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On the role of salt formation and structural similarity of co-formers in co-amorphous drug delivery systems
In conclusion, structural similarity of the co-formers does not lead to similar co-former performance for a given drug. Salt formation is not a prerequisite for the formation of a co-amorphous system, but if a co-amorphous salt system is formed, improved dissolution rate and physical stability are observed. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

DNA interaction, anti-proliferative effect of copper oxide nanocolloids prepared from metallosurfactant based microemulsions acting as precursor, template and reducing agent
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Gurpreet Kaur, Varsha Dogra, Rajeev Kumar, Sandeep Kumar, Gaurav Bhanjana, Neeraj Dilbaghi, Nitin Kumar Singhal In the present study, we have synthesized mixed cuprous/copper oxide nanosuspensions by metallosurfactant based microemulsion technique. Three metallosurfactants were synthesized which includes two non-ionic double chained metallosurfactants with C12, C16 chains with coordinated copper i.e. Cudda and Cuhexa, respectively. Another cationic double chained metallosurfactant with loosely bound met...
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

Demonstration of pharmaceutical tablet coating process by injection molding technology
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Vibha Puri, David Brancazio, Eranda Harinath, Alexander R. Martinez, Parind M. Desai, Keith D. Jensen, Jung-Hoon Chun, Richard D. Braatz, Allan S. Myerson, Bernhardt L. Trout We demonstrate the coating of tablets using an injection molding (IM) process that has advantage of being solvent free and can provide precision coat features. The selected core tablets comprising 10% w/w griseofulvin were prepared by an integrated hot melt extrusion-injection molding (HME-IM) process. Coating trials were conducted...
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

Sequential therapy with redox-responsive glucolipid nanocarrier separately delivering siRNA and doxorubicin to overcome multidrug resistance
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Tingting Meng, Binbin Lu, Shihong Shao, Ming Yuan, Xuan Liu, Hong Yuan, Xuan Huang, Fuqiang Hu P-glycoprotein (P-gp) is a major efflux transporter overexpressed on multidrug resistant tumor cells and responsible for pumping drugs out. If anti-tumor drugs are given when P-gp level is low, satisfactory treatment efficiency may be achieved. Thus, a P-gp down-regulating siRNA (siMDR1) and doxorubicin (DOX) were applied to eliminate multidrug resistant breast cancer cells (MCF-7/ADR). A redox-responsive glu...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Development of pre-activated α-cyclodextrin as a mucoadhesive excipient for intra-vesical drug delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Muhammad Ijaz, Maximilian Prantl, Noemi Lupo, Flavia Laffleur, Mulazim Hussain Asim, Barbara Matuszczak, Andreas Bernkop-Schnürch The study was designed to synthesize and characterize pre-activated α-cyclodextrin (α-CD) derivatives as mucus adhering excipients for intra-vesical drug delivery. Sodium periodate (NaIO4) was used to oxidize α-CD and subsequently cysteamine was covalently attached to carbonyl groups of oxidized α-CD via reductive amination to produce thiolated &...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Chitosan based Pickering emulsion as a promising approach for topical application of rutin in a solubilized form intended for wound healing: In vitro and in vivo study
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Marwa Hasanein Asfour, Heba Elmotasem, Dina Mahmoud Mostafa, Abeer A.A. Salama The aim of the present study is to formulate the hydrophobic drug rutin in a solubilized form, intended for wound healing, via its loading into a novel Pickering emulsion stabilized by self aggregated chitosan particles (SACP). Rutin-loaded Pickering emulsion formulae were prepared using a high speed homogenizer. They were characterized by drop test, optical microscopy, droplet size and zeta potential determination. The resu...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

