Effect of PEGylation on the biological properties of cationic carbosilane dendronized gold nanoparticles
Publication date: Available online 22 November 2019Source: International Journal of PharmaceuticsAuthor(s): Andrea Barrios-Gumiel, Javier Sánchez-Nieves, Elzbieta Pedziwiatr-Werbicka, Viktar Abashkin, Natallia Shcharbina, Dzmitry Shcharbin, Sława Glińska, Karol Ciepluch, Dorota Kuc-Ciepluch, Dominika Lach, Maria Bryszewska, Rafael Gómez, F. Javier de la MataAbstractHeterofunctionalized gold nanoparticles (AuNP) were obtained in a one pot reaction of gold precursor with cationic carbosilane dendrons (first to third generations, 1-3G) and (polyethylene)glycol (PEG) ligands in the presence of a reducing agent....
Source: International Journal of Pharmaceutics - November 23, 2019 Category: Drugs & Pharmacology Source Type: research

A Method to Rapidly Analyze the Simultaneous Release of Multiple Pharmaceuticals from Electrospun Fibers
In this study, we developed a method to analyze the release of multiple pharmaceuticals from a single electrospun fiber scaffold and determine how each pharmaceutical’s loading concentration affects the release rate of each pharmaceutical. Our analysis methods were tested on electrospun fibers loaded with two pharmaceuticals: 6-aminonicotinamide (6AN) and ibuprofen. Pharmaceutical concentration in electrospun fibers ranged from 1.5% to 8.5% by weight. We found that 6AN release was dependent on the concentration of 6AN and ibuprofen loaded into the fibers, while ibuprofen release was only dependent on the loading conc...
Source: International Journal of Pharmaceutics - November 23, 2019 Category: Drugs & Pharmacology Source Type: research

Gastro-resistant encapsulation of amorphous solid dispersions containing darunavir by coaxial electrospraying
In this study, amorphous solid dispersions of a hydroxypropyl methylcellulose or polyvinlypyrrolidone based polymer matrix containing the active pharmaceutical ingredient darunavir were coated with a gastro-resistant shell polymer that does not dissolve at lower pH present in the stomach, but only later at a higher pH in the small intestine. A multitude of shell polymers were tested with the aim to identify a material that limits the drug release to less than 10 % after two hours at a pH of 1 to comply with the European Pharmacopoeia regarding gastro-resistant formulations. In parallel, the core-shell structure of the part...
Source: International Journal of Pharmaceutics - November 23, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of hydrophobic tails of plier-like cationic lipids on nucleic acid delivery and intracellular trafficking
In this study, the plier-like cationic niosomes (PCNs) containing PCL (A, B, and C) were evaluated their performance to deliver pDNA and siRNA to HeLa cells. Among the PCNs, PCN-B with saturated asymmetric hydrocarbon tails (C18 and C12) provided the highest efficiency for pDNA and siRNA delivery. Furthermore, the results revealed that the structure of the cationic lipids affected the internalization pathway and the intracellular trafficking. PCL-B and PCL-C with asymmetric tails preferred clathrin- and caveolae-mediated endocytosis as the predominant internalization pathways and were also involved in the polymerization pr...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Hyaluronic acid based nanohydrogels fabricated by microfluidics for the potential targeted release of Imatinib: characterization and preliminary evaluation of the antiangiogenic effect
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Flavia Bongiovì, Calogero Fiorica, Fabio Salvatore Palumbo, Giovanna Pitarresi, Gaetano GiammonaAbstractMicrofluidics is emerging as an innovative technique for the “on chip” fabrication of nanoparticles for drug delivery applications. Here, by using an amphiphilic derivative of hyaluronic acid as a starting macromolecule, nanohydrogels loaded with Imatinib were produced by the microfluidic procedure in order to develop an innovative therapeutic tool for the treatment of retinal neovascularization....
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Investigation on the effect of deep eutectic formation on drug-polymer miscibility and skin permeability of rotigotine drug-in-adhesive patch
In conclusion, a reduced administration area (75%) and low risk of crystallization were introduced by the ROT deep eutectics, which demonstrated the feasibility of improving drug-polymer miscibility and skin permeability of transdermal drug. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Barrier-disrupted skin: Quantitative analysis of tape and cyanoacrylate stripping efficiency by multiphoton tomography
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Pin Dong, Viktor Nikolaev, Marius Kröger, Christian Zoschke, Maxim E. Darvin, Christian Witzel, Jürgen Lademann, Alexa Patzelt, Monika Schäfer-Korting, Martina C. MeinkeAbstractNumerous studies have employed tape stripping (TS) or cyanoacrylate stripping (CS) to induce skin barrier disruption of the stratum corneum (SC) in human and porcine skin. However, the thickness of the remaining SC and the respective changes of the skin permeability have been rarely quantified. By using high-resolution multiphot...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of induction methods for supersaturation: pH shift versus solvent shift
This study investigates the impact of the induction method of supersaturation for nine basic drugs, A0619, A2853, albendazole, cinnarizine, dipyridamole, intraconazole, JNJ39393406, ketoconazole, and posaconazole, on four parameters: highest apparent degree of supersaturation, induction time, precipitation rate and solid form of the precipitate, using a novel standardized small-scale supersaturation and precipitation method. For eight of the nine drugs, the same highest apparent degree of supersaturation was obtained with both induction methods. For the induction time, precipitation rate and the solid form of the precipita...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

