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Daniel Dantzic, Pawan Noel, Fabrice Merien, Dong-Xu Liu, Jun Lu, Haiyong Han, Mark J McKeage, Yan Li
Multidrug resistance (MDR) is a major hurdle which must be overcome to effectively treat cancer. ATP-binding cassette transporters (ABC transporters) play pivotal roles in drug absorption and disposition, and overexpression of ABC transporters has been shown to attenuate cellular/tissue drug accumulation and thus increase MDR across a variety of cancers. Overcoming MDR is one desired approach to improving the survival rate of patients. To date, a number of modulators have been identified which block the function and/or decrease the expression of ABC transporters, thereby restoring the efficacy of a range of anticancer drugs...
August 9, 2018: Pharmaceutics
Volha Dzmitruk, Evgeny Apartsin, Aliaksei Ihnatsyeu-Kachan, Viktar Abashkin, Dzmitry Shcharbin, Maria Bryszewska
The lack of an appropriate intracellular delivery system for therapeutic nucleic acids (TNAs) is a major problem in molecular biology, biotechnology, and medicine. A relatively new class of highly symmetrical hyperbranched polymers, called dendrimers, shows promise for transporting small TNAs into both cells and target tissues. Dendrimers have intrinsic advantages for this purpose: their physico-chemical and biological properties can be controlled during synthesis, and they are able to transport large numbers of TNA molecules that can specifically suppress the expression of single or multiple targeted genes...
August 8, 2018: Pharmaceutics
Ravindranath Reddy Gilibili, Vishwanath Kurawattimath, Bokka Venkata Murali, Yurong Lai, T Thanga Mariappan, Hong Shen, Sagnik Chatterjee
Previously we reported that coproporphyrin-I (CP-I) is an optimal probe substrate for multidrug resistance-associated protein 2 (MRP2), and stimulation of MRP2-mediated transport is probe substrate-dependent. In the present investigation, we assessed if the in vitro stimulation is physiologically relevant. Similar to human MRP2 transport, CP-I was transported by rat Mrp2 in a typical Michaelis-Menten kinetics with apparent Km and Vmax values of 15 ± 6 µM and 161 ± 20 pmol/min/mg protein, respectively. In vivo Mrp2 functions were monitored by biliary and renal secretion of CP-I and its isomer CP-III, in bile-duct cannulated rats before and after treatment with mitoxantrone, progesterone, and verapamil...
August 8, 2018: Pharmaceutics
Zhi-Yuan Zhang, Hua Zhang, Dan Liu, Ying-Yuan Lu, Xin Wang, Pu Li, Ya-Qing Lou, Bao-Xue Yang, Ya-Xin Lou, Chuang Lu, Qiang Zhang, Guo-Liang Zhang
Methyl 3-amino-6-methoxythieno [2,3-b] quinoline-2-carboxylate (PU-48) is a novel diuretic urea transporter inhibitor. The aim of this study is to investigate the profile of plasma pharmacokinetics, tissue distribution, and excretion by oral dosing of PU-48 in rats. Concentrations of PU-48 within biological samples are determined using a validated high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. After oral administration of PU-48 (3, 6, and 12 mg/kg, respectively) in self-nanomicroemulsifying drug delivery system (SNEDDS) formulation, the peak plasma concentrations ( C max ), and the area under the curve (AUC0⁻∞ ) were increased by the dose-dependent and linear manner, but the marked different of plasma half-life ( t 1/2 ) were not observed...
August 8, 2018: Pharmaceutics
Lingzhi Wang, Do-Dang Khoa Phan, Nicholas Syn, Xiaoqiang Xiang, Hongyan Song, Win Lwin Thuya, Shili Yang, Andrea Li-Ann Wong, Alan Prem Kumar, Wei Peng Yong, Gautam Sethi, Paul Chi-Lui Ho, Boon Cher Goh
A sensitive and robust liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the determination of nimbolide in mouse serum. Exemestane was used as the internal standard (IS). Here, we employed acetonitrile-based protein precipitation (PPT) for serum sample preparation, and performed chromatographic separation using an ODS Hypersil C18 column (100 mm × 2.1 mm, 5 µm) with gradient elution (0.1% formic acid in water vs 100% acetonitrile). The run time was 6 min. Instrumental analysis was performed by electrospray ionization tandem mass spectrometry (ESI-MS/MS) in the multiple-reaction monitoring (MRM) under positive mode...
