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

Development of fine solid-crystal suspension with enhanced solubility, stability, and aerosolization performance for dry powder inhalation
In this study, fine solid-crystal suspension (FSCS) was proposed as a solvent-free method to improve the solubility of a drug with poor solubility (itraconazole) and achieve high deposition efficiency simultaneously. The FSCS, in which the crystalline drug particle was highly dispersed in the crystalline excipient, was initially prepared as drug-excipient extrudate by hot melt extrusion, followed by jet milling into fine particles. Unlike the amorphous solid dispersion in the high-energy state, which is liable to recrystallize and aggregate, the FSCS was expected not only to improve the solubility of itraconazole, but also...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Co-delivery strategies to overcome multidrug resistance in ovarian cancer
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Ikram Ullah Khan, Rizwan Ullah Khan, Hira Asif, Alamgeer, Syed Haroon Khalid, Sajid Asghar, Mohammad Saleem, Kifayat Ullah Shah, Shefat Ullah Shah, Syed A.A. Rizvi, Yasser Shahzad Cancer is one of the leading causes of death and equally strikes both genders. Among women, ovarian cancer is responsible for many deaths as it remains symptomless in the earlier stages and generally diagnosed in third stage. At this point it becomes difficult to carry out de-bulking surgery and treatment with different chemotherapeut...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Spontaneous nano-emulsification: Process optimization and modeling for the prediction of the nanoemulsion ’s size and polydispersity
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): G. Lefebvre, J. Riou, G. Bastiat, E. Roger, K. Frombach, J-C. Gimel, P. Saulnier, B. Calvignac The aim of the present study was to optimize the size and polydispersity of a lipid nanoemulsion as a function of the oil (Labrafac® WL1349), surfactant (Kolliphor® HS 15) and cosurfactant (Span® 80) phase composition and temperature. The nanoemulsions were prepared using a low-energy self-emulsification method. The Z-average diameter and the polydispersity index (PDI) were modeled with mixture ex...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Functionalized hBN as targeted photothermal chemotherapy for complete eradication of cancer cells
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Shazid Md. Sharker, Md. Ashraful Alam, Manik Chandra Shill, G.M.Sayedur Rahman, Hasan Mahmud Reza The development of combined anticancer therapeutic techniques has drawn increased attention for enhanced therapeutic efficacy. In this work, we synthesized Near Infrared (NIR) responsive ICG (I) functionalized hexagonal boron-nitride (hBN) as photothermal therapeutic agent (hBNI) and Doxorubicin (Dox)-conjugated Hyaluronic acid (HA) as tumor targeted chemotherapeutic agent (d-HA-Dox). Using adhesion proper...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Sapofectosid – Ensuring non-toxic and effective DNA and RNA delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Simko Sama, Gerold Jerz, Peter Schmieder, Eric Woith, Matthias F. Melzig, Alexander Weng Different methods are being deployed for non-viral DNA/RNA delivery. However non-viral formulations for DNA/RNA-delivery are often accompanied by severe toxicity and thus low efficiency. Particular costly cell culture media are required as well. Here we introduce sapofection as a valuable enhancing method for non-viral DNA/RNA delivery. Sapofection is based on the application of DNA/RNA nanoplexes and sapofectosid,...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

ZnO-based nanocarriers for drug delivery application: From passive to smart strategies
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Xiao Huang, Xi Zheng, Zuojuan Xu, Caixia Yi Due to the excellent biocompatibility as well as the low cost, nanoscale ZnO shows a great potential in drug delivery application. The richness of the structures, easy modification and pleasant properties of nanoscale ZnO make these materials reasonable choices for drug delivery. In the recent decade, various ZnO nanostructures as well as nanohybrids have been carried out for optimizational drug loading and carrying. To control the drug release behavior, many...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

In situ hydrogels enhancing postoperative functional recovery by reducing iron overload after intracerebral haemorrhage
In this study, human hair keratose hydrogel (KG) loading with minocycline hydrochloride (MH) were prepared to reduce iron overload for the improvement of the postoperative functional recovery after ICH aspiration surgery. Hemoglobin-induced iron accumulation in rat primary neuronal culture was delayed by the adsorptive capacity of blank KG, while MH-loaded KG displayed a stronger and more thorough cytoprotective effect than blank KG due to the combined effect of absorptive action to iron and sustained release of the iron chelator. Moreover, high iron-chelating efficiency in the hematoma region supplied by MH-loaded KG sign...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Polymeric microspheres for the sustained release of a protein-based drug carrier targeting the PDGF β-receptor in the fibrotic kidney
