21,763 results match your criteria Journal of Pharmaceutical Sciences [Journal]


A new alternative for intravenous lipid emulsion 20% w/w from superolein oil and its effect on lipid and liver profiles in an animal model.

Daru 2019 Apr 24. Epub 2019 Apr 24.

Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia.

Purpose: Intravenous lipid emulsion (IVLE) was first used to prevent essential fatty acids deficiency. IVLE with α-tocopherol was reported to provide protection against parenteral nutrition-associated liver disease. This study aims to determine the optimal parameters and conditions in developing a physically stable IVLE from superolein palm oil (SoLE 20%) and its effect on lipid and liver profiles in an animal model. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00262-7DOI Listing

Co-spray-dried urea cross-linked hyaluronic acid and sodium ascorbyl phosphate as novel inhalable dry powder formulation.

J Pharm Sci 2019 Apr 19. Epub 2019 Apr 19.

Respiratory Technology, Woolcock Institute of Medical Research and Discipline of Pharmacology, Faculty of Medicine and Health, The University of Sydney, 431 Glebe Point Road, Glebe, NSW 2037, Australia. Electronic address:

The pathogenesis and progression of several lung disorders is propagated by inflammatory and oxidative processes which can be controlled by adjunctive inhaled therapies. The present study aimed to develop an inhalable dry powder formulation consisting of co-spray-dried urea-crosslinked hyaluronic acid and sodium ascorbyl phosphate (SD HA-CL - SAP), a novel combination which was recently shown to possess anti-inflammatory, antioxidant and wound healing properties. Native HA and SAP were co-spray dried (SD HA - SAP) and evaluated as control formulation. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.015DOI Listing
April 2019
2 Reads

Freeze-Dryer Equipment Capability Limit: Comparison of Computational Modeling with Experiments at Laboratory Scale.

J Pharm Sci 2019 Apr 17. Epub 2019 Apr 17.

School of Aeronautics and Astronautics, Purdue University, West Lafayette, IN 47907, United States. Electronic address:

The equipment capability curve is one of the bounding elements of the freeze-drying design space and understanding it is critical to process design, transfer and scale-up. The second bounding element of the design space is the product temperature limit beyond which the product collapses. The high cost associated with freeze drying any product renders it crucial to operate using the most efficient cycle within the limits of the equipment and the product. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.016DOI Listing

Investigation of Electrostatic Behavior of Dry Powder Inhaled Model Formulations.

J Pharm Sci 2019 Apr 17. Epub 2019 Apr 17.

Novartis Pharma AG, Global Development, Novartis Campus, 4056 Basel, Switzerland.

The accumulation of electrostatic charge on drug particles and excipient powders arising from interparticulate collisions or contacts with other surfaces can lead to agglomeration and adhesion problems during the manufacturing process, filling and delivery of dry powder inhaler (DPI) formulations. The objective of the study was to investigate the role of triboelectrification to better understand the influence of electrostatic charge on the performance of DPIs with two capsule based dimensionally similar devices constructed with different materials. In addition, strategies to reduce electrostatic charge build up during the manufacturing process and the processes involved in this phenomenon were investigated. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193024
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.013DOI Listing
April 2019
1 Read

Vacuum Induced Surface Freezing for the Freeze-Drying of the Human Growth Hormone: How does Nucleation Control Affect Protein Stability?

J Pharm Sci 2019 Apr 16. Epub 2019 Apr 16.

Standardisation Science, National Institute for Biological Standards and Control, Blanche Lane, Medicines & Healthcare products Agency, South Mimms, Potters Bar, Hertfordshire, EN6 3QG, UK. Electronic address:

In the present work, the effect of controlled nucleation on the stability of human growth hormone (hGH) during freeze-drying has been investigated. More specifically, the vacuum induced surface freezing technique has been compared to conventional freezing, both with and without an annealing step. Size exclusion chromatography and cell-based potency assays have been used to characterize the formation of soluble aggregates and the biological activity of hGH, respectively. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.014DOI Listing

Pharmacokinetics and tissue distribution of pilocarpine after eyelid skin application to rats.

J Pharm Sci 2019 Apr 16. Epub 2019 Apr 16.

Graduate School of Pharmaceutical Sciences; Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, Saitama, Japan. Electronic address:

Extending the delivery of drugs into the eyes while reducing systemic bioavailability is of utmost importance in the management of chronic ocular diseases. Topical application onto the lower eyelid skin, as an alternative to eye drops, is seen to be a valuable strategy in the treatment of chronic eye diseases. To elucidate the critical value of delivering drugs in solution onto the eyeball through the eyelid skin, pharmacokinetic studies of pilocarpine were conducted, and the results were verified using a direct pharmacodynamic study in rats. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.012DOI Listing

Binding characterization of aptamer-drug layered microformulations and in vitro release assessment.

