The effect of conformation on membrane permeability of an acyloxyalkoxy-linked cyclic prodrug of a model hexapeptide.

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...

journal_title：Pharmaceutical research

authors： Ogura J,Sato T,Higuchi K,Bhutia YD,Babu E,Masuda M,Miyauchi S,Rueda R,Pereira SL,Ganapathy V

更新日期：2019-04-17 00:00:00

abstract：PURPOSE:To investigate the effect of γ-irradiation of poly(lactic-co-glycolic acid) (PLGA)/Al(OH)₃/0 or 5 wt% diethyl phthalate (DEP) microspheres for active self-healing encapsulation of vaccine antigens. METHODS:Microspheres were irradiated with ⁶⁰Co at 2.5 and 1.8 MRad and 0.37 and 0.20 MRad/h. Encapsulation of tet...

journal_title：Pharmaceutical research

authors： Desai KG,Kadous S,Schwendeman SP

更新日期：2013-07-01 00:00:00

abstract：:The influence of the jejunal bloodflow on the absorption of theophylline was investigated. The bloodflow through a segment under investigation was varied by changing the systemic blood pressure by means of a donor blood infusion into the jugular vein or by an infusion of isoprenaline or levarterenol into a femoral vei...

journal_title：Pharmaceutical research

authors： Schurgers N,de Blaey CJ

更新日期：1984-01-01 00:00:00

abstract：PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...

journal_title：Pharmaceutical research

authors： Costantino HR,Firouzabadian L,Hogeland K,Wu C,Beganski C,Carrasquillo KG,Córdova M,Griebenow K,Zale SE,Tracy MA

更新日期：2000-11-01 00:00:00

abstract：PURPOSE:Locoregional recurrence is the most common complication after adenocarcinoma resection in the colon, despite adjuvant chemotherapy. Therapy efficacy could be improved if designed to target malignant cells by incorporating specific recognition factors in the drugs or the drug vehicles. The aim of this study was ...

journal_title：Pharmaceutical research

authors： Azab AK,Kleinstern J,Srebnik M,Rubinstein A

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:To investigate the feasibility of using the Aerosol Solvent Extraction System (ASES) to produce fine powders of recombinant human deoxyribonuclease (rhDNase), lysozyme-lactose and rhDNase-lactose powders from aqueous based solutions. METHODS:The ASES technique using high pressure carbon dioxide modified with e...

journal_title：Pharmaceutical research

authors： Bustami RT,Chan HK,Sweeney T,Dehghani F,Foster NR

更新日期：2003-12-01 00:00:00

abstract：:The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...

journal_title：Pharmaceutical research

authors： Garren KW,Topp EM,Repta AJ

更新日期：1989-11-01 00:00:00

abstract：PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

journal_title：Pharmaceutical research

authors： Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

更新日期：1996-05-01 00:00:00

abstract：PURPOSE:To characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of a new polyethylene glycol (PEG) conjugate formulation of interferon (IFN)-beta la following subcutaneous (SC) administration in monkeys. METHODS:Single SC injections of 0.3, 1, and 3 million international units (MIU)/kg of PEG-IFN-beta 1...

journal_title：Pharmaceutical research

authors： Mager DE,Neuteboom B,Jusko WJ

更新日期：2005-01-01 00:00:00

abstract：PURPOSE:The combination of morphine and gabapentin seems promising for the treatment of postoperative and neuropathic pain. Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions. The aim of this study was to evaluate whether co-administration of the two ...

journal_title：Pharmaceutical research

authors： Papathanasiou T,Juul RV,Gabel-Jensen C,Kreilgaard M,Lund TM

更新日期：2016-11-01 00:00:00

abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...

journal_title：Pharmaceutical research

authors： Valsami GN,Macheras PE,Koupparis MA

更新日期：1991-07-01 00:00:00

abstract：:Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...

journal_title：Pharmaceutical research

authors： Kobayashi S,Kondo S,Juni K

更新日期：1994-09-01 00:00:00

abstract：:Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...

journal_title：Pharmaceutical research

authors： Vrkljan M,Foster TM,Powers ME,Henkin J,Porter WR,Staack H,Carpenter JF,Manning MC

更新日期：1994-07-01 00:00:00

abstract：PURPOSE:Oral bioavailability for antisense oligonucleotides has recently been reported but the mechanistic details are not known. The proposed oral delivery of nucleic acids will, therefore, require an understanding of the membrane binding interactions, cell uptake and transport of oligonucleotides across the human gas...

journal_title：Pharmaceutical research

authors： Beck GF,Irwin WJ,Nicklin PL,Akhtar S

更新日期：1996-07-01 00:00:00

abstract：PURPOSE:This work describes a method for functionalisation of nanoparticle surfaces with hydrophilic "nano-shields" and the application of advanced surface characterisation to determine PEG amount and accumulation at the outmost 10 nm surface that is the predominant factor in determining protein and cellular interactio...

journal_title：Pharmaceutical research

authors： Ebbesen MF,Whitehead B,Ballarin-Gonzalez B,Kingshott P,Howard KA

更新日期：2013-07-01 00:00:00

abstract：:Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...

