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Journal of Pharmaceutical Sciences

Susumu Ishiguro, Nabil A Alhakamy, Deepthi Uppalapati, Jennifer Delzeit, Cory J Berkland, Masaaki Tamura
To evaluate the potential of cell-penetrating peptide-based delivery of apoptosis-inducer gene in cancer therapy, a modified HIV-1 TAT peptide (dimerized TAT peptide, dTAT) was studied. The dTAT and plasmid DNA (pDNA) complexes (dTAT-pDNA) were condensed using calcium chloride (dTAT-pDNA-Ca(2+)). This simple nonviral formulation approach showed high levels of gene expression in vitro without any cytotoxicity. In mouse studies, a single intratracheal (IT) aerosol spray or 2 intravenous (IV) injections of the dTAT, apoptosis-inducer gene, angiotensin II type 2 receptor (AT2R), and Ca(2+) complexes (dTAT-pAT2R-Ca(2+)) significantly attenuated the acutely growing mouse Lewis lung carcinoma allografts in mouse lungs...
October 18, 2016: Journal of Pharmaceutical Sciences
Sarsvat Patel, Xiang Kou, Hao Helen Hou, Ye Bill Huang, John C Strong, Geoff G Z Zhang, Changquan Calvin Sun
Amorphous solid dispersions (ASDs) consisting of acetaminophen (APAP) and copovidone were systematically studied to identify effects of drug loading and moisture content on mechanical properties, thermal properties, and tableting behavior. ASDs containing APAP at different levels were prepared by film casting and characterized by differential scanning calorimetry and nanoindentation. The glass transition temperature (Tg) continuously decreased with increasing amount of APAP, but the hardness of ASDs was increased at a low APAP content and reduced at high APAP content...
October 18, 2016: Journal of Pharmaceutical Sciences
Singkome Tima, Siriporn Okonogi, Chadarat Ampasavate, Chad Pickens, Cory Berkland, Songyot Anuchapreeda
This study aimed at developing a curcumin (CM) nanoparticle targeted to Feline McDonough Sarcoma (FMS)-like tyrosine kinase 3 (FLT3) protein on the surface of leukemic cells and at evaluating their properties, specificity, cytotoxicity, and inhibitory effect on FLT3 protein level in FLT3-overexpressing leukemic cells, EoL-1, and MV-4-11 cells. FLT3-specific peptides were conjugated onto modified poloxamer 407 using the copper-catalyzed azide-alkyne cycloaddition reaction. The thin film hydration method was performed for FLT3-specific CM-loaded polymeric micelles (FLT3-CM-micelles) preparation...
October 14, 2016: Journal of Pharmaceutical Sciences
Lucjan Jerzykiewicz, Adam Sroka, Irena Majerz
The crystal structure of fenamic acid-acridine complex is determined by X-ray diffraction. The strong OHN hydrogen bond linking the complex components and other interactions responsible for packing of the molecules into a crystal are investigated within the Quantum Theory of Atom in Molecule theory. The crystal structure is compared with the structure optimized at B3LYP/6-311++G** level and with the theoretical structures optimized under systematically changed pressure. Analysis of the lattice constants, hydrogen bond lengths, and angles of the inter- and intramolecular hydrogen bond under compression is performed...
October 14, 2016: Journal of Pharmaceutical Sciences
Rodrigo Cristofoletti, Jennifer B Dressman
In vitro-in vivo extrapolation techniques combined with physiologically based pharmacokinetic models represent a feasible approach to establishing links between critical quality attributes and the time course of drug concentrations in vivo. By further integrating the results with pharmacodynamic (PD) models, scientists can also explore the time course of drug effect. The aim of this study was to assess whether differences in dissolution rates would affect the onset, magnitude, and duration of the time course of ibuprofen-mediating pain relief...
October 14, 2016: Journal of Pharmaceutical Sciences
Ajit S Narang, Timothy Stevens, Mario Hubert, Srinivasa Paruchuri, Kevin Macias, Dilbir Bindra, Zhihui Gao, Sherif Badawy
Real-time process monitoring using a process analytical technology for granule size distribution can enable quality-by-design in drug product manufacturing. In this study, the resolution and sensitivity of chord length distribution (CLD) measured inline inside a high shear granulator using focused beam reflectance measurement (FBRM) C35 probe was investigated using different particle size grades of microcrystalline cellulose (MCC). In addition, the impact of water and impeller tip speed on the measurement accuracy as well as correlation with offline particle sizing techniques (FBRM, laser diffraction [Malvern Mastersizer(®)], microscopy [Sympatec QicPic(®)], and nested sieve analysis) was studied...