J Pharm Sci 2019 Apr 16. Epub 2019 Apr 16.

Department of Chemical Engineering, Curtin University, Sarawak 98009, Malaysia.

Efficient delivery of adequate active ingredients to targeted malignant cells is critical, attributing to recurrent biophysical and biochemical challenges associated with conventional pharmaceutical delivery systems. These challenges include drug leakage, low targeting capability, high systemic cytotoxicity, and poor pharmacokinetics and pharmacodynamics. Targeted delivery system is a promising development to deliver sufficient amounts of drug molecules to target cells in a controlled release pattern mode. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.037DOI Listing

Safety assessment of the pharmacological excipient, diethylene glycol monoethyl ether (DEGEE), using in vitro and in vivo systems.

Daru 2019 Apr 18. Epub 2019 Apr 18.

Division of Toxicology and Experimental Medicine, CSIR- Central Drug Research Institute, Lucknow, Uttar Pradesh, 226031, India.

Background: Diethylene glycol monoethyl ether (DEGEE) is widely used as a solubilizer in cosmetics as well as in oral, topical, transdermal and injectable pharmaceutical formulations. Due to the unavailability of detailed toxicological studies on DEGEE, the Scientific Committee on Consumer Products (SCCP) found its toxicological reports to be unsatisfactory, comprising only summaries. Also, a few reports have raised concern on the use of DEGEE as it might cause damage to the kidneys. Read More

View Article

Download full-text PDF

Source
https://darujps.biomedcentral.com/articles/10.1007/s40199-01
Publisher Site
http://dx.doi.org/10.1007/s40199-019-00264-5DOI Listing
April 2019
1 Read

Population Pharmacokinetics of Baloxavir Marboxil in Japanese Pediatric Influenza Patients.

J Pharm Sci 2019 Apr 15. Epub 2019 Apr 15.

Project Management Department, Shionogi & Co., Ltd., Osaka, Japan.

Baloxavir marboxil is a prodrug of baloxavir acid, an inhibitor of cap-dependent endonuclease, and suppresses the replication of influenza virus. The aim of this study is to investigate its pharmacokinetic characteristics in Japanese pediatrics. Population pharmacokinetic analysis was conducted for baloxavir acid with 328 plasma concentration data points in a clinical study of 107 Japanese pediatric influenza patients. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193023
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.010DOI Listing
April 2019
3 Reads

Coating with Chitooligosaccharides enhances the Cytokine induction of Listeria ivanovii based vaccine strain.

J Pharm Sci 2019 Apr 14. Epub 2019 Apr 14.

West China School of Public Health and Healthy Food Evaluation Research Center, Sichuan University, Chengdu, China; Department of Public Health Laboratory Sciences, West China School of Public Health Sichuan University, Chengdu 610041, China; Research Center for Public Health and Preventive Medicine, West China School of Public Health, Sichuan University, Chengdu 610041, China. Electronic address:

Listeria ivanovi (LI) is an available live bacterial vaccine vector. This work attempted to coat LI based vaccine candidates (LI-Rv0129c) with chitooligosaccharides (COS) as an adjuvant to enhance the cellular immune responses induced. COS-bacteria composite was achieved by mixing the bacteria suspension with equal volume of COS solution, and this process accompanied with the increase of bacteria superficial zeta potential and formation of special superficial configurations. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193023
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.011DOI Listing
April 2019
1 Read

Rifampin induces expression of P-glycoprotein on the THP1 cell- derived macrophages, causing decrease intra-macrophage concentration of prothionamide.

J Pharm Sci 2019 Apr 13. Epub 2019 Apr 13.

Department of Pharmacology and Clinical Pharmacology, PharmacoGenomics Research Center, Inje University College of Medicine, Busan, Republic of Korea; Centerfor Personalized Precision Medicine of Tuberculosis, Inje University College of Medicine, Busan, Republic of Korea. Electronic address:

Rifampin (RIF) has been widely used for the treatment of bacterial infections, including tuberculosis. Treatment of drug-resistant tuberculosis (TB) is a global problem due to reduced drug efficacy. The present study determined the effect of rifampin (RIF) on MDR1 gene (P-glycoprotein, P-gp) expression in THP1 macrophages and analyzed the intracellular concentration of the anti-TB drug prothionamide in the presence of RIF. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193023
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.009DOI Listing
April 2019
1 Read

The Degradation Chemistry of Prasugrel Hydrochloride. Part 1: Drug Substance.

J Pharm Sci 2019 Apr 11. Epub 2019 Apr 11.