An optimized two-vial formulation lipid nanoemulsion of paclitaxel for targeted delivery to tumor
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Lina Chen, Bingchen Chen, Li Deng, Baoan Gao, Yuansheng Zhang, Chan Wu, Nong Yu, Qinqin Zhou, Jianzhong Yao, Jianming Chen The discovery of new intravenous drug delivery carrier for water-insoluble drug is a challenging task. In this paper, novel two-vial formulation of paclitaxel (PTX)-loaded lipid nanoemulsions (TPLEs) with particle sizes of 110nm (TPLE-1), 220nm (TPLE-2) and 380nm (TPLE-3), which were formed by mixing a PEG400 solution of PTX and 10% (w/w) blank lipid emulsions (BLEs) with different...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and characterization of an amylase-triggered dextrin-linked graphene oxide anticancer drug nanocarrier and its vascular permeability
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Siaw Fui Kiew, Yan Teck Ho, Lik Voon Kiew, James Chen Yong Kah, Hong Boon Lee, Toyoko Imae, Lip Yong Chung We synthesized a dextrin (DEX)-conjugated graphene oxide (GO) nanocarrier (GO100-DEX) as a potential drug delivery system to respond to a tumor-associated stimulus, α-amylase, that has high permeability through the fenestrated endothelial barrier to the tumor site. At acidic pH and in the presence of α-amylase to simulate tumor conditions, GO100-DEX released a 1.5-fold higher amount of...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of factors affecting the stability of lysozyme spray dried from ethanol-water solutions
In this study, lysozyme was chosen as a model pharmaceutical protein to study these aspects when spray drying from water-ethanol mixtures. The effect of formulation additives (trehalose, Tween 20 and phosphate-buffered saline) and processing conditions (inlet temperature and storage time of lysozyme in the feed solution before the spray drying process) on the protein bioactivity was investigated. The results showed that the bioactivities of spray dried lysozyme with these additives were about 5–10% higher than that without additives. The bioactivity of the spray dried lysozyme was found to increase with a decrease in...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Bubble-generating nano-lipid carriers for ultrasound/CT imaging-guided efficient tumor therapy
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Nan Zhang, Jia Li, Ruirui Hou, Jiangnan Zhang, Pei Wang, Xinyang Liu, Zhenzhong Zhang Ideal therapeutic effectiveness of chemotherapy is obtained only when tumor cells are exposed to a maximal drug concentration, which is often hindered by dose-limiting toxicity. We designed a bubble-generating liposomal delivery system by introducing ammonium bicarbonate and gold nanorods into folic acid-conjugated liposomes to allow both multimodal imaging and the local release of drug (doxorubicin) with hyperthermia...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical properties of inclusion complexes of highly soluble β-cyclodextrins with highly hydrophobic testosterone propionate
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Christian Celia, Angela Scala, Rosanna Stancanelli, Emanuela Surdo, Donatella Paolino, Alessandro Grattoni, Nicola Micale, Vincenza Crupi, Domenico Majolino, Massimo Fresta, Silvana Tommasini, Valentina Venuti, Cinzia Anna Ventura Hydroxypropyl-β-cyclodextrin (HP-β-CyD) and sulfobutyl ether-β-cyclodextrin (SBE-β-CyD) were used to generate hydrophilic complexes of the poorly water-soluble drug testosterone propionate (TP). The inclusion complexes were obtained by freeze-drying, and t...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Novel dissolving microneedles for enhanced transdermal delivery of levonorgestrel: In vitro and in vivo characterization
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Gangtao Yao, Guilan Quan, Shiqi Lin, Tingting Peng, Qingqing Wang, Hao Ran, Hangping Chen, Qian Zhang, Lili Wang, Xin Pan, Chuanbin Wu Dissolving microneedles (DMN) have been studied as a drug delivery system to enhance the transport of drug molecules across the skin with almost no pain. However, the poor dissolving ability of microneedles in the skin and low drug loading have limited their potential application. The aim of this study was to develop a novel dissolving microneedle system with improved d...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Prediction of human percutaneous absorption from in vitro and in vivo animal experiments