P-glycoprotein (ABCB1/MDR1) limits brain accumulation and Cytochrome P450-3A (CYP3A) restricts oral availability of the novel FGFR4 inhibitor fisogatinib (BLU-554)
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Wenlong Li, Rolf Sparidans, Mujtaba El-lari, Yaogeng Wang, Maria C. Lebre, Jos H. Beijnen, Alfred H. SchinkelAbstractFisogatinib (BLU-554) is a highly selective and potent oral fibroblast growth factor receptor 4 (FGFR4) inhibitor currently in Phase I clinical trials for treatment of hepatocellular carcinoma (HCC). Using (male) genetically modified mouse models, we investigated the roles of the multidrug efflux transporters ABCB1 and ABCG2, the OATP1A/1B uptake transporters, and the drug-metabolizing CYP3A complex in...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

pH-responsive Chimeric Liposomes: From Nanotechnology to Biological Assessment
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Nikolaos Naziris, Francesca Saitta, Varvara Chrysostomou, Marcin Libera, Barbara Trzebicka, Dimitrios Fessas, Stergios Pispas, Costas DemetzosAbstractThe utilization of liposomes in biomedical applications has greatly benefited the diagnosis and treatment of various diseases. These biomimetic nano-entities have been very useful in the clinical practice as drug delivery systems in their conventional form, comprising lipids as structural components. However, the scientific efforts have recently shifted towards the deve...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Dendrimers in the context of nanomedicine
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Ana Paula Dias, Soraya da Silva Santos, João Vitor da Silva, Roberto Parise Filho, Elizabeth Igne Ferreira, Omar El Seoud, Jeanine GiarollaAbstractDendrimers are globular structures, presenting an initiator core, repetitive layers starting radially from the core and terminal groups on the surface, resembling tree architecture. These structures have been studied in many biological applications, as drug, DNA, RNA and proteins delivery, as well as imaging and radiocontrast agents. With reference to that, this rev...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Mucoadhesive Thin Films For The Simultaneous Delivery Of Microbicide And Anti-Inflammatory Drugs In The Treatment Of Periodontal Diseases
Publication date: Available online 20 November 2019Source: International Journal of PharmaceuticsAuthor(s): Sim Yee Lim, Mali Dafydd, JieJi Ong, Launa A. Ord-McDermott, Emma Board-Davies, Kirsty Sands, David Williams, Alastair J. Sloan, Charles M. HeardAbstractThere is an unmet clinical need for new products to address the high percentage of the populous who present with periodontal diseases. Drug dose retention at the point of application would facilitate sustained release and more efficacious treatments. The aim of this study was to evaluate mucoadhesive polymeric thin films for simultaneous in situ delivery chlorhexidin...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Ex vivo (human skin) and in vivo (minipig) permeation of propylene glycol applied as topical crisaborole ointment, 2%
Publication date: Available online 21 November 2019Source: International Journal of PharmaceuticsAuthor(s): Avinash Thombre, Susanna Tse, Thean Yeoh, Raymond Chen, Robert North, Marc BrownAbstractCrisaborole ointment, 2%, is a non-steroidal phosphodiesterase 4 inhibitor for the treatment of mild-to-moderate atopic dermatitis. It contains 9% w/w propylene glycol (PG). Although PG is generally considered to be safe when used as a pharmaceutical excipient or food additive, the European Medicines Agency has recommended maximum daily limits for PG exposure. To determine the potential skin permeation of PG from crisaborole ointm...
Source: International Journal of Pharmaceutics - November 21, 2019 Category: Drugs & Pharmacology Source Type: research

