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Pharmaceutical Research

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https://www.readbyqxmd.com/read/28748398/intranasal-delivery-of-topically-acting-levofloxacin-to-rats-a-proof-of-concept-pharmacokinetic-study
#1
Joana Sousa, Gilberto Alves, Ana Fortuna, Amílcar Falcão
PURPOSE: To evaluate the potential of levofloxacin intranasal administration as a promising alternative approach to treat local infections such as chronic rhinosinusitis, by delivering drug concentrations directly to the site of infection. METHODS: Drug concentrations were measured in plasma, olfactory bulb and nasal mucosa of anterior (ANM) and posterior regions after intranasal (0.24 mg/kg) and intravenous (10 mg/kg) administration to rats, and pharmacokinetic parameters were compared between routes...
July 26, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28741064/injectable-sustained-release-depots-of-plga-microspheres-for-insoluble-drugs-prepared-by-hot-melt-extrusion
#2
Yuting Guo, Yunning Yang, Luying He, Rong Sun, Chenguang Pu, Bin Xie, Haibing He, Yu Zhang, Tian Yin, Yanjiao Wang, Xing Tang
PURPOSE: Progesterone (PRG) was selected as a model drug to develop a long-acting injection system for poorly water-soluble drugs. METHODS: Microspheres with high density-low porosity were prepared by hot-melt extrusion (HME) combined with wet-milling as the representative formulation, and a microcrystal suspension was also studied as a comparison. The morphology, particle size and distribution, polymorphism, drug distribution, density and porosity were characterized by scanning electron microscopy, laser diffraction particle size analyzer, power X-ray diffraction and DSC respectively...
July 24, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28733781/bitc-and-s-carvone-restrain-high-fat-diet-induced-obesity-and-ameliorate-hepatic-steatosis-and-insulin-resistance
#3
Sary Alsanea, Dexi Liu
PURPOSE: To investigate the preventative activity of benzyl isothiocyante and S-carvone against high-fat diet-induced obesity and metabolic complications. METHODS: Ten-week-old C57BL/6 male mice were fed a high-fat diet and injected intraperitoneally twice per week with benzyl isothiocyante, S-carvone, or vehicle for 8 weeks. The body weight, food intake, and body composition were monitored, and glucose tolerance and insulin tolerance tests were performed at the end of the experiment...
July 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28726003/chitooligosaccharides-modified-reduction-sensitive-liposomes-enhanced-cytoplasmic-drug-delivery-and-osteosarcomas-tumor-inhibition-in-animal-models
#4
Xuelei Yin, Yingying Chi, Chuanyou Guo, Shuaishuai Feng, Jinhu Liu, Kaoxiang Sun, Zimei Wu
PURPOSE: To investigate the potential of a reduction-sensitive and fusogenic liposomes, enabled by surface-coating with chotooligosaccharides (COS) via a disulfide linker, for tumor-targeted cytoplasmic drug delivery. METHODS: COS (MW2000-5000) were chemically tethered onto the liposomes through a disulfide linker (-SS-) to cholesterol (Chol). Doxorubicin (DOX) was actively loaded in the liposomes. Their reduction-sensitivities, cellular uptake, cytotoxicity, pharmacokinetics and antitumor efficacy were investigated...
July 19, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28721446/rhamnolipids-enhance-in-vivo-oral-bioavailability-of-poorly-absorbed-molecules
#5
El-Sayed Khafagy, Mona F El-Azab, Mohamed E H ElSayed
PURPOSE: This report describes the effect of rhamnolipids (RLs) on the tight junctions (TJ) of the intestinal epithelium using the rat in-situ closed loop model. METHODS: We investigated the transport of 5 (6)-carboxyfluorescein (CF) and fluorescein isothiocyanate-labeled dextrans with average molecular weights of 4.4 and 10 kDa (FD-4 and FD-10) when co-administered with different concentrations of RLs. Lactate dehydrogenase (LDH) leakage assay and histopathological examination of treated intestinal loops were used to assess potential toxicity of RLs...