In conclusion, minipigs appear to be a promising model animal for predicting percutaneous drug absorption in humans, however, more in vivo and in vitro studies are needed to improve predictability. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Simplified stratum corneum model membranes for studying the effects of permeation enhancers
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Barbora Amélie Čuříková, Kamila Procházková, Barbora Filková, Petra Diblíková, Jan Svoboda, Andrej Kováčik, Kateřina Vávrová, Jarmila Zbytovská The activity of transdermal permeation enhancers is usually evaluated in vitro on human or animal skin, but skin samples can be hard to source and highly variable. To provide a more consistent basis for evaluating the activity of permeation enhancers, we prepared relatively ...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Understanding die fill variation during mini-tablet production
In this study, flow properties of different types of granules were characterised. Mini-tablets of 1.8 and 3mm diameters were prepared from the granules using a rotary press with multiple-tip compression tooling. A methodology was established to evaluate mini-tablet die fill variation within and across compaction cycles using data from compression roller displacement and mini-tablet weight. Both sizes of mini-tablets showed similar extents of inter-cycle weight variation that could be associated with granules’ inter-particulate friction. However, smaller mini-tablets had higher intra-cycle weight variation due to thei...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Different effects of silica added internal or external on in vitro dissolution of indomethacin hot-melt extrudates
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Yulong Xia, Meng Yuan, Yueyang Deng, Xue Ke, Tianyuan Ci The purpose of this work was to investigate the effect on the dissolution behavior when silica was added in different ways. The solid dispersion was prepared by hot-melt extrusion (HME) using indomethacin (IND) as a model drug and Kollidon VA64 as a carrier. In order to change the dissolution behavior, the silica was added during or after the HME respectively, to obtain the corresponding silica internal-added solid dispersion (InSD) and silica ex...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Cationic nanoemulsions as nucleic acids delivery systems
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Helder Ferreira Teixeira, Fernanda Bruxel, Michelle Fraga, Roselena Silvestri Schuh, Giovanni Konat Zorzi, Ursula Matte, Elias Fattal Since the first clinical studies, knowledge in the field of gene therapy has advanced significantly, and these advances led to the development and subsequent approval of the first gene medicines. Although viral vectors-based products offer efficient gene expression, problems related to their safety and immune response have limited their clinical use. Thus, design and opt...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Melt extrusion with poorly soluble drugs – An integrated review
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Michael A. Repka, Suresh Bandari, Venkata Raman Kallakunta, Anh Q. Vo, Haley McFall, Manjeet B. Pimparade, Ajinkya M. Bhagurkar Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This review is focused on the recent reports on the solubility enhancem...
Source: International Journal of Pharmaceutics - November 5, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring the feasibility of the use of biopolymers as a carrier in the formulation of amorphous solid dispersions – Part I: Gelatin
This study shows the potential of gelatin as a carrier to formulate amorphous solid dispersions. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 4, 2017 Category: Drugs & Pharmacology Source Type: research

