Mechanistic studies on effervescent-induced permeability enhancement.


PURPOSE:To determine the mechanism(s) by which effervescence induces penetration enhancement of a broad range of compounds ranging in size, structure, and other physiocochemical properties across rat and rabbit small intestinal epithelium. METHODS:Effervescent induced penetration enhancement was investigated in vitro by utilization of a modified Ussing chamber diffusion cell apparatus and in vivo by single-pass intestinal perfusion. RESULTS:Carbon dioxide (CO2) bubbling directly onto rabbit ileum epithelium induced an increase in drug permeability. Mechanistic studies indicated that effects due to CO2 bubble evolution, such as increased drug dissolution rates, mucus thinning/stripping, and pH buffer effects did not contribute to increases in drug flux. Cellular enzyme (5'-ND and LDH) and total protein release assays did not indicate cell membrane perturbation and/or damage. CO2 bubbling induced a reduction in transepithelial electrical resistance (TEER) indicating epithelial disruption due to a structural change of the paracellular pathway. This was further substantiated by a MW dependence on paracellular marker flux. In addition, tissue recovery was relatively rapid, approximately 20 min. CONCLUSIONS:CO2 bubbling directly onto the intestinal epithelium induced enhanced drug permeability due to an alteration of the paracellular pathway. This, in addition to fluid flow and membrane hydrophobicity concepts, may account for observed increases in drug flux.


Pharm Res


Pharmaceutical research


Eichman JD,Robinson JR




Has Abstract


1998-06-01 00:00:00












  • lontophoretic Devices for Drug Delivery.

    abstract::Transdermal drug delivery of ionized drugs can be enhanced by iontophoresis. Drug in the ionic form, contained in some reservoir, can be "phoresed" through the skin with a small current across two electrodes, one above the reservoir and one at a distal skin location. Positive ions can be introduced from the positive p...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Tyle P

    更新日期:1986-12-01 00:00:00

  • Microbial and mammalian metabolism studies of the semisynthetic antimalarial, anhydrodihydroartemisinin.

    abstract::Microbial metabolism studies of the semisynthetic antimalarial anhydrodihydroartemisinin (1), have shown that it is metabolized by a number of microorganisms. Large scale fermentation with Streptomyces lavendulae L-105 and Rhizopogon species (ATCC 36060) have resulted in the isolation of four microbial metabolites. Th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Khalifa SI,Baker JK,Rogers RD,el-Feraly FS,Hufford CD

    更新日期:1994-07-01 00:00:00

  • Improving the selectivity of HAV-peptides in modulating E-cadherin-E-cadherin interactions in the intercellular junction of MDCK cell monolayers.

    abstract:PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Makagiansar IT,Avery M,Hu Y,Audus KL,Siahaan TJ

    更新日期:2001-04-01 00:00:00

  • Probing beta relaxation in pharmaceutically relevant glasses by using DSC.

    abstract:PURPOSE:This study was conducted to demonstrate the use of differential scanning calorimetry (DSC) in detecting and measuring beta-relaxation processes in amorphous pharmaceutical systems. METHODS:DSC was employed to study amorphous samples of poly(vinylpyrrolidone) (PVP), indomethacin (IM), and ursodeoxycholic acid (...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Vyazovkin S,Dranca I

    更新日期:2006-02-01 00:00:00

  • The influence of regional deposition on the pharmacokinetics of pulmonary-delivered human growth hormone in rabbits.

    abstract::The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

    更新日期:1995-03-01 00:00:00

  • Pharmaceutical properties of loracarbef: the remarkable solution stability of an oral 1-carba-1-dethiacephalosporin antibiotic.

    abstract::Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Lor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Pasini CE,Indelicato JM

    更新日期:1992-02-01 00:00:00

  • Designer gene delivery vectors: molecular engineering and evolution of adeno-associated viral vectors for enhanced gene transfer.

