Drug combination using an injectable nanomedicine hydrogel for glioblastoma treatment
Publication date: Available online 28 January 2019Source: International Journal of PharmaceuticsAuthor(s): Chiara Bastiancich, Elia Bozzato, Urszula Luyten, Fabienne Danhier, Guillaume Bastiat, Véronique PréatAbstractLauroyl-gemcitabine lipid nanocapsules (GemC12-LNC) hydrogel, administered intratumorally or perisurgically in the tumor resection cavity, increases animal survival in several orthotopic GBM models. We hypothesized that GemC12-LNC can be used as nanodelivery platform for other drugs, to obtain a combined local therapeutic approach for GBM. Paclitaxel (PTX) was selected as a model molecule and PTX...
Source: International Journal of Pharmaceutics - January 29, 2019 Category: Drugs & Pharmacology Source Type: research

Peptide release from SEDDS containing hydrophobic ion pair therapeutic peptides measured by Taylor dispersion analysis
In conclusion, this work demonstrates that TDA is a rapid, straightforward and useful technique for developing SEDDS formulations.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 29, 2019 Category: Drugs & Pharmacology Source Type: research

Advances of nanosystems containing cyclodextrins and their applications in pharmaceuticals
Publication date: Available online 29 January 2019Source: International Journal of PharmaceuticsAuthor(s): Paula dos Passos Menezes, Tatianny de Araújo Andrade, Luiza Abrahão Frank, Eloísa Portugal Barros Silva Soares de Souza, Gabriela das Graças Gomes Trindade, Igor Araújo Santos Trindade, Mairim Russo Serafini, Sílvia Stanisçuaski Guterres, Adriano Antunes de Souza AraújoAbstractFor many years, researchers have worked with supramolecular structures involving inclusion complexes with cyclodextrins. These studies have resulted in new commercially available drugs whic...
Source: International Journal of Pharmaceutics - January 29, 2019 Category: Drugs & Pharmacology Source Type: research

Hot-melt extrusion process impact on polymer choice of Glyburide solid dispersions: The effect of wettability and dissolution
Publication date: Available online 27 January 2019Source: International Journal of PharmaceuticsAuthor(s): Maen Alshafiee, Mohammad K. Aljammal, Daniel Markl, Adam Ward, Karl Walton, Liam Blunt, Sachin Korde, Sudhir K. Pagire, Adrian L. Kelly, Anant Paradkar, Barbara R. Conway, Kofi Asare-AddoAbstractThe aim of this study was to evaluate the choice of polymer and polymer level on the performance of the microstructure and wettability of hot-melt extruded solid dispersion of Glyburide (Gly) as a model drug. The produced solid dispersion were characterised using scanning electron microscopy (SEM), image analysis using a focus...
Source: International Journal of Pharmaceutics - January 28, 2019 Category: Drugs & Pharmacology Source Type: research

Saporin-loaded CD44 and EGFR dual-targeted nanogels for potent inhibition of metastatic breast cancer in vivo
Publication date: Available online 27 January 2019Source: International Journal of PharmaceuticsAuthor(s): Jing Chen, Hua He, Chao Deng, Lichen Yin, Zhiyuan ZhongAbstractMetastasis poses a long-standing treatment challenge for many cancers including breast cancer. Once spreading out, cell-selective delivery of drug appears especially critical. Here, we report on epidermal growth factor receptor and CD44 dual-targeted hyaluronic acid nanogels (EGFR/CD44-NGs) that afford enhanced targetability and protein therapy for metastatic 4T1 breast cancer in vivo. Flow cytometry in CD44 and EGFR-positive 4T1 metastatic breast cancer c...
Source: International Journal of Pharmaceutics - January 28, 2019 Category: Drugs & Pharmacology Source Type: research

A new melatonin oral delivery platform based on orodispersible films containing solid lipid microparticles
In conclusion, the proposed drug delivery system maintains the advantages of ODFs, i.e. the suitability to be swallowed without water, and permits the tuning of drug release according to the clinical needs by modulating the ratio of free and microencapsulated drug in the ODF.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 26, 2019 Category: Drugs & Pharmacology Source Type: research

