Modulation Of Alendronate Release From A Calcium Phosphate Bone Cement: An In Vitro Osteoblast-Osteoclast Co-Culture Study
In this study, we loaded a biomimetic calcium phosphate bone cement (CPC) with relatively high amounts of a bisphosphonate through the use of Solid Lipid Microparticles (MPs) and investigated bone cells response to the composite cements. 10, 20 and 30% w/w of Alendronate (AL) were successfully introduced into microparticles of Cutina HR and Precirol, which were prepared by means of spray-congealing technique. Addition of AL-loaded MPs to the cement composition provoked a lengthening of the setting and of the hardening processes. However, setting times were still in a range useful for clinical applications, except for the c...
Source: International Journal of Pharmaceutics - November 11, 2018 Category: Drugs & Pharmacology Source Type: research

Multifunctional magnetic-gold nanoparticles for efficient combined targeted drug delivery and interstitial photothermal therapy
In this study, we developed multifunctional magnetic gold nanoparticles (MGNPs) that are able to (i) selectively deliver the drug to the tumor site in a controlled-release manner, either passively or by using magnetic targeting; (ii) induce photothermal therapy by producing heat by near-infrared (NIR) laser absorption; and (iii) serve as contrast agents for magnetic resonance imaging (MRI) (imaging-guided therapy). The prepared MGNPs were characterized by different physical techniques. They were then coated and conjugated with polyethylene glycol (PEG) and doxorubicin (DOX) to form MGNP-DOX conjugates. The high efficacy of...
Source: International Journal of Pharmaceutics - November 11, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced topical delivery of non-complexed molecular iodine for Methicillin-resistant Staphylococcus aureus decolonization
Publication date: 10 January 2019Source: International Journal of Pharmaceutics, Volume 554Author(s): Satoshi Uchiyama, Samira Dahesh, Victor Nizet, Jack KesslerAbstractStaphylococcus aureus, a leading cause of serious human infections in both healthcare and community settings, is increasingly difficult to control due to expanding resistance to multiple antibiotic classes. Methicillin-resistant S. aureus (MRSA) strains have disseminated on a global scale and are associated with adverse patient outcomes, increased hospital stays, and significant economic costs to the healthcare system. A proximal step in S. aureus infection...
Source: International Journal of Pharmaceutics - November 11, 2018 Category: Drugs & Pharmacology Source Type: research

Development of novel zero-order release budesonide tablets for the treatment of ileo-colonic inflammatory bowel disease and comparison with formulations currently used in clinical practice
Publication date: Available online 8 November 2018Source: International Journal of PharmaceuticsAuthor(s): Bahez Gareb, Gerard Dijkstra, Jos G.W. Kosterink, Henderik W. FrijlinkAbstractUp to 50% of Crohn’s disease and ulcerative colitis patients suffer from ileo-colonic inflammation. Topically delivered budesonide is an effective treatment but in vitro as well as clinical data suggest that oral formulations currently used in clinical practice are not optimal to treat the ileo-colon. The aim of this in vitro study was to develop ileo-colonic-targeted zero-order sustained-release tablets containing 3 mg or 9 mg budeson...
Source: International Journal of Pharmaceutics - November 9, 2018 Category: Drugs & Pharmacology Source Type: research

Toxicological study of doxorubicin-loaded PLGA nanoparticles for the treatment of glioblastoma
The objective of the present study was to evaluate the acute and chronic toxicity of this nanoformulation. The parent drug was used as a reference formulation. Acute toxicity of doxorubicin-loaded nanoparticles in mice and rats was similar to that of free doxorubicin. The chronic toxicity study was conducted in Chinchilla rabbits; the treatment regimen consisted of 30 daily intravenous injections using two dosage levels: 0.22 mg/kg/day and 0.15 mg/kg/day. The study included assessment of the body weight, hematological parameters, blood biochemical parameters, urinalysis, and pathomorphological evaluation of the internal or...
Source: International Journal of Pharmaceutics - November 8, 2018 Category: Drugs & Pharmacology Source Type: research