Powder flow analysis: A simple method to indicate the ideal amount of lactose fines in dry powder inhaler formulations
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Mats Hertel, Eugen Schwarz, Mirjam Kobler, Sabine Hauptstein, Hartwig Steckel, Regina Scherließ Many efforts have been made in the past to understand the function of lactose fines which are given as a ternary component to carrier-based dry powder inhaler formulations. It is undisputed that fines can significantly improve the performance of such formulations, but choosing the right amount of fines is a crucial point, because too high concentrations can have negative effects on the dispersion perfor...
Source: International Journal of Pharmaceutics - November 4, 2017 Category: Drugs & Pharmacology Source Type: research

Lipid nanocarriers as skin drug delivery systems: Properties, mechanisms of skin interactions and medical applications
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): M. Sala, R. Diab, A. Elaissari, H. Fessi During the past decades, lipid nanocarriers are gaining momentum with their multiple advantages for the management of skin diseases. Lipid nanocarriers enable to target the therapeutic payload to deep skin layers or even to reach the blood circulation making them a promising cutting-edge technology. Lipid nanocarriers refer to a large panel of drug delivery systems. Lipid vesicles are the most conventional, known to be able to carry lipophilic and hydrophilic act...
Source: International Journal of Pharmaceutics - November 3, 2017 Category: Drugs & Pharmacology Source Type: research

Lipid/alginate nanoparticle-loaded in situ gelling system tailored for dexamethasone nasal delivery
In conclusion, this study showed the potential of the proposed system to provide local therapeutic effect upon administration of a lower corticosteroid dose and minimize the possibility for adverse effects as it can be easily sprayed as solution and delivered beyond nasal valve, ensure prolonged contact time with nasal mucosa upon gelation, and moderate corticosteroid release and permeation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Planetary ball milling and supercritical fluid technology as a way to enhance dissolution of bicalutamide
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Joanna Szafraniec, Agata Antosik, Justyna Knapik-Kowalczuk, Mateusz Kurek, Karolina Syrek, Krzysztof Chmiel, Marian Paluch, Renata Jachowicz Dissolution of bicalutamide processed with polyvinylpyrrolidone by either supercritical carbon dioxide or ball milling has been investigated. Various compositions as well as process parameters were used to obtain binary systems of the drug with the carrier. Thermal analysis and powder X-ray diffractometry confirmed amorphization of bicalutamide mechanically activated by ba...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Clarithromycin and N-acetylcysteine co-spray-dried powders for pulmonary drug delivery: A focus on drug solubility
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Michele Dario Manniello, Pasquale Del Gaudio, Rita P. Aquino, Paola Russo Cystic fibrosis (CF) lungs are usually susceptible to Pseudomonas aeruginosa colonization and this bacterium is resistant to immune system clearance and drug control. Particularly, the biofilm mode of growth protects several microorganisms from host defenses and antibacterial drugs, mainly due to a delayed penetration of the drug through the biofilm matrix. Biofilm, together with lung mucus viscosity and tenacity, reduces, therefore, the ...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Development and characterization of mucoadhesive buccal gels containing lipid nanoparticles of ibuprofen
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Ana Camila Marques, Ana Isabel Rocha, Paula Leal, Marilene Estanqueiro, José Manuel Sousa Lobo The lipid nanoparticles, namely Nanostructured Lipid Carriers (NLC), as drug delivery systems have been investigated for several years. One of the delivery routes for which these carriers can be applied is buccal administration. However, the liquid dispersions of lipid nanoparticles can be rapidly removed from oral cavity by saliva. Thus, the development of a system that allows increased retention time on the m...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Olivera Kaljević, Jelena Djuris, Bojan Čalija, Zoran Lavrič, Julijana Kristl, Svetlana Ibrić Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, χ, and the difference between the total solubility parameters, Δdt . A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characteri...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Microstructure evaluation of dermally applicable liquid crystals as a function of water content and temperature: Can electron paramagnetic resonance provide complementary data?
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Mirjam Gosenca Matjaž, Janez Mravljak, Marija Bešter Rogač, Marjeta Šentjurc, Mirjana Gašperlin, Alenka Zvonar Pobirk Insight into the microstructure of lyotropic liquid crystals (LCs) is of crucial importance for development of novel dermal delivery systems. Our aim was to evaluate the phase behaviour of dermally applicable LCs composed of isopropyl myristate/Tween 80/lecithin/water, along the dilution line, where phase transitions are predominantly driven by increased water content. Add...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Sanela M. Đorđević, Anja Santrač, Nebojša D. Cekić, Bojan D. Marković, Branka Divović, Tanja M. Ilić, Miroslav M. Savić, Snežana D. Savić This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing the prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperi...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

