Novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan for efficient ocular delivery.

Abstract:

:The objective of this study was to propose novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan (NLC-PDSC) as an efficient ocular delivery system to improve its transcorneal penetration and precorneal retention. PDSC with a deacetylation degree of around 50% was synthesized using an improved method. NLC loaded with flurbiprofen (FB) were prepared by melt emulsification method. They presented spherical morphology under both transmission electron microscope and scanning electron microscope. After coating with 0.15% (w/v) PDSC solution, the NLC showed a core-shell structure and a reversed zeta potential. The enhanced transcorneal penetration of the coated NLC was evaluated using isolated rabbit corneas, with significantly increased apparent permeability coefficient being 1.40- and 1.75-fold of the NLC and FB phosphate solution (FB-sol; p < 0.05), respectively. Precorneal retention assessed by gamma scintigraphy in vivo showed that the area under the remaining activity-time curve of the PDSC-coated formulation was 1.3-fold of the NLC and 2.4-fold of FB-sol. Moreover, in vivo ocular tolerance study indicated that there was no difference in irritation between the coated and noncoated NLC. In conclusion, novel NLC demonstrate high potential for ocular drug delivery.

journal_name

J Pharm Sci

authors

Tian B,Luo Q,Song S,Liu D,Pan H,Zhang W,He L,Ma S,Yang X,Pan W

doi

10.1002/jps.22813

subject

Has Abstract

pub_date

2012-03-01 00:00:00

pages

1040-9

issue

3

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)31668-3

journal_volume

101

pub_type

杂志文章
  • Development of Novel Drug and Gene Delivery Carriers Composed of Single-Walled Carbon Nanotubes and Designed Peptides With PEGylation.

    abstract::Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.03.031

    authors: Ohta T,Hashida Y,Yamashita F,Hashida M

    更新日期:2016-09-01 00:00:00

  • Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors.

    abstract::The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21372

    authors: Shaik N,Pan G,Elmquist WF

    更新日期:2008-12-01 00:00:00

  • Degradation kinetics of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770) and structure-stability relationship among its analogues in aqueous solution.

    abstract::The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780115

    authors: Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

    更新日期:1989-01-01 00:00:00

  • A site-directed mutagenesis study of drug-binding selectivity in genetic variants of human alpha(1)-acid glycoprotein.

    abstract::Human alpha(1)-acid glycoprotein (AGP), a major carrier of many basic drugs in circulation, consists of at least two genetic variants, namely A and F1*S variant. Interestingly, the variants of AGP have different drug-binding properties. The purpose of this study was to identify the amino acid residues that are respons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21697

    authors: Nishi K,Ueno M,Murakami Y,Fukunaga N,Akuta T,Kadowaki D,Watanabe H,Suenaga A,Maruyama T,Otagiri M

    更新日期:2009-11-01 00:00:00

  • Diffusion model for fluidized-bed drying.

    abstract::A sucrose-lactose-starch granulation was used to study particulate motion and attrition in a fluid bed dryer. There is some classification of material in the dryer as drying proceeds; fine particles are dried faster and become less dense, and the less dry but denser large particles show some (although not great) accum...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600641127

    authors: Zoglio MA,Streng WH,Carstensen JT

    更新日期:1975-11-01 00:00:00

  • A Mechanistic Model for Predicting the Physical Stability of Amorphous Solid Dispersions.

    abstract::In this paper, we establish a mechanistic model for the prediction of amorphous solid dispersion (ASD) stability. The novel approach incorporates fundamental physical parameters, principally supersaturation, diffusivity, and interfacial energy, to model crystallization in ASDs accounting for both kinetic and thermodyn...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.08.006

    authors: Ojo AT,Lee PI

    更新日期:2020-08-18 00:00:00

  • Label-Free Ferrocene-Loaded Nanocarrier Engineering for In Vivo Cochlear Drug Delivery and Imaging.

    abstract::It is hypothesized that ferrocene (FC)-loaded nanocarriers (FC-NCs) are safe label-free contrast agents for cochlear biodistribution study by transmission electron microscopy (TEM). To test this hypothesis, after engineering, the poly(epsilon-caprolactone)/polyglycolide NCs are tested for stability with various types ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.04.012

    authors: Youm I,Musazzi UM,Gratton MA,Murowchick JB,Youan BC

    更新日期:2016-10-01 00:00:00

  • The physical stability of the recombinant tuberculosis fusion antigens h1 and h56.