Injectability as a Function of Viscosity and Dosing Materials for Subcutaneous Administration
This article focuses on force measurements related to injectability, namely: force to expel syringe contents (expulsion force – a mimic for in vivo injection force), needle-penetration force, and needle-bending force, and these results are supplemented by expulsion time measurements with 18 participants, as well as injections in a porcine model. Based on the expulsion time measurements, where 80 N injection force was found to be difficult for most people, we consider the maximum acceptable injection force to be 40 N, and recommend targeting no more than 20 N, especially if the configuration may be used in an autoinje...
Source: International Journal of Pharmaceutics - November 8, 2018 Category: Drugs & Pharmacology Source Type: research

Prolonged release from orodispersible films by incorporation of diclofenac-loaded micropellets
Publication date: Available online 7 November 2018Source: International Journal of PharmaceuticsAuthor(s): Isabell Speer, Vincent Lenhart, Maren Preis, Jörg BreitkreutzAbstractProlonged drug release provided by multiple-unit dosage forms is highly beneficial to enhance the compliance and safety of the pharmacotherapy even for patients with swallowing deficiencies. To facilitate the intake for these patients, multiple-unit tablets and capsules have to be crushed or opened. An attempt to overcome these issues has been made by the introduction of orodispersible films (ODFs), which rapidly disintegrate within the oral cav...
Source: International Journal of Pharmaceutics - November 8, 2018 Category: Drugs & Pharmacology Source Type: research

Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions
Publication date: Available online 8 November 2018Source: International Journal of PharmaceuticsAuthor(s): Jelena Djuris, Stoja Milovanovic, Djordje Medarevic, Vladimir Dobricic, Aleksandra Dapčević, Svetlana IbricAbstractSolid dispersions production is one of the substantial approaches for improvement of poor drug solubility. Additionally, supercritical fluid assisted method for preparation of solid dispersions can offer many advantages in comparison to the conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance for selection of the most appropriate polymeric carrier for disp...
Source: International Journal of Pharmaceutics - November 8, 2018 Category: Drugs & Pharmacology Source Type: research

Modified Gelatin Nanoparticles for Gene Delivery
This article also considers several advantages of these modifications and their contribution to the improvement in the efficiency of these systems, resulting in superior transfection and enhanced gene delivery in general.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 7, 2018 Category: Drugs & Pharmacology Source Type: research

Development and in vitro evaluation of a self-emulsifying drug delivery system (SEDDS) for oral vancomycin administration
Publication date: Available online 5 November 2018Source: International Journal of PharmaceuticsAuthor(s): Sergey Zaichik, Christian Steinbring, Cagri Caliskan, Andreas Bernkop-SchnürchAbstractThe aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the glycopeptide antibiotic vancomycin (VAN) with improved intestinal mucosa permeating properties in order to increase oral drug absorption. VAN was effectively incorporated into SEDDS increasing the lipophilicity of the drug via hydrophobic ion pairing (HIP) with cetyltrimethylammonium bromid (CTAB). Newly developed SEDDS formulatio...
Source: International Journal of Pharmaceutics - November 7, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoparticle Eluting-Angioplasty Balloons to Treat Cardiovascular Diseases
Publication date: Available online 5 November 2018Source: International Journal of PharmaceuticsAuthor(s): Roshni Iyer, Aneetta E. Kuriakose, Serkan Yaman, Lee-Chun Su, Dingying Shan, Jian Yang, Jun Liao, Liping Tang, Subhash Banerjee, Hao Xu, Kytai T. NguyenAbstractNanoparticles (NPs) can be used to locally deliver anti-restenosis drugs when they are infused directly to the injured arteries after intervention procedures such as angioplasty. However, the efficacy of transferring NPs via infusion to the arterial wall is limited, at least partially, due to poor NP retention on the inner artery wall. To improve NP retention, ...
Source: International Journal of Pharmaceutics - November 7, 2018 Category: Drugs & Pharmacology Source Type: research

Oral siRNA Delivery Using Dual Transporting Systems to Efficiently Treat Colorectal Liver Metastasis
Publication date: Available online 3 November 2018Source: International Journal of PharmaceuticsAuthor(s): Eun-Ju Hyun, Mohammad Nazmul Hasan, Sung Hun Kang, Sungpil Cho, Yong-Kyu LeeAbstractOral siRNA delivery is an ideal way to translate siRNA therapeutic effects in the clinic due to its ability to be administered in convenient and multiple dosages. However, an effective oral delivery system requires overcoming both a hostile gastrointestinal (GI) environment and non-specific targeting. Here, an HTsRP-NC system is a new oral siRNA delivery system consisting of a siRNA/protamine (sRP) nano-complex protected by a multi-fun...
Source: International Journal of Pharmaceutics - November 4, 2018 Category: Drugs & Pharmacology Source Type: research

