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International Journal of Pharmaceutics

Tobias Tadken, Michael Weiss, Christiane Modess, Danilo Wegner, Tarek Roustom, Claudia Neumeister, Ulrich Schwantes, Hans-Ulrich Schulz, Werner Weitschies, Werner Siegmund
Intestinal P-glycoprotein is regio-selectively expressed and is a high affinity, low capacity efflux carrier for the cationic, poorly permeable trospium. Organic cation transporter 1 (OCT1) provides lower affinity but higher capacity for trospium uptake. To evaluate regional intestinal permeability, absorption profiles after gastric infusion of trospium chloride (30mg/250ml=[I]2) for 6h and after swallowing 30mg immediate-release tablets in fasted and fed healthy subjects, were evaluated using an inverse Gaussian density function to model input rate and mean absorption time (MAT)...
October 17, 2016: International Journal of Pharmaceutics
Yuuki Kasashima, Shinya Uchida, Keiichi Yoshihara, Takehiko Yasuji, Kazuhiro Sako, Noriyuki Namiki
The objective of this study was to evaluate the feasibility of lauryl sulfate (LS) salt/complex as a novel carrier in oral sustained-release suspensions. Mirabegron, which has a pH-dependent solubility, was selected as the model drug. Sodium lauryl sulfate (SLS) was bound to mirabegron in a stoichiometric manner to form a LS salt/complex. LS salt/complex formulation significantly reduced the solubility of mirabegron and helped mirabegron achieve sustained-release over a wide range of pH conditions. Microparticles containing the LS salt/complex were prepared by spray drying with the aqueous dispersion of ethylcellulose (Aquacoat(®) ECD)...
October 17, 2016: International Journal of Pharmaceutics
Takanori Kanazawa, Takahiro Endo, Naoki Arima, Hisako Ibaraki, Yuuki Takashima, Yasuo Seta
This study aimed to build an innovative system to deliver a systemic small interfering RNA (siRNA) treatment for rheumatoid arthritis. We combined arginine-histidine-cysteine based oligopeptide-modified polymer micelles with siRNA targeting the nuclear factor κB subunit, RelA (siRelA). This is a key molecule in the control of inflammation. We tested the cellular uptake of siRNA and its effects on inflammatory cytokine levels in vitro using synoviocytes, and siRNA distribution and therapeutic effects in vivo in mice with collagen-induced arthritis (CIA)...
October 17, 2016: International Journal of Pharmaceutics
Pramod Kumar, Gajanand Sharma, Rajendra Kumar, Bhupinder Singh, Ruchi Malik, Om Prakash Katare, Kaisar Raza
In various neurological disorders, antioxidants are frequently prescribed along with the specific treatment modalities. One such promising natural flavonoid is quercetin, offering better outcomes than established vitamins E and C. Though with immense promises, various challenges like poor oral-bioavailability (<2%), extensive first-pass metabolism, poor brain permeability, hydrophobic nature and physiological pH instability hinder its proper usage. Hence, it was planned to prepare quercetin-loaded nano lipidic carriers (NLCs) employing biocompatible components like phospholipids and tocopherol acetate for enhanced brain delivery...
October 15, 2016: International Journal of Pharmaceutics
Sungmun Lee, Yeu-Chun Kim, Ji-Ho Park
Reactive oxygen species (ROS) play an important role in the development of inflammatory bowel diseases. Superoxide dismutase (SOD) has a great therapeutic potential by scavenging superoxide that is one of ROS; however, in vivo application is limited especially when it is orally administered. SOD is easily degraded in vivo by the harsh conditions of gastrointestinal tract. Here, we design a zein-alginate based oral drug delivery system that protects SOD from the harsh conditions of gastrointestinal tract and releases it in the environment of the small intestine...
October 15, 2016: International Journal of Pharmaceutics
Dujuan Zhao, Huiyuan Zhang, Shengfeng Yang, Wenxiu He, Yuxia Luan
The main cause of multidrug resistance (MDR) is overexpression of active efflux transporters, such as P-glycoprotein (P-gp). To reverse MDR and improve the chemotherapy effect of paclitaxel (PTX), we propose a new drug delivery system based on mixed micelles constructed with d-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS) and the mPEG-SS-PTX conjugate with consideration that TPGS is a P-gp inhibitor that can block the cancer cell action of pumping drugs outside of cells and can enhance the anticancer effect...
October 13, 2016: International Journal of Pharmaceutics
Yanan Gao, Xuejing Qi, Yiping Zheng, Hongyu Ji, LinhuaWu, Nannan Zheng, Jingling Tang
The vitamin E analogue, α-tocopherol succinate (α-TOS), has a broad anti-tumor effect. α-TOS can induce cancer cells apoptosis and suppress tumor growth by targeting mitochondria. Low bioavailability of α-TOS is the major problem encountered with formulation development. In our study, α-TOS nanoemulsion (α-TOS-NE) was demonstrated as a new drug delivery system of α-TOS to increase the bioavailability. MTT-based cytotoxicity assay and mitochondrial membrane potential (ΔY) were performed on human breast cancer cell lines MCF-7 and human oral epithelial cancer cell lines KB to evaluate in vitro anticancer efficacy of α-TOS-NE...
