Dual-effect liposomes with increased antitumor effects against 67-kDa laminin receptor-overexpressing tumor cells
In conclusion, EPL appear to have superior antitumor activity against high 67LR-expressing tumor cells, as the liposomes had dual effects, namely antitumor effects due to the loaded DOX and apoptosis induced by the bound EGCG. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 28, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of a semi-batch tablet coating process for a continuous manufacturing line by design of experiments
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Shirin Barimani, Rok Šibanc, Peter Kleinebudde The aim of the study was to optimize a tablet coating process for a continuous manufacturing line. High throughputs should be achieved while inter-tablet coating variability should be as small as possible. Drug-free cores were coated with a colored suspension. All processes were monitored in-line with Raman spectroscopy. A statistical design of experiment was performed to find optimum process parameters. Tablet loading, spray rate and drum rotation spe...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro stabilization and in vivo improvement of ocular pharmacokinetics of the multi-therapeutic agent baicalin: Delineating the most suitable vesicular systems
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Orchid Ashraf, Maha Nasr, Marianne Nebsen, Azza Mohamed Ahmed Said, Omaima Sammour Baicalin is a multi-purpose flavonoid used in the treatment of different ocular diseases. Owing to its poor stability in basic pH and its poor solubility, a suitable carrier system is needed to enhance its ocular therapeutic potential. Therefore, the objective of this work was to prepare and contrast different baicalin vesicular systems; namely liposomes, penetration enhancer vesicles PEVs and transfersomes. Results reveale...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Quantitative estimation of phenytoin sodium disproportionation in the formulations using vibration spectroscopies and multivariate methodologies
In conclusion, chemometric models based on NIR and Raman spectroscopies provides a fast and easy way to monitor the disproportionation of PS in the drug products. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Membrane properties for permeability testing: Skin versus synthetic membranes
In this study, the permeability of human skin was compared using two synthetic membranes: cellulose acetate and Strat-M® membrane and lipophilic and hydrophilic compounds either as saturated or formulated solutions as well as marketed dosage forms. Our data suggests that hydrophilic compounds have higher permeation in Strat-M membranes compared with lipophilic ones. High variation in permeability values, a typical property of biological membranes, was not observed with Strat-M. In addition, the permeability of Strat-M was closer to that of human skin than that of cellulose acetate (CA > Strat-M > ...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Statistical Design of Experiment (DoE) based development and optimization of DB213 in situ thermosensitive gel for intranasal delivery
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Qianwen Wang, Chun-Ho Wong, H.Y. Edwin Chan, Wai-Yip Lee, Zhong Zuo DB213 is an HIV-1 replication inhibitor targeting the Central Nervous System for the treatment of HIV-associated neurocognitive disorders. Current study aims to develop an in situ thermosensitive gelling system for intranasal delivery of DB213 facilitated by Statistical Design of Experiment (DoE) to conduct a more efficient experimentation by extracting the maximum amount of information from limited experiments. In our current study, info...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

When drugs plasticize film coatings: Unusual formulation effects observed with metoprolol and Eudragit RS
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Youness Karrout, Florence Siepmann, Youcef Benzine, Laurent Paccou, Yannick Guinet, Alain Hedoux, Juergen Siepmann Metoprolol tartrate and metoprolol free base loaded pellet starter cores were coated with Eudragit RS, plasticized with 25% triethyl citrate (TEC). The initial drug loading and coating level were varied from 10 to 40 and 0 to 20%, respectively. Drug release was measured in 0.1 N HCl and phosphate buffer pH 7.4. The water uptake and swelling kinetics, mechanical properties and TEC leaching o...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Mechanochemical effect on swelling and drug release of natural polymer matrix tablets by X-ray computed tomography
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Yusuke Hattori, Tomomi Takaku, Makoto Otsuka The relationships between the physicochemical properties of milled starch and drug release from tablets were investigated quantitatively using a drug release kinetic method and X-ray computed tomography (XCT). The samples were prepared from raw β-starch by milling in a planetary ball mill. The tablets, containing 5% theophylline (TH), 94% milled starch, and 1% magnesium stearate, were compressed at 6 kN. The drug-release and gel-forming processes were me...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of surfactant-based permeation enhancers on mannitol permeability, histology, and electrogenic ion transport responses in excised rat colonic mucosae
