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

Lipid- and polymer-based plexes as therapeutic carriers for bioactive molecules
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Pravin Shende, Narayan Ture, R.S. Gaud, F. TrottaAbstractRecently, promising strategies of plexes include the complexation of nucleic acids with lipids (lipoplexes) and different kinds of polymers (polyplexes) for delivery of actives and genetic material in abnormal conditions like cancer, cystic fibrosis and genetic disorders. The present review article focuses on the comparative aspects of lipoplexes and polyplexes associated with molecular structure, cellular transportation and formulation aspects. The major advant...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of pH of processing-medium on re-dispersion of spray dried, crystalline nanoparticles of pure naproxen
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Veronika Braig, Christoph Konnerth, Wolfgang Peukert, Geoffrey LeeAbstractCrystalline nanodispersions of naproxen stabilized with hydroxypropyl cellulose were prepared at different pHs both below and above the pKa of the drug. After spray drying together with lactose, the measured particle size of the rehydrated dispersions using laser light scattering/Mie analysis was found to depend strongly on the pH of the original, processed nanodispersion. The pH-dependent solubility of this weak acid resulted in formation of a ...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Tunable Sustained Release Drug Delivery System Based on Mononuclear Aqueous Core-Polymer Shell Microcapsules
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Samer R. Abulateefeh, Mahmoud Y. Alkawareek, Alaaldin M. AlkilanyAbstractPoly(D,L-lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) polymers were used successfully in the preparation of polymer shell microcapsules with mononuclear aqueous cores by the internal phase separation method. These microcapsules were prepared with varying amounts of polymer and water and loaded with fluorescein sodium as a model water soluble drug. Evaluation of drug loading and encapsulation efficiency reveals an optimum polymer to wa...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Dimensional analysis of in-situ crystal formation in droplet undergoing rapid dehydration
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): S. Shakiba, S. Mansouri, C. Selomulya, M.W. WooAbstractThe surface structure of the crystalline particles affects the functionality of the particles in drug delivery. Prediction of the final structure of particles that crystallize easily within the spray dryer is of interests of many applications. A theoretical framework was developed for the prediction of crystal structure precipitating on the surface of the particle. Mannitol was produced under different processing conditions in order to validate the theoretical mod...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of ice fog methods and monitoring of controlled nucleation success after freeze-drying
Publication date: 10 March 2019Source: International Journal of Pharmaceutics, Volume 558Author(s): Ilona Vollrath, Wolfgang Friess, Angelika Freitag, Andrea Hawe, Gerhard WinterAbstractImproving freeze-drying processes regarding drying time and batch homogeneity is subject of ongoing research work. In this context, controlled nucleation raised great expectations. However, practically we face some challenges, e.g. how to non-destructively monitor successfully performed controlled nucleation. The question if different controlled nucleation methods lead to comparable products, as not every method can easily be implemented in...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Albumin fusion improves the pharmacokinetics and in Vivo antitumor efficacy of canine interferon gamma
In this study, N- and C-terminal canine albumin fusions with canine IFN-γ were expressed in the baculovirus expression system. The fusion proteins stimulated Stat1 phosphorylation at levels similar to that of the recombinant IFN. The antiviral, anti-proliferative and promote apoptosis activity of CSA-IFN-γ was lower than IFN-γ-CSA and both were less than that of recombinant IFN-γ. In vivo pharmacokinetics demonstrated a significantly longer half-life for CSA-IFN-γ (21.73 h) than for IFN-γ-CSA (6.51 h) and canine reIFN-γ (2.22 h) in Wistar rats. CSA-IFN-γ was also more effecti...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of pH-responsive DOX-loaded chitosan nanoparticles using supercritical assisted atomization with an enhanced mixer
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Hu-Hong Peng, Dong-Xiao Hong, Yi-Xin Guan, Shan-Jing YaoAbstractChemotherapeutics are used extensively in cancer and encapsulating the drug in nanoparticles is an effective method to enhance therapeutic efficacy and reduce side effect. In this work, DOX-loaded chitosan nanoparticles were prepared using supercritical fluid assisted atomization introduced by a hydrodynamic cavitation mixer (SAA-HCM) from aqueous solution. The influences of solution concentration, CO2/solution ratio, mixer pressure, chitosan/DOX ratio and...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Immobilization of antimicrobial and anti-quorum sensing enzymes onto GMA-grafted poly(vinyl chloride) catheters
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Alejandro Costoya, Luis E. Velázquez Becerra, H. Iván Meléndez-Ortiz, Luis Díaz-Gómez, Celia Mayer, Ana Otero, Angel Concheiro, Emilio Bucio, Carmen Alvarez-LorenzoAbstractCatheter-associated infections still represent a challenging thread because of the likelihood of biofilm formation. The aim of this work was the surface modification of catheters to immobilize lysozyme and acylase under mild conditions while preserving antimicrobial and anti-quorum sensing performances. Glycidyl met...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