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): N. Teekamp, F. Van Dijk, A. Broesder, M. Evers, J. Zuidema, R. Steendam, E. Post, J.L. Hillebrands, H.W. Frijlink, K. Poelstra, L. Beljaars, P. Olinga, W.L.J. Hinrichs Injectable sustained release drug delivery systems are an attractive alternative for the intravenous delivery of therapeutic proteins. In particular, for chronic diseases such as fibrosis, this approach could improve therapy by reducing the administration frequency while avoiding large variations in plasma levels. In fibrotic tissues the...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Doxorubicin-loaded micelles of amphiphilic diblock copolymer with pendant dendron improve antitumor efficacy: In vitro and in vivo studies
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Siew Hui Voon, Chin Siang Kue, Toyoko Imae, Wen Shang Saw, Hong Boon Lee, Lik Voon Kiew, Lip Yong Chung, Shin-ichi Yusa Previously reported amphiphilic diblock copolymer with pendant dendron moieties (P71D3) has been further evaluated in tumor-bearing mice as a potential drug carrier. This P71D3-based micelle of an average diameter of 100nm was found to be biocompatible, non-toxic and physically stable in colloidal system up to 15days. It enhanced the in vitro potency of doxorubicin (DOX) in 4T1 breast...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Development and implementation of an advanced model predictive control system into continuous pharmaceutical tablet compaction process
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Aparajith Bhaskar, Fernando N. Barros, Ravendra Singh In the context of continuous pharmaceutical oral dosage manufacturing, a control system is essential to ensure that the critical quality attributes (CQAs) are maintained within the regulatory constraints by mitigating variations generated in upstream operations. Such a system is essential to the Quality by Design (QbD) paradigm shift, which can ensure that predefined end quality attributes are achieved within an optimal economic and time bracket. In...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Quality by Design (QbD) approach to optimize the formulation of a bilayer combination tablet (Telmiduo ®) manufactured via high shear wet granulation
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ah Ram Lee, Seok Young Kwon, Du Hyung Choi, Eun Seok Park A bilayer tablet, which consisted of telmisartan and amlodipine besylate, was formulated based on a Quality by Design (QbD) approach. The control and response factors were determined based on primary knowledge and the target values of the control tablet (Twynsta®). A D-optimal mixture design was used to obtain the optimal formulations in terms of D-mannitol, crospovidone, and MCC for the telmisartan layer, and CCM-Na, PVP K25, and Prosolv fo...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Cyanine derivative as a suitable marker for thermosensitive in situ gelling delivery systems: In vitro and in vivo validation of a sustained buccal drug delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ni Zeng, Johanne Seguin, Pierre-Louis Destruel, Gilles Dumortier, Marc Maury, Hélène Dhotel, Michel Bessodes, Daniel Scherman, Nathalie Mignet, Vincent Boudy Buccal administration route is a promising way for a large number of drugs exhibiting a low oral bioavailability. The present work describes the formulation and evaluation of a mucoadhesive and thermosensitive in situ gelling delivery system based on poloxamer 407, poloxamer 188 and xanthan gum for buccal drug delivery. First, the mu...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Thermal properties of compacted pharmaceutical excipients
In this study, various analytical methods were used to measure the thermal properties of widely used pharmaceutical excipients including microcrystalline cellulose (MCC) of three different grades (Avicel PH 101; Avicel PH 102 and Avicel DG), lactose and mannitol. The effect of relative density on the measured thermal properties was investigated by compressing the powders into specimen of different relative densities. Differential thermal analysis (DTA) was employed to explore endothermic or exothermic events in the temperature range endured during typical pharmaceutical manufacturing processes, such as tabletting and roll ...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ruiping Kong, Xingyi Zhu, Elizaveta S. Meteleva, Yulia S. Chistyachenko, Lyubov P. Suntsova, Nikolay E. Polyakov, Mikhail V. Khvostov, Dmitry S. Baev, Tatjana G. Tolstikova, Jianming Yu, Alexander V. Dushkin, Weike Su In the present work, complexes of simvastatin (SIM) with polysaccharide arabinogalactan (AG) or disodium salt of glycyrrhizin acid (Na2GA) have been prepared using mechanochemical technique to improve the solubility of SIM and enhance its oral bioavailability. The interactions of SIM with...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