Prasugrel hydrochloride is the active ingredient in Effient™, a thienopyridine platelet inhibitor. An extensive study of the degradation chemistry of prasugrel hydrochloride (LY640315 hydrochloride, Table 4) has been carried out on the drug substance (Part I) and on the drug product (Part II, future paper) using a multi-dimensional approach including hydrolytic, oxidative, and photolytic stressing, computational chemistry, HPLC analysis, and structure elucidation by various spectroscopic techniques. The major degradation products formed from the drug substance under the various stress conditions have been isolated and structures unambiguously determined, and the pathways leading to these products have been proposed. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.008DOI Listing
April 2019
1 Read

Design and synthesis of galactose/biotin lipid materials for liposomes to promote the hepatoma-cell targeting effect.

J Pharm Sci 2019 Apr 11. Epub 2019 Apr 11.

College of Life Science and Technology, Guangxi University, Nanning 530004, China. Electronic address:

A series of novel low toxic hepatoma-cell targeting lipid materials were designed and synthesized, in which mono-galactose, di-galactose and galactose-biotin were used as targeting moieties and hydrophilic heads while stearate was used as hydrophobic tail (Mono-Gal-ST, Di-Gal-ST and Gal-Biotin-ST). The corresponding galactose/biotin modified liposomes (Mono-Gal-LPs, Di-Gal-LPs and Gal-Biotin-LPs) and conventional liposomes (LPs) were prepared. These galactose/biotin modified liposomes can distinguish hepatoma cells from other tissue cells owing to the recognition of ASGPR by galactose group. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193023
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.007DOI Listing
April 2019
4 Reads

Investigation of the size distribution for diffusion-controlled drug release from Drug Delivery Systems of various geometries.

J Pharm Sci 2019 Apr 10. Epub 2019 Apr 10.

School of Environment and Sciences, Griffith University, Gold Coast, Queensland, 4222, Australia; Institute of Molecular Medicine, Sechenov First Moscow State Medical University, Moscow, Russia. Electronic address:

Various Drug Delivery Systems (DDSs) are often used in modern medicine to achieve controlled and targeted drug release. Diffusional release of drugs from DDSs is often the main mechanism, especially at early times. Generally, average dimensions of DDS are used to model the drug release, but our recent work on drug release from fibers demonstrated that taking into account diameter distribution is essential. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.036DOI Listing

Effect of amorphous nanoparticle size on bioavailability of anacetrapib in dogs.

J Pharm Sci 2019 Apr 10. Epub 2019 Apr 10.

Pharmaceutical Sciences, Merck & Co, Inc, West Point, PA, USA.

Amorphous solid dispersions (ASDs) are used as bioavailability enhancing formulations on the premise of the increased solubility of the amorphous form over its crystalline counterpart. Recent studies have shown that ASDs can, during dissolution, generate amorphous nanoparticles that were initially postulated to serve as a source of rapidly dissolving compound during absorption. Researchers have proposed that nanoparticles, including crystalline nanoparticles, may provide additional benefits to absorption such as drifting in the mucous layer. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193022
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.006DOI Listing
April 2019
3 Reads

An ex vivo Evaluation of Moxifloxacin Nanostructured Lipid Carrier enriched in situ gel for Transcorneal permeation on Goat Cornea.

J Pharm Sci 2019 Apr 9. Epub 2019 Apr 9.

Department of Pharmaceutical Engineering and Technology, IIT (BHU), Varanasi. Electronic address:

The study was designed to fabricate the moxifloxacin nanostructured lipid carriers (MOX-NLC) loaded in-situ gel for opthalmic application to improve the corneal permeation, retention and also subside the toxic effect associated with intracameral injection of moxifloxacin in endopthalmitis treatment. Initially, Box-Behnken design was employed to optimize the various factors significantly affecting the final formulation attributes. MOX-NLCs with particle size 232. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.005DOI Listing

Population Pharmacokinetics of Doripenem in Pediatric Patients and Monte-Carlo Pharmacokinetic/Pharmacodynamic Simulations for Dosing Regimen Assessment.

J Pharm Sci 2019 Apr 8. Epub 2019 Apr 8.

Clinical Pharmacology & Pharmacokinetics, Project Management Department, Shionogi & Co., Ltd.

The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg two or three times daily and to evaluate the dosing regimens by using Monte-Carlo pharmacokinetic/pharmacodynamic simulations. Population pharmacokinetic analysis was performed by using 190 plasma concentrations of doripenem from 99 patients (2months - 13years old). The two-compartment model well described the doripenem plasma concentrations in pediatric patients. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.002DOI Listing
April 2019
1 Read

Entirely S-protected thiolated silicone: A novel hydrophobic muco- and skin adhesive.

J Pharm Sci 2019 Apr 8. Epub 2019 Apr 8.

Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens-University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria. Electronic address:

The aim of this study was the synthesis and evaluation of an entirely S-protected thiolated silicone as novel hydrophobic mucoadhesive and skin adhesive. 2-[(2-Amino-2-carboxyethyl)disulfanyl]nicotinic acid was covalently attached to a poly(dimethylsiloxane)-graft-polyacrylate via amide bond formation. Adhesive properties were determined via the rotating cylinder method and tensile studies on porcine small intestinal mucosa besides on porcine abdominal skin. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193022
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.04.003DOI Listing
April 2019
3 Reads

Effects of Processing on a Sustained Release Formulation Prepared by Twin-Screw Dry Granulation.

J Pharm Sci 2019 Apr 6. Epub 2019 Apr 6.

Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, MS 38677, USA; Pii Center for Pharmaceutical Technology, The University of Mississippi, University, MS 38677, USA. Electronic address:

Dry granulation is an indispensable process used to improve the flow property of moisture-sensitive materials. Considering the limitations of currently available dry granulation techniques, it is necessary to develop a novel technique. In this study, a twin-screw dry granulation (TSDG) technology was successfully applied to produce a sustained-release dry granule formulation, which was subsequently compressed into sustained-release tablets. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.004DOI Listing
April 2019
9 Reads

Pharmacokinetics and tolerability of a novel 17β-estradiol and progesterone intravaginal ring in sheep.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

Daré Bioscience, Inc, San Diego, CA, USA. Electronic address:

This study reports the preparation, in vitro release, pharmacokinetics and local tolerability of novel ethylene-vinyl acetate (EVA) intravaginal rings (IVRs) delivering 17β-estradiol (E) and progesterone (P), in drug-naïve ovariectomized female Dorset crossbred sheep. Following preparation and assessment of in vitro release of E and P, animals were randomized to treatment Groups 1 or 2 (comparator rings releasing 50 or 100 μg/day E, respectively), Groups 3 or 4 [EVA IVRs, 160 μg/day E with 4 (160/4 IVR) or 8 mg/day P (160/8 IVR), respectively], or Group 5 (160 μg E and 10 mg P administered intravenously). IVRs were placed on Day 1 and remained in place through Day 29. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.032DOI Listing
April 2019
3 Reads

The use of a microfluidic device to encapsulate a poorly water-soluble drug CoQ in lipid nanoparticles and an attempt to regulate intracellular trafficking to reach mitochondria.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

Faculty of Pharmaceutical Sciences, Hokkaido University, 1-1 Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan. Electronic address:

A number of drugs that are currently on the market, as well as new candidates for drugs are poorly water soluble. Because of this, a need exists to develop drug formulations that will permit the expanded use of such drugs. The use of liposomes and lipid nanoparticles (LNP) for drug delivery has attracted attention as a technique for solubilizing molecules that are poorly water-soluble, but this technique faces serious scale-up risks. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.04.001DOI Listing
April 2019
2 Reads

Characterization of human recombinant N-acetylgalactosamine-6-sulfate sulfatase produced in Pichia pastoris as potential enzyme for Mucopolysaccharidosis IVA treatment.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

Institute for the Study of Inborn Errors of Metabolism, School of Sciences, Pontificia Universidad Javeriana, Bogotá, Colombia. Electronic address:

Mucopolysaccharidosis IVA (MPS IVA or Morquio A syndrome) is a lysosomal storage disease caused by the deficiency of N-acetylgalactosamine-6-sulfate sulfatase (GALNS), leading to lysosomal storage of keratan sulfate (KS) and chondroitin-6-sulfate. Currently, enzyme replacement therapy (ERT) using an enzyme produced in CHO cells represents the main treatment option for MPS IVA patients. As an alternative, we reported the production of an active GALNS enzyme produced in the yeast Pichia pastoris (prGALNS), which showed internalization by cultured cells through a potential receptor-mediated process and similar post-translational processing as human enzyme. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.034DOI Listing
April 2019
2 Reads
2.590 Impact Factor

In Vitro Simulation of Tissue Back-Pressure for Pen Injectors and Auto-Injectors.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

Department of Mechanical Engineering, Technical University of Denmark, Kgs, Lyngby, Denmark.

Purpose: The aim of this project was to show that tissue back-pressure can be measured in vitro using a simple pneumatic model.

Methods: A thorough literature study revealed four relevant papers all describing in vivo studies. One of these studies where the subcutaneous tissue back-pressure was determined in 11 patients was used as a reference for the present work. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.035DOI Listing
April 2019
2 Reads

Rat Kidney Slices for Evaluation of Apical Membrane Transporters in Proximal Tubular Cells.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan. Electronic address:

Kidney slice has been often used as a tool reflecting basolateral transport in renal tubular epithelial cells. Recently, we reported that several important apical reabsorptive transporters such as Octn1/2, Sglt1/2, and Pept1/2 were functional in mouse kidney slices as well as transporter activities in basolateral side which have been well accepted. Since rats are often used for preclinical pharmacodynamic and pharmacokinetic studies as well as mice, it is important to confirm applicability of rat kidney slices for evaluation of apically-expressed transporters. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.031DOI Listing
April 2019
1 Read
2.590 Impact Factor

The diffusion of hydrogen peroxide into the liquid product during filling operations inside vaporous hydrogen peroxide-sterilized isolators can be predicted by a mechanistic model.

