Brain delivery of proteins by the intranasal route of administration: a comparison of cationic liposomes versus aqueous solution formulations.

Abstract:

:The goal of this research was to evaluate the effectiveness of cationic liposomes for intranasal administration of proteins to the brain. Cationic liposomes were loaded with a model protein, ovalbumin (OVAL), and a 50 microg dose was administered intranasally to rats. In qualitative studies, liposomes were loaded with Alexa 488-OVAL and delivery was assessed by fluorescence microscopy. By 6 and 24 h after administration, Alexa 488-OVAL deposits were widely distributed throughout brain, with apparent cellular uptake in midbrain by 6 h after administration. In quantitative studies, liposomes were loaded with (111)In-OVAL, and distribution to brain and peripheral tissues was monitored by gamma counting at 1, 4, 6, and 24 h after administration. The highest brain concentrations were achieved at the shortest time point, 1 h, for both liposomal and aqueous OVAL. However, the liposomes yielded higher (111)In-OVAL concentrations in brain than (111)In-OVAL in PBS. Moreover, a 2 microg/microL form of liposomal OVAL yielded a higher percentage of dose in brain, and a lower percentage in stomach and intestines, than twice the volume of a 1 microg/microL preparation. Cationic liposomes may provide a novel, noninvasive strategy for delivery of neuroactive proteins to the brain for treatment of central nervous system disorders.

journal_name

J Pharm Sci

authors

Migliore MM,Vyas TK,Campbell RB,Amiji MM,Waszczak BL

doi

10.1002/jps.21939

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

1745-61

issue

4

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)30505-6

journal_volume

99

pub_type

杂志文章
  • Hybrid films from blends of chitosan and egg phosphatidylcholine for localized delivery of paclitaxel.

    abstract::Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20379

    authors: Grant J,Blicker M,Piquette-Miller M,Allen C

    更新日期:2005-07-01 00:00:00

  • Prediction of solubility in nonideal multicomponent systems using the UNIFAC group contribution model.

    abstract::There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740610

    authors: Ochsner AB,Sokoloski TD

    更新日期:1985-06-01 00:00:00

  • Design and development of adjuvant-active nonionic block copolymers.

    abstract::Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980072c

    authors: Newman MJ,Todd CW,Balusubramanian M

    更新日期:1998-11-01 00:00:00

  • Stable isotopic analysis of porcine, bovine, and ovine heparins.

    abstract::The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24134

    authors: Jasper JP,Zhang F,Poe RB,Linhardt RJ

    更新日期:2015-02-01 00:00:00

  • Antiangiogenic drugs: current knowledge and new approaches to cancer therapy.

    abstract::Angiogenesis--process of new blood-vessel growth from existing vasculature--is an integral part of both normal developmental processes and numerous pathologies such as cancer, ischemic diseases and chronic inflammation. Angiogenesis plays a crucial role facilitating tumour growth and the metastatic process, and it is ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.21286

    authors: Mauriz JL,González-Gallego J

    更新日期:2008-10-01 00:00:00

  • Evaluating a possible pharmacokinetic interaction between remifentanil and esmolol in the rat.

    abstract::Remifentanil (Ultiva) is a novel, ultra-short-acting opioid which has recently been approved for use as an analgesic during induction and maintenance of general anesthesia. Esmolol is a short-acting beta-blocker used during surgical procedures to reduce heart rate and blood pressure. Both drugs are metabolized by nons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970079e

    authors: Haidar SH,Moreton JE,Liang Z,Hoke JF,Muir KT,Eddington ND

    更新日期:1997-11-01 00:00:00

  • Cocrystalline Solids of Telaprevir with Enhanced Oral Absorption.

    abstract::A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24534

    authors: Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

    更新日期:2015-10-01 00:00:00

  • In Vivo Fluid Volume in Rat Gastrointestinal Tract: Kinetic Analysis on the Luminal Concentration of Nonabsorbable FITC-Dextran After Oral Administration.

    abstract::Previously, 1 mL of purified water (hyposmotic) or saline (isosmotic) which dissolved 200 μM of FITC-dextran (FD-4), a nonabsorbable marker, was orally administered to rats, and luminal concentration-time profile of FD-4 was directly measured. In this study, at first, luminal FD-4 concentration was measured after oral...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.03.005

    authors: Tanaka Y,Higashino H,Kataoka M,Yamashita S

    更新日期:2020-06-01 00:00:00

  • Therapeutic tolerance, hemodynamic effects, and oral dose kinetics of dilazep dihydrochloride in hypertensive patients.

