Journal of Pharmaceutical Sciences

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  1. Echogenic liposome compositions for increased retention of ultrasound reflectivity at physiologic temperature.

    Journal of Pharmaceutical Sciences 97(6):2242 (2008) PMID 17894368 PMCID PMC3119526

    Targetable echogenic liposomes (ELIP) for ultrasound enhancement of atheroma have recently been developed; however, their retention of echogenicity at physiological temperature is less than desirable. The purpose of this study was to improve ELIP stability and increase clinical potential. The ap...
  2. Combination particles containing salmeterol xinafoate and fluticasone propionate: Formulation and aerodynamic assessment.

    Journal of Pharmaceutical Sciences 97(6):2299 (2008) PMID 17879293

    A precipitation process is used to produce combined particles consisting of two antiasthmatic drugs: salmeterol xinafoate and fluticasone propionate. To control the crystallisation of these particles, a micromixer is used to mix solvent and antisolvent flow. To produce particles in the respirabl...
  3. Stable-form screening: overcoming trace impurities that inhibit solution-mediated phase transformation to the stable polymorph of sulfamerazine.

    Journal of Pharmaceutical Sciences 97(6):2130 (2008) PMID 17879974

    Solution-mediated phase transformation (SMPT) has been used as a focused technique to rapidly identify the stable polymorph of a given substance. Despite ample precedence for acetonitrile being a good solvent for SMPT of sulfamerazine (SMZ), samples from specific lots of SMZ failed to convert fr...
  4. Solvent diversity in polymorph screening.

    Journal of Pharmaceutical Sciences 97(6):2145 (2008) PMID 17847073

    Selecting a diverse set of solvents to be included in polymorph screening assignments can be a challenging task. As an aid to decision making, a database of 218 organic solvents with 24 property descriptors was explored and visualized using multivariate tools. The descriptors included, among oth...
  5. Modifications in low-density lipoprotein receptor expression affects Cyclosporin A cellular uptake and cytotoxicity.

    Journal of Pharmaceutical Sciences 97(6):2350 (2008) PMID 17823952

    The purpose of this study was to test the effect of modulating the expression of the human low-density lipoprotein receptor (LDLr) in human embryonic kidney (293T) cells on Cyclosporin A (CsA) cellular uptake and CsA-mediated cytotoxicity. LDLr expression was modulated using RNA interference (RN...
  6. Effect of structural relaxation on the preparation and drug release behavior of poly(lactic-co-glycolic)acid microparticle drug delivery systems.

    Journal of Pharmaceutical Sciences 97(6):2022 (2008) PMID 17828755

    Control of burst release is a major challenge in the development of poly(lactide-co-glycolide) (PLGA) microparticle drug delivery systems. It has been well-documented in previous literature that formulation and processing variables determine particle morphology, which in turn, governs drug diffu...
  7. ABCB1 G1199A polymorphism and ovarian cancer response to paclitaxel.

    Journal of Pharmaceutical Sciences 97(6):2045 (2008) PMID 17828752

    P-glycoprotein (P-gp), encoded by the ABCB1 gene, confers multi-drug resistance to a variety of antineoplastic agents, for example, paclitaxel. Recently, the G1199T/A polymorphism in the ABCB1 gene was shown to be important for the function of P-gp as well as for the resistance to several chemot...
  8. Evaluating computational predictions of the relative stabilities of polymorphic pharmaceuticals.

    Journal of Pharmaceutical Sciences 97(6):2121 (2008) PMID 17828731

    The ability of computational methods to describe the relative energies of polymorphic pharmaceuticals is investigated for a diverse array of compounds. The initial molecular geometries were taken from crystal structures, and energy differences between polymorphic pairs were calculated with vario...
  9. Rapid throughput screening of apparent KSP values for weakly basic drugs using 96-well format.

    Journal of Pharmaceutical Sciences 97(6):2080 (2008) PMID 17879292

    A rapid-throughput screening assay was developed to estimate the salt solubility parameter, K(SP), with a minimal quantity of drug. This assay allows for early evaluation of salt limited solubility with a large number of counter-ions and biologically promising drug leads. Drugs dissolved (typica...
  10. Inhibition of aggregation of aluminum hydroxide adjuvant during freezing and drying.

    Journal of Pharmaceutical Sciences 97(6):2049 (2008) PMID 17879291

    Aluminum-salt adjuvants are widely used to increase immunogenicity of recombinant protein vaccines. However, when vaccines formulated with these adjuvants are frozen or lyophilized, losses of efficacy are often reported. This loss of potency is usually attributed to the aggregation of adjuvant p...
  11. Prediction of drug tissue to plasma concentration ratios using a measured volume of distribution in combination with lipophilicity.