    abstract::Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审


    authors: Kwon I,Schaffer DV

    更新日期:2008-03-01 00:00:00

  • Unconventional Passive Enhancement of Transdermal Drug Delivery: toward a Mechanistic Understanding of Penetration Enhancers Releasing from Acrylic Pressure-Sensitive Adhesive of Patches.

    abstract:PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Zeng L,Song W,He W,Zhang J,Wang Y,Bian J,Mao Z,Quan D,Liu J

    更新日期:2020-08-13 00:00:00

  • Dual Receptor Targeting Cell Penetrating Peptide Modified Liposome for Glioma and Breast Cancer Postoperative Recurrence Therapy.

    abstract:PURPOSE:Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Qiu Y,Yu Q,Liu Y,Tang J,Wang X,Lu Z,Xu Z,He Q

    更新日期:2018-04-26 00:00:00

  • High-performance liquid chromatographic (HPLC) assay using fluorescence detection for the simultaneous determination of gallopamil and norgallopamil in human plasma.

    abstract::Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: McLean AM,Babcock-Atkinson E,Rein K,Ruggirello DA,Gonzalez MA,Noonan PK

    更新日期:1987-08-01 00:00:00

  • Rapid aromatic hydrogen exchange in the antimalarial primaquine.

    abstract::Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: McChesney JD,Sarangan S

    更新日期:1984-07-01 00:00:00

  • Predicting skin permeability.

    abstract::Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Potts RO,Guy RH

    更新日期:1992-05-01 00:00:00

  • Oxaliplatin degradation in the presence of chloride: identification and cytotoxicity of the monochloro monooxalato complex.

    abstract:PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Jerremalm E,Hedeland M,Wallin I,Bondesson U,Ehrsson H

    更新日期:2004-05-01 00:00:00

  • The relationship of pKa and acute skin irritation in man.

    abstract::The relationship between pKa and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15-88 micrograms/cm2/hr). Skin irritation and pKa are correlated for pKa less than or equal to 4. Laser Doppler velocimetric assessment of skin ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Berner B,Wilson DR,Guy RH,Mazzenga GC,Clarke FH,Maibach HI

    更新日期:1988-10-01 00:00:00

  • The effect of formulation on the antimicrobial activity of cetylpyridinium chloride in candy based lozenges.

    abstract:PURPOSE:The purpose of this investigation was to determine the influence on the antimicrobial activity of cetylpyridinium chloride of the various components of the formulation of each of six candy based lozenges. METHODS:In vivo activity was investigated using six volunteers by determining the reduction in colony form...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章


    authors: Richards RM,Xing JZ,Weir LF

    更新日期:1996-04-01 00:00:00

  • Direct observation of single particle electrostatic charging by atomic force microscopy.

    abstract:PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Bunker MJ,Davies MC,James MB,Roberts CJ

    更新日期:2007-06-01 00:00:00

  • Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration.

    abstract:PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Nicolaides E,Symillides M,Dressman JB,Reppas C

    更新日期:2001-03-01 00:00:00

  • Absorptive-mediated endocytosis of an adrenocorticotropic hormone (ACTH) analogue, ebiratide, into the blood-brain barrier: studies with monolayers of primary cultured bovine brain capillary endothelial cells.

    abstract::The internalization of a neuromodulatory adrenocorticotropic hormone (ACTH) analogue, [125I]ebiratide (H-Met(O2)-Glu[125I]His-Phe-D-Lys-Phe-NH(CH2)2NH2), was examined in cultured monolayers of bovine brain capillary endothelial cells (BCEC). HPLC analysis of the incubation solution showed that [125I]ebiratide was not ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Terasaki T,Takakuwa S,Saheki A,Moritani S,Shimura T,Tabata S,Tsuji A

    更新日期:1992-04-01 00:00:00

  • Contribution of lysosomes to the subcellular distribution of basic drugs in the rat liver.