This study examined the interaction of a test panel of surfactant-based PEs with isolated rat colonic mucosae mounted in Ussing chambers in an attempt to determine if increases in transepithelial permeability can be separated from induction of mucosal perturbation. The aim was to assess the effects of PEs on (i) apparent permeability coefficient (Papp) of [14C]-mannitol (ii) histology score and (iii) short-circuit current (ΔIsc) responses to a cholinomimetic (carbachol, CCh). Enhancement ratio increases for Papp values followed the order: C10 > C9 = C11:1 > a bile salt blend > sod...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

The relevance of shear, sedimentation and diffusion during spin freezing, as potential first step of a continuous freeze-drying process for unit doses
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Joris Lammens, Séverine Thérèse F.C. Mortier, Laurens De Meyer, Brecht Vanbillemont, Pieter-Jan Van Bockstal, Simon Van Herck, Jos Corver, Ingmar Nopens, Valérie Vanhoorne, Bruno G. De Geest, Thomas De Beer, Chris Vervaet Recently, a continuous freeze-drying process for the production of unit doses was presented and evaluated. In this concept, the freezing step is modified compared to traditional batch freeze-drying, as glass vials filled with a liquid formulation, are rotated ...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Inorganic nanoparticles: A potential cancer therapy for human welfare
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Arivalagan Pugazhendhi, Thomas Nesakumar Jebakumar Immanuel Edison, Indira Karuppusamy, Brindhadevi Kathirvel Cancer is an abnormal condition leading to uncontrolled cell division which causes damage to the body tissues. Around 100 types of cancer are studied so far namely breast cancer, lung cancer, skin cancer, prostate cancer, colon cancer and lymphoma. Major cancer therapies include chemotherapy, surgery and radiations but their major drawbacks are non-specifically distributed antitumor agents, uneven...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Interdependence of particle properties and bulk powder behavior of indomethacin in quench-cooled molten two-phase solid dispersions
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Kristian Semjonov, Maia Salm, Tiina Lipiäinen, Karin Kogermann, Andres Lust, Ivo Laidmäe, Osmo Antikainen, Clare J. Strachan, Henrik Ehlers, Jouko Yliruusi, Jyrki Heinämäki Solid dispersions (SDs) hold a proven potential in formulating poorly water-soluble drugs. The present paper investigates the interfacial phenomena associated with the bulk powder flow, water sorption, wetting and dissolution of the SDs prepared by a modified melt and quench-cooling (QC) method. Poorly water-soluble...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Buccal drug delivery technologies for patient-centred treatment of radiation-induced xerostomia (dry mouth)
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Osamah S. Malallah, Cristina M. Aller Garcia, Gordon B. Proctor, Ben Forbes, Paul G. Royall Radiotherapy is a life-saving treatment for head and neck cancers, but almost 100% of patients develop dry mouth (xerostomia) because of radiation-induced damage to their salivary glands. Patients with xerostomia suffer symptoms that severely affect their health as well as physical, social and emotional aspects of their life. The current management of xerostomia is the application of saliva substitutes or systemic ...
Source: International Journal of Pharmaceutics - February 25, 2018 Category: Drugs & Pharmacology Source Type: research

Relationships between surface coverage ratio and powder mechanics of binary adhesive mixtures for dry powder inhalers
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Jonas Rudén, Göran Frenning, Tobias Bramer, Kyrre Thalberg, Göran Alderborn The aim of this paper was to study relationships between the content of fine particles and the powder mechanics of binary adhesive mixtures and link these relationships to the blend state. Mixtures with increasing amounts of fine particles (increasing surface coverage ratios (SCR)) were prepared using Lactopress SD as carrier and micro particles of lactose as fines (2.7 µm). Indicators of unsettled bulk de...
Source: International Journal of Pharmaceutics - February 24, 2018 Category: Drugs & Pharmacology Source Type: research

The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Jeroen Van Renterghem, Heleen Dhondt, Glenn Verstraete, Michiel De Bruyne, Chris Vervaet, Thomas De Beer It was the aim of this study to elucidate the impact of the injection mold temperature upon the polymer crystallinity, its microstructure and the resulting drug release from immediate and sustained release tablets containing semi-crystalline polymers. The immediate release formulation contained 20% (w/w) ketoprofen (KETO) in poly (ethylene oxide) (PEO) and the sustained release formulation contained 20...