Angelica sinensis polysaccharide encapsulated into PLGA nanoparticles as a vaccine delivery and adjuvant system for ovalbumin to promote immune responses
In this study, the immunopotentiator Angelica sinensis polysaccharide (ASP) and model protein antigen ovalbumin (OVA) were encapsulated into Poly(lactic-co-glycolic acid) (PLGA) to formulate the novel NPs-based vaccine delivery system (ASP-PLGA/OVA). These formulations were subcutaneously administered to mice, then the magnitude and kinetics of antibody and cellular immune responses were assessed. The ASP-PLGA/OVA NPs were pherical in shape with smooth surfaces, approximately 225.2 nm in average size, negatively charged (around -11.27 mV), and the encapsulation efficiency of OVA at around 66.28 %, respectively. Furthermore...
Source: International Journal of Pharmaceutics - November 4, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of friction between powder and tooling on the die-wall pressure evolution during tableting: experimental and numerical results for flat and concave punches
Publication date: Available online 2 November 2018Source: International Journal of PharmaceuticsAuthor(s): V. Mazel, H. Diarra, P. TchoreloffAbstractTablets final properties are mainly determined during the compaction process by the evolution of the stresses applied to the powder. Any process or product parameter that may influence this stress evolution may have a direct impact on the tablet final properties. In this article, we studied the influence of the friction between the tooling and the powder on the evolution of the die-wall pressure during compaction using flat and concave punches.Experimental studies were perform...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Variability in the α and β anomer content of commercially available lactose
Publication date: Available online 2 November 2018Source: International Journal of PharmaceuticsAuthor(s): Mohamad Jamal Altamimi, Kim Wolff, Ali Nokhodchi, Gary P. Martin, Paul G. RoyallAbstractLactose, a disaccharide is a ubiquitous excipient in many pharmaceutical formulations which exists in two anomeric forms; either as α- or β-lactose. The anomers have different properties which can affect their application. Nevertheless, batches of lactose products are widely produced by many manufacturers, and is available in many grades. However, the anomeric content of these batches has not been accurately characterize...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Designed inorganic porous nanovector with controlled release and MRI features for safe administration of doxorubicin
Publication date: Available online 2 November 2018Source: International Journal of PharmaceuticsAuthor(s): Simo Näkki, Julie T.-W. Wang, Jianwei Wu, Li Fan, Jimi Rantanen, Tuomo Nissinen, Mikko I. Kettunen, Matilda Backholm, Robin H.A. Ras, Khulosud T. Al-Jamal, Vesa-Pekka Lehto, Wujun XuAbstractThe inability of traditional chemotherapeutics to reach cancer tissue reduces the treatment efficacy and leads to adverse effects. A multifunctional nanovector was developed consisting of porous silicon, superparamagnetic iron oxide, calcium carbonate, doxorubicin and polyethylene glycol. The particles integrate magnetic prope...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Biopharmaceutical profile of a clotrimazole nanoemulsion: Evaluation on skin and mucosae as anticandidal agent
Publication date: Available online 2 November 2018Source: International Journal of PharmaceuticsAuthor(s): José L. Soriano-Ruiz, Ana C. Calpena-Capmany, Cristina Cañadas-Enrich, Nuria Bozal-de Febrer, Joaquim Suñer-Carbó, Eliana B. Souto, Beatriz Clares-NaverosAbstractClotrimazole (CLT) was formulated in a nanoemulsion (NE) for the topical treatment of candidiasis consisting of 10% labrafac® lipophile, 60% labrasol®:capryol® 90 mixture (ratio 4:1) and 30% propylene glycol. Physicochemical properties, stability, rheology, in vitro drug release, ex vivo drug permeation through human sk...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of balloon coating process for paclitaxel coated balloons via micro-pipetting method
This study describes the process for an in-house micro-pipetting coating method that incorporates a laboratory-developed coating equation for determining optimal coating parameters. The coating solutions included a common drug of choice, paclitaxel, along with a hydrophilic excipient, such as iopromide. It was found that using a revolution rate of 240 rev/min, a flow rate of 25 µL/min and a translational speed of 0.033 cm/s resulted in visually uniform coatings. High performance liquid chromatography (HPLC) allowed for the determination of paclitaxel content on the balloon surface. Scanning electron microscopy (SEM) ...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

