当前位置： SCI文献检索 > MOLECULAR PHARMACEUTICS期刊下所有文献 > In Vitro Characterization of the Biomimetic Properties of Poly(dimethylsiloxane) To Simulate Oral Drug Absorption.

In Vitro Characterization of the Biomimetic Properties of Poly(dimethylsiloxane) To Simulate Oral Drug Absorption.

Abstract：

:The potential use of poly(dimethylsiloxane) (PDMS) as an in vitro biomimetic analogue of the passive drug absorption process in the human gastrointestinal tract (GI) is assessed. PDMS is biomimetic because of similarities in small molecule transport, such as mechanism, ionization selectivity, lipophilicity. Nine molecular probes are used to evaluate the transport pathways and properties used to predict human oral absorption rates. The transport pathways through PDMS (bulk/pore) are analogous to transcellular (TCDT) and paracellular (PCDT) drug transport pathways. PDMS PCDT is assessed using positronium annihilation lifetime spectroscopy (PALS) and partition experiments; TCDT using diffusion and partition experiments. PALS determined that PDMS pores were uniform (D ∼ 0.85 nm), isolated, and void volume was unaffected by drug accumulation after equilibrium partitioning. Therefore, there is no PCDT or convective flow through PDMS. A strong linear correlation exists between predicted octanol-water partition coefficients and PDMS partition coefficients (LogKPDMS = 0.736 × LogPO-W - 0.971, R2 = 0.981). The pH-partition hypothesis is confirmed in PDMS using ibuprofen over pH 2-12. Diffusivity through PDMS is a function of lipophilicity and polar surface area K × DPDMS = 4.46 × 10-8 × e2.91×LogKPDMS(R2 = 0.963) and [Formula: see text] (R2 = 0.973). Varying the mass% of curing agent changed the lipophilicity and diffusivity (p < 0.02), but not practically (K × D = 2.23 × 10-5cm2s-1 vs 2.60 × 10-5cm2s-1), and does affect elastic modulus (3.2% = 0.3 MPa to 25% = 3.2 MPa).

journal_name

Mol Pharm

journal_title

Molecular pharmaceutics

authors

Sinko PD,Gidley D,Vallery R,Lamoureux A,Amidon GL,Amidon GE

doi

10.1021/acs.molpharmaceut.7b00798

subject

Has Abstract

pub_date

2017-12-04 00:00:00

pages

4661-4674

issue

12

eissn

1543-8384

issn

1543-8392

journal_volume

14

pub_type

杂志文章

相关文献

MOLECULAR PHARMACEUTICS文献大全
  • Delivering siRNA and Chemotherapeutic Molecules Across BBB and BTB for Intracranial Glioblastoma Therapy.

    abstract：:For aggressive brain glioblastoma, the therapy is significantly impaired by blood-brain barrier (BBB) and blood-tumor barrier (BTB). Choosing more than one target from the pool of tumor-stroma interactions is profoundly beneficial to therapeutic approaches. Thus, a multifunctional liposomal system based on anchoring t...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.6b00819

    authors： Yang ZZ,Gao W,Liu YJ,Pang N,Qi XR

    更新日期：2017-04-03 00:00:00

  • Efficient Click Synthesis of a Protonized and Reduction-Sensitive Amphiphilic Small-Molecule Prodrug Containing Camptothecin and Gemcitabine for a Drug Self-Delivery System.

    abstract：:Drug self-delivery systems consisting of small-molecule active drugs with nanoscale features for intracellular delivery without the need for additional polymeric carriers have drawn much attention recently. In this work, we proposed a highly efficient strategy to fabricate protonized and reduction-responsive self-asse...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.9b00349

    authors： Dong S,He J,Sun Y,Li D,Li L,Zhang M,Ni P

    更新日期：2019-09-03 00:00:00

  • High-Content Surface and Total Expression siRNA Kinase Library Screen with VX-809 Treatment Reveals Kinase Targets that Enhance F508del-CFTR Rescue.

    abstract：:The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.7b00928

    authors： Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

    更新日期：2018-03-05 00:00:00

  • Gastric and Duodenal Ethanol Concentrations after Intake of Alcoholic Beverages in Postprandial Conditions.

    abstract：:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crosso...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.7b00252

    authors： Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

    更新日期：2017-12-04 00:00:00

  • Development of a poly(d,l-lactic-co-glycolic acid) nanoparticle formulation of STAT3 inhibitor JSI-124: implication for cancer immunotherapy.