Mangiferin glycethosomes as a new potential adjuvant for the treatment of psoriasis
Publication date: Available online 18 November 2019Source: International Journal of PharmaceuticsAuthor(s): M. Pleguezuelos-Villa, Octavio Diez-Sales, Maria Letizia Manca, Maria Manconi, Amparo Ruiz Sauri, Elvira Escribano-Ferrer, Amparo NácherAbstractMangiferin, a natural compound isolated from Mangifera indica L, was incorporated in glycerosomes, ethosomes and alternatively in glycerol-ethanol phospholipid vesicles (glycethosomes). Actually, only glycethosomes were able to stably incorporate the mangiferin that was loaded at increasing concentrations (2, 4, 6, 8 mg/mL). The morphology, size distribution, rheologic...
Source: International Journal of Pharmaceutics - November 20, 2019 Category: Drugs & Pharmacology Source Type: research

Compartmental approach for modelling twin-screw granulation using population balances
In this study, a compartmental population balance model (CPBM) is developed as a predictive tool of particle size distribution (PSD) for wet granulation in co-rotating twin-screw granulator (TSG). This model is derived in terms of liquid to solid ratio (L/S) and screw speed representing the main process parameters of the TSG. The mathematical model accounts for aggregation and breakage of the particles occurring in five compartments of the TSG with inhomogeneous screw configurations (3 conveying zones and 2 kneading zones). Kapur’s aggregation kernel is implemented in granulation and finite volume numerical method is...
Source: International Journal of Pharmaceutics - November 20, 2019 Category: Drugs & Pharmacology Source Type: research

A facile di-acid mono-amidation strategy to prepare cyclization-activating mono-carboxylate transporter 1-targeting gemcitabine prodrugs for enhanced oral delivery
Publication date: Available online 19 November 2019Source: International Journal of PharmaceuticsAuthor(s): Yang Wang, Gang Wang, Hongxiang Chen, Yixin Sun, Mengchi Sun, Xiaohong Liu, Wang Jian, Zhonggui He, Jin SunAbstractIntestinal mono-carboxylate transporter 1 (MCT1) plays an important role in the oral absorption of short-chain fatty acids that were used as oxidative metabolite. However, the prodrug strategy targeting intestinal MCT1 for oral delivery is rarely exploited. The oral bioavailability of Gemcitabine (Gem) is low mainly due to its poor intestinal permeability and rapid metabolism. Herein, a facile di-acid mo...
Source: International Journal of Pharmaceutics - November 20, 2019 Category: Drugs & Pharmacology Source Type: research

Study of Drug Particle Distributions within Mini-tablets Using Synchrotron X-ray Microtomography and Superpixel Image Clustering
Publication date: Available online 19 November 2019Source: International Journal of PharmaceuticsAuthor(s): Leonie Wagner-Hattler, Gabriela Québatte, Jennifer Keiser, Joachim Schoelkopf, Christian M. Schlepütz, Jörg Huwyler, Maxim PuchkovAbstractUniform drug distribution within fast disintegrating tablets is a key quality measure to ensure a reliable, steady, and targeted release of the contained active pharmaceutical ingredients. In this work, the drug particle distribution in mini-tablets was studied with synchrotron phase contrast X-ray microtomography. Mini-tablets had a weight of 9.5 mg and a drug loa...
Source: International Journal of Pharmaceutics - November 20, 2019 Category: Drugs & Pharmacology Source Type: research

Amplification of tumor antigen presentation by NLGplatin to improve chemoimmunotherapy
Publication date: Available online 19 November 2019Source: International Journal of PharmaceuticsAuthor(s): Yong Zhu, Lei Xing, Xiao Zheng, Chen-Xi Yang, Yu-Jing He, Tian-Jiao Zhou, Qing-Ri Jin, Hu-Lin JiangAbstractOxaliplatin is a chemotherapeutic agent widely used in cancer treatment whereas its immunosuppressive effect hinders the progress of immunotherapy. Here we have synthesized a new compound NLGplatin constructed by combining oxaliplatin (OXA) and indoleamine 2,3-dioxygenase (IDO) inhibitor NLG919. The NLGplatin acquires chemotherapeutic properties of OXA and can activate the immune system, and also retains the abi...
Source: International Journal of Pharmaceutics - November 20, 2019 Category: Drugs & Pharmacology Source Type: research