IEnhanced Topical Delivery of Non-complexed Molecular Iodine for Methicillin-Resistant Staphylococcus aureus Decolonization
Publication date: Available online 2 November 2018Source: International Journal of PharmaceuticsAuthor(s): Satoshi Uchiyama, Samira Dahesh, Victor Nizet, Jack KesslerAbstractStaphylococcus aureus, a leading cause of serious human infections in both healthcare and community settings, is increasingly difficult to control due to expanding resistance to multiple antibiotic classes. Methicillin-resistant S. aureus (MRSA) strains have disseminated on a global scale and are associated with adverse patient outcomes, increased hospital stays, and significant economic costs to the healthcare system. A proximal step in S. aureus infe...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation and evaluation of trityl-loaded lipid nanocapsules as oxygen sensors for Electron Paramagnetic Resonance oximetry
Publication date: Available online 3 November 2018Source: International Journal of PharmaceuticsAuthor(s): Janske Nel, Céline M. Desmet, Benoit Driesschaert, Patrick Saulnier, Laurent Lemaire, Bernard GallezAbstractOxygen is essential in physiology and pathophysiology. Electron Paramagnetic Resonance (EPR) oximetry, using oxygen sensitive paramagnetic materials, could be attractive for measuring oxygen in tissues. The aim of the present study was to assess the properties of lipid nanocapsules (LNCs) loaded with the nitroxide tempo-benzoate (TB) or tetrathiatriarylmethyl (TAM) radicals. LNCs loaded with the EPR probe...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation of aripiprazole-loaded pH-modulated solid dispersions via hot-melt extrusion technology: In vitro and In vivo studies
The objective of this study was to formulate aripiprazole (ARI)-loaded pH-modulated solid dispersions (SD) to enhance solubility, dissolution, and bioavailability via hot-melt extrusion (HME) technology. Kollidon® 12 PF (PVP) and succinic acid (SA) were selected after solubility screenings of various polymers and acidifiers. Several formulations, varying in screw speed and drug/polymer/acidifier ratios, were extruded using an 11 mm twin-screw extruder and were investigated for the effect of these variables. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were use...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of solvent selection on drug loading and amorphisation in mesoporous silica particles
Publication date: Available online 3 November 2018Source: International Journal of PharmaceuticsAuthor(s): Marek Šoltys, Pavel Kovačík, Ondřej Dammer, Josef Beránek, František ŠtěpánekAbstractIncreasing the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) is a key strategy used for improving their oral bioavailability. One of the formulation approaches is API loading to mesoporous carrier particles, which can increase the dissolution rate through the combination of improved powder wettability and dispersion, higher surface area, and API conversio...
Source: International Journal of Pharmaceutics - November 3, 2018 Category: Drugs & Pharmacology Source Type: research

Revisiting dispersible milk-drug tablets as a solid lipid formulation in the context of digestion
Publication date: Available online 31 October 2018Source: International Journal of PharmaceuticsAuthor(s): Syaza Y. Binte Abu Bakar, Malinda Salim, Andrew J. Clulow, Adrian Hawley, Ben J. BoydAbstractOral delivery of dispersible tablets is a preferred route of administration for paediatrics due to ease of administration and dose control. Milk has gained interest as a drug delivery system due to its ability to dissolve poorly water-soluble drugs. There are no reports of milk tablet formulations being assessed in the context of lipid digestion, which is critical in influencing orally administered drug solubility and bioavail...
Source: International Journal of Pharmaceutics - November 1, 2018 Category: Drugs & Pharmacology Source Type: research