J Pharm Sci 2019 Apr 5. Epub 2019 Apr 5.

GSK, Technical Research & Development, Drug Product, Rixensart, Belgium. Electronic address:

Isolators are commonly used in filling operations of pharmaceutical products. To ensure an aseptic inner environment, isolators are regularly sterilized with vaporised hydrogen peroxide (VHP). However, despite extensive purging with air, some residual HO remains within the isolator atmosphere, and may thus end up in the liquid pharmaceutical drug product, which subsequently may cause oxidation and impact the product's safety and efficacy. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193021
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.03.033DOI Listing
April 2019
1 Read

Identification of major esterase involved in hydrolysis of soft anticholinergic (2R3'R-SGM) designed from glycopyrrolate in human and rat tissues.

J Pharm Sci 2019 Apr 4. Epub 2019 Apr 4.

Graduate School of Pharmaceutical Sciences, Kumamoto University, Kumamoto, Japan. Electronic address:

The glycopyrrolate soft analogue, SGM, designed to be easily hydrolyzed into the significantly less active zwitterionic metabolite, SGa, typifies soft drug that reduces systemic side effects (a problem often seen with traditional anticholinergics) following local administration. In this study, hydrolysis of 2R3'R-SGM, the highest pharmacologically active stereoisomer of SGM, was investigated in human and rat tissues. In both species, 2R3'R-SGM was metabolized to 2R3'R-SGa in plasma, but stable in liver and intestine. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.030DOI Listing
April 2019
1 Read

Establishment of evaluation method for gene-silencing by serial pulmonary administration of siRNA and pDNA powders: Naked siRNA inhalation powder suppresses luciferase gene expression in lung.

J Pharm Sci 2019 Apr 4. Epub 2019 Apr 4.

Department of Drug Delivery Research, Faculty of Pharmacy, Meijo University, 150 Yagotoyama, Tempaku-ku, Nagoya 468-8503, Japan. Electronic address:

In order to evaluate the in-vivo effect of inhaled formulations, it is a gold standard to create a lung metastasis model by intravenously injecting cancer cells into an animal. Since the cancer grows from the blood vessel side, there is a possibility of underestimating the effect of an inhaled formulation administered to the lung epithelium side. In addition, the metastasis model has disadvantages in terms of preparation time and expense. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.029DOI Listing
April 2019
6 Reads

Comparison of three processes for parenteral nanoemulsion production: ultrasounds, microfluidizer and premix membrane emulsification.

J Pharm Sci 2019 Apr 1. Epub 2019 Apr 1.

Univ Lyon, Universit´e Claude Bernard Lyon 1, CNRS, LAGEP UMR 5007, 43 boulevard du 11 novembre 1918, F-69100, Villeurbanne, France. Electronic address:

Nanoemulsions are of great interest for pharmaceutical applications, including parenteral dosage forms. However, their production is still limited and requires more efficient and adaptive technologies. The more common systems are high-shear homogenization like microfludizers (MF) at industrial scale and ultrasounds at research scale, both based on high energy limiting their application for sensitive drugs. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.026DOI Listing
April 2019
4 Reads

In vitro investigation of the effects of boron nitride nanotubes and curcumin on DNA damage.

Daru 2019 Apr 2. Epub 2019 Apr 2.

Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Hacettepe University, 06100 Sıhhıye, Ankara, Turkey.

Backround: Stem cells provide an opportunity to analyse the effects of xenobiotic on cell viability, differentiation and cell functions. Evaluation of the possible cytotoxic and DNA damaging effects on bone marrow CD34 stem cells is important for their ability to differentiate into blood cells, and also for bone marrow diseases therapy. Boron nitride nanotubes and curcumin are potential nanoformulation agents that can be used together in the treatment of cancer or bone marrow diseases. Read More

View Article

Download full-text PDF

Source
https://darujps.biomedcentral.com/articles/10.1007/s40199-01
Publisher Site
http://dx.doi.org/10.1007/s40199-019-00263-6DOI Listing
April 2019
6 Reads

Optimal dosing regimen of phenytoin for Korean epilepsy patients: from premature babies to the elderly.

J Pharm Sci 2019 Mar 30. Epub 2019 Mar 30.