Glycyrrhizic acid as a multifunctional drug carrier – from physicochemical properties to biomedical applications: a modern insight on the ancient drug
Publication date: Available online 25 January 2019Source: International Journal of PharmaceuticsAuthor(s): O.Yu. Selyutina, N.E. PolyakovAbstractGlycyrrhizic acid is the main active component of Licorice root which has been known in traditional Chinese and Japanese medicine since ancient times. In these cultures glycyrrhizic acid (GA) is one of the most frequently used drugs. However, only in 21-st century a novel unusual property of the GA to enhance the activity of other drugs has been discovered. The review describes briefly the experimental evidences of wide spectrum of own biological activities of glycyrrhizic acid as...
Source: International Journal of Pharmaceutics - January 26, 2019 Category: Drugs & Pharmacology Source Type: research

In Situ Thermo-co-Electroresponsive Mucogel for Controlled Release of Bioactive Agent
Publication date: Available online 26 January 2019Source: International Journal of PharmaceuticsAuthor(s): Olufemi D. Akilo, Pradeep Kumar, Yahya E. Choonara, Lisa C. du Toit, Priyamvada Pradeep, Girish Modi, Viness PillayAbstractThe purpose of this work was to develop an in situ thermosensitive electro-responsive mucoadhesive gel loaded with bioactive agent (nanocomposite) meant for nose to brain delivery in a controllable manner when electric stimulation is applied. Nanocomposite was developed using a combinatorial blending of chitosan, hydroxypropylmethylcellulose, pluronic F127 and polyaniline which was then loaded wit...
Source: International Journal of Pharmaceutics - January 26, 2019 Category: Drugs & Pharmacology Source Type: research

Vesicle-like structure of lipid-based nanoparticles as drug delivery system revealed by molecular dynamics simulations
Publication date: Available online 23 January 2019Source: International Journal of PharmaceuticsAuthor(s): Maryam Khalkhali, Sarah Mohammadinejad, Farhad Khoeini, Kobra RostamizadehAbstractLipid-based drug delivery systems are considered as promising vehicles for hydrophobic drug compounds. Lipid distribution within the droplet can affect drug loading capacity in these carriers. However, it is extremely challenging to determine the nanostructure within these carriers through the implementation of the direct experimental methods due to the ultrafine size. Therefore, coarse grained molecular dynamics (MD) simulation was util...
Source: International Journal of Pharmaceutics - January 24, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of levofloxacin polyethylene glycol decorated nanoliposomes for enhanced management of acute otitis media: Statistical optimization, trans-tympanic permeation and in-vivo evaluation
Publication date: Available online 23 January 2019Source: International Journal of PharmaceuticsAuthor(s): Aly A. Abdelbary, Wessam H. Abd-Elsalam, Abdulaziz M. Al-mahallawiAbstractAcute otitis media (AOM), an infection in the middle ear, is usually treated through systemic administration of antibiotics because the stratum corneum of the intact tympanic-membrane (TM) possesses low permeability that holds against the ototopical antibiotics use. Therefore, the objective of this work was to encapsulate levofloxacin (LFX) into polyethylene glycol 400 (PEG 400) decorated nanoliposomes (PNLs) as an approach for drug delivery thr...
Source: International Journal of Pharmaceutics - January 24, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro dissolution testing of respirable size anti-tubercular drug particles using a small volume dissolution apparatus
Publication date: Available online 23 January 2019Source: International Journal of PharmaceuticsAuthor(s): Basanth Babu Eedara, Ian G. Tucker, Shyamal C. DasAbstractA dissolution apparatus that uses a small volume of stationary medium (25 μL) has been developed for in vitro dissolution testing of respirable drug particles and used to evaluate the dissolution of two anti-tubercular drugs, moxifloxacin and ethionamide. Solubilities of moxifloxacin and ethionamide in phosphate buffered saline (PBS, pH 7.4) were 17.68 ± 0.85 mg mL-1 and 0.46 ± 0.02 mg mL-1 whereas in the presence of lung surfactant (0.4% w/v C...
Source: International Journal of Pharmaceutics - January 24, 2019 Category: Drugs & Pharmacology Source Type: research

