO-SA micelles. The results indicated that the CSO-SA micelles with modified cores could be useful as a drug delivery vehicle for cancer chemotherapy.


J Pharm Sci


Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY




Has Abstract


2009-02-01 00:00:00














  • Iontophoretic transport across a multiple membrane system.

    abstract::The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Molokhia SA,Zhang Y,Higuchi WI,Li SK

    更新日期:2008-01-01 00:00:00

  • Coated Lipidic Nanoparticles as a New Strategy for Enhancing Nose-to-Brain Delivery of a Hydrophilic Drug Molecule.

    abstract::Oral Almotriptan maleate (ALM) is used in the treatment of migraine; however, due to its extreme aqueous solubility, shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. Being flexible and lipophilic in nature, nanostructured lipid carriers (NLCs) represent a promising tool...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Salem LH,El-Feky GS,Fahmy RH,El Gazayerly ON,Abdelbary A

    更新日期:2020-07-01 00:00:00

  • Enhancing the Pharmaceutical Behavior of Nateglinide by Cocrystallization: Physicochemical Assessment of Cocrystal Formation and Informed Use of Differential Scanning Calorimetry for Its Quantitative Characterization.

    abstract::The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures wi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bruni G,Maggi L,Mustarelli P,Sakaj M,Friuli V,Ferrara C,Berbenni V,Girella A,Milanese C,Marini A

    更新日期:2019-04-01 00:00:00

  • Development and evaluation of method for simultaneous determination of phenobarbital and diphenylhydantoin in plasma by high-pressure liquid chromatography.

    abstract::A procedure for the simultaneous analysis of diphenylhydantoin and phenobarbital in plasma by high-pressure liquid chromatography was developed and evaluated. Separation is effected on a porous particle silicic acid column with chloroform dioxane-isopropanol-acetic acid (310:9.7:1.0:0.1 by volume) and is monitored at ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Atwell SH,Green VA,Haney WG

    更新日期:1975-05-01 00:00:00

  • Biological distribution of chemical analogs of fatty acids and long chain hydrocarbons containing a strong chelating agent.

    abstract::The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Karesh SM,Eckelman WC,Reba RC

    更新日期:1977-02-01 00:00:00

  • Amphotericin B/emulsion admixture interactions: an approach concerning the reduction of amphotericin B toxicity.

    abstract::Mixing Fungizone with a fat emulsion used for nutritional purpose (Intralipid or Lipofundin ) was reported to decrease Amphotericin B (AmB) toxicity in clinical use. In an effort to understand the reason for this phenomenon, spectral and morphological analyses were done for the Fungizone and Fungizone /Lipofundin admi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Egito ES,Araújo IB,Damasceno BP,Price JC

    更新日期:2002-11-01 00:00:00

  • Determination of (+)- and (-)-nilvadipine in human plasma using chiral stationary-phase liquid chromatography and gas chromatography-mass spectrometry, and a preliminary pharmacokinetic study in humans.

    abstract::A stereoselective and sensitive method for the determination of nilvadipine, a new dihydropyridine calcium antagonist, in human plasma was developed. An internal standard, the deuterated analogue of racemic nilvadipine, was added to the plasma and extracted with an n-hexane:ethyl acetate (92.5:7.5) mixture under alkal...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tokuma Y,Fujiwara T,Noguchi H

    更新日期:1987-04-01 00:00:00

  • Molecular modeling of beta-cyclodextrin complexes with nootropic drugs.

    abstract::The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

    更新日期:1992-12-01 00:00:00

  • Evaluation of 2-azabicyclo[2.2..2]octane analogs of 4-anilidopiperidine analgesics.

    abstract::Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Borne RF,Law SJ,Kapeghian JC,Masten LW

    更新日期:1980-09-01 00:00:00

  • Kinetics of drug-drug interactions in sheep: tolbutamide and sulfadimethoxine.

    abstract::The interaction between sulfadimethoxine and tolbutamide in sheep involving displacement from protein binding sites was investigated quantitatively. A 52% increase in the unbound plasma concentration of tolbutamide was observed in vitro at 37 degrees after the addition of sulfadimethoxine (100 microgram/ml) to sheep p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Thiessen JJ,Rowland M