A Novel Antimicrobial Peptide-Derived Vehicle for Oligodeoxynucleotide Delivery to Inhibit TNF-α Expression
This study provides a useful strategy of peptide vehicle design, which may facilitate the delivery of not only ODN but also other oligonucleotides, including siRNA and miRNA, to promote gene silence application.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Smartphone-based Ellman’s colourimetric methods for the analysis of D-penicillamine formulation and thiolated polymer
In conclusion, smartphone-based colourimetry has been proved to be a reliable, fast, simple and affordable alternative means for the analysis of d-penicillamine and cysteine-conjugated polymer and can be potentially applied to other thiol-containing drugs and excipients.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of Dermal Tissue Regeneration Using Resveratrol Loaded Fibrous Matrix in a Preclinical Mouse Model of Full-Thickness Ischemic Wound
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Rajesh Lakhsmanan, Jacob Campbell, Gopi Ukani, André O'Reilly Beringhs, Vaithinathan Selvaraju, Mahesh Thirunavukkarasu, Xiuling Lu, J. Alexander Palesty, Nilanjana MaulikAbstractThe complete loss of dermal tissue due to ischemia is a serious challenge facing clinicians. Frequently, the failure of wound healing is due to ischemic conditions prevailing at the site of damaged tissue. Restoration of lost vasculature at the ischemic site can be achieved by supplementing proangiogenic stimuli through an engineered sc...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Assessment of Doxorubicin Delivery Devices based on tailored bare Polycaprolactone against Glioblastoma
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Enrique Niza, José A. Castro-Osma, Inmaculada Posadas, Carlos Alonso-Moreno, Iván Bravo, Andrés Garzón, Jesús Canales-Vázquez, Valentín Ceña, Agustín Lara-Sánchez, José Albaladejo, Antonio OteroAbstractBare polycaprolactones with controlled molar mass and dispersity were employed to manufacture biodegradable devices, which were applied for doxorubicin delivery in glioblastoma. Micro- and nanoscale devices were prepared by emulsion formation or...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Lipids and polymers in pharmaceutical technology: lifelong companions
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann, Amina Faham, Sophie-Dorothée Clas, Ben J. Boyd, Vincent Jannin, Andreas Bernkop-Schnürch, Hang Zhao, Sébastien Lecommandoux, James C. Evans, Christine Allen, Olivia M. Merkel, Gabriella Costabile, Morgan R. Alexander, Ricky D. Wildman, Clive J. Roberts, Jean-Christophe LerouxAbstractIn pharmaceutical technology, lipids and polymers are considered pillar excipients for the fabrication of most dosage forms, irrespective of the administration route. They play various roles ranging from...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