Localized Drug Delivery with Mono and Bilayered Mucoadhesive Films and Wafers for Oral Mucosal Infections
In this study, monolayer and bilayered mucoadhesive film and wafer formulations were developed as local drug delivery platforms using chitosan and hydroxypropyl methycellulose (HPMC). Cefuroxime axetil (CA) was used as the model drug. Surface morphology, mechanical strength, water uptake, in vitro adhesion, disintegration and in vitro release properties of the formulations were investigated. Furthermore, antimicrobial activity of the formulations was evaluated against E.coli and S.aureus. HPMC based formulations were found to disintegrate within less than 30 min whereas chitosan based formulations remained intact...
Source: International Journal of Pharmaceutics - January 23, 2019 Category: Drugs & Pharmacology Source Type: research

Roller compaction: Ribbon splitting and sticking
Publication date: Available online 22 January 2019Source: International Journal of PharmaceuticsAuthor(s): Osama Mahmah, M.J. Adams, Chalak S.Omar, Bindhu Gururajan, Agba D. SalmanAbstractRoller compaction is the main technique employed in dry granulation. Ribbon sticking and splitting are among the major factors that can hinder the use of this process for some formulations. Ribbon splitting can occur either transversally (through the ribbon thickness) or longitudinally (through the ribbon width). It was observed that transverse splitting is commonly associated with sticking of the split ribbons to the rollers and results ...
Source: International Journal of Pharmaceutics - January 23, 2019 Category: Drugs & Pharmacology Source Type: research

Formulation And Comparison Of Spray Dried Non-Porous And Large Porous Particles Containing Meloxicam For Pulmonary Drug Delivery
Publication date: Available online 21 January 2019Source: International Journal of PharmaceuticsAuthor(s): Anita Chvatal, Rita Ambrus, Petra Party, Gábor Katona, Orsolya Jójárt-Laczkovich, Piroska Szabó-Révész, Elias Fattal, Nicolas TsapisAbstractMeloxicam is an anti-inflammatory drug that could be interesting to deliver locally to the lungs to treat inflammation occurring in cystic fibrosis or chronic obstructive pulmonary disease (COPD). Spray drying conditions were optimized to prepare inhalable dry powders, from meloxicam aqueous solution with pH adjustment. A comparison study ...
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

Efficient ovalbumin delivery using a novel multifunctional micellar platform for targeted melanoma immunotherapy
Publication date: Available online 21 January 2019Source: International Journal of PharmaceuticsAuthor(s): Muye He, Lei Huang, Xinyu Hou, Chen Zhong, Zaina Ait Bachir, Minbo Lan, Rongjun Chen, Feng GaoAbstractCancer immunotherapy is considered to be one of the alternatives to traditional chemotherapy. It’s known that foreign antigen, such as ovalbumin (OVA), can label tumor cells, leading to neoantigen recognition by cytotoxic T lymphocytes. Herein, a novel multifunctional micelle coated with PEGylated hyaluronic acid (HA) was prepared through self-assembly and electrostatic interaction. The OVA-loaded micelle with u...
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-tumor efficiency of gemcitabine prodrug by FAPα-mediated activation
Publication date: Available online 21 January 2019Source: International Journal of PharmaceuticsAuthor(s): Jing Sun, Dan Yang, Shi-He Cui, Hai-Tao Zhang, Yu Fu, Jian-Cheng Wang, Qiang ZhangAbstractGemcitabine (Gem) as an anti-cancer agent has been limited by its short circulation time and rapid metabolism that reflects in low tumor uptake and low therapeutic efficiency. To improve its anti-tumor activity, a novel FAPα enzyme-activated prodrug of Z-GP-Gem modified at 4-amino group of Gem was developed, which could effectively release parent Gem based on the specific cleavage via FAPα enzyme-activation in tumor m...
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