3D printed orodispersible films with Aripiprazole
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Witold Jamróz, Mateusz Kurek, Ewelina Łyszczarz, Joanna Szafraniec, Justyna Knapik-Kowalczuk, Karolina Syrek, Marian Paluch, Renata Jachowicz Three dimensional printing technology is gaining in importance because of its increasing availability and wide applications. One of the three dimensional printing techniques is Fused Deposition Modelling (FDM) which works on the basis of hot melt extrusion–well known in the pharmaceutical technology. Combination of fused deposition modelling with preparation...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

An explorative analysis of process and formulation variables affecting comilling in a vibrational mill: The case of praziquantel
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Beatrice Perissutti, Nadia Passerini, Ramona Trastullo, Jennifer Keiser, Debora Zanolla, Guglielmo Zingone, Dario Voinovich, Beatrice Albertini Praziquantel, a BCS II class anthelmintic drug used for the treatment of schistosome infections, was coground in a vibrational mill with different polymers (linear and crosslinked povidone, copovidone and sodium starch glycolate). An explorative analysis of formulation variables (drug-polymer wt ratio and polymer type) and process parameters (type of grinding media, gri...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Efficacy assessment of self-assembled PLGA-PEG-PLGA nanoparticles: Correlation of nano-bio interface interactions, biodistribution, internalization and gene expression studies
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Simona Dimchevska, Nikola Geskovski, Rozafa Koliqi, Nadica Matevska-Geskovska, Vanessa Gomez Vallejo, Boguslaw Szczupak, Eneko San Sebastian, Jordi Llop, Delyan R. Hristov, Marco P. Monopoli, Gjorgji Petruševski, Sonja Ugarkovic, Aleksandar Dimovski, Katerina Goracinova The aim of our study was to develop and compare the biological performance of two types of biodegradable SN-38 loaded nanoparticles (NPs) with various surface properties, composed of low and high Mw triblock PLGA-PEG-PLGA copolymers, appl...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Computational and experimental model of transdermal iontophorethic drug delivery system
In this study we investigated, experimentally and numerically, in vitro drug delivery of dexamethasone sodium phosphate to porcine skin. Different current densities, delivery durations and drug loads were investigated experimentally and introduced as boundary conditions for numerical simulations. Nernst–Planck equation was used for calculation of active substance flux through equivalent model of homogeneous hydrogel and skin layers. The obtained numerical results were in good agreement with experimental observations. A comprehensive in-silico platform, which includes appropriate numerical tools for fitting, could con...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Analysis of pellet coating uniformity using a computer scanner
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Rok Šibanc, Matevž Luštrik, Rok Dreu A fast method for pellet coating uniformity analysis, using a commercial computer scanner was developed. The analysis of the individual particle coating thicknesses was based on using a transparent orange colored coating layer deposited on white pellet cores. Besides the analysis of the coating thickness the information of pellet size and shape was obtained as well. Particle size dependent coating thickness and particle size independent coating variability was...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Tracing molecular and structural changes upon mucolysis with N-acetyl cysteine in human airway mucus
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Branko Vukosavljevic, Xabier Murgia, Konrad Schwarzkopf, Ulrich F. Schaefer, Claus-Michael Lehr, Maike Windbergs The conducting airways of the human lungs are lined by mucus, which lubricates the lung epithelium and provides a first-line protection against airborne threats. As a novel approach for visualization of the human mucus microstructure, we applied confocal Raman microscopy as a label-free and chemically selective technique. We were successfully able to chemically resolve the pulmonary surfactant from t...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Comparison of the properties of implantable matrices prepared from degradable and non-degradable polymers for bisphosphonate delivery
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Tamás Sovány, Anna Csüllög, Ernő Benkő, Géza Regdon, Klára Pintye-Hódi The aim of the present study was the development of directly compressed tablets for implantable delivery of risedronate sodium for osteoporosis treatment and the comparison of the mechanism and kinetics of drug release from biogradable (chitosan) and non-degradable (PVC) polymer matrices. The compositions and process parameters were optimized in accordance to a mixed 2 and 3 level full factorial...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Designing optimal formulations for hot-melt coating
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Diogo Gomes Lopes, Sharareh Salar-Behzadi, Andreas Zimmer Hot-melt coating (HMC) as a solvent-free technology grants faster and more economic coating processes with reduced risk of dissolving the drug during the process. Moreover, traditional coating equipment can be modified to enable the HMC process. Despite the indubitable advantages and feasibility of the process, HMC is not well-known to pharmaceutical industry and its employment is still limited. The main aspect hindering the widespread application of thi...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Modeling in the quality by design environment: Regulatory requirements and recommendations for design space and control strategy appointment
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Jelena Djuris, Zorica Djuric Mathematical models can be used as an integral part of the quality by design (QbD) concept throughout the product lifecycle for variety of purposes, including appointment of the design space and control strategy, continual improvement and risk assessment. Examples of different mathematical modeling techniques (mechanistic, empirical and hybrid) in the pharmaceutical development and process monitoring or control are provided in the presented review. In the QbD context, mathematical m...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Overview of solidification techniques for self-emulsifying drug delivery systems from industrial perspective
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): J. Mandić, A. Zvonar Pobirk, F. Vrečer, M. Gašperlin Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different so...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Production of aprepitant nanocrystals by wet media milling and subsequent solidification
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): F. Toziopoulou, M. Malamatari, I. Nikolakakis, K. Kachrimanis The present study investigates the effects of formulation and process parameters on the production of aprepitant nanosuspensions applying wet media milling and subsequent solidification. Six stabilizers were used: two brands of hydroxylpropylmethyl cellulose (HPMC E-15LV and Pharmacoat 603), hydroxypropyl cellulose (HPC-SSL), polyvinylpyrollidone (PVP), D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS 1000), Poloxamer P188 and sodium dod...
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

