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Journal of Pharmaceutical Sciences

Le Zhang, Lei Yu, Jian Zhang-Van Enk, Gang Huang, Jifeng Zhang
Modulation of liquid-liquid phase separation temperature (Tph) for liquid-liquid phase separation (LLPS) of a Fc-fusion protein was studied at pH values below, near and above its pI where the net charge of the protein was positive, neutral and negative, respectively, in KF, KCl, KSCN and MgCl2 solutions. At the pH value near the pI, the monotonic drop in Tph for all the salt solutions suggests that both the anion and cation can disrupt attractive protein-protein interactions, effectively salting-in the protein...
July 21, 2017: Journal of Pharmaceutical Sciences
Zhengwei Huang, Xiaona Chen, Han Fu, Xinguo Wen, Cheng Ma, Jiwen Zhang, Chuanyu Wu, Ying Huang, Xin Pan, Chuanbin Wu
Ultra-fine particle processing system (UPPS) was developed previously by our group to provide a new solution to microspheres fabrication. The UPPS was supposed to possess many featured advantages, but the microspheres formation mechanism during UPPS processing was still unknown. The objective of this study was to perform the formation mechanism investigation and in vitro evaluation on risperidone-containing PLGA microspheres (RIS-PLGA MS) fabricated by UPPS. Evaporation profile and viscosity of the PLGA containing solutions were considered as the critical factors for the microspheres formation mechanism, and were determined in present study...
July 20, 2017: Journal of Pharmaceutical Sciences
Christopher Thompson, Kelly Wilson, Yoen Joo Kim, Min Xie, William K Wang, Michaela Wendeler
Stainless steel containers are widely used in the pharmaceutical and biopharmaceutical industry for the storage of buffers, process intermediates, and purified drug substance. They are generally held to be corrosion resistant, biocompatible, and non-reactive, although it is well established that trace amounts of metal ions can leach from stainless steel equipment into biopharmaceutical products. We report here that the use of stainless steel containers in conjunction with magnetic stirring bars leads to significantly aggravated metal contamination, consisting both of metal particles and significantly elevated metal ions in solution, the degree of which is several orders of magnitude higher than described for static conditions...
July 19, 2017: Journal of Pharmaceutical Sciences
Joshua Boateng
Despite significant advances in pharmaceutical and biotechnological drug discovery, the global population is plagued with many challenging diseases. These are further compounded by anticipated explosion in an ageing population, which presents several problems such as polypharmacy, dysphagia and neurological conditions, resulting in non-compliance and disease complications. For antibiotics, poor compliance, can result in development of drug resistant infections which can be fatal. Further, children, especially, in developing countries die unnecessarily from easily treatable diseases (e...
July 19, 2017: Journal of Pharmaceutical Sciences
A Santoveña, C Monzón, C Alvarez-Lorenzo, C Del Rosario, A Delgado, C Evora, A Concheiro, M Llabrés, J B Fariña
PLGA-PEG-PLGA synthesis conditions have an impact on the physicochemical features of the copolymer and its usefulness as biomaterial. This study reports on an analysis of the composition and structural properties of PLGA-PEG-PLGA copolymers applying a variety of analytical techniques. Viscoelastic properties and particularly the temperature-responsive behavior of PLGA-PEG-PLGA showed a marked dependence on copolymer structural features. Physicochemical and biological properties, such as bioadhesion, biocompatibility and cell viability, of the raw copolymers and their gels were also evaluated...
July 18, 2017: Journal of Pharmaceutical Sciences
Renata Negrini, Simone Aleandri, Martin Kuentz
Nanosuspensions provide a drug delivery approach to cope with erratic absorption of poorly water-soluble compounds. Despite of extensive research over the last years, there are still open pharmaceutical challenges so it is often unclear how quality attributes such as viscosity and physical stability are generated, which requires a more thorough study of the colloidal structures and interactions in nanosuspensions. In this study, diffusing wave spectroscopy and microfluidics-based rheology were used for the first time to assess pharmaceutical nanosuspensions that were obtained by wet milling...
July 18, 2017: Journal of Pharmaceutical Sciences
Jing Tao, Sophia Robertson-Lavalle, Preetanshu Pandey, Sherif Badawy
A multi-layer tablet is one of the formulation options utilized to mitigate chemical and/or physical incompatibility between different drug substances. Feasibility studies of multi-layer tablets are often conducted using round flat-faced punch tooling. However the link between different tooling designs and multi-layer tablet performance is not well established. This study uses a prototype tri-layer tablet and examines tooling design considerations when conducting small-scale studies to gauge the risk of interfacial defects...