Updates on Thermosensitive Hydrogel for Nasal, Ocular and Cutaneous Delivery
Publication date: Available online 21 January 2019Source: International Journal of PharmaceuticsAuthor(s): Qianwen Wang, Zhong Zuo, Cheuk Kit Chucky Cheung, Sharon Shui Yee LeungAbstractThermosensitive hydrogels are in situ gelling systems composed of hydrophilic homopolymers or block copolymers which remain as solutions at room temperature and form gels after administration into the body. Its application in advanced drug delivery has gained significant attention in recent years. The tunable characteristics of thermosensitive hydrogels make them versatile and capable of incorporating both hydrophilic and lipophilic compoun...
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

A Comparative Study of Polydopamine Modified and Conventional Chemical Synthesis Method in Doxorubicin Liposomes form the Aspect of Tumor Targeted Therapy
This study demonstrated the PDA method could achieve therapeutic levels similar to traditional methods in a simpler and safer way, which can be useful and promising nanocarriers for drug delivery system in the future.Graphical abstractSchematic representation of the preparation of PDA coated DOX liposomes. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

A large-scale experimental comparison of batch and continuous technologies in pharmaceutical tablet manufacturing using ethenzamide
Publication date: Available online 22 January 2019Source: International Journal of PharmaceuticsAuthor(s): Kensaku Matsunami, Takuya Nagato, Koji Hasegawa, Hirokazu SugiyamaAbstractThis paper compares batch and continuous technologies in terms of product quality and process performance in pharmaceutical tablet manufacturing using ethenzamide as the active pharmaceutical ingredient. Batch and continuous processes using wet granulation were investigated by performing experiments on the scale of 5 and up to 100 kg/lot, using the same raw materials. Three technologies were tested and compared: (i) batch technology using fluidi...
Source: International Journal of Pharmaceutics - January 22, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of multifunctional Janus nanoparticles on the basis of SPIONs as targeted drug delivery system
In this study, multifunctional amphiphilic Janus nanoparticles have been prepared on the basis of superparamagnetic iron oxide nanoparticles. This Janus platform is armed with folic acid targeting agent and Doxorubicin (DOX) drug that have been conjugated on different sides of the nanoparticles. DOX has been conjugated via imine bond that makes these particles pH sensitive. Chemo-physical characters, in-vitro drug release pattern and toxicity of nanoparticles on rat C6 glioma cell line were studied that confirmed the preparation and pH-dependent behavior of nanoparticles. Microscopy observations showed the Janus morphology...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Controlled release of methotrexate from functionalized silica-gelatin aerogel microparticles applied against tumor cell growth
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Gábor Nagy, Gábor Király, Péter Veres, István Lázár, István Fábián, Gáspár Bánfalvi, István Juhász, József KalmárAbstractMethotrexate functionalized silica-gelatin hybrid aerogel (SGM) was synthesized by the sol-gel method and co-gelation. The drug methotrexate (MTX) is covalently linked to the collagen molecules of the hybrid aerogel backbone by amide-bond. The characteristic MTX content of the funct...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

The innovation ecosystem: an analysis of a decade of approved and failed drugs
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Xiong Liu, Craig E. Thomas, Christian C. FelderAbstractPharmaceutical companies are relying more often on external sources of innovation to boost their discovery research productivity. However, more in-depth knowledge about how external innovation may translate to successful product launches is still required in order to better understand how to best leverage the innovation ecosystem. We analyzed the pre-approval publication histories for FDA-approved new molecular entities (NMEs) and new biologic entities (NBEs) laun...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Improving dermal delivery of hydrophilic macromolecules by biocompatible ionic liquid based on choline and malic acid
In conclusion, CM-IL could be potentially used as enhancers or vehicles for dermal delivery of hydrophilic macromolecules.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Continuous, one-step synthesis of pharmaceutical cocrystals via hot melt extrusion from neat to matrix-assisted processing - state of the art
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Maciej Gajda, Karol P. Nartowski, Janusz Pluta, Bożena KarolewiczAbstractUse of hot melt extrusion (HME) as continuous manufacturing process in the cocrystal synthesis is of increasing interest from both industrial and academic perspective and it is seen as a newly developing branch of mechanochemistry with possible broad application in single step synthesis and formulation of pharmaceutical cocrystals. Furthermore, one-step formulation of pharmaceutical products results in combined processing of pharmaceutical cocry...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Development of iron(II) sulfate nanoparticles produced by hot-melt extrusion and their therapeutic potentials for colon cancer
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Ja Seong Koo, Song Yi Lee, Md Obyedul Kalam Azad, Minju Kim, Sung Jun Hwang, Suyeong Nam, Sungyun Kim, Byung-Jo Chae, Wie-Soo Kang, Hyun-Jong ChoAbstractParticle size reduction of FeSO4 (iron(II) sulfate, IS) from micron to nano size was achieved by a combination of hot-melt extrusion (HME) processing and the input of Span 80, Tween 80, and poly(ethylene glycol) (PEG) 6000. Conveying, kneading, and extruding steps of the HME process and a decrease in the surface tension by surfactants were introduced to produce FeSO4 ...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Combination of Hyaluronic Acid and PLGA Particles as Hybrid Systems for Viscosupplementation in Osteoarthritis
This study showed that empty PLGA particles presented a mean size of 373 nm, while particles containing HA and oleic acid showed a marked particle size increase. The HA association efficiency was of 73.6% and 86.2% for PLGA particles without and with oleic acid, respectively. The in vitro HA release from PLGA particles revealed a sustained profile. Particles showed a good in vitro cell compatibility and the risk of hemolysis was less
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