Application of feeding guiders to improve the powder distribution in the two scales of roller compactors
Publication date: Available online 18 November 2019Source: International Journal of PharmaceuticsAuthor(s): Mingzhe Yu, Marcus Weidemann, Chalak S. Omar, Alexander Schmidt, James D. Litster, Agba D. SalmanAbstractRoller compaction is a continuous dry granulation process, where the powder is compressed between two counter-rotating rollers and compacted into ribbons. The quality and homogeneity of the granulate is determined by the uniformity and porosity of the ribbon, which depends on the feeding process of the primary powder to the rollers, the flow properties of the primary powder and process parameters such as roller fo...
Source: International Journal of Pharmaceutics - November 18, 2019 Category: Drugs & Pharmacology Source Type: research

A novel wound dressing consisting of PVA-SA hybrid hydrogel membrane for topical delivery of bacteriophages and antibiotics
Publication date: Available online 15 November 2019Source: International Journal of PharmaceuticsAuthor(s): Prabhjot Kaur, Vijay Singh Gondil, Sanjay ChhibberAbstractThe emergence of antibiotic-resistant pathogens has made the treatment of infected burn wounds even more problematical than the pre-antibiotic era. Phage therapy is now being considered a promising treatment options to fight against antibiotic resistant pathogens. Hence, we introduce a novel PVA-SA hydrogel based wound dressing system for topical delivery of bacteriophages and antibiotic to treat infected burn injuries. Hydrogel membrane provides wound healing...
Source: International Journal of Pharmaceutics - November 17, 2019 Category: Drugs & Pharmacology Source Type: research

aQbD as a platform for IVRT method development – A regulatory oriented approach
Publication date: 15 December 2019Source: International Journal of Pharmaceutics, Volume 572Author(s): Margarida Miranda, Alberto A.C.C. Pais, Catarina Cardoso, Carla VitorinoAbstractThe EMA draft guideline on quality and equivalence of topical products and the FDA non-binding product specific guidances release has encouraged the establishment of a regulatory background for in vitro release testing (IVRT). Herein, a novel framework applicable to the development of a discriminatory IVRT method is described, according to analytical quality by design (aQbD) principles. A commercially available diclofenac emulgel formulation w...
Source: International Journal of Pharmaceutics - November 14, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanistic explanation of the (up to) 3 release phases of PLGA microparticles: Diprophylline dispersions
Publication date: Available online 11 November 2019Source: International Journal of PharmaceuticsAuthor(s): F. Tamani, C. Bassand, M. Hamoudi-Ben Yelles, F. Danede, J.F. Willart, F. Siepmann, J. SiepmannAbstractThe aim of this study was to better understand the root causes for the (up to) 3 drug release phases observed with poly (lactic-co-glycolic acid) (PLGA) microparticles containing diprophylline particles: The 1st release phase (“burst release”), 2nd release phase (with an “about constant release rate”) and 3rd release phase (which is again rapid and leads to complete drug exhaust). The behavio...
Source: International Journal of Pharmaceutics - November 12, 2019 Category: Drugs & Pharmacology Source Type: research

Efficient delivery of anti-miR-210 using Tachyplesin, a cell penetrating peptide, for glioblastoma treatment
Publication date: Available online 11 November 2019Source: International Journal of PharmaceuticsAuthor(s): Anirban Jana, Pankhuri Narula, Archana Chugh, Ritu KulshreshthaAbstractThe levels of microRNAs (miRNAs) are altered in various diseases including glioblastoma (GBM) and this alteration may have widespread effects on various hallmarks of cancer cells. MiR210 is overexpressed in GBM and functions as an oncogenic miRNA. Anti-miR210 therapy holds great promise but its efficient delivery remains a major challenge. Our work here explores a novel role of Tachyplesin (Tpl), a cell-penetrating antimicrobial peptide, as a nano...
Source: International Journal of Pharmaceutics - November 12, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis of hyaluronic acid-based polymersomes for doxorubicin delivery to metastatic breast cancer
Publication date: Available online 11 November 2019Source: International Journal of PharmaceuticsAuthor(s): Mahsa Shahriari, Seyed Mohammad Taghdisi, Khalil Abnous, Mohammad Ramezani, Mona AlibolandiAbstractIn the current research, the synthesis of polysaccharide-based polymersomes for targeted delivery of doxorubicin is reported. To this aim, doxorubicin was encapsulated in aqueous compartment of hyaluronan-polycaprolactone polymersomes via nanoprecipitation method. Then the therapeutic index of the prepared formulation was studied in metastatic breast cancer model in vitro and in vivo.The size of obtained polymersomes wa...
Source: International Journal of Pharmaceutics - November 12, 2019 Category: Drugs & Pharmacology Source Type: research