Engineering of Acetaminophen Particle Attributes Using a Wet Milling Crystallisation Platform
Publication date: Available online 31 October 2018Source: International Journal of PharmaceuticsAuthor(s): Bilal Ahmed, Cameron J. Brown, Thomas McGlone, Deborah L. Bowering, Jan Sefcik, Alastair J. FlorenceAbstractWet milling coupled with crystallisation has considerable potential to deliver enhanced control over particle attributes. The effect of process conditions and wet mill configuration on particle size, shape and surface energy has been investigated on acetaminophen using a seeded cooling crystallisation coupled with a wet mill unit generating size controlled acetaminophen crystals through an interchangeable rotor-...
Source: International Journal of Pharmaceutics - November 1, 2018 Category: Drugs & Pharmacology Source Type: research

Process analytical technologies and injectable drug products: is there a future?
The objective was to offer the industry an alternative to the time and money consuming sterility testing, without compromising the sterility of the products. The rationale was that quality cannot be tested into products, instead it must be planned (the principle of quality by design, QbD). This can be implemented by setting appropriate in-process controls supported on process analytical technologies (PAT). Two of the most versatile and promising PAT tools are the near infrared spectroscopy (NIRS) and the Raman spectroscopy. However, their application to injectable drug product development and manufacturing has been scarce....
Source: International Journal of Pharmaceutics - October 31, 2018 Category: Drugs & Pharmacology Source Type: research

Structure-activity relationship of serotonin derived tocopherol lipids
Publication date: Available online 30 October 2018Source: International Journal of PharmaceuticsAuthor(s): Venkanna Muripiti, Thasneem Yoosuf Mujahid, Venkata Harsha Vardhan Boddeda, Shrish Tiwari, Srujan Kumar Marepally, Srilakshmi V Patri, Vijaya GopalAbstractTocopherol-based lipids are widely used for nucleic acid delivery. Using tocopherol molecules, we designed and synthesized 5-HT functionalized lipids by tethering 5-hydroxytryptamine (5-HT), a small molecule ligand as the head group to a natural amphiphilic molecule namely α-tocopherol (Vitamin E). This is with the aim of delivering nucleic acids specifically ...
Source: International Journal of Pharmaceutics - October 31, 2018 Category: Drugs & Pharmacology Source Type: research

Physostigmine-loaded liposomes for extended prophylaxis against nerve agent poisoning
Publication date: Available online 30 October 2018Source: International Journal of PharmaceuticsAuthor(s): Ju-Hwan Park, Jae-Young Lee, Ki-Taek Kim, Hae-Eun Joe, Hyun-Jong Cho, Young-Kee Shin, Dae-Duk KimAbstractPre-administration of physostigmine can prevent poisoning against nerve agent exposure by reversibly binding to cholinesterase. However, its cholinesterase protection-based prophylactic effect can be eliminated rapidly due to short biological half-life. Liposomes are useful for encapsulating hydrophilic drugs like physostigmine, and can be used for sustained release after parenteral injection. Thus, physostigmine l...
Source: International Journal of Pharmaceutics - October 31, 2018 Category: Drugs & Pharmacology Source Type: research

Application of in vitro lipolysis for the development of oral self-emulsified delivery system of Nimodipine
The objective of the current study was to optimize for the first time the formulation variables of self-emulsified drug delivery system (SEDDS) based on drug solubilization during lipolysis under a biorelevant condition of digestion such as lipase activity, temperature, pH, fed-fasting state, etc. Nimodipine (ND), a BCS class II, was used as a model drug to prepare the SEDDS. Various oils, surfactants, and cosurfactants were screened for their solubilization potential of ND. Area of self-emulsification was identified using various ternary phase diagrams. Box-Behnken design was employed to investigate effects of formulation...
Source: International Journal of Pharmaceutics - October 30, 2018 Category: Drugs & Pharmacology Source Type: research

SDF-1-loaded PLGA Nanoparticles for the Targeted Photoacoustic Imaging and Photothermal Therapy of Metastatic Lymph Nodes in Tongue Squamous Cell Carcinoma
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Jun Xiong, JiaLi Feng, Lihua Qiu, Zhi Gao, Pan Li, Liang Pang, Zewei ZhangAbstractThe combination of photothermal therapy and targeted chemotherapy can produce much greater cytotoxicity than chemotherapy. Herein, we developed multifunctional targeted polymeric nanoparticles (NPs) loaded with indocyanine green (ICG) and doxorubicin (DOX) for the targeted photoacoustic imaging and photothermal ablation of oral cancer cells. The chemokine SDF-1, a specific antibody, was conjugated to NPs by the carbodiimide method. The N...
Source: International Journal of Pharmaceutics - October 30, 2018 Category: Drugs & Pharmacology Source Type: research

