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Journal of Pharmaceutical Sciences

Xin Zhou, Qiubing Chen, Ya Ma, Yamei Huang, Shuangquan Gou, Bo Xiao
Porous microparticles (MPs) have been regarded as a promising vehicle for drug delivery. Herein, porous MPs and their counterparts (non-porous MPs) were produced by a conventional emulsion-solvent evaporation method in the presence and absence of ammonium bicarbonate, and curcumin (CUR) was encapsulated into these MPs during the preparation process. The obtained MPs possessed desirable diameters of around 1.2 μm and negative zeta potentials of approximately -28 mV. It was found that the release rate of CUR was remarkably increased with the introduction of pores in MPs...
February 16, 2019: Journal of Pharmaceutical Sciences
Erizal Zaini, Lili Fitriani, Risda Yulia Sari, Henni Rosaini, Ayano Horikawa, Hidehiro Uekusa
A novel multicomponent crystal of mefenamic acid (MA) and N-methyl-D-glucamine (MG) had been prepared in order to improve the physicochemical properties of poorly soluble drugs, and was characterized for its physicochemical properties by powder X-ray diffraction analysis, DSC thermal analysis, FT-IR spectroscopy, in vitro dissolution rate and physical stability. Also, the crystal structure was determined by single crystal X-ray diffraction analysis. The DSC thermogram of the MA-MG binary system exhibits a single and sharp endothermic peak at 151...
February 16, 2019: Journal of Pharmaceutical Sciences
Neal Whitaker, John M Hickey, Kawaljit Kaur, Jian Xiong, Nishant Sawant, Albert Cupo, Wen-Hsin Lee, Gabriel Ozorowski, Max Medina-Ramírez, Andrew B Ward, Rogier W Sanders, John P Moore, Sangeeta B Joshi, David B Volkin, Antu K Dey
The induction of broadly neutralizing antibodies (bNAb) is a major goal in the development of an effective vaccine against HIV-1. A soluble, trimeric, germline (gI) bNAb-targeting variant of the HIV-1 envelope glycoprotein (termed BG505 SOSIP.v4.1-GT1.1 gp140, abbreviated to GT1.1) has recently been developed. Here, we have compared this new immunogen with the parental trimer from which it was derived, BG505 SOSIP.664 gp140. We used a comprehensive suite of biochemical and biophysical methods to determine physicochemical similarities and differences between the two trimers, and thereby assessed whether additional formulation development efforts were needed for the GT1...
February 15, 2019: Journal of Pharmaceutical Sciences
Jibin Li, Li-Bin Li, Nourdine Nessah, Yuehua Huang, Carlos Hidalgo, Albert Owen, Ismael J Hidalgo
The in vitro dissolution absorption system (IDAS2), a recent invention comprised of a conventional dissolution vessel containing two permeation chambers with Caco-2 cell monolayers mounted with their apical side facing the dissolution media, permits simultaneous measurement of dissolution and permeation of drugs from intact clinical dosage forms. The objectives of this study were 1) to assess the utility of IDAS2 in the determination of the effect of particle size on in vitro performance of indomethacin and 2) to find out whether the behavior in IDAS2 of two indomethacin products differing in particle size is correlated with their in vivo behavior...
February 15, 2019: Journal of Pharmaceutical Sciences
Yuxiang Zhao, Wenlong Li, Zhenqi Shi, James K Drennen, Carl A Anderson
This study utilized multiple modeling approaches to predict immediate release tablet dissolution profiles of two model drugs: theophylline and carbamazepine. Two sets of designs of experiments were applied based on individual drug characteristics to build in adequate dissolution variability. The tablets were scanned using a near infrared (NIR) spectrometer and then subjected to in vitro dissolution test at critical time points. Due to the inherent difference in dissolution profiles, a hierarchical modeling approach was applied for theophylline data while global models were constructed from Carbamazepine data...
February 8, 2019: Journal of Pharmaceutical Sciences
Mitchell P McInerney, Yijun Pan, Irene Volitakis, Ashley I Bush, Jennifer L Short, Joseph A Nicolazzo
Previous studies have demonstrated that the ionophore clioquinol (CQ), in conjunction with the biometals copper and zinc, increases the expression of P-glycoprotein (P-gp) in human cerebral microvascular endothelial (hCMEC/D3) cells. As P-gp expression and function at the blood-brain barrier (BBB) is of great interest regarding CNS drug access and endogenous toxin trafficking (e.g. amyloid beta), the current study assessed the in vivo translation of these previous in vitro findings. Swiss outbred mice received an 11-day treatment of CQ (30 mg/kg) by oral gavage, after which brain microvessel-enriched fractions (MEF) and surrounding interfaces (subcortical brain tissue and plasma) were extracted...