Department of Pharmacology, Yonsei University College of Medicine, Seoul, Korea. Electronic address:

Phenytoin has been decreasingly used due to the high inter-individual variability in drug concentration and the narrow therapeutic window. In spite of such drawbacks, phenytoin is still essential as a second-line therapy for status epilepticus when patients are resistant to benzodiazepines. This study aimed to develop a population pharmacokinetic model of phenytoin and to propose the optimal dose regimen of phenytoin in Korean epilepsy patients. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.022DOI Listing
March 2019
2 Reads

Prediction of Ticagrelor and its Active Metabolite in Liver Cirrhosis Populations Using a Physiologically Based Pharmacokinetic Model Involving Pharmacodynamics.

J Pharm Sci 2019 Mar 28. Epub 2019 Mar 28.

Department of Pharmacy, The First Affiliated Hospital of Fujian Medical University, 20 Cha Zhong M. Rd, Fuzhou 350005, People's Republic of China. Electronic address:

Ticagrelor, a P2Y receptor antagonist, has been highly recommended for use in acute coronary syndrome. The major active metabolite (AM) is similar to the parent drug, which exhibits antiplatelet activity. The inhibition of platelet aggregation (IPA) is used as an assay to demonstrate the anticoagulant efficacy of ticagrelor. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.028DOI Listing
March 2019
2 Reads

Genus Sideritis, section Empedoclia in southeastern Europe and Turkey - studies in ethnopharmacology and recent progress of biological activities.

Daru 2019 Mar 30. Epub 2019 Mar 30.

Faculty of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Background: Over the last two decades there has been a substantial increase of the number of studies on the species of genus Sideritis. Species of section Empedoclia, occurring in the Eastern Mediterranean region and in part of Western Asia possess some remarkable characteristics and are known as valuable medicinal plants used by local people in the traditional medicine and for herbal tea. The objective of the review is to make a survey on the recent studies on the ethnopharmacology and biological activity of the species in Southeastern Europe and in Turkey, which is the center of distribution and their main occurrence. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00261-8DOI Listing
March 2019
1 Read

New Insight Into Thermodynamical Stability of Carbamazepine.

J Pharm Sci 2019 Mar 26. Epub 2019 Mar 26.

Department of Soft Matter Research Institute of Nuclear Physics Polish Academy of Sciences, PL-31342 Krakow, Poland.

Carbamazepine (CBZ)-an antiepileptic drug-belongs to Biopharmaceutics Classification System II Class. It has low solubility and consequently limited bioavailability. One of the ways to improve drugs solubility is amorphization of their structure. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.027DOI Listing

Analysis of the Complicated Nonlinear Pharmacokinetics of Orally Administered Telmisartan in Rats Using a Stable Isotope-IV Method.

J Pharm Sci 2019 Mar 26. Epub 2019 Mar 26.

Faculty of Pharmaceutical Sciences, Setsunan University, 45-1 Nagaotoge-cho, Hirakata, Osaka 573-0101, Japan.

This study aimed to kinetically analyze the nonlinear absorption and systemic exposure of telmisartan (TEL) after oral administration to rats by using a stable isotope-IV method. Rats were orally administered different dose of TEL, followed by the intravenous injection of 0.005 mg/kg of deuterium-labeled TEL (TEL-d3). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.023DOI Listing
March 2019
4 Reads

Backgrounded Membrane Imaging (BMI) for High-Throughput Characterization of Subvisible Particles During Biopharmaceutical Drug Product Development.

J Pharm Sci 2019 Mar 23. Epub 2019 Mar 23.

Coriolis Pharma Research, Fraunhoferstr. 18 b, 82152 Martinsried, Germany. Electronic address:

Backgrounded membrane imaging (BMI) is a novel automated, 96-well plate-based microscopic approach for subvisible particle analysis. We scientifically evaluated BMI with respect to sizing and counting accuracy, working range, impact of refractive index, and interferences by silicone oil droplets, and compared BMI to state-of-the-art dynamic image analysis (DIA). Image quality was found to be comparable to current DIA methodologies. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.024DOI Listing
March 2019
1 Read

Preparation and Characterization of Cellulose Ether Liposomes for the Inhibition of Prion Formation in Prion-Infected Cells.

J Pharm Sci 2019 Mar 23. Epub 2019 Mar 23.

Department of Neurochemistry, Tohoku University Graduate School of Medicine, Sendai, Miyagi, Japan. Electronic address:

Prion accumulation in the brain and lymphoreticular system causes fatal neurodegenerative diseases. Our previous study revealed that cellulose ethers (CE) have anti-prion activities in vivo and in prion-infected cells when administered at high doses. This study aims to improve the bioavailability of a representative CE using a liposomal formulation and characterized CE-loaded liposomes in cultured cells. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.025DOI Listing
March 2019
2 Reads

Polymorphs of Curcumin and Its Cocrystals With Cinnamic Acid.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Department of Chemical Engineering, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, India. Electronic address:

We report formation of polymorphs and new eutectics and cocrystals of curcumin, a sparingly water-soluble active component in turmeric, structurally similar to cinnamic acid. The curcumin polymorphs were formed using liquid antisolvent precipitation, where acetone acted as a solvent and water was used as the antisolvent. The metastable form 2 of curcumin was successfully prepared in varied morphology over a wide range of solvent-to-antisolvent ratio and under acidic pH conditions. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.014DOI Listing
March 2019
2 Reads

Effect of rifampicin on the plasma concentrations of bile acid-O-sulfates in monkeys and human liver-transplanted chimeric mice with or without bile flow diversion.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Laboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, University of Tokyo, Tokyo, Japan.