October 13, 2016: Journal of Pharmaceutical Sciences
Huixin Luo, Huimin Li, Xiaoyuan Yang, Jing Li, Xinge Zhang, Zhongming Wu
To overcome the chemical penetration enhancer-associated toxicities, without sacrificing delivery efficiency, a functional ε-polylysine (EPL-g-Cetyl) as polymeric permeation enhancers was synthesized by the hydrophobic modification of amino groups of ε-polylysine. The obtained EPL-g-Cetyl nanoparticles had about 200 nm in size with narrower distribution, high positive charge, and good stability. A high loading capacity (up to 17%) of the formulation provided a sustained and controlled release pattern of insulin from the nanoparticles...
October 13, 2016: Journal of Pharmaceutical Sciences
William F Weiss, John P Gabrielson, Wasfi Al-Azzam, Guodong Chen, Darryl L Davis, Tapan K Das, David B Hayes, Damian Houde, Satish K Singh
Characterization of the higher order structure (HOS) of protein-based biopharmaceutical products is an important aspect of their development. Opinions vary about how best to apply biophysical methods, in which contexts to use these methods, and how to use the resulting data to make technical decisions as drug candidates are commercialized [Gabrielson JP, Weiss WF IV. J Pharm Sci. 2015;104(4):1240-1245]. The aim of this commentary is to provide guidance for the development and implementation of a robust and comprehensive HOS characterization strategy...
October 12, 2016: Journal of Pharmaceutical Sciences
Mounir Maafi, Wassila Maafi
New semi-empirical rate-law system of equations is proposed for the first time for consecutive photoreactions that involve up to 4 photoreaction steps, AB4(4Φ). The equation system was developed, tested, and validated against synthetic kinetic traces generated by fifth-order Runge-Kutta calculations. The model accurately fitted the kinetic traces of Riboflavin photodegradation in ethanol which decomposes via the AB2(2Φ) mechanism involving 2 consecutive photoreaction steps. A kinetic elucidation methodology useful for consecutive photoreactions was also proposed to determine all the kinetic parameters and reaction attributes defining AB2(2Φ) reactions...
October 6, 2016: Journal of Pharmaceutical Sciences
Yassmin O Samak, Magda El Massik, Allan G A Coombes
Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion into blank microparticles or by direct encapsulation. Homogenization method produced smaller microparticles (45-50 μm), compared to aerosolization (65-90 μm). High drug loadings (40% wt/wt) were obtained for diffusion-loaded aerosolized microparticles...
September 29, 2016: Journal of Pharmaceutical Sciences
Siyuan Huang, Chen Mao, Robert O Williams, Chia-Yi Yang
The solubility of a drug is ultimately governed by its chemical potential as it is present in the undissolved solute. For a pharmaceutical amorphous solid dispersion (ASD), its solubility depends on the state and composition of the undissolved solute when the ASD is equilibrated with water. Concerning the undissolved solute phase that can contain up to 3 components (drug, polymer, and water), we developed a complete thermodynamic model to calculate the chemical potential of a drug in the multicomponent, amorphous system...
September 28, 2016: Journal of Pharmaceutical Sciences
Davide Fissore
This article is focused on the design of a fuzzy logic-based control system to optimize a drug freeze-drying process. The goal of the system is to keep product temperature as close as possible to the threshold value of the formulation being processed, without trespassing it, in such a way that product quality is not jeopardized and the sublimation flux is maximized. The method involves the measurement of product temperature and a set of rules that have been obtained through process simulation with the goal to obtain a unique set of rules for products with very different characteristics...
September 28, 2016: Journal of Pharmaceutical Sciences
Israel Borges Sebastião, Thomas D Robinson, Alina Alexeenko
Atmospheric spray freeze-drying (ASFD) represents a novel approach to dry thermosensitive solutions via sublimation. Tests conducted with a second-generation ASFD equipment, developed for pharmaceutical applications, have focused initially on producing a light, fine, high-grade powder consistently and reliably. To better understand the heat and mass transfer physics and drying dynamics taking place within the ASFD chamber, 3 analytical models describing the key processes are developed and validated. First, by coupling the dynamics and heat transfer of single droplets sprayed into the chamber, the velocity, temperature, and phase change evolutions of these droplets are estimated for actual operational conditions...
