abstract：:Within the last decade, Quality by Design (QbD) has been getting increased attention in its implementation in the development of pharmaceutical drug products. Understanding of the impact of formulation composition and process on clinical performance is a centerpiece of QbD. Physiologically based pharmacokinetic modeli...

journal_title：Journal of pharmaceutical sciences

authors： Kesisoglou F

更新日期：2017-04-01 00:00:00

abstract：:Montelukast, a cysteinyl leukotriene type 1 receptor antagonist, exhibits secondary anti-inflammatory properties when used at higher concentrations. Low-molecular-weight heparin (LMWH) evokes pronounced anti-inflammatory effects by interrupting leukocyte adhesion and migration. We hypothesized that inhalable particles...

journal_title：Journal of pharmaceutical sciences

authors： Patel B,Rashid J,Gupta N,Ahsan F

更新日期：2017-04-01 00:00:00

abstract：:Repetitive administration is routinely used to maintain therapeutic drug levels, but previous studies have documented an accelerated blood clearance of some lipid-based delivery systems under these conditions. To assess the effect of repetitive administration, non-PEGylated lipoplexes (+/-0.5) were administered 4 time...

journal_title：Journal of pharmaceutical sciences

authors： Betker JL,Anchordoquy TJ

更新日期：2017-03-01 00:00:00

abstract：:Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2017-02-01 00:00:00

abstract：:We have previously reported the development of novel nanocapsules made of polyarginine (PArg) specifically designed for the delivery of small anticancer drugs into cells. Our goal, in this work, has been to investigate the potential of these nanocarriers for oral delivery of peptide anticancer drugs. To reach this obj...

journal_title：Journal of pharmaceutical sciences

authors： Lollo G,Gonzalez-Paredes A,Garcia-Fuentes M,Calvo P,Torres D,Alonso MJ

更新日期：2017-02-01 00:00:00

abstract：:To evaluate the potential of cell-penetrating peptide-based delivery of apoptosis-inducer gene in cancer therapy, a modified HIV-1 TAT peptide (dimerized TAT peptide, dTAT) was studied. The dTAT and plasmid DNA (pDNA) complexes (dTAT-pDNA) were condensed using calcium chloride (dTAT-pDNA-Ca2+). This simple nonviral fo...

journal_title：Journal of pharmaceutical sciences

authors： Ishiguro S,Alhakamy NA,Uppalapati D,Delzeit J,Berkland CJ,Tamura M

更新日期：2017-01-01 00:00:00

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...

journal_title：Journal of pharmaceutical sciences

authors： Samak YO,El Massik M,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 00:00:00

abstract：:The purpose of the present study was to develop guidance toward rational choice of blenders and processing conditions to make robust and high performing adhesive mixtures for dry-powder inhalers and to develop quantitative experimental approaches for optimizing the process. Mixing behavior of carrier (LH100) and Astra...

journal_title：Journal of pharmaceutical sciences

authors： Sarkar S,Minatovicz B,Thalberg K,Chaudhuri B

更新日期：2017-01-01 00:00:00

abstract：:This study aims at investigating factors influencing humidity-induced recrystallization of amorphous lactose, produced by co-spray drying with particles of cellulose nanocrystals or sodium montmorillonite. In particular, the focus is on how the nanoparticle shape and surface properties influence the nanometer to micro...

journal_title：Journal of pharmaceutical sciences

authors： Hellrup J,Mahlin D

更新日期：2017-01-01 00:00:00

abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...

journal_title：Journal of pharmaceutical sciences

authors： Teo SY,Yew MY,Lee SY,Rathbone MJ,Gan SN,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:The solubility of a drug is ultimately governed by its chemical potential as it is present in the undissolved solute. For a pharmaceutical amorphous solid dispersion (ASD), its solubility depends on the state and composition of the undissolved solute when the ASD is equilibrated with water. Concerning the undissolved ...

journal_title：Journal of pharmaceutical sciences

authors： Huang S,Mao C,Williams RO 3rd,Yang CY

更新日期：2016-12-01 00:00:00

abstract：:The positively charged amino acids are commonly used excipients in biopharmaceutical formulations for stabilization of therapeutic proteins, yet the mechanisms for their modulation of protein stability are poorly understood. In this study, both lysine and histidine are shown to affect the thermal stability of myoglobi...

journal_title：Journal of pharmaceutical sciences

authors： Platts L,Darby SJ,Falconer RJ

更新日期：2016-12-01 00:00:00

abstract：:The human immunodeficiency virus has infected millions of people and the epidemic continues to grow rapidly in some parts of the world. Antiretroviral (ARV) therapy has provided improved treatment and prolonged the life expectancy of patients. Moreover, there is growing interest in using ARVs to protect against new in...