Design of Coenzyme Q10 solid dispersion for improved solubilization and stability
In conclusion, a CQ10 SD formulation with significantly improved dissolution (%) and stability was developed. Thus, the SD7 formulation is expected to show improved bioavailability and effectiveness in the treatment of aging-related and cardiovascular diseases.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 12, 2019 Category: Drugs & Pharmacology Source Type: research

Impact of mixed counter ion on saturation solubility of esylate salt of a weak basic drug to formulate physically stable and non-hemolytic ready to use injectable solution
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Gautam Dalwadi, Yan Sun, Lihong Wang, Jordan Shick, Kaitlin Hicks, Stephanie Lam, Vinod Tuliani, Kamlesh PatelAbstractCurrent work investigates a typical issue in formulating a physically stable solution especially when more than one counter ions exist in the composition. The impact of different counter ions on solubilization of an esylate salt of GSK-497, [BH+-CH3SO-3H2O] (1:1) and free base (pKa value 8.0) was investigated to formulate ready to use small volume injectable solution. The concentration dependent aggreg...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Biofabrication of microcapsules encapsulating beta-TC-6 cells via scalable device and in-vivo evaluation in type 1 diabetic mice
This study aims at the fabrication and evaluation of alginate-chitosan microcapsules encapsulating insulin-secreting beta-TC-6 cells using an automated spraying nozzle. Uniform spherical microcapsules (250-350 µm) encapsulated with beta-TC-6 cells were fabricated in large quantities in a short span of time. Microencapsulated beta-TC-6 cells were transplanted intraperitoneally into streptozotocin (STZ) induced diabetic mice and monitored for immune tolerance and decrease in blood glucose levels. Mice that received microencapsulated beta-TC-6 cells maintained normoglycemia for 35±5 days before rejection. However...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Impact of nanostructured lipid carriers on dapsone delivery to the skin; in vitro and in vivo studies
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Mohammed Elmowafy, Khaled Shalaby, Hazim M. Ali, Nabil K. Alruwaili, Ayman Salama, Mohamed F. Ibrahim, Mohamed A. Akl, Tarek A. AhmedAbstractThe main objective of this study was to develop, characterize and evaluate the potential use of dapsone-loaded nanostructured lipid carriers (NLCs) as a topical treatment for acne. Differently charged NLC formulations were successfully prepared using an emulsification/sonication method. The particle sizes ranged from 106.2±5.6 nm to 151.3±7.4 nm, and the NLCs posses...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanistic Modelling of Fluid Bed Granulation, Part II: Eased process development via Degree of Wetness
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Maryam Askarishahi, Mohammad-Sadegh Salehi, Martin Maus, Daniela Schröder, David Slade, Dalibor JajcevicAbstractThe performance of a fluid bed granulator was investigated through experimental and numerical study to develop a stand-alone fluid bed granulation model. The single-compartment model proposed in part I (for agglomeration modeling) was extended to account for i) evaporation of freely-flowing droplets, and ii) particle drying. This model enables us to predict the granule liquid content and temperature bes...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Fluticasone propionate nanosuspensions for sustained nebulization delivery: An in vitro and in vivo evaluation
This study intended to investigate the in vivo pulmonary fate of intratracheally dosed nanosuspensions of fluticasone propionate (FP). Three FP suspensions, including a microsuspension and two nanosuspensions with different dissolution profiles, were prepared and they exhibited comparable aerodynamic performances after nebulization via a jet nebulizer. Following intratracheal administration to rats, the microsuspension underwent extensive mucociliary clearance, leading to a limited absorption time whereas the nanosuspensions decreased the mucociliary clearance and allowed dissolution rate-limiting and extended pulmonary ab...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Fenoldopam mesylate for treating psoriasis: A new indication for an old drug
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Sindhu Doppalapudi, Anjali Jain, Wahid Khan, Abraham J. DombAbstractFenoldopam, a highly selective dopamine receptor agonist, is available in clinics as Corlopam™ i.v. for the management of severe hypertension. Recent reports demonstrate its anti-proliferative activity in vitro in a dose dependent manner. However, stability issues of the drug due to its susceptibility to oxidation, pH sensitivity, poor transdermal flux, and the barrier properties of skin present challenges to develop a topical formulation of fen...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Assessment of Impact Breakage of Carbamazepine Dihydrate due to Aerodynamic Dispersion