Source: International Journal of Pharmaceutics - February 24, 2018 Category: Drugs & Pharmacology Source Type: research

Physico-chemical properties of aqueous drug solutions: From the basic thermodynamics to the advanced experimental and simulation results
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Barbara Bellich, Amelia Gamini, John W. Brady, Attilio Cesàro The physical chemical properties of aqueous solutions of model compounds are illustrated in relation to hydration and solubility issues by using three perspectives: thermodynamic, spectroscopic and molecular dynamics simulations. The thermodynamic survey of the fundamental backgrounds of concentration dependence and experimental solubility results show some peculiar behavior of aqueous solutions with several types of similar solutes. Seco...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

The development of progesterone-loaded nanofibers using pressurized gyration: A novel approach to vaginal delivery for the prevention of pre-term birth
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Francis Brako, Bahijja Tolulope Raimi-Abraham, Suntharavathanan Mahalingam, Duncan Q.M. Craig, Mohan Edirisinghe Recent evidence has continued to support the applicability of progesterone in preventing preterm birth, hence the development of an appropriate vaginal delivery system for this drug would be of considerable interest. Here, we describe the development of progesterone-loaded bioadhesive nanofibers using pressurized gyration for potential incorporation into a vaginal insert, with a particular view ...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Stable and sustained release liposomal formulations of celecoxib: In vitro and in vivo anti-tumor evaluation
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): M. Matbou Riahi, A. Sahebkar, K. Sadri, S. Nikoofal-Sahlabadi, M.R. Jaafari Celecoxib (CLX) is a selective COX-2 inhibitor with anticancer potential in a COX-2 dependent and independent manner. CLX’s low water solubility has a dose limiting effect on its utilization in cancer treatment. Here, we developed liposomal drug delivery systems to allow a systemic administration and increase tumor accumulation of CLX based on the enhanced permeability and retention (EPR) mechanism. Nine liposomal formulation...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

A novel dexamethasone-loaded liposome alleviates rheumatoid arthritis in rats
In this study, an inflammation-targeted delivery system based on a liposomal carrier was developed to deliver hydrophobic dexamethasone against arthritis. Using two FDA-approved excipients for intravenous injection, dexamethasone loaded liposome (Dex-Lip) was prepared by a thin-film hydration method. The biodistribution of 1,1’-dioctadecyl-3,3,3’,3’-tetramethylindodicarbocyanine-loaded liposomes (DiD-Lips) were performed in rats with adjuvant-induced arthritis and demonstrated specific targeting efficacy in the disease site. DiD-Lips showed prolonged retention time in the inflammatory joint tissues compar...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Effective light-triggered contents release from helper lipid-incorporated liposomes co-encapsulating gemcitabine and a water-soluble photosensitizer
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Toshiki Fuse, Tatsuaki Tagami, Masafumi Tane, Tetsuya Ozeki Triggered drug release is a promising strategy for delivering anticancer drugs to cancer cells and tissues. We found that liposomes co-encapsulating calcein (a water-soluble model drug and fluorescence marker) and talaporfin sodium (TPS, a water-soluble photosensitizer) released the drug upon irradiation with a near-infrared (NIR)-laser. The liposomes were composed of phospholipid (DSPC)/helper lipid (DOPE)/cholesterol/PEG-lipid (PEG2000-DSPE) at ...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalization of nanodiamond with vitamin E TPGS to facilitate oral absorption of curcumin
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Bingchao Cheng, Hao Pan, Dandan Liu, Dongyang Li, Jinyu Li, Shihui Yu, Guoxin Tan, Weisan Pan The purpose of this work was to develop a d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) decorated nanodiamond (ND) system loading water-insoluble curcumin (ND/CUR/TPGS) to improve the colloidal dispersity and oral bioavailability of the preparation. CUR was physically loaded into ND clusters, then TPGS was coated to the ND/CUR complex forming amorphous nanostructure on the interparticle nanocage o...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Computational prediction of drug solubility in water-based systems: Qualitative and quantitative approaches used in the current drug discovery and development setting
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Christel A.S. Bergström, Per Larsson In this review we will discuss recent advances in computational prediction of solubility in water-based solvents. Our focus is set on recent advances in predictions of biorelevant solubility in media mimicking the human intestinal fluids and on new methods to predict the thermodynamic cycle rather than prediction of solubility in pure water through quantitative structure property relationships (QSPR). While the literature is rich in QSPR models for both solubility ...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Study of petrolatum structure: Explaining its variable rheological behavior
