Self-microemulsifying drug delivery system for camptothecin using new bicephalous heterolipid with tertiary-amine as branching element
Publication date: Available online 17 February 2018 Source:International Journal of Pharmaceutics Author(s): Dinesh M. Dhumal, K.G. Akamanchi Camptothecin (CPT) has a potent and broad-spectrum anti-tumor activity but its clinical use is limited due to its poor water solubility, stability at physiological conditions and toxicity. The aim of our study was to evaluate bicephalous heterolipid E1E for enhancing the solubility and stability of CPT through the development of a selfmicroemulsifying drug delivery system (SMEDDS). The solubility of CPT in heterolipid E1E was found to be 82 and 5.86 folds higher than oleic acid and ...
Source: International Journal of Pharmaceutics - February 18, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of Formulation Excipients on the Thermal, Mechanical, and Electrokinetic Properties of Hydroxypropyl methylcellulose acetate succinate (HPMCAS)
This study facilitated the understanding of the HPMCAS aggregation mechanism, in addition to identifying suitable stabilizing agents. These stabilizing excipients could potentially be used to develop a stable aqueous coating formulation that does not exhibit polymer aggregation and nozzle clogging during the coating process. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

The use of fatty acids as absorption enhancer for pulmonary drug delivery
In this study, the potential of sodium decanoate (Na dec), docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) as absorption enhancers has been investigated to increase pulmonary paracellular permeability by modulating epithelial cells’ tight junctions. By incorporating Na dec, DHA and EPA, separately, into a nebulising formulation, the aim was to enhance the absorption of a fluorescent marker (flu-Na, used as model drug) across pulmonary epithelial cells (Calu-3). Results indicate that the aerosol performance of all the nebulizing formulations containing absorption enhancers was significantly better than cont...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Mucoadhesive Self-Emulsifying Delivery Systems for Ocular Administration of Econazole
Conclusion Accordingly, these mucoadhesive SEDDS can be considered as promising ocular delivery system for EN. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of a solid self-microemulsifying drug delivery system by hot-melt extrusion
This study sought to prepare enteric S-SMEDDS by HME and evaluate the effects of the process and formulation variables on S-SMEDDS properties via Box-Behnken design. Liquid SMEDDS were developed, and carvedilol was used as a class II model drug. Mean size, polydispersity index (PdI) and zeta potential of the resulting microemulsions were determined. The extrudates were then obtained by blending the lipid mixture and HPMCAS using a twin-screw hot-melt extruder. SEM, optical microscopy and PXRD were used to characterize the extrudates. In vitro microemulsion reconstitution and drug release were also studied. L-SMEDDS gave ri...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Developing a Stable Aqueous Enteric Coating Formulation with Hydroxypropyl methylcellulose acetate succinate (HPMCAS-MF) and Colloidal Silicon Dioxide as Anti-tacking Agent
Publication date: Available online 16 February 2018 Source:International Journal of Pharmaceutics Author(s): Tanvi M. Deshpande, Anisul Quadir, Sakae Obara, Ahmed Ibrahim, Stephen W. Hoag The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can minimize hydroxypropyl methylcellulose acetate succinate aggregation and minimize spray-nozzle clogging at elevated processing temperatures. The mechanisms of stabilization (i.e. charge stabilization and molecular interactions) were studied b...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