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Wei Pin Goh, Muzammil Ali, Kushal Sinha, Nandkishor K. Nere, Raimundo Ho, Shailendra Bordawekar, Ahmad Sheikh, Mojtaba GhadiriAbstractAcicular crystals are very common in pharmaceutical manufacturing. They are very prone to breakage, causing unwanted particle size degradation and problems such as segregation and lump formation. We investigate the breakage pattern of carbamazepine dihydrate, an acicular and platy crystal with cleavage planes. It readily undergoes attrition during isolation and drying stage, causing pro...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Bio-nanotechnological advancement of orally administered insulin nanoparticles: Comprehensive review of experimental design for physicochemical characterization
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Chun Y. Wong, Giuseppe Luna, Jorge Martinez, Hani Al-Salami, Crispin R. DassAbstractTherapeutic proteins are labile macromolecules that are prone to degradation during production, freeze-drying and storage. Recent studies showed that nanoparticles can enhance the stability and oral bioavailability of encapsulated proteins. Several conventional approaches (enzyme inhibitors, mucoadhesive polymers) and novel strategies (surface modification, ligand conjugation, flash nano-complexation, stimuli-responsive drug delivery s...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Making Tablets for Delivery of Poorly Soluble Drugs Using Photoinitiated 3D Inkjet Printing
In this study, we investigate the viability of three-dimensional (3D) inkjet printing with UV curing to produce solid dosage forms containing a known poorly soluble drug, carvedilol. The formulation consists of 10 wt% carvedilol, Irgacure 2959, and a photocurable N-vinyl-2-pyrrolidone (NVP) and poly(ethylene glycol) diacrylate matrix, with the intention of forming an amorphous solid solution for release of carvedilol. Characterization of the printed tablets showed that the drug is an amorphous state and indicated hydrogen bonding interactions between the drug and cross-linked matrix. Several simple geometries (ring, mesh, ...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Dermal smartPearls – Optimized silica particles for commercial products & mechanistic considerations
In this study 5 different silica particles were investigated regarding loading capacity and long-term stability of the amorphous form. Five different silica were used ranging in pore mean size from 3 to 25 nm, pore volume 0.4 to 1.8 mL/g, and BET surface from 740 to 320 m2/g. As model active avobenzone was used, because it is a challenging molecule by its high crystallisation tendency. To be industrially feasible, a loading capacity of about 50% pore volume was investigated. The particles were loaded by an immersion evaporation method, being able to be used in industrial production. A theory of the active precipitation in ...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Metronidazole/Hydroxypropyl-β-Cyclodextrin Inclusion Complex Nanofibrous Webs as Fast-dissolving Oral Drug Delivery System
In this study, Metronidazole/Hydroxypropyl-β-Cyclodextrin (HP-β-CyD) inclusion complex nanofibrous webs were produced via electrospinning for the purpose of fast-dissolving oral drug delivery. The Metronidazole/HP-β-CyD inclusion complex aqueous solutions having two different molar ratio of Metronidazole/HP-β-CyD (1/1 and 1/2) were prepared by using very high concentration of HP-β-CyD (200 %, w/v) in order to achieve polymer-free electrospinning of Metronidazole/HP-β-CyD nanofibers (NF). Metronidazole was totally encapsulated and preserved without any loss during the electrospinning process in...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanistic Modelling of Fluid Bed Granulation, Part I: Agglomeration in Pilot Scale Process
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Maryam Askarishahi, Martin Maus, Daniela Schröder, David Slade, Michael Martinetz, Dalibor JajcevicAbstractThe present study aims to develop a mechanistic model to predict the performance of a fluid bed granulation process. Therefore, the behavior of the bed was investigated experimentally for various operating conditions. It was observed that the granule Loss on Drying (LoD) and granule size are strongly interrelated. In detail, the maximum final granule size was observed at an intermediate final LoD. Consequent...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Design, Synthesis and Characterization of a PEGylated Stanozolol for Potential Therapeutic Applications