A review on 5-aminosalicylic acid colon-targeted oral drug delivery systems
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Hossein Shahdadi Sardo, Farinaz Saremnejad, Sara Bagheri, Abbas Akhgari, Hadi Afrasiabi Garekani, Fatemeh SadeghiAbstractSite-specific colon drug delivery is a practical approach for the treatment of local diseases of the colon with several advantages such as rapid onset of action and reduction of the dosage of the drug as well as minimization of harmful side effects. 5-aminosalicylic acid (5-ASA) is a drug of choice in the treatment of inflammatory bowel disease and colitis. For the efficient delivery of this drug, i...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Test Models for the Evaluation of Immunogenicity of Protein Aggregates
Publication date: Available online 18 January 2019Source: International Journal of PharmaceuticsAuthor(s): Teresa Kraus, Gerhard Winter, Julia EngertAbstractProtein aggregates have been discussed for a long time as a potential risk factor for immunogenicity in patients. Meanwhile, many research groups have investigated the immunogenicity of differently produced aggregates using in vitro or in vivo models. Despite all knowledge gained in these studies still little is known about the mechanisms of immunogenicity and the kind of protein aggregates bearing the greatest risk for immunogenicity. The choice of a suitable test mod...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of flow pattern, device and formulation on particle size distribution of nebulized aerosol
In this study, the aerosol concentration and particle size distribution (PSD) were measured under a realistic breathing pattern and constant flow. Two types of nebulizer (i.e., breath-enhanced nebulizer and vibrating-mesh nebulizer) and two formulations (i.e., budesonide suspension and albuterol solution) were chosen for comparison. The aerosol concentration under the realistic pattern was not constant, which was different from the result at constant flow. The changing trend of aerosol concentration varied with the operation process of each device. The aerosol concentration profile was similar between budesonide suspension...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Silver Nanoparticle Impregnated Chitosan-PEG Hydrogel Enhances Wound Healing in Diabetes induced Rabbits
Publication date: Available online 19 January 2019Source: International Journal of PharmaceuticsAuthor(s): Nosheen Masood, Rashid Ahmed, Muhammad Tariq, Zahoor Ahmed, Muhammad Shareef Masoud, Imran Ali, Rehana Asghar, Anisa Andleeb, Anwarul HasanAbstractNon-healing wounds are among the serious complications of type-2-diabetes around the globe, associated with high incidence of bacterial infection, chronic nerve and blood vessel damage, and eventually repeated amputation of limbs and organs. Silver nanoparticles offer strong wound healing potential due to their well-known antibacterial activities. The present study reports ...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanical testing methods for drug-releasing vaginal rings
Publication date: Available online 19 January 2019Source: International Journal of PharmaceuticsAuthor(s): Clare F. McCoy, Bronagh G. Millar, Diarmaid J. Murphy, Wendy Blanda, Bashir Hansraj, Brid Devlin, R. Karl Malcolm, Peter BoydAbstractVaginal rings (VRs) are currently marketed for contraceptive or hormone regulation purposes, and investigationally, have been widely reported for delivery of antiretrovirals to reduce HIV transmission. To date, there is no national or international standard for the mechanical testing and minimum performance characteristics of any VR based products. Here, we describe a a series of mechani...
Source: International Journal of Pharmaceutics - January 20, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of Thermal Binders on Chemical Stabilities and Tabletability of Gabapentin Granules Prepared by Twin-Screw Melt Granulation
Publication date: Available online 17 January 2019Source: International Journal of PharmaceuticsAuthor(s): Nada Kittikunakorn, John J Koleng, Tony Listro, Changquan Calvin Sun, Feng ZhangAbstractThe effect of thermal binders on the physicochemical properties of gabapentin, a thermally labile drug, in granules prepared using twin-screw melt granulation was investigated in this study. Hydroxypropyl cellulose (HPC), a thermoplastic high molecular-weight binder, was compared against conventional low molecular-weight semi-crystalline thermal binders PEG 8000 and Compritol. Both the chemical degradation and polymorph form change...
Source: International Journal of Pharmaceutics - January 18, 2019 Category: Drugs & Pharmacology Source Type: research