Chitosan-based thermosensitive hydrogel for nasal delivery of exenatide: Effect of magnesium chloride
Publication date: Available online 30 October 2018Source: International Journal of PharmaceuticsAuthor(s): Ying Li, Jintian He, Xiaolin Lyu, Yuan Yuan, Gaizhen Wang, Baohua ZhaoAbstractThe aim of this research was to evaluate the potential of two chitosan (CS)-based hydrogel systems for nasal delivery of exenatide (EXT) in rats. Both of the EXT-loaded CS/glycerophosphate (GP)/CaCl2 (EXT/CS/GP/CaCl2) and EXT/CS/GP/MgCl2 hydrogel systems had similar in vitro release profiles. However, a difference in metal salt surprisingly resulted in multifaceted differences between the two hydrogel systems, such as EXT stability, gelation...
Source: International Journal of Pharmaceutics - October 30, 2018 Category: Drugs & Pharmacology Source Type: research

Recent advances in gold and silver nanoparticle based therapies for lung and breast cancers
Publication date: Available online 28 October 2018Source: International Journal of PharmaceuticsAuthor(s): Parth Malik, Tapan K. MukherjeeAbstractIn recent years, gold (Au) and silver (Ag) nanoparticles (NPs) have been the centerstage of improving cancer treatments and therapies, substantially attributed to their size and shape tuneable chemical, optical and photonic properties. Owing to such specialties, diverse shapes of Au and Ag NPs have enabled an efficient cellular uptake along with remarkable improvements in early stage diagnosis of tumors. Robust synthesis methods employing several reducing agents have been the bac...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced oral insulin delivery via surface hydrophilic modification of chitosan copolymer based self-assembly polyelectrolyte nanocomplex
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Chang Liu, Yongqiang Kou, Xin Zhang, Wei Dong, Hongbo Cheng, Shirui MaoAbstractIt is desirable to design nanoparticles for oral insulin delivery that can cross mucus layer and epithelial membrane in the intestine in the meantime. Thus, using chitosan (CS) as the nanocarrier, the objective of this study is to elucidate the contribution of surface hydrophilic and hydrophobic modification on the oral absorption of insulin and the essential for these two strategies combination. First of all, the polyelectronic nanocomplex...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Improving solid-state properties of berberine chloride through forming a salt cocrystal with citric acid
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Qi Lu, Jiangnan Dun, Jia-Mei Chen, Shuyu Liu, Changquan Calvin SunAbstractBerberine chloride (BCl) can exist as an anhydrate, monohydrate, dihydrate, and tetrahydrate. Therefore, it faces the problem of humidity dependent solid phase change when environmental humidity varies during manufacturing and storage of berberine tablets. We have discovered a new 1:1 cocrystal formed between berberine chloride and citric acid (BCl–CA) that exhibits better stability against variations in humidity while maintaining similar ...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of spray nozzle aperture during high shear wet granulation on granule properties and its compression attributes
In this study, nozzles of different aperture sizes were used to introduce the granulating liquid in high shear wet granulation using different process parameters. Design of experiment approach was utilised to assess effect of process parameters on granule properties. Granules produced with different spray nozzles were evaluated for binder distribution inhomogeneity, size, shape, flowability and compression attributes such as tabletability and yield pressure. Coarser granules with better flow properties were produced using the smaller aperture size nozzle. On the other hand, granules had better tabletability and lower yield...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Anti-inflammatory and Anti-cancer Activity of Citral: Optimization of Citral-loaded Solid Lipid Nanoparticles (SLN) using Experimental Factorial Design and LUMiSizer®
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Aleksandra Zielińska, Carlos Martins-Gomes, Nuno R. Ferreira, Amélia M. Silva, Izabela Nowak, Eliana B. SoutoAbstractEssential oils containing monoterpenes are widely used in pharmaceuticals and cosmetic products on account of their wide range of bioactive properties (including anti-cancer activity). Two monoterpenes (citral and geraniol) were firstly tested for their anti-inflammatory activity in a RAW 264.7 cell line, demonstrating citral to have enhanced capacity to inhibit NO production (ca. 84% for citral...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Facile fabrication of highly photothermal-effective albumin-assisted gold nanoclusters for treating breast cancer
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Sungin Lee, Changkyu Lee, Sanghyun Park, Kyungseop Lim, Sung Soo Kim, Jong Oh Kim, Eun Seong Lee, Kyung Taek Oh, Han-Gon Choi, Yu Seok YounAbstractGold nanoclusters (AuNCs) have been considered to be a promising candidate for hyperthermia-based anticancer therapy. Herein, we introduce albumin-assisted AuNCs composed of small gold nanoparticles (AuNPs,
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Critical Parameters Dictating Efficiency of Membrane-mediated Drug Transfer using Nanoparticles
In this study, we formulated curcumin in two-structurally distinct NPs: a nanoemulsion (Cur-NE) and a Niosome (Cur-NIO), evaluated their in-vitro cytotoxic effects and examined their mechanisms of drug delivery. The use of Cur-NIO resulted in an unexpected increase in the intracellular accumulation of curcumin and induced a potent cytotoxic effect compared to Cur-NE. To our surprise, however, the effects of the endocytosis of NIO as well as that for NE on the cellular delivery of curcumin were negligible. Consequently, we concluded that Cur-NIO delivers curcumin directly to the cytosol via transfer from the NIO to the cell...
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