July 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28718050/dissolving-microneedle-patches-for-dermal-vaccination
#6
REVIEW
M Leone, J Mönkäre, J A Bouwstra, G Kersten
The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (e.g. pain, needle-stick injuries or needle re-use). This review focuses on dissolving microneedles that after penetration into the skin dissolve releasing the encapsulated antigen. The microneedle patch fabrication techniques and their challenges are discussed as well as the microneedle characterization methods and antigen stability aspects...
July 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28718049/good-things-in-small-packages-an-innovative-delivery-approach-for-inhaled-insulin
#7
James B Fink, Lisa Molloy, John S Patton, Valdecir Castor Galindo-Filho, Jacqueline de Melo Barcelar, Luciana Alcoforado, Simone Cristina Soares Brandão, Armèle Dornelas de Andrade
PURPOSE: The design development of a small, hand held, battery operated, breath actuated inhaler as a drug/device platform for inhaled insulin posed a number of technical challenges. Our goal was to optimize lung deposition and distribution with aerosol generators producing 3-6 μm particle size distribution. METHODS: In silico modeling with computational fluid dynamics (CFD) and in vitro testing of device components were assessed using an Alberta idealized adult airway (Copley, UK) to optimize mouthpiece and aerosol path design for dose delivered distal to the trachea...
July 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28707165/design-preparation-and-evaluation-of-hpmc-based-paa-or-sa-freeze-dried-scaffolds-for-vaginal-delivery-of-fluconazole
#8
Carmen Anatolia Gafitanu, Daniela Filip, Corina Cernatescu, Daniela Rusu, Cristina Gabriela Tuchilus, Doina Macocinschi, Mirela-Fernanda Zaltariov
PURPOSE: Aim of this work was preparation of bioadhesive gel formulations based on Hydroxypropyl methylcellulose (HPMC), Poly(acrylic acid) (PAA) or Sodium alginate (SA) loaded with anise/fluconazole β-cyclodextrin inclusion complexes in 1:2 and 1:3 ratios intended for vaginal applications. METHODS: Freeze-drying method was effectively utilized and superporous morphology was obtained. The superporous morphology of the lyophilized gels, dynamic water vapor sorption measurements, drug release kinetics studies and their antimicrobial activities are presented...
July 13, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28707164/optimizing-the-bioavailability-of-subcutaneously-administered-biotherapeutics-through-mechanochemical-drivers
#9
REVIEW
D S Collins, L C Kourtis, N R Thyagarajapuram, R Sirkar, S Kapur, M W Harrison, D J Bryan, G B Jones, J M Wright
The subcutaneous route offers myriad benefits for the administration of biotherapeutics in both acute and chronic diseases, including convenience, cost effectiveness and the potential for automation through closed-loop systems. Recent advances in parenteral administration devices and the use of additives which enhance drug dispersion have generated substantial additional interest in IV to SQ switching studies. Designing pre-clinical and clinical studies using SQ mediated delivery however requires deep understanding of complex inter-related physiologies and transport pathways governing the interstitial matrix, vascular system and lymphatic channels...
July 13, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28702798/the-differential-absorption-of-a-series-of-p-glycoprotein-substrates-in-isolated-perfused-lungs-from-mdr1a-1b-genetic-knockout-mice-can-be-attributed-to-distinct-physico-chemical-properties-an-insight-into-predicting-transporter-mediated-pulmonary-specific
#10
Daniel F Price, Chris N Luscombe, Peter J Eddershaw, Chris D Edwards, Mark Gumbleton
PURPOSE: To examine if pulmonary P-glycoprotein (P-gp) is functional in an intact lung; impeding the pulmonary absorption and increasing lung retention of P-gp substrates administered into the airways. Using calculated physico-chemical properties alone build a predictive Quantitative Structure-Activity Relationship (QSAR) model distinguishing whether a substrate's pulmonary absorption would be limited by P-gp or not. METHODS: A panel of 18 P-gp substrates were administered into the airways of an isolated perfused mouse lung (IPML) model derived from Mdr1a/Mdr1b knockout mice...