Cardiovascular therapies utilizing targeted delivery of nanomedicines and aptamers
This article categorically provides an overview of nanoparticle-mediated targeted delivery systems and their implications in handling cardiovascular diseases, including their intrinsic benefits and encountered procedural trials and challenges. Additionally, the solicitations of aptamers in targeted drug delivery with identical objectives, are presented. This includes a detailed appraisal on various aptamer-navigated nanoparticle targeted delivery platforms in the diagnosis and treatment of cardiovascular maladies. Despite a few impending challenges, subject to additional investigations, both nanoparticles as well as aptame...
Source: International Journal of Pharmaceutics - January 18, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of fused-filament fabrication to direct compression and injection molding in the manufacture of oral tablets
This study aimed to compare three manufacturing processes in the production of flat-faced oral tablets using the same formulation composed of a polymer blend and caffeine as a model drug: fused-filament fabrication (FFF), direct compression (DC) and injection molding (IM). Hot-melt extrusion was used to convert a powder blend into feedstock material for FFF and IM processes, while DC was performed on the powder mixture. Tablets were produced with the same dimensions and were characterised for their physical and dissolution properties. There were statistical differences in the physical properties and drug release profiles o...
Source: International Journal of Pharmaceutics - January 17, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro characterization of physico-chemical properties, cytotoxicity, bioactivity of urea-crosslinked hyaluronic acid and sodium ascorbyl phosphate nasal powder formulation
In conclusion, these results suggest that HA–CL and SAP had anti-inflammatory activity and acted in combination to accelerate wound healing. Therefore, LYO HA–CL – SAP could be a potential adjuvant in nasal anti-inflammatory formulations.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 17, 2019 Category: Drugs & Pharmacology Source Type: research

Building a Better Particle: Leveraging Physicochemical Understanding of Amorphous Solid Dispersions and a Hierarchical Particle Approach for Improved Delivery at High Drug Loadings
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Luke Schenck, Amanda Mann, Zhen Liu, Mikolaj Milewski, Siwei Zhang, Jie Ren, Kristel Dewitt, Andre Hermans, Aaron CoteGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