The present study examined the significance of enterohepatic circulation and the effect of rifampicin (an inhibitor of organic anion transporting polypeptide 1B (OATP1B)) on the plasma concentrations of bile acid-O-sulfates (glycochenodeoxycholate-O-sulfate (GCDCA-S), lithocholate-O-sulfate (LCA-S), glycolithocholate-O-sulfate (GLCA-S), and taurolithocholate-O-sulfate (TLCA-S)) in monkeys and human liver-transplanted chimeric mice (PXB mouse). Rifampicin significantly increased the area under the curve (AUC) of bile acid-O-sulfates in monkeys (13-69 times) and PXB mice (13-25 times) without bile flow diversion. Bile flow diversion reduced the concentration of plasma bile acid-O-sulfates under control conditions in monkeys and the concentration of plasma GCDCA-S in PXB mice. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.021DOI Listing
March 2019
1 Read

Predicting Drug Binding to Human Serum Albumin and Alpha One Acid Glycoprotein in Diseased and Age Patient Populations.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone, TODD 361, Lexington, Kentucky 40536-0596.

Plasma protein binding, namely the fraction unbound (f), can be an important determinant of the disposition and response of drugs. The primary objective of this study was to predict f values of 183 drugs utilizing either a single binding protein model, where the predominant binding protein had been established, or a multiple binding protein model (MBPM), where the relative binding contribution of human serum albumin (HSA) or alpha 1 acid glycoprotein (AAG) is known. Mean protein concentrations, dependent on disease or age, were used to account for changes in f. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.018DOI Listing

Prediction Accuracy of Mechanism-Based Oral Absorption Model for Dogs.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Molecular Pharmaceutics Lab., College of Pharmaceutical Sciences, Ritsumeikan University, 1-1-1 Noji-higashi, Kusatsu, Shiga 525-8577, Japan.

The purpose of the present study was to evaluate the prediction accuracy of a mechanism-based oral absorption model for the fraction of a dose absorbed (Fa) in dogs, focusing on poorly soluble drugs. As an open mechanism-based model, the gastrointestinal unified theoretical framework was used in this study. The prediction accuracy of the gastrointestinal unified theoretical framework was evaluated using Fa data in dogs (63 data sets for marketed drugs and proprietary compounds). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.015DOI Listing
March 2019
1 Read

Delivery and Biodistribution of Traceable Polymeric Micellar Diclofenac in the Rat.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada. Electronic address:

The nonsteroidal anti-inflammatory drugs elevate cardiovascular risk, perhaps, due to their accumulation in the heart and kidneys. We designed nanodelivery systems for cardiotoxic diclofenac to reduce its presence in these organs. Diclofenac ethyl ester (DFEE) was encapsulated in traceable micelles based on poly(ethylene oxide)-b-poly(ε-caprolactone) (DFEE-PCL-TM) or poly(ethylene oxide)-b-poly(α-benzyl carboxylate-ε-caprolactone) (DFEE-PBCL-TM). Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193016
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.03.016DOI Listing
March 2019
7 Reads

Applications of In Silico Solvent Screening and an Interactive Web-Based Portal for Pharmaceutical Crystallization Process Development.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Eli Lilly and Company, Small Molecule Design and Development, Indianapolis, IN, 46285.

In an effort to reduce development time and costs associated with API process solvent selection and crystallization design, a tiered approach to crystallization solvent selection was developed that leverages different solubility modeling tools selected on the basis of available data and the intended use of the prediction. To facilitate easy access to routine solubility modeling functionality with a high level of automation and parallelization, a web-based in-silico solvent screening tool was also developed as well as a user interface to visualize and interpret the large number of predicted results. Examples are presented to illustrate the utility of the workflow and solvent screening tool at various stages of development for a diverse range of crystallization processes. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.013DOI Listing
March 2019
1 Read

Silk Reservoirs for Local Delivery of Cisplatin for Neuroblastoma Treatment: In Vitro and In Vivo Evaluations.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Department of Surgery, Stanford University, Stanford, California. Electronic address:

Neuroblastoma is the most common extracranial childhood tumor, and current treatment requires surgical resection and multidrug chemotherapy. Local, perioperative delivery of chemotherapeutics is a promising treatment method for solid tumors that require surgical removal. In this study, we have aimed to develop a controlled-release implant system to deliver cisplatin in tumor or tumor resection area. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193016
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.03.019DOI Listing
March 2019
3 Reads