July 15, 2017: Journal of Pharmaceutical Sciences
E Elisei, J F Willart, F Danède, J Siepmann, F Siepmann, M Descamps
In this paper, solid state amorphization induced by mechanical milling is shown to be a useful tool to explore the polymorphism of drugs and their mechanism of devitrification. We show in particular how the recrystallization of amorphous chlorhexidine dihydrochloride obtained by milling reveals a complex polymorphism that involves several polymorphic forms. Two new crystalline forms are identified, one of them appearing as a highly disordered precursor state which however clearly differs from the amorphous one...
July 14, 2017: Journal of Pharmaceutical Sciences
Pasquino Rossana, Bruno De Gennaro, Danila Gaudino, Nino Grizzuti
Surfactant molecules can give rise to different morphological structures, depending on numerous parameters such as temperature, surfactant concentration and salinity. Specifically, the salt content can be easily tuned in a way to induce morphological transitions and modulate the rheological response. It is shown that non steroidal anti-inflammatory drugs can be used in the same way as classical binding salts in changing the rheological properties of the resulting gel-like system. On the one hand, the experimental results show that by tuning small details in the molecular conformation of the drug and its concentration in the micellar solution it is possible to obtain the desired mechanical response...
July 13, 2017: Journal of Pharmaceutical Sciences
Amanda K P Mann, Luke Schenck, Athanas Koynov, Alfred C F Rumondor, Xiaoling Jin, Melanie Marota, Chad Dalton
Many small molecule active pharmaceutical ingredients (APIs) exhibit low aqueous solubility, and benefit from generation of amorphous dispersions of the API and polymer to improve their dissolution properties. Spray drying and hot melt extrusion are two common methods to produce these dispersions; however, for some systems these approaches may not be optimal, and it would be beneficial to have an alternative route. Herein, amorphous solid dispersions of Compound A, a low solubility weak acid, and copovidone were made by conventional spray drying and co-precipitation...
July 12, 2017: Journal of Pharmaceutical Sciences
Asha Hewarathna, Olivier Mozziconacci, Maulik K Nariya, Peter A Kleindl, Jian Xiong, Adam C Fisher, Sangeeta B Joshi, C Russell Middaugh, M Laird Forrest, David B Volkin, Eric J Deeds, Christian Schöneich
As the second of a three part series of articles in this issue concerning the development of a mathematical model for comparative characterization of complex mixture drugs using Crofelemer (CF) as a model compound, this work focuses on the evaluation of the chemical stability profile of CF. CF is a biopolymer containing a mixture of proanthocyanidin oligomers which are primarily composed of gallocatechin with a small contribution from catechin. CF extracted from drug product was subjected to molecular weight-based fractionation and thiolysis...
July 5, 2017: Journal of Pharmaceutical Sciences
Vinod L Gaikwad, Neela M Bhatia, Indrajeet Singhvi, Kakasaheb R Mahadik, Manish S Bhatia
In the present research, predictive models were developed by correlating polymeric properties with characteristics of a formulation containing a drug with basic heterocycle (glipizide). Glipizide tablets containing different polymers from three categories (immediate, moderate and extended release) were prepared and evaluated. Dissolution kinetics indicated Korsmeyer-peppas as the best fit model, whereas transportability was influenced by release rate and hydrophobicity of the drug. Calculated polymeric descriptors were correlated with formulation properties for the development of predictive quantitative structure-property relationship models...
July 5, 2017: Journal of Pharmaceutical Sciences
Vibha Puri, Dave Brancazio, Parind M Desai, Keith D Jensen, Jung-Hoon Chun, Allan S Myerson, Bernhardt L Trout
The combination of hot melt extrusion and injection molding (HME-IM) is a promising process technology for continuous manufacturing of tablets. However, there has been limited research on its application to formulate crystalline drug containing immediate release tablets. Further, studies that have applied the HME-IM process to molded tablets have used a non-continuous two-step approach. The current study develops maltodextrin (MDX) based extrusion molded immediate release tablets for a crystalline drug (griseofulvin, GRIS) using an integrated twin-screw HME-IM continuous process...
July 3, 2017: Journal of Pharmaceutical Sciences
Az Alddien Natfji, Divyashree Ravishankar, Helen M I Osborn, Francesca Greco
The enhanced permeability and retention (EPR) effect constitutes the rationale by which nanotechnologies selectively target drugs to tumors. Despite promising pre-clinical and clinical results, these technologies have, in our view, underachieved compared to their potential, possibly due to a suboptimal exploitation of the EPR effect. Here, we have systematically analyzed clinical data to identify key parameters affecting the extent of the EPR effect. An analysis of 17 clinical studies showed that the magnitude of the EPR effect was varied and was influenced by tumor type and size...
