A Comparison of Aerosolization and Homogenization Techniques for Production of Alginate Microparticles for Delivery of Corticosteroids to the Colon.

Abstract:

:Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion into blank microparticles or by direct encapsulation. Homogenization method produced smaller microparticles (45-50 μm), compared to aerosolization (65-90 μm). High drug loadings (40% wt/wt) were obtained for diffusion-loaded aerosolized microparticles. Aerosolized microparticles suppressed drug release in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) prior to drug release in simulated colonic fluid (SCF) to a higher extent than homogenized microparticles. Microparticles prepared using aerosolization or homogenization (1 M CaCl2, diffusion loaded) released 5% and 17% of drug content after 2 h in SGF and 4 h in SIF, respectively, and 75% after 12 h in SCF. Thus, aerosolization and homogenization techniques show potential for producing alginate microparticles for colonic drug delivery in the treatment of inflammatory bowel disease.

journal_name

J Pharm Sci

authors

Samak YO,El Massik M,Coombes AGA

doi

10.1016/j.xphs.2016.08.015

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

208-216

issue

1

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)41678-3

journal_volume

106

pub_type

杂志文章
  • Rapid and simple GLC determination of valproic acid and ethosuximide in plasma of epileptic patients.

    abstract::A GLC method for the determination of valproic acid and ethosuximide in plasma was developed. The procedure involved a single solvent extraction of drugs from acidified plasma samples, followed by a GLC injection of the unconcentrated organic phase. This rapid, sensitive, specific, and reproducible method has been use...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710126

    authors: Riva R,Albani F,Baruzzi A

    更新日期:1982-01-01 00:00:00

  • Rapid determination of gold in whole blood of arthritis patients using flameless atomic absorption spectrophotometry.

    abstract::An assay for gold in whole blood of arthritis patients was developed using the graphite furnace atomic absorption spectrophotometer. This method involves no pretreatment of the whole blood except for simple dilution, thereby eliminating some variables and saving laboratory time and expense. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670943

    authors: Barrett MJ,DeFries R,Henderson WM

    更新日期:1978-09-01 00:00:00

  • Understanding Subcutaneous Tissue Pressure for Engineering Injection Devices for Large-Volume Protein Delivery.

    abstract::Subcutaneous injection allows for self-administration of monoclonal antibodies using prefilled syringes, autoinjectors, and on-body injector devices. However, subcutaneous injections are typically limited to 1 mL due to concerns of injection pain from volume, viscosity, and formulation characteristics. Back pressure c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.04.009

    authors: Doughty DV,Clawson CZ,Lambert W,Subramony JA

    更新日期:2016-07-01 00:00:00

  • Novel Insights to Enhance Therapeutics With Acyclovir in the Management of Herpes Simplex Encephalitis.

    abstract::Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2021.01.003

    authors: Gurgel Assis MS,Fernandes Pedrosa TC,de Moraes FS,Caldeira TG,Pereira GR,de Souza J,Ruela ALM

    更新日期:2021-01-13 00:00:00

  • Regulation of Tight-Junction Integrity by Insulin in an In Vitro Model of Human Blood-Brain Barrier.

    abstract::Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.04.036

    authors: Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

    更新日期:2017-09-01 00:00:00

  • Physical characterization of clostridium difficile toxins and toxoids: effect of the formaldehyde crosslinking on thermal stability.

    abstract::Nosocomial diarrhea and pseudomembranous colitis causing toxins A and B from Clostridium difficile were studied at pH 5-8 and over the temperature range of 10-85 degrees C. The proteins were crosslinked with formaldehyde to inactivate them to toxoid forms and permit their use as vaccines. Structural changes and aggreg...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21261

    authors: Salnikova MS,Joshi SB,Rytting JH,Warny M,Middaugh CR

    更新日期:2008-09-01 00:00:00

  • Computer modeling of adsorption on an activated charcoal surface.

    abstract::The molecular modeling program SYBYL was used to simulate the adsorption of various barbiturates by an activated charcoal surface. The compounds barbituric acid (BA), barbital (B), phenobarbital (PB), mephobarbital (M), and primidone (Pr) were modeled, and their structures were energetically minimized. These structure...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600831214

    authors: Wurster DE,Kolling WM,Knosp BM

    更新日期:1994-12-01 00:00:00

  • Inclusion of acitretin into cyclodextrins: phase solubility, photostability, and physicochemical characterization.

    abstract::Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10495

    authors: Liu X,Lin HS,Thenmozhiyal JC,Chan SY,Ho PC

    更新日期:2003-12-01 00:00:00

  • Study of morphology of reactive dissolution interface using fractal geometry.