    abstract::The recombinant fusion proteins hybrid 1 [H1 (Ag85B-ESAT-6)] and hybrid 56 [H56 (Ag85B-ESAT-6-Rv2660c)] derived from Mycobacterium tuberculosis are promising antigens for subunit vaccines against tuberculosis. Both antigens are early batches of antigens to be enrolled in human clinical trials and it is therefore impor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23669

    authors: Hamborg M,Kramer R,Schanté CE,Agger EM,Christensen D,Jorgensen L,Foged C,Middaugh CR

    更新日期:2013-10-01 00:00:00

  • Analysis of coating structures and interfaces in solid oral dosage forms by three dimensional terahertz pulsed imaging.

    abstract::Three dimensional terahertz pulsed imaging (TPI) was evaluated as a novel tool for the nondestructive characterization of different solid oral dosage forms. The time-domain reflection signal of coherent pulsed light in the far infrared was used to investigate film-coated tablets, sugar-coated tablets, multilayered con...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20789

    authors: Zeitler JA,Shen Y,Baker C,Taday PF,Pepper M,Rades T

    更新日期:2007-02-01 00:00:00

  • A novel multivariate approach for estimating the degree of similarity in bioavailability between two pharmaceutical products.

    abstract::Statistical assessment of bioavailability and bioequivalence of drug products is generally carried out with a univariate analysis by independently comparing each relevant parameter [such as, area under the drug concentration curve (AUC) and peak drug concentration (Cmax)] of the test and reference products. The assump...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840620

    authors: Hsu HC,Lu HL,Chan KK

    更新日期:1995-06-01 00:00:00

  • Simultaneous determination of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations by gas chromatography.

    abstract::An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730136

    authors: Schieffer GW,Palermo PJ,Pollard-Walker S

    更新日期:1984-01-01 00:00:00

  • Carrier-mediated transport systems for glucose in mucosal cells of the human oral cavity.

    abstract::The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1021/js980298f

    authors: Oyama Y,Yamano H,Ohkuma A,Ogawara K,Higaki K,Kimura T

    更新日期:1999-08-01 00:00:00

  • Disposition of norgestimate in the presence and absence of ethinyl estradiol after oral administration to humans.

    abstract::The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671020

    authors: Weintraub HS,Abrams LS,Patrick JE,McGuire JL

    更新日期:1978-10-01 00:00:00

  • Physiologically Based Pharmacokinetic Modeling to Supplement Nilotinib Pharmacokinetics and Confirm Dose Selection in Pediatric Patients.

    abstract::In adult patients, nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.01.028

    authors: Heimbach T,Lin W,Hourcade-Potelleret F,Tian X,Combes FP,Horvath N,He H

    更新日期:2019-06-01 00:00:00

  • Polyamidoamine dendrimers can improve the pulmonary absorption of insulin and calcitonin in rats.

    abstract::The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22428

    authors: Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

    更新日期:2011-05-01 00:00:00

  • Pharmacokinetics and tissue distribution after intravenous administration of a single dose of amphotericin B cochleates, a new lipid-based delivery system.

    abstract::Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10173

    authors: Segarra I,Movshin DA,Zarif L

    更新日期:2002-08-01 00:00:00

  • Anthrax vaccine powder formulations for nasal mucosal delivery.

    abstract::Anthrax remains a serious threat worldwide as a bioterror agent. A second-generation anthrax vaccine currently under clinical evaluation consists of a recombinant Protective Antigen (rPA) of Bacillus anthracis. We have previously demonstrated that complete protection against inhalational anthrax can be achieved in a r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20484

    authors: Jiang G,Joshi SB,Peek LJ,Brandau DT,Huang J,Ferriter MS,Woodley WD,Ford BM,Mar KD,Mikszta JA,Hwang CR,Ulrich R,Harvey NG,Middaugh CR,Sullivan VJ

    更新日期:2006-01-01 00:00:00

  • Improved delivery through biological membranes XD: Percutaneous absorption and metabolism of methylsulfinylmethyl 2-acetoxybenzoate and related aspirin prodrugs.

    abstract::Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700710

    authors: Loftsson T,Bodor N

    更新日期:1981-07-01 00:00:00

  • Sensitive radioimmunoassay and enzyme-linked immunosorbent assay for the simultaneous determination of chloroquine and its metabolites in biological fluids.