July 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28695401/item-response-theory-as-an-efficient-tool-to-describe-a-heterogeneous-clinical-rating-scale-in-de-novo-idiopathic-parkinson-s-disease-patients
#11
Simon Buatois, Sylvie Retout, Nicolas Frey, Sebastian Ueckert
PURPOSE: This manuscript aims to precisely describe the natural disease progression of Parkinson's disease (PD) patients and evaluate approaches to increase the drug effect detection power. METHODS: An item response theory (IRT) longitudinal model was built to describe the natural disease progression of 423 de novo PD patients followed during 48 months while taking into account the heterogeneous nature of the MDS-UPDRS. Clinical trial simulations were then used to compare drug effect detection power from IRT and sum of item scores based analysis under different analysis endpoints and drug effects...
July 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28687987/evaluation-of-the-crystallization-tendency-of-commercially-available-amorphous-tacrolimus-formulations-exposed-to-different-stress-conditions
#12
Niraj S Trasi, Hitesh S Purohit, Lynne S Taylor
PURPOSE: Tacrolimus, an immunosuppressant, is a poorly water soluble compound whereby the commercially available capsule formulations contain the drug in amorphous form. The goal of this study was to evaluate the robustness of the innovator product and five generic formulations to crystallization following storage at stress conditions. METHODS: Products were purchased from a pharmacy and stored at 40°C/75% relative humidity (RH), open dish conditions. Crystallinity was determined using X-ray diffraction...
July 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28685299/conjugated-and-entrapped-hpma-pla-nano-polymeric-micelles-based-dual-delivery-of-first-line-anti-tb-drugs-improved-and-safe-drug-delivery-against-sensitive-and-resistant-mycobacterium-tuberculosis
#13
Seema Upadhyay, Iliyas Khan, Avinash Gothwal, Praveen K Pachouri, N Bhaskar, Umesh D Gupta, Devendra S Chauhan, Umesh Gupta
PURPOSE: First line antiTB drugs have several physical and toxic manifestations which limit their applications. RIF is a hydrophobic drug and has low water solubility and INH is hepatotoxic. The main objective of the study was to synthesize, characterize HPMA-PLA co-polymeric micelles for the effective dual delivery of INH and RIF. METHODS: HPMA-PLA co-polymer and HPMA-PLA-INH (HPI) conjugates were synthesized and characterized by FT-IR and (1)H-NMR spectroscopy...
July 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28685298/benchmarking-of-human-dose-prediction-for-inhaled-medicines-from-preclinical-in-vivo-data
#14
Therese Ericsson, Markus Fridén, Carina Kärrman-Mårdh, Ian Dainty, Ken Grime
PURPOSE: A scientifically robust prediction of human dose is important in determining whether to progress a candidate drug into clinical development. A particular challenge for inhaled medicines is that unbound drug concentrations at the pharmacological target site cannot be easily measured or predicted. In the absence of such data, alternative empirical methods can be useful. This work is a post hoc analysis based on preclinical in vivo pharmacokinetic/pharmacodynamic (PK/PD) data with the aim to evaluate such approaches and provide guidance on clinically effective dose prediction for inhaled medicines...
July 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28685297/hemodynamic-effects-of-lipid-based-oxygen-microbubbles-via-rapid-intravenous-injection-in-rodents
#15
Katherine J Black, Andrew T Lock, Lindsay M Thomson, Alexis R Cole, Xiaoqi Tang, Brian D Polizzotti, John N Kheir
PURPOSE: Low oxygen levels, or hypoxemia, is a common cause of morbidity and mortality in critically ill patients. Hypoxemia is typically addressed by increasing the fraction of inspired oxygen, the use of mechanical ventilation, or more invasive measures. Recently, the injection of oxygen gas directly into the bloodstream by packaging it within lipid-based oxygen microbubbles (LOMs) has been explored. The purpose of this work is to examine the acute hemodynamic effects of intravenous injections of LOMs...