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): A.J.P. van Heugten, J. Landman, A.V. Petukhov, H. Vromans The rheological properties of petrolatum are dependent on both temperature and thermal history. How this thermal dependency can be explained is unclear. In the past it has been suggested that the structure of petrolatum consists of a three-dimensional crystalline network. This has been established using old microscopic techniques only. Therefore a study on the microstructure of petrolatum was conducted using rheometry, DSC, pulsed NMR, polarized lig...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of tablet formulation and subsequent film coating on the supersaturated dissolution behavior of amorphous solid dispersions
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Toshiro Sakai, Daiki Hirai, Shin-ichiro Kimura, Yasunori Iwao, Shigeru Itai The effects of tablet preparation and subsequent film coating with amorphous solid dispersion (ASD) particles that were composed of a drug with poor water solubility and hydrophilic polymers were investigated. ASD particles were prepared with a drug and vinylpyrrolidone–vinyl acetate copolymer (PVPVA) or polyvinylpyrrolidone (PVP) at a weight ratio of 1:1 or 1:2 using a melt extrusion technique. Tablets were prepared by conve...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of formulation and process parameters for the production of carvedilol nanosuspension by wet media milling
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Djordje Medarević, Jelena Djuriš, Svetlana Ibrić, Miodrag Mitrić, Kyriakos Kachrimanis The aim of this study is to develop nanosuspension of carvedilol (CRV) by wet media milling. Concentration of polymeric stabilizer (hydroxypropyl cellulose-HPC-SL), milling speed and size of milling beads were identified as critical formulation and process parameters and their effect on CRV particle size after 60 min of milling was assessed using a Box-Behnken experimental design. Optimized nanosuspension was...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Compressibility and tablet forming ability of bimodal granule mixtures: Experiments and DEM simulations
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Josefina Nordström, Göran Alderborn, Göran Frenning Compressibility and tablet forming ability (compactibility) of bimodal mixtures of differently sized granules formed from microcrystalline cellulose were studied experimentally and numerically with the discrete element method (DEM). Compression data was analysed using the Kawakita equation. A multi-body contact law that accounts for contact dependence resulting from plastic incompressibility/geometric hardening was used in the DEM simulatio...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Surface area normalized dissolution to study differences in itraconazole-copovidone solid dispersions prepared by spray-drying and hot melt extrusion
This study provides insight into the complex interplay between formulation, processing and performance of amorphous solid dispersion systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of two DSC-based methods to predict drug-polymer solubility
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Malte Bille Rask, Matthias Manne Knopp, Niels Erik Olesen, René Holm, Thomas Rades The aim of the present study was to compare two DSC-based methods to predict drug-polymer solubility (melting point depression method and recrystallization method) and propose a guideline for selecting the most suitable method based on physicochemical properties of both the drug and the polymer. Using the two methods, the solubilities of celecoxib, indomethacin, carbamazepine, and ritonavir in polyvinylpyrrolidone, hy...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Dry-powder formulations of non-covalent protein complexes with linear or miktoarm copolymers for pulmonary delivery
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Alejandro Nieto-Orellana, David Coghlan, Malcolm Rothery, Franco H. Falcone, Cynthia Bosquillon, Nick Childerhouse, Giuseppe Mantovani, Snow Stolnik Pulmonary delivery of protein therapeutics has considerable clinical potential for treating both local and systemic diseases. However, poor protein conformational stability, immunogenicity and protein degradation by proteolytic enzymes in the lung are major challenges to overcome for the development of effective therapeutics. To address these, a family of stru...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Curcumin marinosomes as promising nano-drug delivery system for lung cancer