In-situ dissolution and permeation studies of nanocrystal formulations with second-derivative UV spectroscopy
In this study, in-situ dissolution-permeation studies of a nanosuspension of mefenamic acid (MFA) were carried out using second-derivative UV spectroscopy. This method enabled us to distinguish between the concentrations of dissolved MFA and nano-suspended MFA via in-situ measurement and showed an improved dissolution rate of the nanosuspension compared to that of the microsuspension. The dissolution-permeation study with second-derivative UV spectroscopy revealed that the improved dissolution rate due to nanosized MFA resulted in an increase in the permeated amount of MFA. In addition, the solubility of MFA determined by ...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Improved histidinylated lPEI polyplexes for skeletal muscle cells transfection
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Jean-Pierre Gomez, Guillaume Tresset, Chantal Pichon, Patrick MidouxAbstractLinear Polyethylenimine (lPEI) is an efficient cationic polymer for transfecting cells, both in vitro and in vivo, but poses concerns regarding cytotoxicity. Histidinylated lPEI (His-lPEI) exhibits also high transfection efficiency but lower cytotoxicity than lPEI. For the first time, we tested polyfection efficiency of polyplexes comprising both lPEI and His-lPEI. A series of pDNA polyplexes was prepared with mixtures of lPEI and His-lPEI and...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of microporous inorganic microneedles by centrifugal casting method for transdermal extraction and delivery
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Samira Gholami, Mohammad-Masoud Mohebi, Ensiyeh Hajizadeh-Saffar, Mohammad-Hossein Ghanian, Ibrahim Zarkesh, Hossein BaharvandAbstractMicroneedle patches have been widely used as transdermal transport systems because of their painless and easy application. Marked rigidity, strength, biocompatibility, and physiological stability are unique features of microneedles fabricated from ceramic materials to be used as microneedle patches. However, the conventional ceramic microneedles are typically dense structures with limit...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Preclinical Studies of Ropivacaine Extended-Release from a Temperature Responsive Hydrogel for Prolonged Relief of Pain at Surgical Wound
In this study, a series of experiments were conducted using rats to investigate the pharmacokinetic, distribution, and efficacy of a temperature responsive hydrogel based drug delivery device (PF-72) containing ropivacaine (0.75%) for extended relief of postoperative pain by allowing prolonged release of ropivacaine. When the ropivacaine was administered using PF-72, its concentration-time curve (AUClast) and peak concentration (Cmax) were 577.0 hr*ng/mL and 271.9 ng/mL, respectively. In contrast when the ropivacaine solution was administered using saline solution, its AUClast and Cmax were 982.8 hr*ng/mL and 423.6 ng/mL, ...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Development of nobiletin–methyl hesperidin amorphous solid dispersion: novel application of methyl hesperidin as an excipient for hot-melt extrusion
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Masazumi Iwashita, Kohjiro Hashizume, Masahiro Umehara, Takaaki Ishigami, Shintaro Onishi, Masaki Yamamoto, Kenjirou Higashi, Kunikazu MoribeAbstractA novel amorphous solid dispersion (ASD) of poorly water-soluble nobiletin (Nob) with highly water-soluble methyl hesperidin (MeHes) was developed. Mixtures of Nob and excipients (MeHes, cellulose derivatives, and synthetic polymers) were processed by hot-melt extrusion (HME). Powder X-ray diffraction analysis proved that most of the HME products were fully amorphized. In...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Exhausting tumor associated macrophages with sialic acid-polyethyleneimine-cholesterol modified liposomal doxorubicin for enhancing sarcoma chemotherapy
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Huangliang Zheng, Jiaqi Li, Mengjing Wang, Xiang Luo, Qiujun Qiu, Ling Hu, Cong LI, Yanzhi Song, Yihui DengAbstractTo overstep the dilemma of chemical drug degradation within powerful lysosomes of tumor associated macrophages (TAMs), a sialic acid-polyethylenimine-cholesterol (SA-PEI-CH) modified liposomal doxorubicin (DOX-SPCL) was designed with both TAMs targeting and smart lysosomal trafficking. The modified liposome DOX-SPCL performed particle size as 103.2 ± 3.1 nm and zeta potential as -4.5 ± 0.9 m...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Reliability of the Hansen Solubility Parameters as Co-Crystal Formation Prediction Tool
Publication date: Available online 14 January 2019Source: International Journal of PharmaceuticsAuthor(s): Ala' Salem, Sándor Nagy, Szilárd Pál, Aleksandar SzéchenyiAbstractPharmaceutical co-crystals present an opportunity to improve the solubility of conventional active pharmaceutical ingredients (APIs). Despite advances in co-crystal screening, the rational design of even the chemically simplest co-crystals remains challenging. Hansen solubility parameters (HSPs) have previously been used as a tool to predict co-crystal formation using only the chemical structure. The aim of this study was to ...
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