    更新日期:1977-08-01 00:00:00

  • Stability of tetrahydrocannabinols II.

    abstract::The biphasic degradation of delta9-tetrahydrocannabinol (I), as monitored by flame-ionization GLC, produced delta8-tetrahydrocannabinol (II), cannabidiol (X), 9-hydroxyhexahydrocannabinol (VI), 9,10-dihydro-9-hydroxyisocannabidiol (VI), and and 6,12-dihydro-6-hydroxycannabidiol (VIII) in acidic solutions. Further iden...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Garrett ER,Gouyette AJ,Roseboom H

    更新日期:1978-01-01 00:00:00

  • Preparation and Characterization of Ascosome Vesicles Loaded with Khellin.

    abstract::Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

    更新日期:2020-10-01 00:00:00

  • Synthesis, cytotoxicity, hypolipidemic and anti-inflammatory activities of amine-boranes and esters of boron analogues of choline and thiocholine.

    abstract::Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

    更新日期:1992-05-01 00:00:00

  • Chromogenic reactions of tertiary amines with polycarboxylic acids and acetic anhydride: carbon suboxide as the reactive species in the malonic acid reagent.

    abstract::Analytical methods based on the title reactions are reviewed, and the malonic acid-acetic anhydride system was selected for detailed study. It is postulated that carbon suboxide, O = C = C = C = O, formed by the action of acetic anhydride on malonic acid, is the effective reactive species in this system. Carbon suboxi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Connors KA,Ifan A

    更新日期:1987-10-01 00:00:00

  • Structural characterization of anhydrous naloxone- and naltrexone hydrochloride by high resolution laboratory X-ray powder diffraction and thermal analysis.

    abstract::The crystal structures of the analgesic compounds anhydrous naloxone and naltrexone hydrochloride were determined ab initio from high resolution laboratory X-ray powder diffraction data. Both compounds crystallize in the orthorhombic space group P2(1)2(1)2(1) with lattice parameters of a = 14.6588(10) A, b = 17.4363(9...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sugimoto K,Dinnebier RE,Zakrzewski M

    更新日期:2007-12-01 00:00:00

  • Development of a nanofiltration process to improve the stability of a novel anti-MRSA carbapenem drug candidate.

    abstract::The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Antonucci V,Yen D,Kelly J,Crocker L,Dienemann E,Miller R,Almarrsson O

    更新日期:2002-04-01 00:00:00

  • Cross-linked low molecular weight glycopeptide-mediated gene delivery: relationship between DNA metabolic stability and the level of transient gene expression in vivo.

    abstract::DNA co-condensates were formed by reacting [125I]DNA with an admixture of a high-mannose glycopeptide (Man9-CWK(18)) and either of two poly(ethylene glycol) peptides (PEG-VS-CWK(18) or PEG-SS-CWK(18)) followed by cross-linking with 6-50 mol equiv of glutaraldehyde. [125I]DNA co-condensates were administered intravenou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yang Y,Park Y,Man S,Liu Y,Rice KG

    更新日期:2001-12-01 00:00:00

  • Single pass mean residence time in peripheral tissues: a distribution parameter intrinsic to the tissue affinity of a drug.

    abstract::The single pass mean residence time in peripheral tissues, tp1, is a characteristic constant of linear pharmacokinetic systems and nonlinear systems with linear distribution kinetics. It is descriptive of distribution kinetics in such systems and is not dependent on elimination kinetics as are other related parameters...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Veng-Pedersen P,Gillespie WR

    更新日期:1986-12-01 00:00:00

  • GI absorption of beta-lactam antibiotics. III: Kinetic evidence for in situ absorption of ionized species of monobasic penicillins and cefazolin from the rat small intestine and structure-absorption rate relationships.