    abstract：:Constitutively activated signal transducer and activator of transcription-3 (STAT3) in tumor and dendritic cells (DCs) plays a critical role in tumor-induced immunosuppression. This is considered a major challenge in effective immunotherapy of cancer. Herein we describe the development of a polymeric nanocarrier for t...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp900145g

    authors： Molavi O,Mahmud A,Hamdy S,Hung RW,Lai R,Samuel J,Lavasanifar A

    更新日期：2010-04-05 00:00:00

  • Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs.

    abstract：:We have recently reported that by converting a perforin inhibitor into an l-type amino acid transporter 1 (LAT1)-utilizing prodrug its cellular uptake can be greatly increased. The aim of the present study was to determine the in vivo and brain pharmacokinetics of two perforin inhibitors and their LAT1-utilizing prodr...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.6b00217

    authors： Gynther M,Pickering DS,Spicer JA,Denny WA,Huttunen KM

    更新日期：2016-07-05 00:00:00

  • Oral delivery of doxorubicin using novel polyelectrolyte-stabilized liposomes (layersomes).

    abstract：:The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acr...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp300202c

    authors： Jain S,Patil SR,Swarnakar NK,Agrawal AK

    更新日期：2012-09-04 00:00:00

  • HER2-Targeted PET Imaging and Therapy of Hyaluronan-Masked HER2-Overexpressing Breast Cancer.

    abstract：:Human epidermal growth factor receptor 2 (HER2) is a biomarker in breast cancer, and its overexpression is required to initiate therapies using HER2-targeted antibodies. Although trastuzumab is one of the most effective therapeutic antibodies in HER2-overexpressing breast cancer, a significant number of patients do no...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.9b01091

    authors： Pereira PMR,Ragupathi A,Shmuel S,Mandleywala K,Viola NT,Lewis JS

    更新日期：2020-01-06 00:00:00

  • Synthesis, transport and mechanism of a type I prodrug: L-carnitine ester of prednisolone.

    abstract：:Aerosol glucocorticoid medications have become more and more important in treating BA (bronchial asthma). Although these agents are dosed to directly target airway inflammation, adrenocortical suppression and other systematic effects are still seen. To tackle this problem in a novel way, two L-carnitine ester derivati...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp100412z

    authors： Mo JX,Shi SJ,Zhang Q,Gong T,Sun X,Zhang ZR

    更新日期：2011-10-03 00:00:00

  • Generation and characterization of a new solid form of trehalose.

    abstract：:We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp400104b

    authors： Pyszczynski SJ,Munson EJ

    更新日期：2013-09-03 00:00:00

  • A novel hPepT1 stably transfected cell line: establishing a correlation between expression and function.

    abstract：:Stably transfected MDCK/hPepT1-V5&His clonal cell lines expressing varying levels of epitope-tagged hPepT1 protein were established to quantify the relationship between transgene hPepT1 expression levels and its functional kinetics in facilitating peptide and peptide-like drug uptake and transport in vitro. The hPepT1...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp034011l

    authors： Herrera-Ruiz D,Faria TN,Bhardwaj RK,Timoszyk J,Gudmundsson OS,Moench P,Wall DA,Smith RL,Knipp GT

    更新日期：2004-03-01 00:00:00

  • Delayed Sequential Co-Delivery of Gefitinib and Doxorubicin for Targeted Combination Chemotherapy.

    abstract：:There are an increasing number of studies showing the order of drug presentation plays a critical role in achieving optimal combination therapy. Here, a nanoparticle design is presented using ion pairing and drug-polymer conjugate for the sequential delivery of gefitinib (Gi) and doxorubicin (Dox) targeting epidermal ...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.7b00669

    authors： Zhou Z,Jafari M,Sriram V,Kim J,Lee JY,Ruiz-Torres SJ,Waltz SE

    更新日期：2017-12-04 00:00:00

  • Application of Nitroimidazole-Carbobane-Modified Phenylalanine Derivatives as Dual-Target Boron Carriers in Boron Neutron Capture Therapy.

    abstract：:Boron neutron capture therapy (BNCT) has received extensive attention as noninvasive cell-level oncotherapy for treating solid cancer tumors. However, boron-containing drugs such as l-boronophenylalanine (BPA) and sodium borocaptate have low boron content and/or poor tumor-targeting ability, limiting their application...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.9b00898

    authors： Li R,Zhang J,Guo J,Xu Y,Duan K,Zheng J,Wan H,Yuan Z,Chen H

    更新日期：2020-01-06 00:00:00

  • Ultrastable and Biofunctionalizable Conjugated Polymer Nanoparticles with Encapsulated Iron for Ferroptosis Assisted Chemodynamic Therapy.