A detailed analysis of the influence of β-cyclodextrin derivates on the thermal denaturation of lysozyme
This study reveals that CDs are promising systems for inhibiting protein aggregation without protein denaturation, only if designing derivative CDs is carefully controlled.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

Stability and compatibility of Basmisanil granules co-administered with soft food
Publication date: Available online 27 October 2018Source: International Journal of PharmaceuticsAuthor(s): Anikó Szepes, Anni Pabst-Ravot, Kirsten Storch, Carsten TimpeAbstractCo-administration of solid oral dosage forms with soft food or beverages is commonly used to facilitate administration and to improve compliance in the paediatric and geriatric population and in patient groups with swallowing difficulties.The present case study was conducted to investigate the compatibility, stability and dissolution of Basmisanil administered as granules mixed with different soft food matrices. The data were generated to just...
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

Dendrimer-like mesoporous silica nanospheres with suitable surface functionality to combat the multidrug resistance
This study indicates that surface functionality design strategy may display the potential of the large pore sized-MSNs as the efficient chemotherapeutic carriers to combat MDR.Graphical abstractThe potential mechanism of surface functionality-modified MSNs carrying DOX to chemotherapeutic-resistant cancer cells to combat the multidrug resistance (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Encapsulation of Poly I:C and the natural phosphodiester CpG ODN enhanced the efficacy of a hyaluronic acid-modified cationic lipid-PLGA hybrid nanoparticle vaccine in TC-1-grafted tumors
In conclusion, the combination of oligonucleotide adjuvants and synthetic particulate systems not only potentiated the immunogenicity of these nanoparticles but also made these adjuvants safer and more economical, which may be helpful for their wide application.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Corneal targeted Sertaconazole nitrate loaded cubosomes: preparation, statistical optimization, in vitro characterization, ex vivo permeation and in vivo studies
Publication date: Available online 26 October 2018Source: International Journal of PharmaceuticsAuthor(s): Nihal Farid Younes, Sally Adel Abdel-Halim, Abdelhalim I. ElassasyAbstractSertaconazole nitrate (STZ) is a poorly soluble antifungal drug commonly used for treating fungal skin infections. Introducing it as a new treatment option for the management of fungal keratitis, requires the development of a delivery system capable of targeting the infected cornea with an adequate STZ concentration. Hence, Sertaconazole nitrate loaded cubosomes (STZ-CUBs) were prepared, characterized and optimized based on a 33 central composit...
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Delimiting the Knowledge Space and the Design Space of Nanostructured Lipid Carriers through Artificial Intelligence Tools
In this study, a two-step experimental design was performed and databases were successfully modelled using Artificial Intelligence techniques as an innovative method to get optimal, reproducible and stable NLC. The initial approach, including a wide range of values for the different variables, was followed by a second set of experiments with variable values in a narrower range, more suited to the characteristics of the system. NLC loaded with rifabutin, a hydrophobic drug model, were produced by hot homogenization and fully characterized in terms of particle size, size distribution, Zeta potential, encapsulation efficiency...
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Early Detection of Capping Risk in Pharmaceutical Compacts
Publication date: Available online 24 October 2018Source: International Journal of PharmaceuticsAuthor(s): Xiaochi Xu, Chaitanya Krishna Prasad Vallabh, Stephen W. Hoag, Vivek S. Dave, Cetin CetinkayaAbstractCapping is a common mechanical defect in tablet manufacturing, exhibited during or after the compression process. Predicting tablet capping in terms of process variables (e.g. compaction pressure and speed) and formulation properties is essential in pharmaceutical industry. In current work, a non-destructive contact ultrasonic approach for detecting capping risk in the pharmaceutical compacts prepared under various com...
Source: International Journal of Pharmaceutics - October 25, 2018 Category: Drugs & Pharmacology Source Type: research