From smart materials to advanced drug delivery systems
Publication date: 30 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 2 Author(s): Svetlana Ibrić, Jelena Parojčić, Aleš Mrhar (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 27, 2017 Category: Drugs & Pharmacology Source Type: research

Ex vivo evaluation of degradation rates of metronidazole and olsalazine in distal ileum and in cecum: The impact of prandial state
Conclusions In the fasted state, bacterial activity is higher in cecum than in distal ileum. Food residues decrease bacterial metabolism degradation rates of drugs in cecum. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 24, 2017 Category: Drugs & Pharmacology Source Type: research

The influence of high shear mixing on ternary dry powder inhaler formulations
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Mats Hertel, Eugen Schwarz, Mirjam Kobler, Sabine Hauptstein, Hartwig Steckel, Regina Scherließ The blending process is a key step in the production of dry powder inhaler formulations, but only little is known about the influence of process parameters. This is especially true for high shear blending of ternary formulations. For this reason, this study aims to investigate the influence of high shear mixing process parameters (mixing time and rotation speed) on the fine particle fraction (FPF) of t...
Source: International Journal of Pharmaceutics - October 21, 2017 Category: Drugs & Pharmacology Source Type: research

Milling solid proteins to enhance activity after melt-encapsulation
This study explores the use of solid-state ball milling to decrease protein particle size before encapsulation within poly(lactic-co-glycolic acid) (PLGA) via HME. The impact of milling on particle dispersion, retained enzymatic activity, secondary structure stability, and release was explored for lysozyme, glucose oxidase, and the virus-like particle derived from Qβ to fully understand the impact of milling on protein systems with different sizes and complexities. The results of this study describe the utility of milling to further increase the stability of protein/polymer systems prepared via HME. Graphical abstract...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Formation of hydrophobic drug nanoparticles via ambient solvent evaporation facilitated by branched diblock copolymers
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Ulrike Wais, Alexander W. Jackson, Tao He, Haifei Zhang Hydrophobic drug nanoparticles have been prepared by ambient solvent evaporation from ethanol at room temperature. Poly(ethylene glycol)-b-(N-isopropylacrylamide) (PEG-b-PNIPAm) branched diblock copolymers are employed to prevent drug crystallization during solvent evaporation and to stabilize the drug nanoparticles once suspended in aqueous media. After the initial solvent evaporation the dry materials obtained exhibit excellent stability during storage a...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Supramolecular nano-engineered lipidic carriers based on diflunisal-phospholipid complex for transdermal delivery: QbD based optimization, characterization and preclinical investigations for management of rheumatoid arthritis