October 13, 2016: International Journal of Pharmaceutics
Nazende Günday Türeli, Akif Emre Türeli, Marc Schneider
Design of Experiments (DoE) is a powerful tool for systematic evaluation of process parameters' effect on nanoparticle (NP) quality with minimum number of experiments. DoE was employed for optimization of ciprofloxacin loaded PLGA NPs for pulmonary delivery against Pseudomonas aeruginosa infections in cystic fibrosis (CF) lungs. Since the biofilm produced by bacteria was shown to be a complicated 3D barrier with heterogeneous meshes ranging from 100nm to 500 nm, nanoformulations small enough to travel through those channels were assigned as target quality...
October 12, 2016: International Journal of Pharmaceutics
Hien Van Nguyen, Van Hong Nguyen, Beom-Jin Lee
The objectives of the present study were to develop a controlled-release bilayered tablet of aceclofenac (AFN) 200mg with dual release and to gain a mechanistic understanding of the enhanced sustained release capability achieved by utilizing a binary mixture of the sustained release materials. Different formulations of the sustained-release layer were formulated by employing hydroxypropyl methylcellulose (HPMC) and hydroxypropyl cellulose (HPC) as the major retarding polymers. The in vitro dissolution studies of AFN bilayered tablets were carried out in intestinal fluid (pH 6...
October 12, 2016: International Journal of Pharmaceutics
Xin Jin, Youwen Zhang, Zhenhai Zhang, Danbiao Che, Huixia Lv
AIM: Investigating the effects of juglone loaded P188/phospholipid mixed micelles (J-MM) in breast cancer. MATERIALS & METHODS: In vitro cytotoxicity, apoptotic effects, in vivo therapeutic efficacy and toxicity were used to assess its antitumour effect. Uptake and imaging were used to evaluate the effect on the uptake and passive targeting. RESULTS: Mixed micelle carrier enhanced the targeting and uptake by MB-231 cells. The tumour inhibition rates in tumour xenograft models for paclitaxel, juglone, J-MM (10mg/kg) and J-MM (40mg/kg) were 46%, 27%, 39% and 53%, respectively...
October 12, 2016: International Journal of Pharmaceutics
Wei-Yuan Wang, Xiu-Fen Zhao, Xiao-Han Ju, Yu Wang, Lin Wang, Shu-Ping Li, Xiao-Dong Li
A novel morphology change of Au-methotrexate (Au-MTX) conjugates that could transform from nanochains to discrete nanoparticles was achieved by a simple, one-pot, and hydrothermal growth method. Herein, MTX was used efficiently as a complex-forming agent, reducing agent, capping agent, and importantly a targeting anticancer drug. The formation mechanism suggested a similarity with the molecular imprinting technology. The Au-MTX complex induced the MTX molecules to selectively adsorb on different crystal facets of gold nanoparticles (AuNPs) and then formed gold nanospheres...
October 12, 2016: International Journal of Pharmaceutics
Vincent Levet, Rémi Rosière, Romain Merlos, Luca Fusaro, Gilles Berger, Karim Amighi, Nathalie Wauthoz
The present study focuses on the development of dry powders for inhalation as adjuvant chemotherapy in lung cancer treatment. Cisplatin was chosen as a potential candidate for a local treatment as it remains the main platinum component used in conventional chemotherapies, despite its high and cumulative systemic toxicities. Bulk cisplatin was reduced to submicron sizes using high-pressure homogenization, mixed with a solubilized lipid and/or PEGylated component and then spray-dried to produce controlled-release dry powder formulations...
October 11, 2016: International Journal of Pharmaceutics
A Mercuri, S Wu, S Stranzinger, S Mohr, S Salar-Behzadi, M Bresciani, E Fröhlich
This work aims to better understand the in vivo behaviour of modified release (MR) formulations (Envarsus(®) tablets and Advagraf(®) capsules) using in vitro properties of tacrolimus and in silico simulations. The in silico concentration profiles of tacrolimus released from the MR formulations were predicted after building a three compartments PK model with GastroPlus™, and using the experimentally determined in vitro physico-chemical properties as input parameters. In vitro-in vivo correlations (IVIVC) were obtained after deconvolution of in vivo data from a clinical trial...