August 8, 2018: Pharmaceutics
Riccardo Ferracini, Isabel Martínez Herreros, Antonio Russo, Tommaso Casalini, Filippo Rossi, Giuseppe Perale
Although bone has a high potential to regenerate itself after damage and injury, the efficacious repair of large bone defects resulting from resection, trauma or non-union fractures still requires the implantation of bone grafts. Materials science, in conjunction with biotechnology, can satisfy these needs by developing artificial bones, synthetic substitutes and organ implants. In particular, recent advances in materials science have provided several innovations, underlying the increasing importance of biomaterials in this field...
August 8, 2018: Pharmaceutics
Apipa Wanasathop, S Kevin Li
Iontophoresis is a noninvasive method to enhance systemic and local drug delivery by the application of an electric field. For systemic drug delivery in the oral cavity, iontophoresis was studied primarily for transbuccal delivery. Significant enhancement of drug delivery was observed in buccal iontophoresis compared to passive transport for different drugs. For local drug delivery in the oral cavity, iontophoresis could enhance drug penetration into the enamel, dentin, and other oral tissues for the treatment of oral diseases...
August 7, 2018: Pharmaceutics
Evgeny K Apartsin, Alina E Grigoryeva, Audrey Malrin-Fournol, Elena I Ryabchikova, Alya G Venyaminova, Serge Mignani, Anne-Marie Caminade, Jean-Pierre Majoral
In this work, we report the assemblage of hydrogels from phosphorus dendrimers in the presence of biocompatible additives and the study of their interactions with nucleic acids. As precursors for hydrogels, phosphorus dendrimers of generations 1⁻3 based on the cyclotriphosphazene core and bearing ammonium or pyridinium acetohydrazones (Girard reagents) on the periphery have been synthesized. The gelation was done by the incubation of dendrimer solutions in water or phosphate-buffered saline in the presence of biocompatible additives (glucose, glycine or polyethylene glycol) to form physical gels...
August 6, 2018: Pharmaceutics
Young A Choi, Im-Sook Song, Min-Koo Choi
A sensitive and simple chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to evaluate memantine in rat plasma. Memantine and propranolol (internal standard) in rat plasma was extracted using a methanol precipitation method. The standard curve value was 0.2⁻1000 ng/mL and selectivity, linearity, inter-day and intra-day accuracy and precision were within acceptance criteria. Using this validated method, drug-drug interactions between memantine and cimetidine was measured following co-administration of memantine and cimetidine intravenously and orally...
August 6, 2018: Pharmaceutics
Reema Narayan, Usha Y Nayak, Ashok M Raichur, Sanjay Garg
Recent advancements in drug delivery technologies utilizing a variety of carriers have resulted in a path-breaking revolution in the approach towards diagnosis and therapy alike in the current times. Need for materials with high thermal, chemical and mechanical properties have led to the development of mesoporous silica nanoparticles (MSNs). These ordered porous materials have garnered immense attention as drug carriers owing to their distinctive features over the others. They can be synthesized using a relatively simple process, thus making it cost effective...
August 6, 2018: Pharmaceutics
Hiep X Nguyen, Ajay K Banga
In this study, we used sonophoresis and iontophoresis to enhance the in vitro delivery of methotrexate through human cadaver skin. Iontophoresis was applied for 60 min at a 0.4 mA/sq·cm current density, while low-frequency sonophoresis was applied at a 20 kHz frequency (2 min application, and 6.9 W/sq·cm intensity). The treated skin was characterized by dye binding, transepidermal water loss, skin electrical resistance, and skin temperature measurement. Both sonophoresis and iontophoresis resulted in a significant reduction in skin electrical resistance as well as a marked increase in transepidermal water loss value ( p < 0...
August 5, 2018: Pharmaceutics
Stella Gänger, Katharina Schindowski
The blood-brain barrier and the blood-cerebrospinal fluid barrier are major obstacles in central nervous system (CNS) drug delivery, since they block most molecules from entering the brain. Alternative drug delivery routes like intraparenchymal or intrathecal are invasive methods with a remaining risk of infections. In contrast, nose-to-brain delivery is a minimally invasive drug administration pathway, which bypasses the blood-brain barrier as the drug is directed from the nasal cavity to the brain. In particular, the skull base located at the roof of the nasal cavity is in close vicinity to the CNS...
August 3, 2018: Pharmaceutics
Weidong Huang, Yaoyao Yang, Biwei Zhao, Gangqiang Liang, Shiwei Liu, Xian-Li Liu, Deng-Guang Yu
Enhancing the dissolution of insoluble active ingredients comprises one of the most important issues in the pharmaceutical and biomaterial fields. Here, a third generation solid dispersion (3rd SD) of ferulic acid was designed and fabricated by a modified coaxial electrospinning process. A traditional second generation SD (2nd SD) was also prepared by common one-fluid blending electrospinning and was used as a control. With poly(vinyl alcohol) as the fiber matrix and polyvinylpyrrolidone K10 as an additive in the 3rd SDs, the two electrospinning processes were investigated...