    Journal of Pharmaceutical Sciences 97(6):2324 (2008) PMID 17724666

    One of the drug specific parameters needed in physiologically based pharmacokinetic (PBPK) models is the tissue to plasma drug concentration ratios (K(p) values). The aim of this study was to develop an empirical method for predicting K(p) values using a preclinically determined in vivo volume o...
  12. Quality control of protease inhibitors.

    Journal of Pharmaceutical Sciences 97(6):2012 (2008) PMID 17828738

    Protease inhibitors (PIs) are potent competitive inhibitors of the human immunodeficiency virus (HIV) widely used in the treatment of the acquired immune deficiency syndrome (AIDS) and prescribed in combination with other antiretroviral drugs. So far ten PIs were approved by the United States Fo...
  13. Conformation and side chains environments of recombinant human interleukin-1 receptor antagonist (rh-IL-1ra) probed by raman, raman optical activity, and UV-resonance Raman spectroscopy.

    Journal of Pharmaceutical Sciences 97(6):2228 (2008) PMID 17914732

    The conformation and local environments of the side chains cysteines and aromatics of recombinant human interleukin-1 receptor antagonist (rh-IL-1ra) have been studied by visible Raman, Raman optical activity (ROA) and UVRR spectroscopy. The results reveal that the secondary structure of rh-IL-1...
  14. Data mining of fractured experimental data using neurofuzzy logic-discovering and integrating knowledge hidden in multiple formulation databases for a fluid-bed granulation process.

    Journal of Pharmaceutical Sciences 97(6):2091 (2008) PMID 17887121

    In the pharmaceutical field, current practice in gaining process understanding by data analysis or knowledge discovery has generally focused on dealing with single experimental databases. This limits the level of knowledge extracted in the situation where data from a number of sources, so called...
  15. Molecular and functional expression of multidrug resistance-associated protein-1 in primary cultured rat alveolar epithelial cells.

    Journal of Pharmaceutical Sciences 97(6):2340 (2008) PMID 17854063

    Multidrug resistance-associated protein-1 (MRP1) is an integral membrane efflux protein that is implicated in multidrug resistance in cancer, but it is also expressed in normal tissues. The objective of this study was to determine the expression, localization and functional activity of MRP1 in p...
  16. Effect of anesthetic structure on inhalation anesthesia: implications for the mechanism.

    Journal of Pharmaceutical Sciences 97(6):2373 (2008) PMID 17847069

    Many previous attempts (e.g., the Meyer-Overton hypothesis) to provide a single set of physical or chemical characteristics that accurately predict anesthetic potency have failed. A finding of a general predictive correlation would support the notion of a unitary theory of narcosis. Using the Ab...
  17. Preparation and evaluation of poly-butylcyanoacrylate nanoparticles for oral delivery of thymopentin.

    Journal of Pharmaceutical Sciences 97(6):2250 (2008) PMID 17853430

    Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samp...
  18. Oral and IV dosing: a method to determine the compartment of drug elimination for two-compartment models.

    Journal of Pharmaceutical Sciences 97(6):2036 (2008) PMID 17847075

    It has been shown previously that it is impossible to measure the volume of distribution at steady state conclusively for a multicompartment system from an iv bolus dose only. The problem lies in deciding from which compartment elimination of the drug occurs in the compartmental model. In this p...
  19. Stabilization of low glass transition temperature indomethacin formulations: impact of polymer-type and its concentration.

    Journal of Pharmaceutical Sciences 97(6):2286 (2008) PMID 17879977

    The objectives of this study were to formulate and stabilize amorphous formulation of low T(g) drug (Indomethacin, INM) with selected polymers and compare these formulations based on solubility and dissolution rate studies. Eudragit EPO (EPO), Polyvinylpyrrolidone-vinyl acetate copolymer (PVP-VA...
  20. Sumatriptan succinate transdermal delivery systems for the treatment of migraine.

    Journal of Pharmaceutical Sciences 97(6):2102 (2008) PMID 17854062

    We have successfully obtained sumatriptan transdermal systems with different polymer compositions: methyl cellulose (MC), polyvinyl pyrrolidone (PVP) and a polyvinyl pyrrolidone (PVP)-polyvinyl alcohol (PVA) mixture. The systems contained 1,2-propylenglycol (MC) or sorbitol as a plasticizer (PVP...