    abstract::The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after administratio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780404

    authors: Sambhi MP,Kannan R,Thananopavarn C,Ookhtens M,Gudenzi M

    更新日期:1989-04-01 00:00:00

  • Physicochemical, crystallographic, thermal, and spectroscopic behavior of crystalline and X-ray amorphous ciclesonide.

    abstract::Single crystal structure experiments revealed that the orthorhombic needles of Ciclesonide crystallized in P2(1)2(1)2(1) space group with four independent molecules in the unit cell. Amorphous Ciclesonide was prepared by lyophilization and characterized in comparison with crystalline material by differential scanning ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21223

    authors: Feth MP,Volz J,Hess U,Sturm E,Hummel RP

    更新日期:2008-09-01 00:00:00

  • A mechanistic study of griseofulvin dissolution into surfactant solutions under laminar flow conditions.

    abstract::The in vivo dissolution of many poorly soluble drugs is enhanced by the action of surfactants secreted into the upper gastrointestinal (GI) tract. These substances may act by solubilizing individual drug molecules into two separate liquid phases: the free aqueous phase and a micellar phase in which the drug is incorpo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9604974

    authors: Rao VM,Lin M,Larive CK,Southard MZ

    更新日期:1997-10-01 00:00:00

  • A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.

    abstract::CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.10.035

    authors: Liu T,Gobburu JVS

    更新日期:2018-03-01 00:00:00

  • Thermodynamic evaluation of activated charcoal as a poison antidote by high-performance liquid chromatography. II: In vitro method for the evaluation of activated charcoal as a poison antidote.

    abstract::A previous report detailed the derivation and validation of an equation for calculating the Gibbs free energy of liquid-solid adsorption via high-performance liquid chromatography (HPLC). This study utilizes an improved form of that equation in conjunction with an in vitro model of solute adsorption to give an ordered...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770609

    authors: Kleeman WP,Bailey LC

    更新日期:1988-06-01 00:00:00

  • Protein adsorption, desorption, and aggregation mediated by solid-liquid interfaces.

    abstract::Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24429

    authors: Perevozchikova T,Nanda H,Nesta DP,Roberts CJ

    更新日期:2015-06-01 00:00:00

  • Adhesive tablet effective for treating canker sores in humans.

    abstract::A new mucoadhesive tablet, which releases natural active agents for pain reduction and rapid healing of canker sores, has been prepared and characterized. Adhesive tablets were prepared by compression molding of mixed powders of crosslinked polyacrylic acid and hydroxypropyl cellulose, absorbed with citrus oil and mag...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1002/jps.20193

    authors: Mizrahi B,Golenser J,Wolnerman JS,Domb AJ

    更新日期:2004-12-01 00:00:00

  • Viscosity and surface tension of dilute salicylic acid-cetrimide systems.

    abstract::The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600661236

    authors: Wan LS

    更新日期:1977-12-01 00:00:00

  • Modified cellulose II powder: preparation, characterization, and tableting properties.

    abstract::The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20747

    authors: de la Luz Reus Medina M,Kumar V

    更新日期:2007-02-01 00:00:00

  • Enhanced potency of human calcitonin when fibrillation is avoided.

    abstract::The peptide hormone calcitonin (CT) is a potent drug for the therapy of different bone diseases. Salmon CT (sCT) is reported to be more active than human CT (hCT). Human CT, but not sCT, has a strong tendency to aggregate and fibrillate in aqueous solutions. Recent investigations of the fibrillation mechanisms contrib...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600840610

    authors: Cudd A,Arvinte T,Das RE,Chinni C,MacIntyre I

    更新日期:1995-06-01 00:00:00

  • Engineering Stability, Viscosity, and Immunogenicity of Antibodies by Computational Design.

    abstract::In recent years, computational methods have garnered much attention in protein engineering. A large number of computational methods have been developed to analyze the sequences and structures of proteins and have been used to predict the various properties. Antibodies are one of the emergent protein therapeutics, and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2020.01.011

    authors: Kuroda D,Tsumoto K

    更新日期:2020-05-01 00:00:00

  • Molecular relaxation behavior and isothermal crystallization above glass transition temperature of amorphous hesperetin.