February 7, 2019: Journal of Pharmaceutical Sciences
Po-Chang Chiang, Karthik Nagapudi, Jia Liu, James J Crawford, Jason R Zbieg, Emile Plise, Yuzhong Deng
It is well acknowledged that the oral absorption of a drug can be influenced by its solubility, which is usually associated with its solid form properties. G1032 is a Retinoic Acid-Related Orphan Receptor inverse agonist. Crystalline solid (Form A) was identified with an aqueous solubility of 130 μg/mL. This form was used in an oral dose escalation study in rodents up to 300 mg/kg and achieved good exposures. Later on, a more stable crystalline hydrate (Form B) was identified and the aqueous solubility was reduced to 55 μg/mL...
February 7, 2019: Journal of Pharmaceutical Sciences
Aditya V Gandhi, Theodore W Randolph, John F Carpenter
The impact of drug conjugation on intra- and intermolecular interactions of trastuzumab (TmAb) was determined by comparing the conformational and colloidal stabilities of TmAb and trastuzumab emtansine (T-DM1). In low ionic strength formulations, drug conjugation to native lysine residues of TmAb significantly reduced the repulsive electrostatic interactions between T-DM1 molecules. When these electrostatic interactions were screened in solutions with high ionic strength, intermolecular interactions between T-DM1 molecules were found to be more attractive than those between TmAb molecules...
February 5, 2019: Journal of Pharmaceutical Sciences
Petra Janská, Ondřej Rychecký, Aleš Zadražil, František Štěpánek, Jitka Čejková
Many new therapeutic candidates - active pharmaceutical ingredients (APIs) are poorly soluble in an aqueous environment resulting in their reduced bioavailability. A promising way of enhancing the release of an API and, thus, its bioavailability seems to be the use of liquid oil marbles (LOMs). A LOM system behaves as a solid form but consists of an oil droplet in which an already dissolved API is encapsulated by a powder. This study aimed to optimize the oil/powder combination for the development of such systems...
February 2, 2019: Journal of Pharmaceutical Sciences
Tycho Heimbach, Wen Lin, Florence Hourcade-Potelleret, Xianbin Tian, Francois Combes, Nicholas Horvath, Handan He
In adult patients nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform dosing regimen. An adult Simcyp PBPK model was established and verified with clinical pharmacokinetic data after a single or multiple oral doses of 400 mg nilotinib (230 mg/m2 ). The model was then applied to a pediatric PBPK model taking account of ontogeny profiles of metabolizing enzymes and pediatric physiological parameters...
February 2, 2019: Journal of Pharmaceutical Sciences
Siwen Wu, Wen Bin, Biyun Tu, Xifeng Li, Wei Wang, Suling Liao, Changshan Sun
Proteins/peptides are poorly absorbed via oral administration because of the gastrointestinal tract environment and lysosomal digestion after apical endocytosis. A delivery system, consisting of a deoxycholic acid-conjugated nanometer-sized carrier, may enhance the absorption of proteins/peptides in the intestine via the bile acid pathway. Deoxycholic acid is first conjugated to chitosan. Liposomes are then prepared and loaded with the model drug insulin. Finally, the conjugates are bound to the liposome surface to form deoxycholic acid conjugate-modified liposomes (DC-LIPs)...
February 2, 2019: Journal of Pharmaceutical Sciences
Weiwei Fan, Aohua Wang, Yue Wu, Jorrit Water, Stephen Buckley, Lars Hovgaard, Mingshi Yang, Yong Gan
Absorption enhancers are often a major component of solid oral peptide formulations as compared to the active pharmaceutical ingredient and excipients. This commonly results in poor tabletability that is hard to mitigate in direct compaction by addition of small amounts of excipients. To improve the tabletability of bulky absorption enhancers, the model absorption enhancers, sodium cholate and deoxycholic acid, were co-spray dried with hydroxypropyl methylcellulose (HPMC) E5 where the percentage of absorption enhancers was not lower than 90% (w/w)...
February 2, 2019: Journal of Pharmaceutical Sciences
Dong-Jun Bae, Sang-Yeob Kim, Sang Mun Bae, Ae-Kyung Hwang, Kwan Cheol Pak, SeokKyu Yoon, Hyeong-Seok Lim
In the current study, we evaluated the pharmacokinetics (PK) of trastuzumab and sought to predict human PK based on animal studies, through the use of optical imaging and a whole-body physiologically based pharmacokinetic (WB-PBPK) modeling approach. The PK study was conducted in 24 mice, where serial blood samples were withdrawn and major organs were isolated after the last blood withdrawal. The drug concentrations in blood and major organs were measured via optical imaging. The WB-PBPK model was constructed using known physiological values including the volumes of major organs and blood/lymphatic flow...