August 2, 2018: Pharmaceutics
Gergő Fülöp, Attila Balogh, Balazs Farkas, Attila Farkas, Bence Szabó, Balázs Démuth, Enikő Borbás, Zsombor Kristóf Nagy, György Marosi
Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone- co -vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM)...
August 2, 2018: Pharmaceutics
Arianna Cecilia Cozzi, Benedetta Briasco, Enrico Salvarani, Barbara Mannucci, Filippo Fangarezzi, Paola Perugini
Plastic material is used for a wide variety of commercial packaging due to being inexpensive, lightweight, and due to its resistance. In pharmaceutics, container-content compatibility studies are required for product authorization. Many guidelines and publications are available; however, the information is often only related to the raw materials used to produce packaging. During the manufacturing process, substances can be added to improve the product characteristics and performance, resulting in a processed material that is considerably different from the unprocessed material...
August 2, 2018: Pharmaceutics
Riya Shrestha, Pil Joung Cho, Sanjita Paudel, Aarajana Shrestha, Mi Jeong Kang, Tae Cheon Jeong, Eung-Seok Lee, Sangkyu Lee
Loxoprofen, a propionic acid derivative, non-steroidal anti-inflammatory drug (NSAID) is a prodrug that is reduced to its active metabolite, trans-alcohol form (Trans-OH) by carbonyl reductase enzyme in the liver. Previous studies demonstrated the hydroxylation and glucuronidation of loxoprofen. However, the specific enzymes catalyzing its metabolism have yet to be identified. In the present study, we investigated metabolic enzymes, such as cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT), which are involved in the metabolism of loxoprofen...
August 2, 2018: Pharmaceutics
Elham Hatami, Prashanth K B Nagesh, Pallabita Chowdhury, Subhash C Chauhan, Meena Jaggi, Amali E Samarasinghe, Murali M Yallapu
Lung cancer (LC) is one of the leading causes of death in both men and women in the United States. Tannic acid (TA), a water-soluble polyphenol, exhibits a wide range of biological activities. TA has received much attention as a promising compound in the biomaterial and drug delivery fields. Lung fluid (LF) is a major barrier for distribution of drugs to the lungs. Therefore, the purpose of this study was to examine TA interaction with LF for effective delivery of anti-cancer drug molecules via pulmonary delivery...
August 1, 2018: Pharmaceutics
Angélica Graça, Lídia Maria Gonçalves, Sara Raposo, Helena Margarida Ribeiro, Joana Marto
Polymer-based eye drops are the most used drug delivery system to treat dry eye disease (DED). Therefore, the mucoadhesion between the polymer and the ocular mucin is crucial to ensure the efficacy of the treatment. In this context, the present study aimed to evaluate the potential use of in vitro methods to study the mucoadhesion of eye drop solutions and, specifically to evaluate the efficacy of two hyaluronic acid-based formulations (HA), HA 0.15% and 0.30% ( w / v ) to treat DED. Rheology methods and zeta potential determination were used to study the mucoadhesive properties of both eye drop solutions...
August 1, 2018: Pharmaceutics
Dasan Mary Jaya Seema, Bullo Saifullah, Mariadoss Selvanayagam, Sivapragasam Gothai, Mohd Zobir Hussein, Suresh Kumar Subbiah, Norhaizan Mohd Esa, Palanisamy Arulselvan
In this study anticancer nanocomposite was designed using graphene oxide (GO) as nanocarrier and Phenethyl isothiocyanate (PEITC) as anticancer agent. The designed formulation was characterized in detailed with XRD, Raman, UV/Vis, FTIR, DLS and TEM etc. The designed anticancer nanocomposite showed much better anticancer activity against liver cancer HepG2 cells compared to the free drug PEITC and was also found to be nontoxic to the normal 3T3 cells. In vitro release of the drug from the anticancer nanocomposite formulation was found to be sustained in human body simulated phosphate buffer saline (PBS) solution of pH 7...
August 1, 2018: Pharmaceutics
Indumathi Sathisaran, Sameer Vishvanath Dalvi
Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aqueous solubility. One of the ways to enhance the aqueous solubility of poorlywater-soluble drugs is to use the principles of crystal engineering to formulate cocrystals of these molecules with water-soluble molecules (which are generally called coformers). Many researchers have shown that the cocrystals significantly enhance the aqueous solubility of poorly water-soluble drugs...
July 31, 2018: Pharmaceutics
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