A Thermo-Responsive and Self-Healing Liposome-in-Hydrogel System as an Antitubercular Drug Carrier for Localized Bone Tuberculosis Therapy
Publication date: Available online 8 January 2019Source: International Journal of PharmaceuticsAuthor(s): Peng Liu, Binbin Guo, Shengfeng Wang, Jinsong Ding, Wenhu ZhouAbstractIsoniazid (INH) is a first-line therapy for bone tuberculosis (TB), but its clinic benefits are limited by severe side-effects after long-time administration. While nano-drug delivery systems present as promising strategies for INH delivery, the therapeutic efficacies are usually suboptimal due to ineffective drug accumulation at diseased sites. Local delivery system can achieve high drug concentration at focus sites with minimal systemic exposure, a...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Interpolymer complexes of Carbopol® 971 and poly(2-ethyl-2-oxazoline): physicochemical studies of complexation and formulations for oral drug delivery
Publication date: Available online 8 January 2019Source: International Journal of PharmaceuticsAuthor(s): Rouslan I. Moustafine, Anastasiya S. Viktorova, Vitaliy V. KhutoryanskiyAbstractCarbopol® 971 and poly(2-ethyl-2-oxazoline) form hydrogen-bonded interpolymer complexes in aqueous solutions and their complexation is strongly dependent on solution pH. This work investigated the complexation between these polymers in aqueous solutions. The compositions of interpolymer complexes as well as the critical pH values of complexation were determined. The structure of these complexes was studied in solutions using transmissio...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Mycobactericidal activity of some micro-encapsulated synthetic Host Defense peptides (HDP) by expediting the permeation of antibiotic: A new paradigm of drug delivery for tuberculosis
In this study, it was supposed that Host Defense peptides (HDP) which are known to permeabilize bacterial membranes may, therefore, help anti-TB antibiotics to target internal sites in bacteria. To test this hypothesis, we examined the effect of suboptimal concentration (10 µg/ml) of selected microencapsulated-HDP (Ub2-MS, K4-MS, and Aurein1.2-MS) with a standard anti-TB drug (Isoniazid, INH, 3 µg/ml). We also examined the combined effect of different concentrations of HDP-MS with a suboptimal concentration of anti-TB drug (INH, 1.5 µg/ml) which showed additive efficacy. A number of cationic HDP were enca...
Source: International Journal of Pharmaceutics - January 8, 2019 Category: Drugs & Pharmacology Source Type: research

Dual drug delivery from intraocular lens material for prophylaxis of endophthalmitis in cataract surgery
Publication date: Available online 7 January 2019Source: International Journal of PharmaceuticsAuthor(s): Ana Topete, A.P. Serro, B. SaramagoAbstractCataract is highly prevalent among old population worldwide and replacement of the opacified crystalline lens by an intraocular lens (IOL) is the safest and the most effective treatment. Although not very frequently (0.02-0.33% of the cases), the patients who undergo cataract surgery may develop endophthalmitis, which is a serious problem eventually leading to blindness. To avoid this complication, the postoperative instillation of antibiotics and anti-inflammatories is almost...
Source: International Journal of Pharmaceutics - January 7, 2019 Category: Drugs & Pharmacology Source Type: research

Advances in Orally-delivered pH-Sensitive Nanocarrier Systems; an Optimistic Approach for the Treatment of Inflammatory Bowel Disease
Publication date: Available online 4 January 2019Source: International Journal of PharmaceuticsAuthor(s): Mahira Zeeshan, Hussain Ali, Salman Khan, Saeed Ahmad Khan, Benno WeigmannAbstractInflammatory bowel disease (IBD) is the inflammation of the gastrointestinal tract (GIT) affecting the colon and ileum in particular. Increasing IBD prevalence worldwide is alarming, and needs to be resolved. Due to the limited therapeutic efficacy, accompanying adverse effects, dependence, and pharmacokinetics issues of the available therapy, IBD patients have compromised quality of life. Meanwhile, conventional drug delivery systems (DD...
Source: International Journal of Pharmaceutics - January 5, 2019 Category: Drugs & Pharmacology Source Type: research