A Review of Implantable Biosensors for Closed-Loop Glucose Control and Other Drug Delivery Applications
Publication date: Available online 16 February 2018 Source:International Journal of Pharmaceutics Author(s): Kee Scholten, Ellis Meng Closed-loop drug delivery promises autonomous control of pharmacotherapy through the continuous monitoring of biomarker levels. For decades, researchers have strived for portable closed-loop systems, capable of treating ambulatory patients with chronic conditions such as diabetes mellitus. After years of development, the first of these systems have left the laboratory and entered commercial use. This long-awaited advance reflects recent development of chronically stable implantable biosenso...
Source: International Journal of Pharmaceutics - February 17, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of ligands property and particle size of gold nanoparticles on the protein adsorption and corresponding targeting ability
In this study, two common used ligands were chosen as the model: transferrin and RGD peptide. Gold nanoparticles were utilized as model particles. Sodium dodecyl sulfate polyacrylamide gel electrophoresis data demonstrated that higher PEG modification and smaller particle size could reduce the plasma protein adsorption, while ligand modification could increase. The cellular uptake results showed that the targeting ability of smaller ligand RGD peptide would be more easily influenced by the proteins corona. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Isomalt and its diastereomer mixtures as stabilizing excipients with freeze-dried lactate dehydrogenase
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Anna-Kaisa Tuderman, Clare J. Strachan, Anne M. Juppo The purpose of this research was to study isomalt as a protein-stabilizing excipient with lactate dehydrogenase (LDH) during freeze-drying and subsequent storage and compare it to sucrose, a standard freeze-drying excipient. Four different diastereomer mixtures of isomalt were studied. The stability of the protein was studied with a spectrophotometric enzyme activity test and circular dichroism after freeze-drying and after 21 days of storage at 16% R...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Proliposome tablets manufactured using a slurry-driven lipid-enriched powders: Development, characterization and stability evaluation
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Iftikhar Khan, Sakib Yousaf, Sneha Subramanian, Mohamed Albed Alhnan, Waqar Ahmed, Abdelbary Elhissi Proliposome powders were prepared via a slurry method using sorbitol or D-mannitol as carbohydrate carriers in 1:10 or 1:15 w/w lipid phase to carrier ratios. Soya phosphatidylcholine (SPC) and cholesterol were employed as a lipid phase and Beclometasone dipropionate (BDP) was incorporated as a model drug. Direct compaction using a Minipress was applied on the lipid-enriched powder in order to manufacture p...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Improving release completeness from PLGA-based implants for the acid-labile model protein ovalbumin
The objectives of this study were to assess the feasibility of hot melt extrusion (HME) for the preparation of PLGA-based ovalbumin-loaded implants as well as to characterize and improve protein release from the implants. Ovalbumin (OVA) was stable during extrusion, which was attributed to a protective effect of the biodegradable matrix. OVA release was characterized by a low burst, a slow release up to day 21, which plateaued thereafter resulting in incomplete release for all evaluated protein loadings. Release incompleteness was accompanied by the formation of an insoluble residual mass. Further characterization of this ...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

A drop penetration method to measure powder blend wettability
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Yifan Wang, Zhanjie Liu, Fernando Muzzio, German Drazer, Gerardo Callegari Water wettability of pharmaceutical blends affects important quality attributes of final products. We investigate the wetting properties of a pharmaceutical blend lubricated with Magnesium Stearate (MgSt) as a function of the mechanical shear strain applied to the blend. We measure the penetration dynamics of sessile drops deposited on slightly compressed powder beds. We consider a blend composed of 9% Acetaminophen 90% Lactose and ...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Development and pre-clinical evaluation in the swine model of a mucosal vaccine tablet for human influenza viruses: A proof-of-concept study
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): V. Busignies, G. Simon, G. Mollereau, O. Bourry, V. Mazel, M. Rosa-Calatrava, P. Tchoreloff Liquid vaccine formulations present some disadvantages such as stability problems, cold chain requirement or administration by trained personnel. Vaccine formulated as tablets would present a wide range of progress such as an increase stability that would facilitate the administration, the distribution and the storage of vaccine formulations. This work investigates the possibility to develop a mucosal tablet vaccine...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Recent trends of nanomedicinal approaches in clinics
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Fahima Dilnawaz, Sarbari Acharya, Sanjeeb Kumar Sahoo Nanotechnology has become the indispensable cutting edge science providing solutions to many problems associated with human being. The application of nanotechnology associated to human health “nanomedicine” has revolutionized the drug delivery system by providing improved pharmacological and therapeutic properties of drugs. These advantageous effects of drug loaded nanocarrier systems are embraced by the pharmaceutical industries for the dev...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Trends in insect repellent formulations: A review
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Melanie Tavares, Márcio Robert Mattos da Silva, Luciana Betzler de Oliveira de Siqueira, Raphaela Aparecida Schuenck Rodrigues, Lolita Bodjolle-d'Almeira, Elisabete Pereira dos Santos, Eduardo Ricci-Júnior The use of natural and synthetic repellents, marketed in different pharmaceutical forms, is growing in the world due to the emerging vector-borne viral diseases as Dengue, Zika, Chikungunya, Yellow Fever and Malaria. The choice of the ideal formulation will depend on a series of factors to...
Source: International Journal of Pharmaceutics - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Dual-responsive lidocaine in situ gel reduces pain of intrauterine device insertion
In conclusion, lidocaine dual-responsive in situ gel can be effectively used in prevention of pain during IUD insertion. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