HM10660A, a long-acting hIFN- α-2b, is a potent candidate for the treatment of hepatitis C through an enhanced biological half-life
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Sungmin Bae, Taehoon Sim, Chaemin Lim, Daejin Kim, Jongsoo Lee, Youngjin Park, Sungyoub Jung, Inyoung Choi, Sechang Kwon, Kyung Taek Oh Interferon-α (IFN-α) has been widely used for the treatment of infections due to the hepatitis C virus (HCV). Because of the short half-life of IFN-α in serum, it must be administered three times per week. To increase the half-life of IFN-α, the immunoglobulin G4 (IgG4) Fc fragment (HMC001) was conjugated with human IFN-α-2b to develop a l...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Clay minerals: Properties and applications to dermocosmetic products and perspectives of natural raw materials for therapeutic purposes —A review
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Jemima Daniela Dias Moraes, Silvana Raquel Alina Bertolino, Silvia Lucia Cuffini, Diego Fernando Ducart, Pedro Eriberto Bretzke, Gislaine Ricci Leonardi Clay minerals are layered materials with a number of peculiar properties, which find many relevant applications in various industries. Since they are easily found everywhere, they are particularly attractive due to their economic viability. In the cosmetic industry, clay minerals are often used as excipients to stabilize emulsions or suspensions and to...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Nanomanufacturing through microfluidic-assisted nanoprecipitation: Advanced analytics and structure-activity relationships
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Roberto Donno, Arianna Gennari, Enrique Lallana, Julio M. Rios De La Rosa, Richard d’Arcy, Kevin Treacher, Kathryn Hill, Marianne Ashford, Nicola Tirelli We have employed microfluidics (cross-shaped chip) for the preparation of drug-loaded poly(lactic acid-co-glycolic acid) (PLGA) nanoparticles. The polymer precipitates from an acetone solution upon its controlled laminar mixing (flow focusing) with an aqueous solution of a surfactant, allowing for an operator-independent, up-scalable and reprodu...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Heating treatments affect the thermal behaviour of doxorubicin loaded in PEGylated liposomes
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Diego R. Perinelli, Marco Cespi, Giulia Bonacucina, Filippo Rendina, Giovanni Filippo Palmieri Doxil® is a stealth marketed PEGylated liposomal formulation, containing the anticancer drug doxorubicin. After loading via a pH gradient, fibrillar supramolecular structures of doxorubicin sulfate originates inside the core of the liposomes. Recently, the crystallinity of doxorubicin sulfate has been confirmed by high-resolution calorimetry. However, no detailed information are available on the nature of...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Dual targeting mesoporous silica nanoparticles for inhibiting tumour cell invasion and metastasis
In this study, a CD44 and N-cadherin dual targeting drug delivery system based on mesoporous silica nanoparticles (MSNs) has been successfully constructed for inhibiting tumour cell invasion and metastasis. Amino modified MSN (MSN/NH2) was first synthesized and then functionalized with hyaluronic acid (HA) and ADH-1, constructing the carrier ADH-1-HA-MSN. Doxorubicin hydrochloride (DOX) was selected as a model anticancer drug. The prepared vector had a spherical shape with a narrow distribution of particle size. Flow cytometry and confocal microscopy studies showed that the modification with HA significantly enhanced CD44-...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Thermostability of the coating, antigen and immunostimulator in an adjuvanted oral capsule vaccine formulation
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Stephanie Longet, Vincenzo Aversa, Daire O’Donnell, Joshua Tobias, Monica Rosa, Jan Holmgren, Ivan S. Coulter, Ed C. Lavelle Oral vaccines present an attractive alternative to injectable vaccines for enteric diseases due to ease of delivery and the induction of intestinal immunity at the site of infection. However, susceptibility to gastrointestinal proteolysis, limited transepithelial uptake and a lack of clinically acceptable adjuvants present significant challenges. A further challenge to mass...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro characterization and mouthfeel study of functionalized calcium carbonate in orally disintegrating tablets
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Leonie Wagner-Hattler, Katharina Wyss, Joachim Schoelkopf, Jörg Huwyler, Maxim Puchkov Orally disintegrating tablets (ODT) are comfortable and safe drug delivery methods beneficial for all age groups of patients. ODTs are characterized by fast disintegration, high physical stability, taste masking and acceptable mouthfeel. In this work, the applicability of Functionalized Calcium Carbonate (FCC) to formulate ODTs with enhanced mouthfeel was elaborated and tested for acceptability on twenty healthy...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Promises and limitations of nanoparticles in the era of cell therapy: Example with CD19-targeting chimeric antigen receptor (CAR)-modified T cells