In Silico study of patient-specific magnetic drug targeting for a coronary LAD atherosclerotic plaque
In conclusion, the external magnetic field has increased the SDP adhered on the targeted surface by 49.4% and 59.7% for 400 and 600 nm particles, respectively.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 15, 2019 Category: Drugs & Pharmacology Source Type: research

Nanodiamonds: minuscule gems that ferry antineoplastic drugs to resistant tumors
Publication date: Available online 11 January 2019Source: International Journal of PharmaceuticsAuthor(s): Moustafa S. Ali, Abdelkader A. Metwally, Rania H. Fahmy, Rihab OsmanAbstractRemarkable efforts are currently devoted to the area of nanodiamonds (NDs) research due to their superior properties viz: biocompatibility, minute size, inert core, and tunable surface chemistry. The use of NDs for the delivery of anticancer drugs has been at the forefront of NDs applications owing to their ability to increase chemosensitivity, sustain drug release, and minimize drug side effects. Accelerated steps towards the move of NDs from...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Double controlled release of highly insoluble cilostazol using surfactant-driven pH dependent and pH-independent polymeric blends and in vivo bioavailability in beagle dogs
Publication date: Available online 11 January 2019Source: International Journal of PharmaceuticsAuthor(s): Kyu-Yeol Nam, Sang Min Cho, Youn-Woong Choi, Chulhun Park, Nileshkumar M. Meghani, Jun-Bom Park, Beom-Jin LeeAbstractCommercially available cilostazol (CIL) tablet releases drug immediately and is given twice a day as an antiplatelet and vasodilatory agent. However, clinical usefulness of immediate release (IR) preparation is limited due to its extremely poor water solubility and the difficulty in sustaining the blood concentration, resulting in unwanted side effects such as headaches, pyknocardia and heavy-headed sym...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

In the triple-negative breast cancer MDA-MB-231 cell line, sulforaphane enhances the intracellular accumulation and anticancer action of doxorubicin encapsulated in liposomes
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Lidia Mielczarek, Pamela Krug, Maciej Mazur, Małgorzata Milczarek, Zdzisław Chilmonczyk, Katarzyna WiktorskaAbstractA new combination of sulforaphane (a natural compound obtained from Brassicaceae vegetables) and the cytostatic drug doxorubicin was entrapped in nanometer-sized liposomes. In vitro experiments were performed to investigate the cytotoxicity of these structures on the human breast cancer cell line MDA-MB-231. Confocal microscopy studies revealed enhanced cellular endocytotic internalization, followed by...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

In situ co-amorphisation in coated tablets – the combination of carvedilol with aspartic acid during immersion in an acidic medium
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Ina Petry, Korbinian Löbmann, Holger Grohganz, Thomas Rades, Claudia S. LeopoldAbstractIn the present study the feasibility of an in situ co-amorphisation of the basic drug carvedilol with the acidic co-former aspartic acid was investigated by immersion of film-coated tablets consisting of the two compounds in 0.1 M HCl. Tablets containing either crystalline carvedilol with aspartic acid or only crystalline carvedilol were prepared and coated with a gastro-resistant but water-permeable coating of a meth...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

In silico predictions of tablet density using a quantitative structure–property relationship model
This study indicates that a QSPR approach is possibly useful for in silico prediction of tablet density for tablets prepared using more than a threshold compression pressure, and to allow a deeper understanding of tablet density.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Delivery of Novel Vancomycin Nanoplexes for Combating Methicillin Resistant staphylococcus aureus (MRSA) Infections
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Daniel Hassan, Calvin A. Omolo, Ramesh Gannimani, Ayman Y. Waddad, Chunderika Mocktar, Sanjeev Rambharose, Nikhil Agrawal, Thirumala GovenderAbstractThe development of novel antibiotic systems is needed to address the methicillin-resistant Staphylococcus aureus (MRSA) infections. The aim of the study was to explore the novel nanoplex delivery method for vancomycin (VCM) against MRSA using dextran sulfate sodium salt (DXT) as a polyelectrolyte complexing agent. Nanoplexes were formulated by the self-assembling amphiphi...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research