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Shaimaa Ibrahim, Tatsuaki Tagami, Toshihiro Kishi, Tetsuya Ozeki Lung cancer is the major cause of cancer-related death worldwide. Curcumin attracted attention due to its promising anti-cancer properties, however its poor aqueous solubility and bioavailability have to be overcome. In the current study curcumin is encapsulated in krill lipids-based liposomes (marinosomes) to develop a potential anticancer therapy from low-cost and readily available nutraceuticals. Reflux followed by thin drug-lipid film met...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Study of a low-dose capsule filling process by dynamic and static tests for advanced process understanding
This study is a further step towards a scientific qualification of dosator nozzles for low-fill weight (1–45 mg) capsule filling. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of chirality on the Glass Forming Ability and the crystallization from the amorphous state of 5-ethyl-5-methylhydantoin, a chiral poor glass former
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Bienvenu Atawa, Nicolas Couvrat, Gérard Coquerel, Eric Dargent, Allisson Saiter The investigation of the glassy state of 5-ethyl-5-methylhydantoin (i.e. 12H, a chiral Active Pharmaceutical Ingredient) was attempted by Differential Scanning Calorimetry (DSC) and Fast Scanning Calorimetry (FSC). This compound exhibits a high crystallization propensity for every enantiomeric composition. Nevertheless, glassy states of pure enantiomer or mixtures between enantiomers were successfully reached by FSC at c...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Statistical moments in modelling of swelling, erosion and drug release of hydrophilic matrix-tablets
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): P. Barmpalexis, K. Kachrimanis, S. Malamataris Statistical moments were evaluated as suitable parameters for describing swelling and erosion processes (along with drug release) in hydrophilic controlled release matrix tablets. The effect of four independent formulation variables, corresponding to the quantity of four polymeric matrix excipients (namely polyethylene glycol, povidone, and two grades of hydroxyl-propylmethyl cellulose) on statistical moments describing swelling (mean swelling time, MST), eros...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Nanomedicine: An effective tool in cancer therapy
Publication date: 5 April 2018 Source:International Journal of Pharmaceutics, Volume 540, Issues 1–2 Author(s): Saima Aftab, Afzal Shah, Akhtar Nadhman, Sevinc Kurbanoglu, Sibel Aysıl Ozkan, Dionysios D. Dionysiou, Shyam S. Shukla, Tejraj M. Aminabhavi Various types of nanoparticles (NPs) have been used in delivering anticancer drugs to the site of action. This area has become more attractive in recent years due to optimal size and negligible undesirable side effects caused by the NPs. The focus of this review is to explore various types of NPs and their surface/chemical modifications as well as attachment of targe...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Fabricating 3D printed orally disintegrating printlets using selective laser sintering
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Fabrizio Fina, Christine M. Madla, Alvaro Goyanes, Jiaxin Zhang, Simon Gaisford, Abdul W. Basit Selective laser sintering (SLS) is a three-dimensional printing (3DP) technology employed to manufacture plastic, metallic or ceramic objects. The aim of this study was to demonstrate the feasibility of using SLS to fabricate novel solid dosage forms with accelerated drug release properties, and with a view to create orally disintegrating formulations. Two polymers (hydroxypropyl methylcellulose (HPMC E5) and v...
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Overcoming the polycation dilemma – Explorative studies to characterise the efficiency and biocompatibility of newly designed lipofection reagents
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Julia Giselbrecht, Christopher Janich, Shashank Reddy Pinnapireddy, Gerd Hause, Udo Bakowsky, Christian Wölk, Andreas Langner In this explorative study of the novel cationic lipid OO4 in two different formulations the complex formation with DNA, the biopharmaceutical stability of the lipid/DNA complexes in physiological media, and the transfection efficiency were analysed. We investigated liposomes composed of two binary mixtures of OO4 with either DOPE or DPPE as co-lipids in the molar ratio of 1:3....
Source: International Journal of Pharmaceutics - February 23, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-based nanosuspensions for oral delivery of peptides, a critical review
This article details different techniques used to produce SLN and NLC with potential or effective peptide encapsulation. Basic principles of covalent and non-covalent lipidization are described and discussed as a prerequisite to improve hydrophilic peptide encapsulation in lipid-based nanosuspensions. The last part of this review provides the key evaluation techniques to assay SLN and NLC for peptide oral bioavailability enhancement. Methods to assess the protective effects of the carriers are described as well as the techniques to evaluate peptide release upon lipid digestion by lipases. Furthermore, this review suggests ...