    abstract:PURPOSE:We examined the subcellular distribution of the basic drugs, chlorpromazine (CPZ), imipramine (IMP) and biperiden (BP), in rat liver, and evaluated the contribution of lysosome (Lys) to their intracellular distribution in comparison with that of mitochondria (Mit). METHODS:In an in vivo distribution, the conce...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Ishizaki J,Yokogawa K,Hirano M,Nakashima E,Sai Y,Ohkuma S,Ohshima T,Ichimura F

    更新日期:1996-06-01 00:00:00

  • Anticancer drug-loaded nanospheres based on biodegradable amphiphilic ε-caprolactone and carbonate copolymers.

    abstract:PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Yan GP,Zong RF,Li L,Fu T,Liu F,Yu XH

    更新日期:2010-12-01 00:00:00

  • Experimental design and efficient parameter estimation in preclinical pharmacokinetic studies.

    abstract::Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Ette EI,Howie CA,Kelman AW,Whiting B

    更新日期:1995-05-01 00:00:00

  • The effect of octanoic acid on the binding of the enantiomers of ibuprofen and naproxen to human serum albumin: a chromatographic implication.

    abstract:PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

    更新日期:1996-01-01 00:00:00

  • Can the enhanced renal clearance of antibiotics in cystic fibrosis patients be explained by P-glycoprotein transport?

    abstract:PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Susanto M,Benet LZ

    更新日期:2002-04-01 00:00:00

  • Evaluation of temperature-sensitive, indocyanine green-encapsulating micelles for noninvasive near-infrared tumor imaging.

    abstract:PURPOSE:Indocyanine green (ICG), an FDA-approved near infrared (NIR) dye, has potential application as a contrast agent for tumor detection. Because ICG binds strongly to plasma proteins and exhibits aqueous, photo, and thermal instability, its current applications are largely limited to monitoring blood flow. To addre...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Kim TH,Chen Y,Mount CW,Gombotz WR,Li X,Pun SH

    更新日期:2010-09-01 00:00:00

  • Evaluation of moisture sorption by tablet cores containing superdisintegrants during the aqueous film coating process.

    abstract::A physical-chemical analysis of the extent of sorption of water by tablets containing superdisintegrants was carried out following the aqueous film coating of formulated tablets. Characterization of the uncoated and coated tablet properties was conducted using thermogravimetric analysis, differential scanning calorime...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Pourkavoos N,Peck GE

    更新日期:1993-08-01 00:00:00

  • Effect of selective lipid extraction from different body regions on epidermal barrier function.

    abstract:PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Monteiro-Riviere NA,Inman AO,Mak V,Wertz P,Riviere JE

    更新日期:2001-07-01 00:00:00

  • Improvement in Thermal Stability of Sucralose by γ-Cyclodextrin Metal-Organic Frameworks.

    abstract:PURPOSE:To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS:Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loade...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Lv N,Guo T,Liu B,Wang C,Singh V,Xu X,Li X,Chen D,Gref R,Zhang J

    更新日期:2017-02-01 00:00:00

  • Physiologically based pharmacokinetic model for composite nanodevices: effect of charge and size on in vivo disposition.

    abstract:PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Mager DE,Mody V,Xu C,Forrest A,Lesniak WG,Nigavekar SS,Kariapper MT,Minc L,Khan MK,Balogh LP

    更新日期:2012-09-01 00:00:00

  • Polymer chemistry influences monocytic uptake of polyanhydride nanospheres.

    abstract:PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Ulery BD,Phanse Y,Sinha A,Wannemuehler MJ,Narasimhan B,Bellaire BH

    更新日期:2009-03-01 00:00:00

  • Investigations into the fate of inhaled salmon calcitonin at the respiratory epithelial barrier.

    abstract:PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Baginski L,Tewes F,Buckley ST,Healy AM,Bakowsky U,Ehrhardt C

    更新日期:2012-01-01 00:00:00