    abstract::Two new methods for the simultaneous determination of chloroquine and its two main metabolites (monodesethylchloroquine and bisdesethylchloroquine) in biological samples, radioimmunoassay (RIA) and enzyme-linked immunosorbent assay (ELISA), are described. Antiserum is produced in rabbits immunized with N-(2-carboxyeth...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790107

    authors: Escande C,Chevalier P,Verdier F,Bourdon R

    更新日期:1990-01-01 00:00:00

  • Development of a Carrier-Free Dry Powder Ofloxacin Formulation With Enhanced Aerosolization Properties.

    abstract::Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.05.027

    authors: Ceschan NE,Rosas MD,Olivera ME,Dugour AV,Figueroa JM,Bucalá V,Ramírez-Rigo MV

    更新日期:2020-09-01 00:00:00

  • Deiodination kinetics of water-soluble radiopaques.

    abstract::Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690616

    authors: Wang YC

    更新日期:1980-06-01 00:00:00

  • A method to predict the equilibrium solubility of drugs in solid polymers near room temperature using thermal analysis.

    abstract::A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23319

    authors: Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

    更新日期:2012-12-01 00:00:00

  • General linearized biexponential model for QSAR data showing bilinear-type distribution.

    abstract::A major impediment of many QSAR-type analyses is that the data show a maximum or minimum and can no longer be adequately described by linear functions that provide unrivaled simplicity and usually give good description over more restricted ranges. Here, a general linearized biexponential (LinBiExp) model is proposed t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20438

    authors: Buchwald P

    更新日期:2005-11-01 00:00:00

  • Influence of asymmetric donor-receiver ion concentration upon transscleral iontophoretic transport.

    abstract::Recent in vitro and in vivo studies have suggested transscleral iontophoresis as a means for non-invasive drug delivery to the eye. However, there remains a lack of information of the iontophoretic transport behavior of the sclera. The objective of the present study was to investigate the effects of permeant concentra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20293

    authors: Li SK,Zhang Y,Zhu H,Higuchi WI,White HS

    更新日期:2005-04-01 00:00:00

  • Controlled transdermal delivery of fentanyl: characterizations of pressure-sensitive adhesives for matrix patch design.

    abstract::Transdermal delivery of fentanyl from various adhesive matrix formulations to achieve a steady-state skin flux was investigated. For this purpose, various pressure-sensitive adhesives selected from the three chemical classes of polymers (polyisobutylene (PIB), acrylate, and silicone adhesives) were characterized with ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950415w

    authors: Roy SD,Gutierrez M,Flynn GL,Cleary GW

    更新日期:1996-05-01 00:00:00

  • Spectrophotometric method for quantitation of peroxides in sorbitan monooleate and monostearate.

    abstract::A rapid and sensitive spectrophotometric method has been developed to quantitate the peroxides present in sorbitan monooleate and monostearate. The method relies on the peroxide conversion of iodide to iodine. The method has also been found to work for polysorbate 60. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731150

    authors: Magill A,Becker AR

    更新日期:1984-11-01 00:00:00

  • A new method of dissolution in vitro, the "Bio-Dis" apparatus: comparison with the rotating bottle method and in vitro: in vivo correlations.

    abstract::The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/jps.2600801017

    authors: Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

    更新日期:1991-10-01 00:00:00

  • Degradation pathways of a corticotropin-releasing factor antagonist in solution and solid states.

    abstract::Stability of the 1,3,5-triazine derivative (1), a corticotropin-releasing factor inhibitor, was studied in acidic solutions and in solid formulations. Degradant structures were elucidated using liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR). Compound 1 was found to undergo hydroly...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21637

    authors: Badawy S,Hussain M,Zhao F,Ye Q,Huang Y,Palaniswamy V

    更新日期:2009-08-01 00:00:00

  • Stereoselective pharmacokinetics and inversion of suprofen enantiomers in humans.

    abstract::The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600801116

    authors: Shinohara Y,Magara H,Baba S

    更新日期:1991-11-01 00:00:00

  • Combined use of pharmacokinetic modeling and a steady-state delivery approach allows early assessment of IkappaB kinase-2 (IKK-2) target safety and efficacy.

    abstract::NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21909

    authors: Chiang PC,Kishore NN,Thompson DC

    更新日期:2010-03-01 00:00:00