Interactions of pluronic block copolymers on P-gp efflux activity: experience with HIV-1 protease inhibitors.

Abstract:

:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were conducted using MDCKII and LLC-PK1 cells transfected with human MDR1 to assess Pluronic modulation of PI efflux. Pluronic P85 inhibited both basal and nelfinavir-stimulated P-gp ATPase activity, while Pluronic F127 had no effect. In cell accumulation studies, Pluronic P85 restored the accumulation of nelfinavir in MDCKII-MDR1 cells while Pluronic F127 and F88 had no effect. Pluronic P85 increased saquinavir accumulation in wild-type and MDR1-transfected cells in both the MDCKII and LLC-PK1 cell models, suggesting inhibition of multiple transporters, including MRPs. In conclusion, this study provides evidence that a block-copolymer, Pluronic P85, effectively inhibits the interaction of P-gp with nelfinavir and saquinavir. These data indicate that effective inhibition of HIV-1 PI efflux by Pluronic P85 may influence the distribution of antiretroviral agents to sites protected by efflux mechanisms, such as the blood-brain barrier, and possibly increase the brain exposure of these drugs resulting in suppression of viral replication and reduction in the incidence of drug resistant mutants.

journal_name

J Pharm Sci

authors

Shaik N,Pan G,Elmquist WF

doi

10.1002/jps.21372

subject

Has Abstract

pub_date

2008-12-01 00:00:00

pages

5421-33

issue

12

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)32798-8

journal_volume

97

pub_type

杂志文章
  • Thermodynamics of the Enantiotropic Pharmaceutical Compound Benzocaine and Solubility in Pure Organic Solvents.

    abstract::The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.07.022

    authors: Cheuk D,Svärd M,Rasmuson ÅC

    更新日期:2020-11-01 00:00:00

  • Characterization of glucose-mediated insulin release from implantable polymers.

    abstract::We characterized a glucose-sensitive, controlled-release insulin delivery system. Insulin release rates increased when glucose was perfused in the release media surrounding the matrix. The system was composed of solid, particulate insulin, incorporated into an ethylene-vinyl acetate copolymer (EVAc) matrix. Feedback c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9600686

    authors: Brown LR,Edelman ER,Fischel-Ghodsian F,Langer R

    更新日期:1996-12-01 00:00:00

  • An Extrusion Spheronization Approach to Enable a High Drug Load Formulation of a Poorly Soluble Drug with a Low Melting Surfactant.

    abstract::Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24585

    authors: Tatavarti A,Kesisoglou F

    更新日期:2015-11-01 00:00:00

  • Prediction of onset of crystallization in amorphous pharmaceutical systems: phenobarbital, nifedipine/PVP, and phenobarbital/PVP.

    abstract::The aim of this work is to determine if a stability testing protocol based on the correlations between crystallization onset and relaxation time above the glass transition temperature (T(g)) can be used to predict the crystallization onsets in amorphous pharmaceutical systems well below their T(g). This procedure assu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22232

    authors: Caron V,Bhugra C,Pikal MJ

    更新日期:2010-09-01 00:00:00

  • Synthesis of N,N'-bis(3-substituted benzylideneaminopropyl)-piperazines and their anti-inflammatory, antiproteolytic, and anticonvulsant properties.

    abstract::Some N,N'-bis(3-substituted benzylideneaminopropyl) piperazines were synthesized and characterized by their sharp melting points and elemental analyses. These substituted piperazines possessed anti-inflammatory activity, and the protection afforded by these compounds against carrageenan-induced edema ranged from 23 to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650323

    authors: Chaturvedi AK,Sastry BV,Chaudhari A,Parmar SS

    更新日期:1976-03-01 00:00:00

  • Impact of glass corrosion on drug substance stability.

    abstract::The delamination of glass contact surfaces because of hydrolytic instability has been well documented. However, the lack of glass surface integrity can also lead to other undesirable outcomes prior to visible glass delamination. This work shows how the early stages of delamination, namely, glass corrosion, can influen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24069

    authors: Watkins MA,Iacocca RG,Shelbourn TL,Dong X,Stobba-Wiley C

    更新日期:2014-08-01 00:00:00

  • Physicochemical and pharmacokinetic characteristics of plasmid DNA/cationic liposome complexes.

    abstract::The objectives of this study were (i) to characterize the plasmid DNA encoding the chloramphenicol acetyltransferase reporter gene (pCAT) complexed with cationic liposomes (Lipofectin and LipofectACE) in terms of particle size and zeta potential, (ii) to compare pharmacokinetic characteristics, and (iii) to study the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600841102

    authors: Mahato RI,Kawabata K,Nomura T,Takakura Y,Hashida M

    更新日期:1995-11-01 00:00:00

  • Evaluating a possible pharmacokinetic interaction between remifentanil and esmolol in the rat.