    abstract::The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960059x

    authors: Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

    更新日期:1996-09-01 00:00:00

  • Explanation of the crystallization rate of amorphous nifedipine and phenobarbital from their molecular mobility as measured by (13)C nuclear magnetic resonance relaxation time and the relaxation time obtained from the heating rate dependence of the glass

    abstract::To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.1033

    authors: Aso Y,Yoshioka S,Kojima S

    更新日期:2001-06-01 00:00:00

  • Testosterone-independent down-regulation of Oct2 in the kidney medulla from a uranyl nitrate-induced rat model of acute renal failure: effects on distribution of a model organic cation, tetraethylammonium.

    abstract::Although acute renal failure (ARF) has been an area of extensive research in recent decades, our understanding of ARF is far from complete. Organic cations (OCs) are primarily excreted via vectorial transport by various renal organic cation transporters (OCTs). It is reasonable to assume that ARF may alter the express...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21442

    authors: Shim WS,Park JH,Ahn SJ,Han L,Jin QR,Li H,Choi MK,Kim DD,Chung SJ,Shim CK

    更新日期:2009-02-01 00:00:00

  • Protein aggregation and particle formation in prefilled glass syringes.

    abstract::The stability of therapeutic proteins formulated in prefilled syringes (PFS) may be negatively impacted by the exposure of protein molecules to silicone oil-water interfaces and air-water interfaces. In addition, agitation, such as that experienced during transportation, may increase the detrimental effects (i.e., pro...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23973

    authors: Gerhardt A,Mcgraw NR,Schwartz DK,Bee JS,Carpenter JF,Randolph TW

    更新日期:2014-06-01 00:00:00

  • Carrier-Mediated Transport of Nicotine Across the Inner Blood-Retinal Barrier: Involvement of a Novel Organic Cation Transporter Driven by an Outward H(+) Gradient.

    abstract::The present study was carried out to investigate the blood-to-retina transport of nicotine across the inner blood-retinal barrier (BRB). Using the in vivo vascular injection method, the blood-to-retina influx clearance of nicotine across the BRB was determined as 131 μL/(min?g retina), which is much higher than that o...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24453

    authors: Tega Y,Kubo Y,Yuzurihara C,Akanuma S,Hosoya K

    更新日期:2015-09-01 00:00:00

  • Pharmacokinetics of aniracetam and its metabolites in rats.

    abstract::The pharmacokinetics of aniracetam (AP), a new cognitive performance enhancer, and its main metabolites was investigated after intravenous (iv) and oral administrations to rat. The plasma levels of AP, 4-p-anisamidobutyric acid (ABA), and p-anisic acid (AA) were determined simultaneously by the HPLC method. The plasma...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970355p

    authors: Ogiso T,Iwaki M,Tanino T,Ikeda K,Paku T,Horibe Y,Suzuki H

    更新日期:1998-05-01 00:00:00

  • Characterization of thymoquinone binding to human α₁-acid glycoprotein.

    abstract::Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23138

    authors: Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

    更新日期:2012-07-01 00:00:00

  • Polymorphism of Alprazolam (Xanax): a review of its crystalline phases and identification, crystallographic characterization, and crystal structure of a new polymorph (form III).

    abstract::A new polymorphic form of Alprazolam (Xanax), 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo-[4,3-alpha][1,4]benzodiazepine, C(17)H(13)ClN(4), has been investigated by means of X-ray powder diffraction (XRPD), single crystal X-ray diffraction, and differential scanning calorimetry (DSC). This polymorphic form (form III...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20930

    authors: de Armas HN,Peeters OM,Van den Mooter G,Blaton N

    更新日期:2007-05-01 00:00:00

  • Surface interactions of monoclonal antibodies characterized by quartz crystal microbalance with dissipation: impact of hydrophobicity and protein self-interactions.

    abstract::Surface adsorption of two monoclonal antibodies (mAb1 and mAb2), with widely different hydrophobicity and self-association behavior in solution, was examined by quartz crystal microbalance with dissipation monitoring to understand how adsorption and protein self-interactions near the surface are impacted by their intr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22771

    authors: Oom A,Poggi M,Wikström J,Sukumar M

    更新日期:2012-02-01 00:00:00

  • Difference spectrophotometric determination of p-hydroxybenzoic acid in presence of its esters.

    abstract::A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670629

    authors: Fink DW,Fink HC,Tolan JW,Blodinger J

    更新日期:1978-06-01 00:00:00

  • Onset of enzyme induction with pregnenolone-16alpha-carbonitrile in male and female rats.