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Cristian Vergallo, Giulia Torrieri, Riccardo Provenzani, Sini Miettinen, Karina Moslova, Markku Varjosalo, Maria Chiara Cristiano, Massimo Fresta, Christian Celia, Hélder A. Santos, Felisa Cilurzo, Luisa Di MarzioAbstractStanozolol (STZ) is a drug used to treat serious disorders like aplastic anemia and hereditary angioedema. It is also indicated as an adjunct therapy for the treatment of vascular disorders and growth failures. Encouraging results obtained using animal models demonstrated that STZ increases bon...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of intestinal permeation enhancement with carboxymethyl chitosan-rhein polymeric micelles for oral delivery of paclitaxel
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Xiaoying Wang, Liangzhen Qiu, Xiaying Wang, Huizhi Ouyang, Tonglei Li, Lifeng Han, Xue Zhang, Wei Xu, Kedan ChuAbstractPolymeric micelles (PMs) are currently under investigation as potential nanocarriers for oral administration of paclitaxel (PTX). Previously, we developed amphiphilic carboxymethyl chitosan-rhein (CR) conjugate for oral delivery of PTX. PTX-loaded CR PMs exhibited a homogeneous and small size (
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers for oral delivery of silymarin: improving its absorption and in vivo efficacy in type 2 diabetes and metabolic syndrome model
This study aimed to investigate the possibility of delivery of SLM via nanostructured lipid carriers (NLCs) to overcome these issues and for preparation of an oral dosage form. NLCs were prepared through an emulsion/evaporation/solidifying method. Cetyl palmitate:Lauroglycol 90 was selected as the lipid mixture and Brij S20 as surfactant. NLCs were chemically and physically characterized. Encapsulation efficiency was more than 92%. The storage stability of the NLC suspension was also investigated and the freeze-drying process was taken into consideration. After assessing the stability of the formulation in a simulated gast...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Silymarin-albumin nanoplex: preparation and its potential application as an antioxidant in nervous system in vitro and in vivo
In this study, we formulated silymarin-HSA nanoplex and assayed its ability to reduce LPS-induced toxicity in vitro and in vivo. Silymarin molecules were encapsulated into HSA nanoplex and the loading efficiency and characterization of fabricated nanoplex were performed by using HPLC, TEM, SEM, DLS, FTIR analysis, and theoretical studies. Afterwards, their protective effect against LPS (20 µg/ml) -induced toxicity in SH-SY5Y cells was investigated by MTT, ROS, and apoptosis assays. For in vivo experiments, rats were pre-treated with either silymarin or silymarin -HSA nanoplex (200 mg/kg) orally for 3 days and at thir...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation and investigation of core-shell nanoparticles containing human interferon-α
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Katalin Kristó, Márta Szekeres, Zsolt Makai, Árpád Márki, András Kelemen, László Bali, Zsolt Pallai, Imre Dékány, Ildikó CsókaAbstractSustained release of active interferon-α (IFN-α) has been achieved from core-shell nanoparticles (NPs) prepared by aqueous precipitation of IFN-α-enriched human serum albumin (HSA-IFN-α) and layer-by-layer (L-b-L) by coating of the IFN-α NPs with poly(sodium-4-styrene) sulph...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Relationship between rheological properties, in vitro release and in vivo equivalency of topical formulations of diclofenac
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): María Pleguezuelos-Villa, Matilde Merino-Sanjuán, Mª Jesús Hernández, Amparo Nácher, Daniel Peris, Irene Hidalgo, Lluís Soler, Marta Sallan, Virginia MerinoAbstractDetermination of bioequivalence remains a challenge in generic topical drug development. To support pharmacokinetic studies, strategies to demonstrate microstructure sameness of the products being compared include in vitro evaluations, such as the comparison of rheological properties, droplet size and in vitro ...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Continuous Production of Celecoxib Nanoparticles Using a Three-Dimensional-Coaxial-Flow Microfluidic Platform
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Donghua Di, Xin Qu, Chao Liu, Liang Fang, Peng QuanAbstractIncreasing the dissolution rate of water insoluble drugs by decreasing the particle size of the drugs into nano-size is a well-known strategy. However, continuous production of drug nanoparticles with uniform particle size is critical for clinical application of the strategy. Here we report a simple microfluidic mixing method that can achieve continuous production of celecoxib nanoparticles with uniform particle size and high dissolution rate. A three-dimensio...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