journal_title：Pharmaceutical research

authors： Yata N,Toyoda T,Murakami T,Nishiura A,Higashi Y

更新日期：1990-10-01 00:00:00

abstract：PURPOSE:The rapid oxidation of rofecoxib under alkaline conditions has been previously reported. The oxidation was reported to involve gamma-lactone ring opening to an alcohol, which further oxidized to a dicarboxyclic acid. The oxidation was suspected to be mediated by peroxy radicals. This work further investigates t...

journal_title：Pharmaceutical research

authors： Harmon PA,Biffar S,Pitzenberger SM,Reed RA

更新日期：2005-10-01 00:00:00

abstract：:The binding of diflunisal to hydroxypropyl-beta-cyclodextrin (HP beta CD), bovine serum albumin (BSA), human serum albumin (HSA), normal human plasma, and mixed solutions of HP beta CD/protein was studied at 25 degrees C, pH 7.4, by potentiometry using an electrode selective to diflunisal. The experimental data for di...

journal_title：Pharmaceutical research

authors： Sideris EE,Koupparis MA,Macheras PE

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:To determine whether a Protected Graft Copolymer (PGC) containing fatty acid can be used as a stabilizing excipient for GLP-1 and whether PGC/GLP-1 given once a week can be an effective treatment for diabetes. METHODS:To create a PGC excipient, polylysine was grafted with methoxypolyethyleneglycol and fatty ac...

journal_title：Pharmaceutical research

authors： Castillo GM,Reichstetter S,Bolotin EM

更新日期：2012-01-01 00:00:00

abstract：PURPOSE:Short linear peptides have a high potential for delivering various drugs with therapeutic potential, including nucleic acids. Recently, we have shown that the cationic amphipathic histidine-rich peptide LAH4 (KKALLALALHHLAHLALHLALALKKA) possesses high plasmid DNA delivery capacities. Since such peptides are tho...

journal_title：Pharmaceutical research

authors： Langlet-Bertin B,Leborgne C,Scherman D,Bechinger B,Mason AJ,Kichler A

更新日期：2010-07-01 00:00:00

abstract：PURPOSE:Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing ...

journal_title：Pharmaceutical research

authors： De Mohac LM,Caruana R,Cavallaro G,Giammona G,Licciardi M

更新日期：2020-02-19 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate the feasibility of delivering vapreotide, a somatostatin analogue, by transdermal iontophoresis. METHODS:In vitro experiments were conducted using dermatomed porcine ear skin and heat-separated epidermis. In addition to quantifying vapreotide transport into and across ...

journal_title：Pharmaceutical research

authors： Schuetz YB,Naik A,Guy RH,Vuaridel E,Kalia YN

更新日期：2005-08-01 00:00:00

abstract：:Antibody drug conjugates (ADCs) are a class of therapeutics that combine the target specificity of an antibody with the potency of a chemotherapeutic. This therapeutic strategy can significantly expand the therapeutic index of a chemotherapeutic by minimizing the systemic exposure and associated toxicity of the chemot...

journal_title：Pharmaceutical research

authors： Lin K,Tibbitts J

更新日期：2012-09-01 00:00:00

abstract：:Inhibition of efflux pumps is an emerging approach in cancer therapy and drug delivery. Since it has been discovered that polymeric pharmaceutical excipients such as Tweens or Pluronics can inhibit efflux pumps, various other polymers have been investigated regarding their potential efflux pump inhibitory activity. Am...

journal_title：Pharmaceutical research

authors： Werle M

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine the effect of experimental parameters on microinfusion through hollow microneedles into skin to optimize drug delivery protocols and identify rate-limiting barriers to flow. METHODS:Glass microneedles were inserted to a depth of 720-1080 microm into human cadaver skin to mi...

journal_title：Pharmaceutical research

authors： Martanto W,Moore JS,Kashlan O,Kamath R,Wang PM,O'Neal JM,Prausnitz MR

更新日期：2006-01-01 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 00:00:00

abstract：PURPOSE:To design and synthesize fatty acid-RGD peptide amphiphiles with ADA linker for their potential delivery of hydrophobic drugs like paclitaxel targeted to α(v)β(3) integrin overexpressing tumors. METHODS:Four amphiphiles - C16 or C18 fatty acid-RGD peptide and ADA linker were designed and synthesized. CMC, size...

journal_title：Pharmaceutical research

authors： Javali NM,Raj A,Saraf P,Li X,Jasti B

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:VLPs displaying tumor targeting single-chain variable fragments (VLP-rscFvs) which targets tumor-associated glycoprotein-72 (TAG-72) marker protein have a potential for immunotherapy against colon carcinoma tumors. In this study, scFvs anchored on VLPs using glycosylphosphatidylinositol (GPI) were prepared to t...

journal_title：Pharmaceutical research

authors： Deo VK,Yui M,Alam J,Yamazaki M,Kato T,Park EY

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:In this work, the alacepril thiolesterase, which catalyzes the hydrolyzing reaction of the thiolester linkage in alacepril and the conversion from alacepril to deacetylalacepril, was purified from rat liver cytosol and characterized. METHODS:A purification procedure for the thiolesterase consisted of ammonium ...

journal_title：Pharmaceutical research

authors： Usui S,Kubota M,Iguchi K,Kiho T,Sugiyama T,Katagiri Y,Hirano K

更新日期：2003-08-01 00:00:00