The application of temperature-composition phase diagrams for hot melt extrusion processing of amorphous solid dispersions to prevent residual crystallinity
In conclusion, phase diagrams provide a rational basis for designing hot melt extrusion processes of amorphous solid dispersions to minimize residual crystalline content, delineating the minimum processing temperature based on thermodynamic considerations.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 25, 2018 Category: Drugs & Pharmacology Source Type: research

Vibrational spectroscopic and Hirshfeld surface analysis of carvedilol crystal forms
This study deals with the spectroscopic (supported by quantum chemistry calculations) characterization of carvedilol structures. Band assignments were performed considering the isolated molecules and periodic calculations. We discuss the correlation between the vibrational modes and the intermolecular forces in the crystalline structures. Towards a better understanding of the intermolecular interactions, Hirshfeld surface was used. Besides band shifts related to stretching vibrations of N−H and O−H groups, differences between other modes have shown the possibility of using infrared spectroscopy to distinguish t...
Source: International Journal of Pharmaceutics - October 24, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 1 December 2018Source: International Journal of Pharmaceutics, Volume 552, Issues 1–2Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 24, 2018 Category: Drugs & Pharmacology Source Type: research

Design of a new disintegration test system for the evaluation of orally disintegrating films
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): Yoshiko Takeuchi, Misaki Kawamoto, Kohei Tahara, Hirofumi TakeuchiAbstractIn the design of the orally disintegrating films (ODFs), it is important to determine the disintegration time (DT) precisely and properly. These films’ DTs are usually assessed by a disintegration test defined in the pharmacopoeias, but under the conditions of such tests, a much larger volume of water is used and a stronger up-down movement is applied compared to the conditions of the human oral cavity. Here we developed and tested our new...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Phospholipid components of the synthetic pulmonary surfactant CHF5633 probed by fluorescence spectroscopy
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): Serena Faggiano, Luca Ronda, Samanta Raboni, Franco Sartor, Valeria Cavatorta, Elisa Sgarbi, Grazia Caivano, Marisa Pertile, Andrea MozzarelliAbstractCHF5633 (Chiesi Farmaceutici, Italy) is a synthetic pulmonary surfactant currently under clinical development for the treatment of Respiratory Distress Syndrome in premature infants. The product is composed of phospholipids in liposomal organization, together with two peptide analogues of human surfactant proteins B and C. Phospholipids in liposomes can undergo oxidation...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics and pharmacodynamics of glimepiride polymorphs
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): André Luiz Machado Viana, Antonio Carlos Doriguetto, Olimpia Maria Martins Santos Viana, André Luís Morais Ruela, Jennifer Tavares Jacon Freitas, Bruno Ewerton Meireles Souto, Magali Benjamim de Araújo, Fernanda Borges de Araújo PaulaAbstractGlimepiride (GLIM) is used as an oral antihyperglycemic agent for treatment of type 2 diabetes. The drug presents two polymorphic forms (GLIM form I and GLIM form II) described in the literature, and according to in vitro data, GLIM form II is ab...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research