Source: International Journal of Pharmaceutics - February 22, 2018 Category: Drugs & Pharmacology Source Type: research

Flexible and precise dosing of enalapril maleate for all paediatric age groups utilizing orodispersible minitablets
In this study, a dilution method has been developed by dispersing the lowest dose strength ODMTs to enable flexible and precise EM dosing during the dose titration phase of the therapy. Furthermore, the physicochemical stability of the ODMTs has been investigated in child-friendly beverages and the administration of ODMTs via nasogastric tubes (NGT) of different sizes and materials has been evaluated. The results for the ODMT dilution procedure reveal that dispersion within an oral syringe is preferred over dispersion in a separate container, leading to flexible and precise dosing down to 0.025 mg EM. Although ODMTs were s...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Aqueous injection of quercetin: an approach for confirmation of its direct in vivo cardiovascular effects
This study reports for the first time an injectable water-soluble formulation of quercetin suitable for confirmation of its vascular effect in vivo. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

DoE based Olanzapine loaded poly-caprolactone nanoparticles decreases extrapyramidal effects in rodent model
Publication date: Available online 21 February 2018 Source:International Journal of Pharmaceutics Author(s): Emil Joseph, Satish Reddi, Vibhu Rinwa, Garima Balwani, Ranendra Saha The purpose of present investigation was to nano-encapsulate atypical antipsychotic such as Olanzapine in polymeric nanoparticles in order to explore the possibility of minimizing drug associated extrapyramidal adverse effects. The polymeric nanoparticulate systems were prepared using FDA approved polymer, polycaprolactone, by simple technique of nanoprecipitation using factorial design by DoE approach. The significant factors selected for the op...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Protective effect of sodium stearate on the moisture-induced deterioration of hygroscopic spray-dried powders
In this study, disodium cromoglycate (DSCG) powder was chosen as a model drug because it is amorphous and highly hygroscopic after spray drying. Sodium stearate (NaSt) was co-spray dried with DSCG at various concentrations (10, 50 and 90% w/w) to investigate its effect against moisture-induced deterioration on the in vitro aerosolization performance of DSCG. Particle size distribution and morphology were measured by laser diffraction and scanning electron microscopy (SEM). Physicochemical properties of the powders were analysed by X-ray powder diffraction (XRPD) and dynamic vapour sorption (DVS). Particle surface chemistry...
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Photostabilization strategies of photosensitive drugs
Conclusions A gold standard strategy suitable for all compounds cannot be proposed. Instead, case-by-case evaluation, supported on the photodegradation mechanism is recommended. Systematic studies that compare different photostabilization strategies undertaken with the same irradiation conditions are also needed. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 21, 2018 Category: Drugs & Pharmacology Source Type: research

Establishment of an Evaluation Method to Detect Drug Distribution in Hair Follicles
Publication date: Available online 19 February 2018 Source:International Journal of Pharmaceutics Author(s): Akinari Abe, Miyuki Saito, Wesam R. Kadhum, Hiroaki Todo, Kenji Sugibayashi Development of an appropriate method to evaluate drug disposition or targeting ability in hair follicles (HFs) is urgently needed in order to develop useful pharmaceutical products with pharmacological effects in HFs. In the present study, a cyanoacrylate biopsy (CB) method was used to measure drug disposition in HFs using a model hydrophilic drug, caffeine (CAF), and a lipophilic drug, 4-butylresorcinol (BR), in excised porcine skin. As a ...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Intestinal Absorption and Activation of Decitabine Amino Acid Ester Prodrugs Mediated by Peptide Transporter PEPT1 and Enterocyte Enzymes
Publication date: Available online 19 February 2018 Source:International Journal of Pharmaceutics Author(s): Wenhui Tao, Dongyang Zhao, Mengchi Sun, Ziyu Wang, Bin Lin, Yu Bao, Yingying Li, Zhonggui He, Yinghua Sun, Jin Sun Decitabine (DAC), a potent DNA methyltransferase (DNMT) inhibitor, has a limited oral bioavailability. Its 5′-amino acid ester prodrugs could improve its oral delivery but the specific absorption mechanism is not yet fully understood. The aim of this present study was to investigate the in vivo absorption and activation mechanism of these prodrugs using in situ intestinal perfusion and pharmacoki...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Transdermal delivery of vitamin K using dissolving microneedles for the prevention of vitamin K deficiency bleeding
The objective of our study was to investigate the manufacture of microneedles for the delivery of vitamin K. Following microneedle fabrication, we performed insertion studies to assess the microneedle’s mechanical properties. Results indicate that vitamin K in a microneedle array was successfully delivered in vitro across neonatal porcine skin with 1.80 ± 0.08 mg delivered over 24 hours. Therefore, this initial study shows that microneedles do have the potential to prevent vitamin K deficiency bleeding. Future work will assess delivery of vitamin K in microneedle array in vivo. Graphical abstract (Source: Inte...