February 1, 2019: Journal of Pharmaceutical Sciences
Zsolt Sáfár, Márton Jani, Ildikó Makai, Zsolt Fekete, Annamária Bui, Éva Molnár, Petra Pádár, Jennifer R Pratt, Emese Kis, Erzsébet Beéry, Péter Krajcsi
No abstract text is available yet for this article.
January 29, 2019: Journal of Pharmaceutical Sciences
Iman Haidar, Ian H Harding, Ian C Bowater, Alasdair W McDowall
We report the colloidal characterisation of halofantrine (Hf) laden soybean oil (SBO) fat emulsions. Hf increased the zeta potential, at all pH values, of the fat emulsions. Concomitant with this, the isoelectric point (i.e.p.) of the emulsion increased to higher pH values. The emulsion was destabilised by a small amount of Hf; interestingly, however, this was ameliorated by increasing the amount of Hf. The particle size and polydispersity of the fat emulsion reflected this with a small Hf concentration resulting in a significant increase in both particle size and polydispersity, but less so as the Hf concentration was increased...
January 28, 2019: Journal of Pharmaceutical Sciences
Sathish Dharani, Sogra F Barakh Ali, Hamideh Afrooz, Mansoor A Khan, Ziyaur Rahman
The commercial product of rifaximin (RFX) contains α form. The α form can change to β form on exposure to high humidity that can occur during manufacturing, stability and/or in-use period. It is critical to maintain α form of the drug in a drug product to avoid variability in clinical response. FDA dissolution method was found to be non-discriminatory for RFX formulations containing either 100 % α or β form. The objective of the study was to develop a discriminatory dissolution method that can detect low levels of α to β transformation in RFX products...
January 24, 2019: Journal of Pharmaceutical Sciences
Aya Hasan Al-Shammari, Yusuke Masuo, Ken-Ichi Fujita, Yuka Yoshikawa, Noritaka Nakamichi, Yutaro Kubota, Yasutsuna Sasaki, Yukio Kato
The multi-kinase inhibitor regorafenib, which is a standard treatment for certain cancer patients after disease progression following other approved therapies, exhibits delayed-onset dermal toxicity. Here, we aimed to clarify the mechanisms that contribute to the increased dermal exposure to active metabolite M-5 of regorafenib after repeated oral administration. The dermal concentration of M-5 at 24 h after the last of five oral administrations of regorafenib in mdr1a/1b/bcrp-/- mice was more than 190 times that in wild-type mice...
January 24, 2019: Journal of Pharmaceutical Sciences
Athanasiadou Ioanna, Dokoumetzidis Aristeidis, Voss Sven Christian, El Saftawy Wesal, Al-Maadheed Mohammed, Valsami Georgia, Georgakopoulos Costas
Excessive fluid intake, i.e., hyperhydration may be adopted by athletes as a masking method during anti-doping sample collection to influence the excretion patterns of doping agents and, therefore, manipulate their detection. The aim of this exploratory study was to assess the hyperhydration effect on the detection sensitivity of recombinant human erythropoietin (rHuEPO) by SAR-PAGE analysis. The influence of hyperhydration on the serum and urinary pharmacokinetic (PK) profiles of rHuEPO was also investigated...
January 23, 2019: Journal of Pharmaceutical Sciences
Francis Kinderman, Brittany Yerby, Vibha Jawa, Marisa K Joubert, Nathan H Joh, Jennifer Malella, Johnathan Herskovitz, Jiansong Xie, John Ferbas, Helen J McBride
Antibody therapeutics with poor solubility in the subcutaneous matrix may carry unintended risks when administered to patients. The objective of this work was to estimate the risk of antibodies that precipitate in vitro at neutral pH by determining the impact of poor solubility on distribution of the drug from the injection site as well as immunogenicity in vivo. Using fluorescence imaging in a mouse model, we show that one such precipitation-prone antibody is retained at the injection site in the subcutaneous space longer than a control antibody...
January 23, 2019: Journal of Pharmaceutical Sciences
Shaimaa S Ibrahim
With the significant advances made in nanotechnology, research efforts focused on developing novel drug delivery platforms that can overcome the multitude of challenges encountered in ophthalmic drug delivery. Surface active agents (SAA) have been extensively used for the formulation of many of the dosage forms targeting ocular tissues. Novel ophthalmic carriers utilizing SAAs were broadly classified into particulate, vesicular and controlled release drug delivery systems. Depending on their physicochemical properties, SAAs can perform a variety of roles ranging from wetting agents, emulsifiers, stabilizers, charge inducers, solubilizers, antimicrobial agents, corneal permeation enhancers and gelling agents...
January 23, 2019: Journal of Pharmaceutical Sciences
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