June 29, 2017: Journal of Pharmaceutical Sciences
Neal Whitaker, Jian Xiong, Samantha E Pace, Vineet Kumar, C Russell Middaugh, Sangeeta B Joshi, David B Volkin
High protein concentration formulations are required for low volume administration of therapeutic antibodies targeted for subcutaneous, self-administration by patients. Ultra-high concentrations (≥ 150 mg/mL) can lead to dramatically increased solution viscosities, which in turn can lead to stability, manufacturing and delivery challenges. In this study, various categories and individual types of pharmaceutical excipients and other additives (58 in total) were screened for their viscosity reducing effects on two different monoclonal antibodies (mAbs)...
June 28, 2017: Journal of Pharmaceutical Sciences
Hao Xu, Yi Shi, Socrates Vela, Patrick Marroum, Ping Gao
This study is to evaluate three fenofibrate formulations including Fournier® 200 mg capsule, Lipidil® 145 mg tablet, and a clinical HME 160 mg tablet by an in vitro biphasic method. Key experimental parameters were evaluated including the selection of biorelevant media, the USP IV flowrate and the USP paddle speed. Varying the hydrodynamic condition resulted in a significant impact on FEN concentration time profiles in both aqueous and octanol phases for these formulations. In vivo pharmacokinetic profiles of the HME tablet, the Lipidil tablet and Fournier capsule under the fasting and low fat fed states are reported...
June 27, 2017: Journal of Pharmaceutical Sciences
Moheb M Nasr, Markus Krumme, Yoshihiro Matsuda, Bernhardt L Trout, Clive Badman, Salvatore Mascia, Charles L Cooney, Keith D Jensen, Alastair Florence, Craig Johnston, Konstantin Konstantinov, Sau L Lee
Continuous manufacturing plays a key role in enabling the modernization of pharmaceutical manufacturing. The fate of this emerging technology will rely, in large part, on the regulatory implementation of this novel technology. This paper, which is based on the 2(nd) International Symposium on the Continuous Manufacturing of Pharmaceuticals, describes not only the advances that have taken place since the first ISCMP in 2014, but the regulatory landscape that exists today. Key regulatory concepts including, Quality Risk Management, batch definition, control strategy, process monitoring and control, Real Time Release Testing, data processing and management, and process validation/verification are outlined...
June 24, 2017: Journal of Pharmaceutical Sciences
Thiagarajan Madheswaran, Rengarajan Baskaran, Bong Kyu Yoo, Prashant Kesharwani
In this study, we developed positively charged liquid crystalline nanoparticles (LCN) coated with chitosan (CHI) to enhance the skin permeation and distribution of 5α-reductase inhibitors for the treatment of androgenetic alopecia. LCN and surface-modified LCN (CHI-LCN) were prepared by ultrasonication method, and their physicochemical properties were characterized. In vitro and in vivo skin permeation and retention were studied using porcine abdominal skin and mice skin by using the Franz diffusion cell. Skin distribution and cellular uptake of LCN and CHI-LCN were also investigated...
June 23, 2017: Journal of Pharmaceutical Sciences
Po-Chang Chiang, Jodie Pang, Jia Liu, Laurent Salphati
It is well acknowledged that drugs with poor aqueous solubility are often associated with poor oral absorption. Fortunately, drugs with a basic pKa can take advantage of solubilization in the stomach under the acidic environment to improve exposure. Consequently, high in vivo variability is often observed when stomach pH is altered. When issue encountered, enabling formulations are often used to solve the problem. However, each enabling formulation has its limitations and the situation can be further complicated by other ADME parameters...
June 23, 2017: Journal of Pharmaceutical Sciences
Britta Furtmann, Justin Tang, Sven Kramer, Thomas Eickner, Frank Luderer, Gert Fricker, Alessandro Gomez, Bianca Heemskerk, Peter S Jähn
Polymer nanoparticles (NP) are of escalating interest for their application as immune stimulatory pharmaceutics. The production of nanosized carrier systems is currently being widely investigated, but commonly used techniques, such as the double emulsion technique, are limited by shortcomings of low encapsulation efficiency and poor control over size distribution. In this study, the electrospray technique was successfully implemented and optimized to produce monodisperse 200 nm poly (lactide-co glycolide) (PLGA) nanoparticles...
June 23, 2017: Journal of Pharmaceutical Sciences
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