    abstract::Remifentanil (Ultiva) is a novel, ultra-short-acting opioid which has recently been approved for use as an analgesic during induction and maintenance of general anesthesia. Esmolol is a short-acting beta-blocker used during surgical procedures to reduce heart rate and blood pressure. Both drugs are metabolized by nons...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970079e

    authors: Haidar SH,Moreton JE,Liang Z,Hoke JF,Muir KT,Eddington ND

    更新日期:1997-11-01 00:00:00

  • Recent Achievements and Current Interests in Research on the Characterization and Quality Control of Biopharmaceuticals in Japan.

    abstract::As reported in the previous commentary (Ishii-Watabe et al., J Pharm Sci 2017), the Japanese biopharmaceutical research group is promoting collaborative multilaboratory studies to evaluate and standardize new methodologies for biopharmaceutical characterization and quality control. We have conducted the studies and he...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.01.001

    authors: Ishii-Watabe A,Shibata H,Suetomo H,Ikeda Y,Telikepalli S,Kiyoshi M,Hayashi Y,Muto T,Tanaka Y,Ueda S,Iwura T,Saitoh S,Aoyama M,Harazono A,Hyuga M,Goda Y,Torisu T,Uchiyama S

    更新日期:2020-05-01 00:00:00

  • Properties and stability of a liquid crystal form of cyclosporine-the first reported naturally occurring peptide that exists as a thermotropic liquid crystal.

    abstract::A new solid-state form of cyclosporine produced by spray-drying exhibited characteristics consistent with a liquid crystal. No sharp diffraction peaks were observed by powder X-ray diffraction; however, analysis by both small-angle X-ray diffraction (SAXR) and microscopic under polarized light (PLM) confirmed the exis...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10444

    authors: Lechuga-Ballesteros D,Abdul-Fattah A,Stevenson CL,Bennett DB

    更新日期:2003-09-01 00:00:00

  • Effects of solvent polarity on the acid dissociation constants of benzoic acids.

    abstract::The pKa values of benzoic acid, p-methylbenzoic, and p-aminobenzoic acid (PABA) were determined by potentiometric titration in mixtures of 0-0.5 volume fractions of various cosolvents and water. The differences between the aqueous and semiaqueous pKa values were similar for the three solutes at a particular cosolvent-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600750217

    authors: Rubino JT,Berryhill WS

    更新日期:1986-02-01 00:00:00

  • Comprehensive high-performance liquid chromatographic methodology for the determination of thiothixene in bulk drug, finished product, and dissolution testing samples.

    abstract::An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760310

    authors: Severin G

    更新日期:1987-03-01 00:00:00

  • Determinants for in vivo antitumor effect of angiogenesis inhibitor SU5416 formulated in PEGylated emulsion.

    abstract::Angiogenesis, the sprouting of capillaries from preexisting ones, is essential for the sustained growth of solid tumors. In this study, we used SU5416, a hydrophobic molecule with potent tyrosine kinase inhibitor of type 2 receptor for vascular endothelial growth factor (VEGF), as PEGylated emulsion (SU5416-PE), and e...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24071

    authors: Ogawara K,Abe S,Un K,Yoshizawa Y,Kimura T,Higaki K

    更新日期:2014-08-01 00:00:00

  • Comparative pharmacokinetics of butylated hydroxyanisole and butylated hydroxytoluene in rabbits.

    abstract::The widespread use of butylated hydroxyanisole (I) and butylated hydroxytoluene (II) as food antioxidants recently has been criticized by the Food and Drug Administration because of their pharmacological and toxicological effects. Interest also has arisen recently in the use of these compounds as anticancer agents. Th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600691233

    authors: El-Rashidy R,Niazi S

    更新日期:1980-12-01 00:00:00

  • Control systems engineering in continuous pharmaceutical manufacturing. May 20-21, 2014 Continuous Manufacturing Symposium.

    abstract::This white paper provides a perspective of the challenges, research needs, and future directions for control systems engineering in continuous pharmaceutical processing. The main motivation for writing this paper is to facilitate the development and deployment of control systems technologies so as to ensure quality of...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.24311

    authors: Myerson AS,Krumme M,Nasr M,Thomas H,Braatz RD

    更新日期:2015-03-01 00:00:00

  • Effects of phenobarbital on the distribution pharmacokinetics and biological half-lives of model nonmicrosomal enzyme metabolizable sulfonamides in rats.

    abstract::The pharmacokinetics of sulfisoxazole and sulfanilamide were studied in control rats and in rats treated for 5 days with a daily 100 mg/kg ip dose of phenobarbital. These drugs represent the organic anionic and nonionized drugs, respectively, whose nonmicrosomal enzymatic metabolisms were unstimulated by phenobarbital...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710412

    authors: Nagwekar JB,Kundu S

    更新日期:1982-04-01 00:00:00

  • Preparation of pH-sensitive beads for NSAID using three-component gel systems.