Source: International Journal of Pharmaceutics - February 20, 2018 Category: Drugs & Pharmacology Source Type: research

Co-spray drying of hygroscopic kanamycin with the hydrophobic drug rifampicin to improve the aerosolization of kanamycin powder for treating respiratory infections
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Mohammad A.M. Momin, Ian G. Tucker, Colin S. Doyle, John A. Denman, Shubhra Sinha, Shyamal C. Das High dose delivery of drugs to the lung using a dry powder inhaler (DPI) is an emerging approach to combat drug-resistant local infections. To achieve this, highly aerosolizable powders are required. We hypothesized that co-spray-drying kanamycin, a hydrophilic hygroscopic antibiotic, with rifampicin, a hydrophobic antibiotic, would produce inhalable particles with surfaces enriched in rifampicin. Such particles would ...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Topical bio(in)equivalence of metronidazole formulations in vivo
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Thalita Pedon de Araujo, Isabelle Moura Fittipaldi, Danilo Cesar Galindo Bedor, Maira Ludna Duarte, Sarah F. Cordery, Richard H. Guy, M. Begonã Delgado-Charro, Davi Pereira de Santana, Leila Bastos Leal The topical bioavailabilities of metronidazole from a commercially available ‘reference’ product (Rozex®) and two extemporaneous test formulations were compared. With the reference drug product, a full skin pharmacokinetic profile, in vivo in human volunteers (following a 6-hour uptake and cle...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

PLGA nanoformulation of Sparfloxacin enhanced antibacterial activity with photoprotective potential under ambient UV-R exposure
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Jyoti Singh, Ashish Dwivedi, Lipika Ray, Deepti Chopra, Divya Dubey, Ajeet K. Srivastva, Smita Kumari, Randheer Kumar, Saroj Kumar Amar, Chandana Haldar, Ratan Singh Ray Sparfloxacin (SPFX) is a broad spectrum antibiotic which inhibits bacterial DNA gyrase enzyme activity. However, photodegradation in the presence of UVA limits its antibacterial activity and induces phototoxicity. Thus, to encounter this problem, we have developed poly d,l-lactic-co- glycolic acid (PLGA) loaded SPFX nanoparticles. Here, we have per...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Dermal anti-oxidant, anti-inflammatory and anti-aging effects of Compritol ATO-based Resveratrol colloidal carriers prepared using mixed surfactants.
In this study, Compritol ATO-based Resveratrol colloidal carriers (CCCs) were prepared. In most formulae, the use of a binary-mixture of surfactants improved the physicochemical properties. CCC6 (containing P407/P188 as bi-surfactants) attained the highest drug loading, release efficiency during 24 hr and occlusive effect for 48 hr; in addition to, a uniform particle size distribution within the desired range. In-vivo studies were done based on the analysis of anti-oxidant markers [catalase (CAT), reduced glutathione (GSH) and superoxide dismutase (SOD)], anti-inflammatory markers [interleukin 6 (IL-6), interleukin 8 (IL-8...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Overcoming the polycation dilemma - Explorative studies to characterise the efficiency and biocompatibility of newly designed lipofection reagents
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Julia Giselbrecht, Christopher Janich, Shashank Reddy Pinnapireddy, Gerd Hause, Udo Bakowsky, Christian Wölk, Andreas Langner In this explorative study of the novel cationic lipid OO4 in two different formulations the complex formation with DNA, the biopharmaceutical stability of the lipid/DNA complexes in physiological media, and the transfection efficiency were analysed. We investigated liposomes composed of two binary mixtures of OO4 with either DOPE or DPPE as co-lipids in the molar ratio of 1:3. These for...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research