journal_title：Journal of pharmaceutical sciences

authors： Kirtane AR,Langer R,Traverso G

更新日期：2016-12-01 00:00:00

abstract：:We report a programed drug delivery system that can tailor the release of anesthetic bupivacaine in a spatiotemporally controlled manner. The drug delivery system was developed through the combination of a collagen-based injectable hydrogel and 2 types of poly(lactic-co-glycolic acid) (PLGA) particles. As a rapid-rele...

journal_title：Journal of pharmaceutical sciences

authors： Dinh VV,Suh YS,Yang HK,Lim YT

更新日期：2016-12-01 00:00:00

abstract：:This work involves the study of the solid-phase and solution crystallization behavior of the N-methylephedrine enantiomers. A systematic investigation of the melt phase diagram of the enantiomeric N-methylephedrine system was performed considering polymorphism. Two monotropically related modifications of the enantiome...

journal_title：Journal of pharmaceutical sciences

authors： Tulashie SK,Polenske D,Seidel-Morgenstern A,Lorenz H

更新日期：2016-11-01 00:00:00

abstract：:AZD1175 and AZD2207 are 2 highly lipophilic compounds with a significant risk of not achieving therapeutic plasma concentrations due to solubility-limited absorption. The compounds have the same molecular weight and minimal structural differences. The aim of the present work was to investigate whether salts could be a...

journal_title：Journal of pharmaceutical sciences

authors： Tannergren C,Karlsson E,Sigfridsson K,Lindfors L,Ku A,Polentarutti B,Carlert S

更新日期：2016-11-01 00:00:00

abstract：:The objective of this study was to determine if a high Tg polymer (Eudragit(®) S100) could be used to stabilize amorphous domains of polyethylene oxide (PEO) and hence improve the stability of binary polymer systems containing celecoxib (CX). We propose a novel method of stabilizing the amorphous PEO solid dispersion ...

journal_title：Journal of pharmaceutical sciences

authors： Jones DS,Tian Y,Li S,Yu T,Abu-Diak OA,Andrews GP

更新日期：2016-10-01 00:00:00

abstract：:Previous studies have shown that protein storage stability in freeze-dried l-arginine-based systems improved in the presence of chloride ions. However, chloride ions reduced the glass transition temperature of the freeze concentrate (Tg') and made freeze drying more challenging. In this study, l-arginine was freeze dr...

journal_title：Journal of pharmaceutical sciences

authors： Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach P

更新日期：2016-10-01 00:00:00

abstract：:Amphiphilic cyclodextrins (CDs) are biocompatible derivatives of natural CDs and are able to form nanoparticles or polyplexes spontaneously. In this study, nanoparticles prepared from nonionic (6OCaproβCD) or cationic amphiphilic CD (PC βCDC6) were used comparatively to develop nanoparticles intended for breast cancer...

journal_title：Journal of pharmaceutical sciences

authors： Varan G,Öncül S,Ercan A,Benito JM,Ortiz Mellet C,Bilensoy E

更新日期：2016-10-01 00:00:00

abstract：:It is hypothesized that ferrocene (FC)-loaded nanocarriers (FC-NCs) are safe label-free contrast agents for cochlear biodistribution study by transmission electron microscopy (TEM). To test this hypothesis, after engineering, the poly(epsilon-caprolactone)/polyglycolide NCs are tested for stability with various types ...

journal_title：Journal of pharmaceutical sciences

authors： Youm I,Musazzi UM,Gratton MA,Murowchick JB,Youan BC

更新日期：2016-10-01 00:00:00

abstract：:In situ lipolysis and synchrotron small-angle X-ray scattering (SAXS) were used to directly detect and elucidate the solid-state form of precipitated fenofibrate from the digestion of a model lipid-based formulation (LBF). This method was developed in light of recent findings that indicate variability in solid-state f...

journal_title：Journal of pharmaceutical sciences

authors： Khan J,Hawley A,Rades T,Boyd BJ

更新日期：2016-09-01 00:00:00

abstract：:To relate the reported positive effect of food on the oral bioavailability of abiraterone to the intraluminal behavior of abiraterone acetate, an in vivo experiment was performed, in which duodenal fluids and plasma samples were collected from healthy volunteers after the administration of abiraterone acetate in faste...

journal_title：Journal of pharmaceutical sciences

authors： Geboers S,Stappaerts J,Mols R,Snoeys J,Tack J,Annaert P,Augustijns P

更新日期：2016-09-01 00:00:00

abstract：:Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...