    abstract::The purpose of this paper was to investigate the relaxation behavior of amorphous hesperetin (HRN), using dielectric spectroscopy, and assessment of its crystallization kinetics above glass transition temperature (Tg ). Amorphous HRN exhibited both local (β-) and global (α-) relaxations. β-Relaxation was observed belo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23766

    authors: Shete G,Khomane KS,Bansal AK

    更新日期:2014-01-01 00:00:00

  • Pharmacokinetics of oral cephalosporins: cephradine cephalexin.

    abstract::A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600671033

    authors: Finkelstein E,Quintiliani R,Lee R,Bracci A,Nightingale CH

    更新日期:1978-10-01 00:00:00

  • A multiphase microscopic diffusion model for stratum corneum permeability. II. Estimation of physicochemical parameters, and application to a large permeability database.

    abstract::The full parameterization for the stratum corneum biphasic microtransport model presented previously in this Journal [95:620-648 (2006)] is developed through a combination of fundamental transport theory and calibration with existing data. Of the five microscopic transport properties, four (D(cor), K(cor/w), D(lip), K...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20883

    authors: Wang TF,Kasting GB,Nitsche JM

    更新日期:2007-11-01 00:00:00

  • Electron microscope study of effect of benzalkonium chloride and edetate disodium on cell envelope of Pseudomonas aeruginosa.

    abstract::Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650115

    authors: Richards RM,Cavill RH

    更新日期:1976-01-01 00:00:00

  • Solubility profiling of HIV protease inhibitors in human intestinal fluids.

    abstract::The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23698

    authors: Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

    更新日期:2013-10-01 00:00:00

  • Hypolipidemic activity of 3-N-(1',8'-Naphthalimido)propionic acid in rodents.

    abstract::3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730724

    authors: Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

    更新日期:1984-07-01 00:00:00

  • The Hypotonic Environmental Changes Affect Liposomal Formulations for Nose-to-Brain Targeted Drug Delivery.

    abstract::Systemic administration of drugs is ineffective in the treatment of central nervous system disorders because of the blood-brain barrier. Nasal administration has been suggested as an alternative administration route as drugs absorbed in the olfactory epithelium bypass the blood-brain barrier and reach the brain within...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.03.006

    authors: Wu IY,Nikolaisen TE,Škalko-Basnet N,di Cagno MP

    更新日期:2019-08-01 00:00:00

  • Mechanisms of corneal drug penetration. I: In vivo and in vitro kinetics.

    abstract::Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770103

    authors: Grass GM,Robinson JR

    更新日期:1988-01-01 00:00:00

  • Relationship between the crystallization rates of amorphous nifedipine, phenobarbital, and flopropione, and their molecular mobility as measured by their enthalpy relaxation and (1)H NMR relaxation times.

    abstract::Isothermal crystallization of amorphous nifedipine, phenobarbital, and flopropione was studied at temperatures above and below their glass transition temperatures (T(g)). A sharp decrease in the crystallization rate with decreasing temperature was observed for phenobarbital and flopropione, such that no crystallizatio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/(SICI)1520-6017(200003)89:3<408::AID-JPS11

    authors: Aso Y,Yoshioka S,Kojima S

    更新日期:2000-03-01 00:00:00

  • Kinetic and mechanistic studies of blue tetrazolium reaction with phenylhydrazines.

    abstract::The reaction kinetics of blue tetrazolium with selected arylhydrazines were investigated under pseudo-first-order conditions. The reaction rate constants were obtained at various temperatures, and the enthalpy (8.4-11.2 kcal/mole) and entropy (-38--45 eu) of activations were calculated. A Hammett plot yielded a straig...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670714

    authors: Biehl ER,Wooten R,Kenner CT,Graham RE

    更新日期:1978-07-01 00:00:00

  • Characterization of polymorphism of gepirone hydrochloride.

    abstract::Gepirone hydrochloride, an investigational anxiolytic drug, was found to have at least three polymorphic forms which melted at 180 degrees C (I), 212 degrees C (II), and 200 degrees C (III). Thermal analytical studies showed that forms I and II were an enantiotropic pair, as were forms I and III. Form III was monotrop...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600741004

    authors: Behme RJ,Brooke D,Farney RF,Kensler TT

    更新日期:1985-10-01 00:00:00