Effect of Extent of Supersaturation on the Evolution of Kinetic Solubility Profiles.

abstract：:The rate and extent of drug dissolution and absorption from solid oral dosage forms is highly dependent on the volume of liquid in the gastrointestinal tract (GIT). However, little is known about the time course of GIT liquid volumes after drinking a glass of water (8 oz), particularly in the colon, which is a targete...

journal_title：Molecular pharmaceutics

authors： Murray K,Hoad CL,Mudie DM,Wright J,Heissam K,Abrehart N,Pritchard SE,Al Atwah S,Gowland PA,Garnett MC,Amidon GE,Spiller RC,Amidon GL,Marciani L

更新日期：2017-08-07 00:00:00

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

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

更新日期：2016-03-07 00:00:00

abstract：:We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). S...

journal_title：Molecular pharmaceutics

authors： Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen M

更新日期：2017-09-05 00:00:00

abstract：:Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment...

journal_title：Molecular pharmaceutics

authors： Zhou QT,Sun SP,Chan JG,Wang P,Barraud N,Rice SA,Wang J,Li J,Chan HK

更新日期：2015-08-03 00:00:00

abstract：:In this paper, we investigate the release of two drugs, nicotine and caffeine, from poly epsilon-caprolactone (PCL) matrices, as a model for the delivery of highly hydrophilic drugs. Since PCL does not degrade over the period of our experiments (<30 days), drug diffusion through the matrix is expected to be the domina...

journal_title：Molecular pharmaceutics

authors： Rosenberg R,Devenney W,Siegel S,Dan N

更新日期：2007-11-01 00:00:00

abstract：:Supersaturable active pharmaceutical ingredients (sAPI), such as salts, cocrystals, and amorphous solids, can form supersaturated solutions after dissolving in the gastrointestinal fluids. However, there are cases in which supersaturation is not observed in an in vitro nonsink dissolution test. The purpose of the pres...

journal_title：Molecular pharmaceutics

authors： Oki J,Watanabe D,Uekusa T,Sugano K

更新日期：2019-04-01 00:00:00

abstract：:Protein drugs play an important role in modern day medicine. Typically, these proteins are formulated as liquids requiring cold chain processing. To circumvent the cold chain and achieve better storage stability, these proteins can be dried in the presence of carbohydrates. We demonstrate that thermal gradient mid- an...

journal_title：Molecular pharmaceutics

authors： Mensink MA,Šibík J,Frijlink HW,van der Voort Maarschalk K,Hinrichs WLJ,Zeitler JA

更新日期：2017-10-02 00:00:00

abstract：:5P12-RANTES is a recently developed chemokine analogue that has shown high level protection from SHIV infection in macaques. However, the feasibility of using 5P12-RANTES as a long-term HIV prevention agent has not been explored partially due to the lack of available delivery devices that can easily be modified for lo...

journal_title：Molecular pharmaceutics

authors： Wang NX,Sieg SF,Lederman MM,Offord RE,Hartley O,von Recum HA

更新日期：2013-10-07 00:00:00

abstract：:In this study, a d-glucosamine derivative with an isonitrile group (CN5DG) was synthesized and it was chosen to coordinate with 99mTc for preparing 99mTc-CN5DG. 99mTc-CN5DG could be readily obtained with high radiochemical purity (>95%) and had great in vitro stability and metabolic stability in urine. The radiotracer...

journal_title：Molecular pharmaceutics

authors： Zhang X,Ruan Q,Duan X,Gan Q,Song X,Fang S,Lin X,Du J,Zhang J

更新日期：2018-08-06 00:00:00

abstract：:Hydrophilic matrices are an effective option for oral controlled release but can face challenges in terms of bioavailability and efficacy when used in conjunction with poorly soluble, weakly basic drugs. Attenuated total reflectance Fourier transform infrared (ATR-FTIR) imaging provides dynamic information relating to...