In-situ forming implants for the treatment of periodontal diseases: Simultaneous controlled release of an antiseptic and an anti-inflammatory drug
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): M. Lizambard, T. Menu, M. Fossart, C. Bassand, K. Agossa, O. Huck, C. Neut, F. SiepmannAbstractDifferent types of in-situ forming implants based on poly(lactic-co-glycolic acid) (PLGA) for the controlled dual release of an antiseptic drug (chlorhexidine) and an anti-inflammatory drug (ibuprofen) were prepared and thoroughly characterized in vitro. N-methyl-pyrrolidone (NMP) was used as water-miscible solvent, acetyltributyl citrate (ATBC) as plasticizer and hydroxypropyl methylcellulose (HPMC) was added to enhance the...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Engineered Extracellular Vesicles with Synthetic Lipids via Membrane Fusion to Establish Efficient Gene Delivery
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Yong-Yu Jhan, Daniel Prasca-Chamorro, Guillermo Palou Zuniga, David Mitchell Moore, Shreedevi Arun Kumar, Akhilesh K. Gaharwar, Corey J. BishopAbstractThe low yield of extracellular vesicle (EV) secretion is a major obstacle for mass production and limits their potential for clinical applications as a drug delivery platform. Here, we mass produced engineered extracellular vesicles (eEVs) by fusing the surface composition of EVs with lipid-based materials via a membrane extrusion technique. A library of lipids (DOTAP, ...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro skin penetration enhancement techniques: a combined approach of ethosomes and microneedles
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): C. Bellefroid, A. Lechanteur, B. Evrard, D. Mottet, F. Debacq-Chainiaux, G. PielAbstractDermal administration of different macromolecules, such as nucleic acids, remains a real challenge because of the difficulty of crossing the main skin barrier, the stratum corneum (SC). To overcome this barrier, the use of deformable lipid-based nanovectors were developed to increase topical penetration through the SC and to promote the intercellular delivery of drugs. The purpose of this study is to compare the skin penetration of...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Solanesol Derived Therapeutic Carriers for Anticancer Drug Delivery
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Yao Xiong, Tian Hou, Lei Liu, Wanjia Peng, Chunyun Wang, Yan Lu, Shuaichao Wang, Jiahua Shi, Shiyong SongAbstractMetabolites of a large number of inert drug carriers can cause long-term exogenous biological toxicity. Therefore, carriers with simultaneous therapeutic effects may be a good choice for drug delivery. Herein, a series of pharmacologically active solanesol derivatives were synthesized and investigated for use as micellar drug carriers for cancer therapy. Solanesyl thiosalicylic acid (STS) was first synthesi...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Use of a quartz crystal microbalance platform to study protein adsorption on aluminum hydroxide vaccine adjuvants: focus on phosphate-hydroxide ligand exchanges
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Jean-François Art, Patrice Soumillion, Christine C. Dupont-GillainAbstractAluminum hydroxide (AH) salts are widely used as vaccine adjuvants and controlling antigen-AH interactions is a key challenge in vaccine formulation. In a previous work, we have developed a quartz crystal microbalance (QCM) platform, based on stable AH-coated sensors, to explore the mechanisms of model antigen adsorption. The QCM study of bovine serum albumin (BSA) adsorption at different pH and ionic strength (I) values showed that prote...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research

Experimental and topological determination of the pressure-temperature phase diagram of racemic etifoxine, a pharmaceutical ingredient with anxiolytic properties
Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): M. Barrio, H. Allouchi, J.-Ll. Tamarit, R. Ceolin, L. Berthon-Cédille, I.B. RietveldAbstractInformation about the solid-state properties of etifoxine has been lacking, even if the active pharmaceutical ingredient has been used for its anxiolytic properties for decennia. The crystal structure of the racemic compound possesses a monoclinic space group P21/n with cell parameters a = 8.489(2) Å, b = 17.674(2) Å, c = 20.883(3) Å, β = 98.860(10)° and a unit-cell volume of 3095.8(9) Å3...
Source: International Journal of Pharmaceutics - November 10, 2019 Category: Drugs & Pharmacology Source Type: research