    abstract::The aim of this study is to prepare novel pH-sensitive beads to obtain a gastric mucosa protective formulation and to ensure drug delivery into the intestine. Diclofenac sodium was used as a model drug. Bead formation was achieved by ionotropic gelation method using three-component gel system containing sodium alginat...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21713

    authors: Fenyvesi Z,Auner A,Schmalz D,Pásztor E,Csóka G,Gyires K,Marton S,Klebovich I,Antal I

    更新日期:2009-11-01 00:00:00

  • Absorption, distribution, and excretion of 14C-meglumine in rats and dogs after administration of 14C-meglumine salicylate.

    abstract::Meglumine labeled with carbon-14 was administered orally as 14C-meglumine salicylate to rats and dogs to study its distribution and excretion. The compound was incompletely absorbed; that which was absorbed was rapidly excreted in the urine. Peak blood levels were about 5-10 mug/ml in rats and 2-8 mug/ml in dogs. Tiss...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660124

    authors: Heeg JF,Born GS,Kessler WV,Shaw SM,Lange WE

    更新日期:1977-01-01 00:00:00

  • An examination of the thermodynamics of fusion, vaporization, and sublimation of (R,S)- and (R)-flurbiprofen by correlation gas chromatography.

    abstract::The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23094

    authors: Umnahanant P,Hasty D,Chickos J

    更新日期:2012-06-01 00:00:00

  • Barriers to nonviral gene delivery.

    abstract::The use of various synthetic lipids and polymers to deliver DNA for gene therapy applications has been the subject of intense examination for the last 15 years. Our understanding of the processes involved in the delivery of DNA, although still limited, can be described in terms of specific physical and chemical barrie...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.10286

    authors: Wiethoff CM,Middaugh CR

    更新日期:2003-02-01 00:00:00

  • Characterization of Factors Affecting Nanoparticle Tracking Analysis Results With Synthetic and Protein Nanoparticles.

    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

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.02.005

    authors: Krueger AB,Carnell P,Carpenter JF

    更新日期:2016-04-01 00:00:00

  • Enrichment of Relevant Oxidative Degradation Products in Pharmaceuticals With Targeted Chemoselective Oxidation.

    abstract::The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.059

    authors: Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

    更新日期:2019-04-01 00:00:00

  • Stability-indicating assay for phenylbutazone: high-performance liquid chromatographic determination of hydrazobenzene and azobenzene in degraded aqueous phenylbutazone solutions.

    abstract::A high-performance liquid chromatographic method was developed for the simultaneous determination of azobenzene, hydrazobenzene, and four other decomposition products in phenylbutazone injectable formulations. Separation was achieved on a C18 column, with 0.1 M Tris-citrate buffer (pH 5.25) and acetonitrile (52:48), a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731211

    authors: Fabre H,Hussam-Eddine N,Mandrou B

    更新日期:1984-12-01 00:00:00

  • Effect of the enantiomers of flurbiprofen, ibuprofen, and ketoprofen on intestinal permeability.

    abstract::Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960276y

    authors: Davies NM,Wright MR,Russell AS,Jamali F

    更新日期:1996-11-01 00:00:00

  • PATH's approach to product introduction in developing countries.

    abstract::Health interventions developed for wealthy nations are difficult to introduce in developing countries due to a lack of sufficient technological, financial, political, or infrastructural resources. Increasingly, however, product developers are creating new technologies that meet the needs of low-resource settings. Expe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21364

    authors: Harner-Jay C,Sherris J

    更新日期:2008-12-01 00:00:00

  • Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt.

    abstract::The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20400

    authors: Creek DJ,Chiu FC,Prankerd RJ,Charman SA,Charman WN

    更新日期:2005-08-01 00:00:00

  • Preparation and release characteristics of potassium chloride microcapsules.

    abstract::The release characteristics of potassium chloride was studied when it was coated with a selection of polymers; from the results obtained, a suitable batch was microencapsulated using a gelatin-gum arabic coacervate system. The microencapsulated product offers better controlled release for this drug when compared to st...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700413

    authors: Harris MS

    更新日期:1981-04-01 00:00:00

  • Microscale titrimetric and spectrophotometric methods for determination of ionization constants and partition coefficients of new drug candidates.

    abstract::This study describes the adaptation of conventional titrimetric and spectrophotometric techniques to a microscale for the determination of drug ionization constants (pKa) and partition coefficients (log P). The apparatus for determining pKa and compound purity (or equivalent weight) consists of a three-port conical gl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970057s

    authors: Morgan ME,Lui K,Anderson BD

    更新日期:1998-02-01 00:00:00

  • Release of polyionizable compounds from submicrometer oil-in-water emulsions.

    abstract::A novel, general, theoretical equation that describes the release of polyionizable compounds from submicrometer emulsions was derived and evaluated. The model accounts for simultaneous partitioning, interfacial activity, and adsorption to surfactant for n independent drug species and j surfactant species in a single e...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810504

    authors: Silvestri S,Wu LL,Bowser B

    更新日期:1992-05-01 00:00:00

  • Polyarginine Nanocapsules as a Potential Oral Peptide Delivery Carrier.

    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

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.09.029

    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