    abstract::Male and female rats treated with a single 20-mg/kg ip dose of pregnenolone-16alpha-carbonitrile (PCN) produced parallel increases in hepatic cytochrome P-450 and aniline hydroxylase activity. However, the onset of increase in aniline hydroxylase activity and cytochrome P-450 content was slower in male than female ani...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650436

    authors: Stohs SJ,Rosenberg H

    更新日期:1976-04-01 00:00:00

  • Control systems engineering in continuous pharmaceutical manufacturing. May 20-21, 2014 Continuous Manufacturing Symposium.

    abstract::This white paper provides a perspective of the challenges, research needs, and future directions for control systems engineering in continuous pharmaceutical processing. The main motivation for writing this paper is to facilitate the development and deployment of control systems technologies so as to ensure quality of...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.24311

    authors: Myerson AS,Krumme M,Nasr M,Thomas H,Braatz RD

    更新日期:2015-03-01 00:00:00

  • N-Acetyl-DL-penicillamine and acetaminophen toxicity in mice.

    abstract::N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690905

    authors: Zera RT,Nagasawa HT

    更新日期:1980-09-01 00:00:00

  • Survival of Staphylococcus aureus in oral administration liquid medicaments and influence of count medium on survival.

    abstract::The survival of Staphylococcus aureus was studied in 30 oral administration liquid medicaments (15 syrups and 15 solutions) to determine the effectiveness of the preservatives, the influence of the culture medium used in the enumeration of the surviving microorganisms, and the loss of the enzyme coagulase, phosphatase...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820211

    authors: Vivar C,de la Rosa C,Mosso A

    更新日期:1993-02-01 00:00:00

  • Determination of mianserin and metabolites in plasma by liquid chromatography with electrochemical detection.

    abstract::A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710812

    authors: Suckow RF,Cooper TB,Quitkin FM,Stewart JW

    更新日期:1982-08-01 00:00:00

  • Exploring a Kinetic Model Approach in Biopharmaceutics: Estimating the Fraction Absorbed of Orally Administered Drugs in Humans.

    abstract::Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.03.015

    authors: Chiang PC,Liu J,Fan P,Wong H

    更新日期:2018-07-01 00:00:00

  • Development of oral liquid dosage forms of acetazolamide.

    abstract::Two oral liquid dosage forms of acetazolamide have been developed. Using the solubility profiles, polyethylene glycol 400 (7%, v/v) was used as the solubilizing agent and propylene glycol (53%, v/v) as the cosolvent to keep acetazolamide in solution. Because of the bitter taste of acetazolamide, sweetening agents (sim...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790919

    authors: Parasrampuria J,Das Gupta V

    更新日期:1990-09-01 00:00:00

  • Colorimetric acetaminophen determination in pharmaceutical formulations.

    abstract::Different approaches for the colorimetric determination of acetaminophen, based on its coupling with diazotized o-nitroaniline, are described. Copper(II) chelation with the coupled compound makes the method highly selective. Sensitivity is increased when the acetaminophen assay is carried out indirectly through the de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680626

    authors: Belal S,Elsayed MA,El-Waliely A,Abdine H

    更新日期:1979-06-01 00:00:00

  • Drug efflux transport properties of 2',7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein acetoxymethyl ester (BCECF-AM) and its fluorescent free acid, BCECF.

    abstract::2',7'-Bis(2-carboxyethyl)-5(6)-carboxyfluorescein (BCECF) is a fluorescent probe used to examine multidrug resistance-associated protein (MRP) transporter activity in cells. BCECF is introduced into the cell as the nonfluorescent membrane permeable acetoxymethyl ester, BCECF-AM, where it is hydrolyzed to the membrane ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20018

    authors: Bachmeier CJ,Trickler WJ,Miller DW

    更新日期:2004-04-01 00:00:00

  • Acetaminophen inhibits intestinal p-glycoprotein transport activity.

    abstract::Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23673

    authors: Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

    更新日期:2013-10-01 00:00:00

  • Novel pH-sensitive physical hydrogels of carboxymethyl scleroglucan.

    abstract::A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22766

    authors: Corrente F,Paolicelli P,Matricardi P,Tita B,Vitali F,Casadei MA

    更新日期:2012-01-01 00:00:00

  • Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride.

    abstract::Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2018.03.009

    authors: Plöger GF,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Mehta MU,Parr A,Polli JE,Shah VP,Tajiri T,Dressman JB

    更新日期:2018-07-01 00:00:00