journal_title：Journal of pharmaceutical sciences

authors： Ohta T,Hashida Y,Yamashita F,Hashida M

更新日期：2016-09-01 00:00:00

abstract：:α-Lipoic acid (ALA) is a powerful antioxidant valuable for prevention and treatment of ophthalmic complications such as diabetic keratopathy and retinopathy. The aim of this work was to develop micelle-based formulations that can enhance the solubility, stability, and corneal permeability of ALA. Compared to a convent...

journal_title：Journal of pharmaceutical sciences

authors： Alvarez-Rivera F,Fernández-Villanueva D,Concheiro A,Alvarez-Lorenzo C

更新日期：2016-09-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:The α-keto carboxylic acid, pyruvic acid (1) was found to be a very effective peroxide scavenger but is subject to an aldol-like self-condensation/polymerization reaction. The purpose of this study was to evaluate the hydrogen peroxide, H2O2, scavenging ability of 3-methyl-2-oxobutanoic acid (2), 4-methyl-2-oxopentano...

journal_title：Journal of pharmaceutical sciences

authors： Lopalco A,Stella VJ

更新日期：2016-09-01 00:00:00

abstract：:The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms ...

journal_title：Journal of pharmaceutical sciences

authors： Bukara K,Schueller L,Rosier J,Daems T,Verheyden L,Eelen S,Martens JA,Van den Mooter G,Bugarski B,Kiekens F

更新日期：2016-08-01 00:00:00

abstract：:This work establishes a predictive model that explicitly recognizes microstructural parameters in the description of the overall mass uptake and local gradients of moisture into tablets. Model equations were formulated based on local tablet geometry to describe the transient uptake of moisture. An analytical solution ...

journal_title：Journal of pharmaceutical sciences

authors： Klinzing GR,Zavaliangos A

更新日期：2016-08-01 00:00:00

abstract：:In this contribution, we present an analysis of the main parameters influencing the efficiency of the (1)H → (13)C multiple-contact cross-polarization nuclear magnetic resonance (NMR) experiment in the context of solid pharmaceutical materials. Using the optimum experimental conditions, quantitative (13)C NMR spectra ...

journal_title：Journal of pharmaceutical sciences

authors： Saïdi F,Taulelle F,Martineau C

更新日期：2016-08-01 00:00:00

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 00:00:00

abstract：:Carbamazepine is the first-line anti-epileptic drug for focal seizures and generalized tonic-clonic seizures. Although sustained-release formulations exist, an initial burst of drug release is still present and this results in side effects. Zero-order release formulations reduce fluctuations in serum drug concentratio...

journal_title：Journal of pharmaceutical sciences

authors： Lim SH,Chia SM,Kang L,Yap KY

更新日期：2016-07-01 00:00:00

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

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

更新日期：2016-07-01 00:00:00

abstract：:Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and al...

journal_title：Journal of pharmaceutical sciences

authors： Hoefer CC,Blair RH,Blanco JG

更新日期：2016-06-01 00:00:00

abstract：:Two generalized modes of erosion kinetics, that is, the power law mode and root type mode, respectively, were found to be able to better describe the reported weight loss data compared to the existing linear mode, for commonly used surface-eroding polymer microspheres. Based on the newly identified modes, a set of dru...

journal_title：Journal of pharmaceutical sciences

authors： You S,Yang Z,Wang CH

更新日期：2016-06-01 00:00:00

abstract：:It is understood that a potential issue for drugs with poor aqueous solubility is low oral absorption. If oral exposure issues arise when working with a low solubility drug candidate, the common action is to rely on enabling formulations to solve the issue. However, this approach becomes troublesome in the pre-clinica...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Sutherlin D,Pang J,Salphati L

更新日期：2016-06-01 00:00:00

abstract：:The ICH Q1B guidance and additional clarifying manuscripts provide the essential information needed to conduct photostability testing for pharmaceutical drug products in the context of manufacturing, packaging, and storage. As the previous 2 papers in this series highlight for drug products administered by injection (...

journal_title：Journal of pharmaceutical sciences

authors： Allain L,Baertschi SW,Clapham D,Foti C,Lantaff WM,Reed RA,Templeton AC,Tønnesen HH

更新日期：2016-05-01 00:00:00

abstract：:Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

journal_title：Journal of pharmaceutical sciences

authors： Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

更新日期：2016-04-01 00:00:00

abstract：:This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

journal_title：Journal of pharmaceutical sciences

authors： Wang G,Wang JJ,Li F,To SS

更新日期：2016-04-01 00:00:00

abstract：:In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...

journal_title：Journal of pharmaceutical sciences

authors： Krueger AB,Carnell P,Carpenter JF

更新日期：2016-04-01 00:00:00