October 11, 2016: International Journal of Pharmaceutics
Eleonora Cianci, Oriana Trubiani, Francesca Diomede, Ilaria Merciaro, Ida Meschini, Pantaleone Bruni, Fausto Croce, Mario Romano
Lipoxin (LX)A4 is a lipoxygenase-formed arachidonic acid metabolite with potent anti-inflammatory, pro-resolution properties. Its therapeutic efficacy has been largely demonstrated in a variety of cellular, preclinical and clinical models. Among these, periodontal disease, where LXA4 promotes tissue repair, also by modulating functions of human periodontal ligament stem cells (hPDLSCs). As medicated biomembranes may be particularly useful in clinical settings, where local stimulation of tissue repair is needed, we used electrospinning to embed LXA4 in membranes made of poly(ethylene oxide) (PEO) and poly(d,l-lactide) (PDLLA)...
October 11, 2016: International Journal of Pharmaceutics
Yoonhee Bae, Eric S Green, Goo-Young Kim, Su Jeong Song, Ji Young Mun, Sunray Lee, Jong-Il Park, Jong-Sang Park, Kyung Soo Ko, Jin Han, Joon Sig Choi
Glioblastoma multiform (GBM) is the most frequent and aggressive form of brain tumors in adults. However, the development of more efficient and safe nonviral vector gene therapy represents a promising therapeutic approach, using a tumor-specific killer gene, named apoptin. In this study, we describe the efficacy of non-viral gene delivery vectors, the amino acid-conjugated PAMAM derivatives (PAMAM-H-R and PAMAM-H-K) in delivering a therapeutic gene, displaying affinity toward human primary glioma cells (GBL-14 cells) and dermal fibroblasts...
October 11, 2016: International Journal of Pharmaceutics
Thiago C Carvalho, John P McCook, Niven R Narain, Jason T McConville
Coenzyme Q10 (CoQ10) is a poorly-water soluble compound that is being investigated for the treatment of carcinomas. The aim of this study was to investigate the feasibility of preparing phospholipid-stabilized dispersions of the anticancer agent for continuous pulmonary delivery using a vibrating-mesh nebulizer. We determined the physicochemical properties (drug particle size distribution in dispersion, zeta potential, surface tension, and rheology) and compared the aerosolization profiles (nebulization performance, aerodynamic drug deposition and total emitted dose) of dispersions of CoQ10 prepared with different phospholipids...
October 11, 2016: International Journal of Pharmaceutics
Alexandros Kourentas, Maria Vertzoni, Mira Symillides, Bart Hens, Joachim Brouwers, Patrick Augustijns, Christos Reppas
Biorelevant Gastrointestinal Transfer system (BioGIT) has been shown to be useful in reproducing concentrations of drugs in the fasted upper small intestine after their administration in the stomach. In the present investigation, we evaluated the impact of gastrointestinal transfer on luminal performance of commercially available products of two highly lipophilic weak bases, posaconazole (Noxafil(®) suspension) and itraconazole (Sporanox(®) hard gelatin capsules and Sporanox(®) oral solution) by comparing % solid fraction, concentrations and supersaturation in the duodenal compartment of BioGIT with recently reported data in the upper small intestine of healthy adults...
October 9, 2016: International Journal of Pharmaceutics
Leena Kumari Prasad, Justin S LaFountaine, Justin M Keen, Robert O Williams, James W McGinity
Electrostatic powder deposition (ESPD) has been developed as a solvent-free method to prepare pharmaceutical films. The aim of this work was to investigate the influence of process parameters during (1) electrostatic powder deposition, (2) curing, and (3) removal of the film from the substrate on the properties of the film. Polyethylene oxide (PEO) was used as the model polymer and stainless steel 316 as the substrate. Deposition efficiency (i.e. deposited weight) was measured with varying charging voltage, gun tip to substrate distance, and environmental humidity...
October 8, 2016: International Journal of Pharmaceutics
Loredana Elena Nita, Aurica P Chiriac, Alina Diaconu, Nita Tudorachi, Liliana Mititelu-Tartau
Over the last 10 years, the development of intelligent biomaterials for medical and pharmaceutical applications has attracted growing interest by combining interdisciplinary efforts. Between them nanogels represent one of the most attractive carriers for innovative drug delivery systems. In the present investigation new variants of multi-responsive nanogels have been synthesized by crosslinking poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro [5.5] undecane) copolymer (having different molar ratios between comonomers) with 1,12-dodecandiol...
October 8, 2016: International Journal of Pharmaceutics
Maryam Parsian, Pelin Mutlu, Serap Yalcin, Aysen Tezcaner, Ufuk Gunduz
Tumor-specific delivery of anticancer drugs by magnetic nanoparticles will maximize the efficacy of the drug and minimize side effects, and reduce systemic toxicity. The magnetic core of these nanoparticles provides an advantage for selective drug targeting as they can be targeted to the tumor site and accumulated in cancer cells by means of an external magnetic field. Magnetic nanoparticles can be coated with Polyamidoamine (PAMAM) dendrimer and loaded with drugs. However, biomedical applications of PAMAM dendrimers are limited due to their toxicity associated with their multiple cationic charges due to terminal NH2 groups...
October 7, 2016: International Journal of Pharmaceutics
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