    abstract::Absorption rates of monobasic beta-lactam antibiotics were measured as a function of lumen solution pH between 4 and 9 by utilizing the rat intestinal recirculating method in situ. Between pH 6.5 and 9, the absorption rate constants of ionized antibiotics were almost identical; but, at pH 4, the unionized species were...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tsuji A,Miyamoto E,Kubo O,Yamana T

    更新日期:1979-07-01 00:00:00

  • Plasma binding of benzodiazepines in humans.

    abstract::Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

    更新日期:1979-10-01 00:00:00

  • Interactions of cyclosporines with lipid membranes as studied by solid-state nuclear magnetic resonance spectroscopy and high-sensitivity titration calorimetry.

    abstract::Cyclosporin A (CyA) interacts with lipid membranes. Binding reaction and membrane location of CyA and analogs were examined with 2H-NMR, high-sensitivity isothermal titration calorimetry (ITC), and CD spectroscopy. Effects of CyA and charged analogs on the phosphocholine head group and on the membrane interior were in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schote U,Ganz P,Fahr A,Seelig J

    更新日期:2002-03-01 00:00:00

  • Enhanced doxorubicin delivery to the brain administered through glutathione PEGylated liposomal doxorubicin (2B3-101) as compared with generic Caelyx,(®)/Doxil(®)--a cerebral open flow microperfusion pilot study.

    abstract::The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Birngruber T,Raml R,Gladdines W,Gatschelhofer C,Gander E,Ghosh A,Kroath T,Gaillard PJ,Pieber TR,Sinner F

    更新日期:2014-07-01 00:00:00

  • Stable isotope coadministration methodology for the estimation of the fraction of imipramine metabolized to desipramine.

    abstract::The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sasaki Y,Shinohara Y,Baba S

    更新日期:1990-02-01 00:00:00

  • Dissolution profiles for finely divided drug suspensions.

    abstract::A suspension of micronized prednisolone acetate was separated into four fractions by the technique of centrifugal elutriation. Data showed that each fraction had a narrow particle size. The dissolution experiments were carried out under sink conditions (less than 10% of saturation concentration) in a dissolution appar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mauger JW,Howard SA,Amin K

    更新日期:1983-02-01 00:00:00

  • Sensitive electron-capture GLC determination of metoclopramide in biological fluids.

    abstract::A highly sensitive and specific electron-capture GLC assay capable of detecting picogram quantities of metoclopramide, a procaine derivative, in biological fluids was developed. This assay consisted of extracting metoclopramide from an alkalinized aqueous layer into benzene. A portion of the organic phase was derivati...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tam YK,Axelson JE

    更新日期:1978-08-01 00:00:00

  • Analysis and prediction of partition coefficients of meta- and para-disubstituted benzenes in terms of substituent effects.

    abstract::The hydrophobic substituent parameter for a system of meta- and para-disubstituted benzenes, XC6H4Y, defined as pi X/PhY = log PXC6H4Y - log PC6H5Y, where P is the octanol-water partition coefficient and X and Y are variable and fixed substituents, respectively, varies from one system to another, according to the vari...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fujita T

    更新日期:1983-03-01 00:00:00

  • Application of gas pycnometry for the density measurement of freeze-dried products.

    abstract::Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stange U,Scherf-Clavel M,Gieseler H

    更新日期:2013-11-01 00:00:00

  • In Vitro and In Vivo Studies of Polyvinyl Pyrrolidone-Coated Sparfloxacin-Loaded Ring Contact Lens to Treat Conjunctivitis.

    abstract::Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ran W,Ma H,Li M

    更新日期:2020-06-01 00:00:00

  • Surfactant Effects on Lipid-Based Vesicles Properties.

    abstract::Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

    更新日期:2018-05-01 00:00:00

  • Developability assessment during the selection of novel therapeutic antibodies.

    abstract::Therapeutic antibodies and antibody derivatives comprise the majority of today's biotherapeutics. Routine methods to generate novel antibodies, such as immunization and phage-display, often give rise to several candidates with desired functional properties. On the contrary, resource-intense steps such as the developme...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Jarasch A,Koll H,Regula JT,Bader M,Papadimitriou A,Kettenberger H

    更新日期:2015-06-01 00:00:00