journal_title：Molecular pharmaceutics

authors： Zahoor FD,Mader KT,Timmins P,Brown J,Sammon C

更新日期：2020-04-06 00:00:00

abstract：:Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacr...

journal_title：Molecular pharmaceutics

authors： Sola-Barrado B,M Leite D,Scarpa E,Duro-Castano A,Battaglia G

更新日期：2020-12-07 00:00:00

abstract：:Diabetic wounds are a worldwide health problem causing extremely heavy public health burden and require effective treatment. Optimal strategies for treating nonhealing diabetic wounds include stem-cell-based therapy and delivery of novel drug substances, such as functional microRNAs (miRNAs); however, miRNA easily deg...

journal_title：Molecular pharmaceutics

authors： Lv Q,Deng J,Chen Y,Wang Y,Liu B,Liu J

更新日期：2020-05-04 00:00:00

abstract：:In previous studies, we developed a new technique (ionic gelation vibrational jet flow; IGVJF) in order to encapsulate pancreatic β-cells, for insulin in vivo delivery, and diabetes treatment. The fabricated microcapsules showed good morphology but limited cell functions. Thus, this study aimed to optimize the IGVJF t...

journal_title：Molecular pharmaceutics

authors： Mooranian A,Negrulj R,Takechi R,Jamieson E,Morahan G,Al-Salami H

更新日期：2017-08-07 00:00:00

abstract：:The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

journal_title：Molecular pharmaceutics

authors： Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

更新日期：2020-06-01 00:00:00

abstract：:Ipratropium bromide, an anticholinergic drug used for the treatment of asthma and chronic obstructive pulmonary disease, has low oral bioavailability, but systemic exposure, superior to oral administration, can be achieved by inhalation. Therefore, we investigated the pulmonary absorption mechanism of ipratropium usin...

journal_title：Molecular pharmaceutics

authors： Nakamura T,Nakanishi T,Haruta T,Shirasaka Y,Keogh JP,Tamai I

更新日期：2010-02-01 00:00:00

abstract：:The tendency of highly supersaturated solutions of poorly water-soluble drugs to undergo liquid-liquid phase separation (LLPS) into drug-rich and water-rich phases when the concentration exceeds the amorphous solubility, for example, during dissolution of some amorphous solid dispersions, is thought to be advantageous...

journal_title：Molecular pharmaceutics

authors： Hate SS,Reutzel-Edens SM,Taylor LS

更新日期：2019-01-07 00:00:00

abstract：:Dry powders from aqueous dispersions, formed by antisolvent precipitation, dissolved to form solutions with supersaturation values up to 12 in 10 min at pH 6.8 with sodium dodecyl sulfate micelles. Itraconazole/hydroxypropylmethylcellulose (HPMC) aqueous particle dispersions were salt flocculated and filtered to produ...

journal_title：Molecular pharmaceutics

authors： Matteucci ME,Paguio JC,Miller MA,Williams RO 3rd,Johnston KP

更新日期：2009-03-01 00:00:00

abstract：:Oxidative stress and inflammation are intertwined contributors to numerous acute vascular pathologies. A novel dual bioactive nanoparticle with antioxidant/anti-inflammatory properties was developed based on the interactions of tocopherol phosphate and the manganese porphyrin SOD mimetic, MnTMPyP. The size and drug in...

journal_title：Molecular pharmaceutics

authors： Howard MD,Hood ED,Greineder CF,Alferiev IS,Chorny M,Muzykantov V

更新日期：2014-07-07 00:00:00

abstract：:Paracetamol has been one of the most commonly used and prescribed analgesic drugs for more than a hundred years. Despite being generally well tolerated, it can result in high liver toxicity when administered in specific conditions, such as overdose, or in vulnerable individuals. We have synthesized and characterized a...

journal_title：Molecular pharmaceutics

authors： Sodano F,Lazzarato L,Rolando B,Spyrakis F,De Caro C,Magliocca S,Marabello D,Chegaev K,Gazzano E,Riganti C,Calignano A,Russo R,Rimoli MG