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Hélène Jakobczyk, Flavien Sciortino, Soizic Chevance, Fabienne Gauffre, Marie-Bérengère Troadec A number of nanoparticles has been developed by chemists for biomedical applications to meet imaging and targeting needs. In parallel, adoptive T therapy with chimeric antigen receptor engineered T cells (CART cells) has recently held great promise in B-cell malignancy treatments thanks to the development of anti-CD19 CAR T cells. Indeed, CD19 is a reliable B cell marker and a validated tar...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Antibiotic incorporation in jet-sprayed nanofibrillar biodegradable scaffolds for wound healing
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Maxime Dzikowski, Naomi Castanié, Amélie Guedon, Bernard Verrier, Charlotte Primard, Jérôme Sohier In view of preparing antibiotic-loaded structures that can be used as dressing to prevent or contain wound infections, this study evaluates biodegradable nanofibrillar matrices obtained by jet-spraying and containing ciprofloxacin (CIF). The matrices were prepared from different blends of poly-(ε-caprolactone) (PCL) and poly-d,l-(lactic acid) (PDLLA) in view of controlling mechani...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Microgels of silylated HPMC as a multimodal system for drug co-encapsulation
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Mohamed Zayed, Corine Tourne-Peteilh, Michel Ramonda, Gildas Rethore, Pierre Weiss, Jean Martinez, Gilles Subra, Ahmad Mehdi, Jean-Marie Devoisselle, Philippe Legrand Combined therapy is a global strategy developed to prevent drug resistance in cancer and infectious diseases. In this field, there is a need of multifunctional drug delivery systems able to co-encapsulate small drug molecules, peptides, proteins, associated to targeting functions, nanoparticles. Silylated hydrogels are alkoxysilane hybrid polymers ...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and validation of an HPLC-fluorescence method for the quantification of IR780-oleyl dye in lipid nanoparticles
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Mathieu Varache, Marie Escudé, Corentin Laffont, Emilie Rustique, Anne-Claude Couffin A reversed-phase (RP) high-performance liquid chromatography (HPLC) method for the content determination of IR780-oleyl (IRO) dye in lipid nanoparticles was developed and validated. Chromatographic separation was performed on a RP C18 column with a gradient program of water and acetonitrile both with 0.1% (v/v) TFA, at a flow rate of 1.0mL/min and a total run of 21min. IRO dye detection was made by fluorescence at emissi...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Tuning complement activation and pathway through controlled molecular architecture of dextran chains in nanoparticle corona
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Jean-Baptiste Coty, Elquio Eleamen Oliveira, Christine Vauthier The understanding of complement activation by nanomaterials is a key to a rational design of safe and efficient nanomedicines. This work proposed a systematic study investigating how molecular design of nanoparticle coronas made of dextran impacts on mechanisms that trigger complement activation. The nanoparticles used for this work consisted of dextran-coated poly(isobutylcyanoacrylate) (PIBCA) nanoparticles have already been thoroughly characteriz...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of injectable nanosized drug delivery systems for apigenin
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Reatul Karim, Claudio Palazzo, Julie Laloy, Anne-Sophie Delvigne, Stéphanie Vanslambrouck, Christine Jerome, Elise Lepeltier, Francois Orange, Jean-Michel Dogne, Brigitte Evrard, Catherine Passirani, Géraldine Piel The purpose of this study was to develop different injectable nanosized drug delivery systems (NDDSs) i.e. liposome, lipid nanocapsule (LNC) and polymeric nanocapsule (PNC) encapsulating apigenin (AG) and compare their characteristics to identify the nanovector(s) that can deliver the la...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Poly-isoprenylated ifosfamide analogs: Preactivated antitumor agents as free formulation or nanoassemblies
We present here, the in vitro activity of the nanoassembly formulations of preactivated IFO derivatives with a C-4 geranyloxy, farnesyloxy and squalenoxy substituent on a large panel of tumor cell lines. The chemical and colloidal stabilities of the geranyloxy-IFO (G-IFO), farnesyloxy-IFO (F-IFO) and squalenoxy-IFO (SQ-IFO) NAs were further evaluated in comparison to their free formulation. Finally, pharmacokinetic parameters and maximal tolerated dose of the most potent preactivated IFO analog (G-IFO) were determined and compared to IFO, paving the way to in vivo studies. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research