July 6, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28681164/influence-of-molecular-size-on-the-clearance-of-antibody-fragments
#16
Zhe Li, Ben-Fillippo Krippendorff, Dhaval K Shah
PURPOSE: To establish a continuous relationship between the size of various antibody fragments and their systemic clearance (CL) in mice. METHODS: Two different orthogonal approaches have been used to establish the relationship. First approach uses CL values estimated by non-compartmental analysis (NCA) to establish a correlation with protein size. The second approach simultaneously characterizes the PK data for all the proteins using a 2-compartment model to establish a relationship between protein size and pharmacokinetic (PK) parameters...
July 5, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28664316/galactosyl-pentadecene-reversibly-enhances-transdermal-and-topical-drug-delivery
#17
Monika Kopečná, Miloslav Macháček, Eva Prchalová, Petr Štěpánek, Pavel Drašar, Martin Kotora, Kateřina Vávrová
PURPOSE: To study new skin penetration/permeation enhancers based on amphiphilic galactose derivatives. METHODS: Two series of alkyl and alkenyl galactosides were synthesized and evaluated for their enhancing effect on transdermal/topical delivery of theophylline (TH), hydrocortisone (HC) and cidofovir (CDV), reversibility of their effects on transepidermal water loss (TEWL) and skin impedance, interaction with the stratum corneum using infrared spectroscopy, and cytotoxicity on keratinocytes and fibroblasts...
June 29, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28660401/individual-bayesian-information-matrix-for-predicting-estimation-error-and-shrinkage-of-individual-parameters-accounting-for-data-below-the-limit-of-quantification
#18
Thi Huyen Tram Nguyen, Thu Thuy Nguyen, France Mentré
PURPOSE: In mixed models, the relative standard errors (RSE) and shrinkage of individual parameters can be predicted from the individual Bayesian information matrix (MBF). We proposed an approach accounting for data below the limit of quantification (LOQ) in MBF. METHODS: MBF is the sum of the expectation of the individual Fisher information (MIF) which can be evaluated by First-Order linearization and the inverse of random effect variance. We expressed the individual information as a weighted sum of predicted MIF for every possible design composing of measurements above and/or below LOQ...
June 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28660400/development-of-a-two-dimensional-model-for-predicting-transdermal-permeation-with-the-follicular-pathway-demonstration-with-a-caffeine-study
#19
Panayiotis Kattou, Guoping Lian, Stephen Glavin, Ian Sorrell, Tao Chen
PURPOSE: The development of a new two-dimensional (2D) model to predict follicular permeation, with integration into a recently reported multi-scale model of transdermal permeation is presented. METHODS: The follicular pathway is modelled by diffusion in sebum. The mass transfer and partition properties of solutes in lipid, corneocytes, viable dermis, dermis and systemic circulation are calculated as reported previously [Pharm Res 33 (2016) 1602]. The mass transfer and partition properties in sebum are collected from existing literature...
June 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28653157/computational-analysis-on-down-regulated-images-of-macrophage-scavenger-receptor
#20
Byeongtaek Oh, Yugyung Lee, Mingui Fu, Chi H Lee
BACKGROUND: Thiolated-graphene quantum dots (SH-GQDs) were developed and assessed for an efficient preventive means against atherosclerosis and potential toxicity through computational image analysis and animal model studies. EXPERIMENTS: Zebrafish (wild-type, wt) were used for evaluation of toxicity through the assessment of embryonic mortality, malformation and ROS generation. The amounts of SH-GQDs uptaken by mouse macrophage cells (Raw264.7) were analyzed using a flow cytometer...
June 26, 2017: Pharmaceutical Research
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