    abstract：:We report the development of novel tumor-targeted conjugated polymer nanoparticles (CPNPs) carrying iron for chemodynamic therapy (CDT). Tumor cell killing proceeds through ferroptosis, a reactive oxygen species (ROS) mechanism that is not dependent on external activation by, for example, light, as is the case in phot...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.9b00737

    authors： Jasim KA,Gesquiere AJ

    更新日期：2019-12-02 00:00:00

  • Calcium condensed LABL-TAT complexes effectively target gene delivery to ICAM-1 expressing cells.

    abstract：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp100393j

    authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

    更新日期：2011-06-06 00:00:00

  • The effect of multiple N-methylation on intestinal permeability of cyclic hexapeptides.

    abstract：:Recent progress in peptide synthesis simplified the synthesis of multiple N-methylation of peptides. To evaluate how multiple N-methylation affects the bioavailability of peptides, a poly alanine cyclic hexapeptide library (n = 54), varying in the number of N-methyl (N-Me) groups (1-5 groups) and their position, was s...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp1003306

    authors： Ovadia O,Greenberg S,Chatterjee J,Laufer B,Opperer F,Kessler H,Gilon C,Hoffman A

    更新日期：2011-04-04 00:00:00

  • Multimodality imaging of breast cancer experimental lung metastasis with bioluminescence and a monoclonal antibody dual-labeled with 89Zr and IRDye 800CW.

    abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp300277f

    authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

    更新日期：2012-08-06 00:00:00

  • Chitosan-g-TPGS nanoparticles for anticancer drug delivery and overcoming multidrug resistance.

    abstract：:To overcome the P-glycoprotein (P-gp)-induced multidrug resistance (MDR) of cancer cells, a novel copolymer, chitosan-graft-D-α-tocopheryl polyethylene glycol 1000 (TPGS) (CT) was synthesized for doxorubicin (DOX) delivery by the P-gp inhibiting virtue of TPGS. DOX-loaded CT nanoparticles (NPs) were fabricated by a mo...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp400514t

    authors： Guo Y,Chu M,Tan S,Zhao S,Liu H,Otieno BO,Yang X,Xu C,Zhang Z

    更新日期：2014-01-06 00:00:00

  • The Influence of High Drug Loading in Xanthan Tablets and Media with Different Physiological pH and Ionic Strength on Swelling and Release.

    abstract：:The formation of a gel coat around xanthan (Xan) tablets, empty or loaded with pentoxifylline (PF), and its release in media differing in pH and ionic strength by NMR, MR imaging, and two release methods were studied. The T1 and T2 NMR relaxation times in gels depend predominantly on Xan concentration; the presence of...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.5b00955

    authors： Mikac U,Sepe A,Baumgartner S,Kristl J

    更新日期：2016-03-07 00:00:00

  • Inflammation Caused by Nanosized Delivery Systems: Is There a Benefit?

    abstract：:Secondary macrophage cytotoxicity induced by nanoparticles was described before. The study aim was to investigate the role of secondary cytotoxic effect in a macrophage-lung cancer coculture model after nanoparticle treatment in the presence and absence of anti-inflammatory drugs. An in vitro coculture model composed ...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.6b00530

    authors： Sarfraz M,Roa W,Bou-Chacra N,Löbenberg R

    更新日期：2016-09-06 00:00:00

  • Targeted delivery of Doxorubicin by folic acid-decorated dual functional nanocarrier.

    abstract：:Doxorubicin (DOX) is one of the most commonly used antineoplastic agents, but its clinical application is oftentimes coupled with severe side effects. Selective delivery of DOX to tumors via nanosized drug carrier represents an attractive approach to this problem. Previously, we developed a dual functional nanomicella...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp500389v

    authors： Lu J,Zhao W,Huang Y,Liu H,Marquez R,Gibbs RB,Li J,Venkataramanan R,Xu L,Li S,Li S

    更新日期：2014-11-03 00:00:00

  • Computational approach for fast screening of small molecular candidates to inhibit crystallization in amorphous drugs.