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Amanpreet Kaur, Bhupinder Singh Bhoop, Sanjay Chhibber, Gajanand Sharma, Vijay Singh Gondil, Om Prakash Katare Diflunisal (DIF) is used for treatment of rheumatoid arthritis, osteoarthritis etc. DIF-phospholipid complex (DIF-PL complex) was prepared by solvent-evaporation method and characterized by molecular docking studies, SEM, FTIR, DSC, PXRD studies. Further, the DIF-PL complex was incorporated into supramolecular nano-engineered lipidic carriers (SNLCs) for transdermal delivery. The optimization exercise ...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Protein-loaded emulsion electrospun fibers optimized for bioactivity retention and pH-controlled release for peroral delivery of biologic therapeutics
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Hannah Frizzell, Tiffany J. Ohlsen, Kim A. Woodrow Biologics are the most rapidly growing class of therapeutics, but commonly suffer from low stability. Peroral administration of these therapeutics is an attractive delivery route; however, this route introduces unique physiological challenges that increase the susceptibility of proteins to lose function. Formulation of proteins into biomaterials, such as electrospun fibers, is one strategy to overcome these barriers, but such platforms need to be optimized to e...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

A novel high drug loading mussel-inspired polydopamine hybrid nanoparticle as a pH-sensitive vehicle for drug delivery
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Jie Hou, Chunlei Guo, Yuzhi Shi, Ergang Liu, Weibing Dong, Bo Yu, Shiyuan Liu, Junbo Gong A novel high drug loading pH-cleavable polymer hybrid nanoparticle was prepared via doxorubicin (DOX) grafted onto PEGylated, mussel-inspired polydopamine (PDA) and then coated onto hollow silica nanoparticles for drug delivery. A series of characterization shed light on the formation mechanisms of PDA coatings on hollow silica. We hypothesized that dopamine was first absorbed onto the surface of hollow silica and then beg...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Skin vaccination using microneedles coated with a plasmid DNA cocktail encoding nucleosomal histones of Leishmania spp.
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Esther Moreno, Juana Schwartz, Alba Calvo, Laura Blanco, Esther Larrea, Juan M. Irache, Carmen Sanmartín, Sion A. Coulman, Manuel Soto, James C. Birchall, Socorro Espuelas Vaccine delivery using microneedles (MNs) represents a safe, easily disposable and painless alternative to traditional needle immunizations. The MN delivery of DNA vaccines to the dermis may result in a superior immune response and/or an equivalent immune response at a lower vaccine dose (dose-sparing). This could be of special interes...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Experimental and computational study of the effect of breath-actuated mechanism built in the NEXThaler ® dry powder inhaler
In conclusion, the NEXThaler® BAM mechanism is a unique feature enabling high emitted fine particle fraction and enhanced drug delivery to the lungs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Eyelid skin as a potential site for drug delivery to conjunctiva and ocular tissues
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Gerard Lee See, Ayano Sagesaka, Satoko Sugasawa, Hiroaki Todo, Kenji Sugibayashi The feasibility of topical application onto the (lower) eyelid skin to deliver hydrophilic and lipophilic compounds into the conjunctiva and ocular tissues was evaluated by comparing with conventional eye drop application. Skin permeation and the concentration of several model compounds, and skin impedance were determined utilizing eyelid skin from hairless rats, as well as abdominal skin in the same animals for comparison. In vitr...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research