更新日期：2019-10-07 00:00:00

abstract：:The complement system plays an important role in host innate immunity, and its activation can be exploited as a potential strategy for vaccine adjuvants. Herein, a pH-responsive micellar vaccine platform (COOH-NPs) was developed using a carboxyl-modified diblock copolymer of poly(2-ethyl-2-oxazoline)-poly(d,l-lactide)...

journal_title：Molecular pharmaceutics

authors： Li C,Lu Y,Chen Q,Hu H,Zhao X,Qiao M,Chen D

更新日期：2019-06-03 00:00:00

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 00:00:00

abstract：:Reversible aqueous lipidization (REAL) at the interdisulfide bond has been shown to improve the deliverability of some peptide drugs. Recently, we developed a nonreversible aqueous lipidization method targeted at the interdisulfide bond of salmon calcitonin (sCT). The resultant derivative had comparable hypocalcemic a...

journal_title：Molecular pharmaceutics

authors： Cheng W,Lim LY

更新日期：2008-07-01 00:00:00

abstract：:Porous silicon microparticles presenting pathogen-associated molecular patterns mimic pathogens, enhancing internalization of the microparticles and activation of antigen presenting dendritic cells. We demonstrate abundant uptake of microparticles bound by the TLR-4 ligands LPS and MPL by murine bone marrow-derived de...

journal_title：Molecular pharmaceutics

authors： Meraz IM,Melendez B,Gu J,Wong ST,Liu X,Andersson HA,Serda RE

更新日期：2012-07-02 00:00:00

abstract：:Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...

journal_title：Molecular pharmaceutics

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 00:00:00

abstract：:Deferoxamine mesylate (DFO) is an FDA-approved, hexadentate iron chelator routinely used to alleviate systemic iron burden in thalassemia major and sickle cell patients. Iron accumulation in these disease states results from the repeated blood transfusions required to manage these conditions. Iron accumulation has als...

journal_title：Molecular pharmaceutics

authors： Farr AC,Xiong MP

更新日期：2021-02-01 00:00:00

abstract：:Peripheral arterial disease (PAD) consists of a persistent obstruction of lower-extremity arteries further from the aortic bifurcation attributable to atherosclerosis. PAD is correlated with an elevated risk of morbidity and mortality as well as of deterioration of the quality of life with claudication and chronic leg...

journal_title：Molecular pharmaceutics

authors： Ferreira CA,Hernandez R,Yang Y,Valdovinos HF,Engle JW,Cai W

更新日期：2018-08-06 00:00:00

abstract：:The Flory-Huggins interaction parameter has been shown to be useful in predicting the thermodynamic miscibility of a polymer and a small molecule in a binary mixture. In the present paper, this concept was extended and evaluated to determine whether or not the Flory-Huggins interaction parameter can be applied to smal...

journal_title：Molecular pharmaceutics

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

更新日期：2010-06-07 00:00:00

abstract：:Major obstacles in the development of new therapeutic anticancer drugs are the low bioavailability of hydrophilic substances and the nonspecific toxicity toward healthy tissues. As such, cell-targeting oligopeptides have emerged as attractive drug delivery vehicles for a variety of different types of cargo. The recent...

journal_title：Molecular pharmaceutics

authors： Liu Y,Steiniger SC,Kim Y,Kaufmann GF,Felding-Habermann B,Janda KD

更新日期：2007-05-01 00:00:00

abstract：:Although nitric oxide (NO) is a bactericidal component of the macrophage's innate response to intracellular infections such as tuberculosis (TB), prolonged inhalation of NO gas has little benefit in chemotherapy of TB. The impact of controlled release of NO through intracellular delivery of NO donors to macrophages in...

journal_title：Molecular pharmaceutics

authors： Verma RK,Singh AK,Mohan M,Agrawal AK,Verma PR,Gupta A,Misra A

更新日期：2012-11-05 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 00:00:00