    abstract：:The applicability of the computational docking approach was investigated to create a novel method for quick additive screening to inhibit the crystallization taking place in amorphous drugs. Surface energy and attachment energy were utilized to recognize the morphologically most important crystal faces. The surfaces (...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp300135h

    authors： Pajula K,Lehto VP,Ketolainen J,Korhonen O

    更新日期：2012-10-01 00:00:00

  • Targeted and Synergic Glioblastoma Treatment: Multifunctional Nanoparticles Delivering Verteporfin as Adjuvant Therapy for Temozolomide Chemotherapy.

    abstract：:Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.8b01001

    authors： Pellosi DS,Paula LB,de Melo MT,Tedesco AC

    更新日期：2019-03-04 00:00:00

  • Modulation of Nanostructure-Based Lipopolysaccharide Active Immunotherapy in Cancer: Size and Composition Determine Short- and Long-Term Tolerability.

    abstract：:Despite holding promise for cancer immunotherapy, the strong pro-inflammatory properties of lipopolysaccharide (LPS) also account for severe localized and systemic side effects, restricting its administrable dosage and the possibility of chronic dosing. Herein, we exploited the surface-active properties of LPS molecul...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.9b00631

    authors： Shetab Boushehri MA,Yazeji T,Stein V,Lamprecht A

    更新日期：2019-11-04 00:00:00

  • Machine Learning Models of Antibody-Excipient Preferential Interactions for Use in Computational Formulation Design.

    abstract：:Preferential interactions of formulation excipients govern their impact on the stability properties of proteins in solution. The ability to predict these interactions without the need to perform experiments would enable formulation design to begin early in the development of a new antibody therapeutic. With that in mi...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.0c00629

    authors： Cloutier TK,Sudrik C,Mody N,Sathish HA,Trout BL

    更新日期：2020-09-08 00:00:00

  • Highly efficient one-pot labeling of new phosphonium cations with fluorine-18 as potential PET agents for myocardial perfusion imaging.

    abstract：:Lipophilic cations such as phosphonium salts can accumulate in mitochondria of heart in response to the negative inner-transmembrane potentials. Two phosphonium salts [(18)F]FMBTP and [(18)F]mFMBTP were prepared and evaluated as potential myocardial perfusion imaging (MPI) agents in this study. The cations were radiol...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp500216g

    authors： Zhao Z,Yu Q,Mou T,Liu C,Yang W,Fang W,Peng C,Lu J,Liu Y,Zhang X

    更新日期：2014-11-03 00:00:00

  • Toward understanding of toxic side effects of a polyene antibiotic amphotericin B: fluorescence spectroscopy reveals widespread formation of the specific supramolecular structures of the drug.

    abstract：:Amphotericin B (AmB) is a lifesaving polyene antibiotic used widely to treat deep-seated mycoses. Both the pharmaceutical effectiveness as well as toxic side effects depend on molecular organization of the drug. In the present study, we analyzed steady-state fluorescence, fluorescence anisotropy spectra, fluorescence ...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp300143n

    authors： Wasko P,Luchowski R,Tutaj K,Grudzinski W,Adamkiewicz P,Gruszecki WI

    更新日期：2012-05-07 00:00:00

  • Cannabinoid CB2 receptor as a new phototherapy target for the inhibition of tumor growth.

    abstract：:The success of targeted cancer therapy largely relies upon the selection of target and the development of efficient therapeutic agents that specifically bind to the target. In the current study, we chose a cannabinoid CB2 receptor (CB2R) as a new target and used a CB2R-targeted photosensitizer, IR700DX-mbc94, for phot...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp5001923

    authors： Jia N,Zhang S,Shao P,Bagia C,Janjic JM,Ding Y,Bai M

    更新日期：2014-06-02 00:00:00

  • Doxorubicin-loaded glycyrrhetinic acid modified recombinant human serum albumin nanoparticles for targeting liver tumor chemotherapy.

    abstract：:Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (D...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/mp500394v

    authors： Qi WW,Yu HY,Guo H,Lou J,Wang ZM,Liu P,Sapin-Minet A,Maincent P,Hong XC,Hu XM,Xiao YL

    更新日期：2015-03-02 00:00:00

  • Application of Solid-State NMR Relaxometry for Characterization and Formulation Optimization of Grinding-Induced Drug Nanoparticle.

    abstract：:The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (P...

    journal_title：Molecular pharmaceutics

    pub_type： 杂志文章

    doi：10.1021/acs.molpharmaceut.5b00781

    authors： Ueda K,Higashi K,Moribe K

    更新日期：2016-03-07 00:00:00