Application of Box-Behnken Design in the Preparation, Optimization, and In Vitro Evaluation of Self-assembly-based Tamoxifen- and Doxorubicin-loaded and Dual Drug-loaded Niosomes for Combinatorial Breast Cancer Treatment.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Gujarat Forensic Sciences University, Nr. DFS Head Quarters, Sector 9, Gandhinagar, Gujarat 382007. Electronic address:

This study was developed with the objective to prepare self-assembled niosomes to support sufficient entrapment and sustained drug release of the drugs having different solubility and mechanisms. In the current work, Tamoxifen- and Doxorubicin-loaded niosomes were prepared for combinatorial breast cancer treatment with statistical optimization by Box-Behnken experimental design. Atomic force microscopy revealed a spherical shape morphology of the niosomes. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.020DOI Listing
March 2019
3 Reads

Using Milling to Explore Physical States: The Amorphous and Polymorphic Forms of Sulindac.

J Pharm Sci 2019 Mar 21. Epub 2019 Mar 21.

Physics Department, University of Lille, CNRS, INRA, ENSCL, UMET - Unité Matériaux et Transformations, UMR 8207, F-59000 Lille, France.

This article shows how milling can be used to explore the phase diagram of pharmaceuticals. This process has been applied to sulindac. A short milling has been found to trigger a polymorphic transformation between form II and form I upon heating which is not seen in the nonmilled material. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193016
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.03.017DOI Listing
March 2019
5 Reads

Effects of Water on Powder Flowability of Diverse Powders Assessed by Complimentary Techniques.

J Pharm Sci 2019 Mar 20. Epub 2019 Mar 20.

The University of Copenhagen, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark. Electronic address:

The storage of bulk powders in suboptimal conditions can affect their handling, processing, and performance. The aim of this work was to assess the influence of storage conditions on powder flowability, which is a crucial property in powder processing. The 7 model compounds were common tablet excipients with varying crystallinity ranging from amorphous to partially crystalline, and 2 crystalline materials. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193015
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.03.012DOI Listing
March 2019
1 Read

Sensor Network Robustness using Model-based Data Reconciliation for Continuous Tablet Manufacturing.

J Pharm Sci 2019 Mar 20. Epub 2019 Mar 20.

Davidson School of Chemical Engineering, Purdue University, West Lafayette, IN 47906, USA.

Advances in continuous manufacturing in the pharmaceutical industry necessitate reliable process monitoring systems that are capable of handling measurement errors inherent to all sensor technologies, as well as detecting measurement outliers to ensure operational reliability. The purpose of this work is to demonstrate data reconciliation (DR) and gross error detection (GED) methods as real-time process management tools to accomplish robust process monitoring. DR mitigates the effects of random measurement errors while GED identifies non-random sensor malfunctions. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.03.011DOI Listing
March 2019
1 Read

Policies to improve access to pharmaceutical products in shortage: the experience of Iran food and drug administration.

Daru 2019 Mar 23. Epub 2019 Mar 23.

Department of Pharmacoeconomics and Pharma Management, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Background: In the past decades, economic sanctions imposed on Iran for its nuclear program. The embargo made difficulty in foreign trade and led to lack of timely access to medicines. As the internationally-led sanctions caused to the shortage of medicine there, healthcare systems need to applied the new policies for maintaining health service quality especially in pharmaceutical sector. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00259-2DOI Listing
March 2019
2 Reads
1.111 Impact Factor

Vitamin B combination reduces fluconazole toxicity in Wistar rats.

Daru 2019 Mar 22. Epub 2019 Mar 22.

Department of Biochemistry, Faculty of Science, King Abdulaziz University, P.O. Box: 80200, Zip Code: 21589, Jeddah, Kingdom of Saudi Arabia.

Background: The major adverse effect associated with systemic administration of Fluconazole (FLZ), is hepatic toxicity. FLZ is most commonly used antifungal drug in treatment of invasive fungal infections.

Methods: FLZ toxicity was challenged by individual and in combination of three vitamins (B1, B2 B3). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00252-9DOI Listing
March 2019
3 Reads

Synthesis and anti-breast cancer activity of novel indibulin related diarylpyrrole derivatives.

Daru 2019 Mar 20. Epub 2019 Mar 20.

Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design & Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 1417614411, Iran.

Background: During recent years, a number of anti-tubulin agents were introduced for treatment of diverse types of cancer. Despite their potential in the treatment of cancer, drug resistance and adverse toxicity, such as peripheral neuropathy, are some of the negative effects of anti-tubulin agents. Among anti-tubulin agents, indibulin was found to cause minimal peripheral neuropathy. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00260-9DOI Listing
March 2019
2 Reads