September 28, 2016: Journal of Pharmaceutical Sciences
Ajit S Narang, Lydia Breckenridge, Hang Guo, Jennifer Wang, Abraham Avi Wolf, Divyakant Desai, Sailesh Varia, Sherif Badawy
Surface erosion of uncoated tablets results in processing problems such as dusting and defects during coating and is governed by the strength of particle bonding on tablet surface. In this study, the correlation between dusting tendency of tablets in a coating pan with friability and laser ablation surface hardness was assessed using tablets containing different concentrations of magnesium stearate and tartaric acid. Surface erosion propensity of different batches was evaluated by assessing their dusting tendency in the coating pan...
September 26, 2016: Journal of Pharmaceutical Sciences
Jon Hilden, Mark Polizzi, Aaron Zettler
The diametrical compression (DC) test, as defined in United States Pharmacopeia <1217> and in American Society for Testing and Materials testing standard D 3967, has been used extensively to derive the tensile strength (TS) of pharmaceutical tablets from the measured breaking force. DC-derived TSs provide a good approach to measuring the consistency of tablet mechanical properties from one batch to the next. For these quality control type applications, method precision is required, but accuracy is not...
September 26, 2016: Journal of Pharmaceutical Sciences
Rebekah L Scheuerle, Richard A Kendall, Catherine Tuleu, Nigel K H Slater, Stephen E Gerrard
An in vitro simulation system was developed to study the effect of an infant's peristaltic tongue motion during breastfeeding on oral rapidly disintegrating tablets in the mouth, for use in rapid product candidate screening. These tablets are being designed for use inside a modified nipple shield worn by a mother during breastfeeding, a proposed novel platform technology to administer drugs and nutrients to breastfeeding infants. In this study, the release of a model compound, sulforhodamine B, from tablet formulations was studied under physiologically relevant forces induced by compression and rotation of a tongue mimic...
September 26, 2016: Journal of Pharmaceutical Sciences
David L Bain, Michael Brenowitz, Christopher J Roberts
Training researchers for positions in the United States biopharmaceutical industry has long been driven by academia. This commentary explores how the changing landscape of academic training will impact the industrial workforce, particularly with regard to the development of protein therapeutics in the area of biophysical and higher order structural characterization. We discuss how to balance future training and employment opportunities, how academic-industrial partnerships can help young scientists acquire the skills needed by their future employer, and how an appropriately trained workforce can facilitate the translation of new technology from academic to industrial laboratories...
September 23, 2016: Journal of Pharmaceutical Sciences
Shadab Shahsavari, Leila Rezaie Shirmard, Mohsen Amini, Farid Abedin Dokoosh
Formulation of a nanoparticulate Fingolimod delivery system based on biodegradable poly(3-hydroxybutyrate-co-3-hydroxyvalerate) was optimized according to artificial neural networks (ANNs). Concentration of poly(3-hydroxybutyrate-co-3-hydroxyvalerate), PVA and amount of Fingolimod is considered as the input value, and the particle size, polydispersity index, loading capacity, and entrapment efficacy as output data in experimental design study. In vitro release study was carried out for best formulation according to statistical analysis...
September 22, 2016: Journal of Pharmaceutical Sciences
Bruno C Hancock
Predicting the crystallization propensity of drug-like molecules is one of the most significant challenges facing pharmaceutical scientists today. Despite the importance of being able to understand what structural features of a molecule (polarity, molecular size, etc.) and which experimental conditions (temperature, concentration, etc.) permit a molecule to crystallize, there has been very little published work focused on this topic. This commentary provides a short overview of recent progress in this area and points to potential experimental and computational approaches that might be used in the future...
September 22, 2016: Journal of Pharmaceutical Sciences
Sunny Bhardwaj, Maya Lipert, Annette Bak
Poor aqueous solubility of a majority of new small molecule chemical entities is a significant challenge in drug discovery since considerably high exposures are often required to enable pharmacokinetic, pharmacology, and toxicology studies. Pharmaceutical cocrystals have received considerable attention in recent years owing to their potential to improve the physicochemical properties and in vivo performance of poorly soluble drugs. However, physical instability in supersaturated solution/suspension formulations is a major concern for their use in preclinical studies...
September 21, 2016: Journal of Pharmaceutical Sciences
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