Is there a correlation between the glass forming ability of a drug and its supersaturation propensity?
In this study, a potential correlation between GFA and supersaturation propensity is investigated. The GFA of 23 different drugs was determined by melt quenching or milling the crystalline drugs to obtain their respective amorphous forms. The inherent propensity of the drug to supersaturate, i.e. the maximal apparent degree of supersaturation (aDS), and the time until precipitation at a given aDS were determined. Supersaturation was induced via a solvent shift method where the drug was initially dissolved in dimethyl sulfoxide and then added to a biorelevant medium (fasted state simulated intestinal fluid).The study showed...
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

A mesoporous silica based platform to enable tablet formulations of low dose drugs by direct compression
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Wei-Jhe Sun, Aktham Aburub, Changquan Calvin Sun Achieving adequate content uniformity (CU) is a significant challenge in the development and manufacturing of low dose oral tablets. Using four model active pharmaceutical ingredients (APIs), we show that loading APIs into a grade of mesoporous silica, Aeroperl®, is effective for achieving excellent CU. All APIs in the Aeroperl® composites were amorphous. After six months under accelerated stability conditions, the drug-Aeoperl composites exhibited ...
Source: International Journal of Pharmaceutics - February 3, 2018 Category: Drugs & Pharmacology Source Type: research

Liquid crystalline drug delivery vehicles for oral and IV/subcutaneous administration of poorly soluble (and soluble) drugs
Publication date: Available online 31 January 2018 Source:International Journal of Pharmaceutics Author(s): Andrew Otte, Bong-Kwan Soh, Gwangheum Yoon, Kinam Park Poorly soluble drug molecules often have low bioavailability issues and absorption problems in the clinical setting. As the number of poorly soluble drugs increases from discovery, developing technologies to enhance their solubility, while also controlling their release is one of the many challenges facing the pharmaceutical industry today. Liquid crystalline systems, nanoparticulate or macro-matrix, self-assemble in the presence of an aqueous environment and ca...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Asymmetric flow field flow fractionation for the characterization of globule size distribution in complex formulations: A cyclosporine ophthalmic emulsion case
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Haiou Qu, Jiang Wang, Yong Wu, Jiwen Zheng, Yellela S.R. Krishnaiah, Mohammad Absar, Stephanie Choi, Muhammad Ashraf, Celia N. Cruz, Xiaoming Xu Commonly used characterization techniques such as cryogenic-transmission electron microscopy (cryo-TEM) and batch-mode dynamic light scattering (DLS) are either time consuming or unable to offer high resolution to discern the poly-dispersity of complex drug products like cyclosporine ophthalmic emulsions. Here, a size-based separation and characterization method f...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Self-emulsifying peptide drug delivery systems: How to make them highly mucus permeating
Conclusion Small droplet size and negative zeta potential of SEDDS could be identified as key parameters for their mucus permeating properties. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Induction of Au-methotrexate conjugates by sugar molecules: production, assembly mechanism, and bioassay studies
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Wei-Yuan Wang, Xiu-Fen Zhao, Xiao-Han Ju, Ping Liu, Jing Li, Ya-Wen Tang, Shu-Ping Li, Xiao-Dong Li, Fu-Gui Song Au-methotrexate (Au-MTX) conjugates induced by sugar molecules were produced by a simple, one-pot, hydrothermal growth method. Herein, the Au(III)-MTX complexes were used as the precursors to form Au-MTX conjugates. Addition of different types of sugar molecules with abundant hydroxyl groups resulted in the formation of Au-MTX conjugates featuring distinct characteristics that could be explained...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Process analytical technology in continuous manufacturing of a commercial pharmaceutical product
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Jenny M. Vargas, Sarah Nielsen, Vanessa Cárdenas, Anthony Gonzalez, Efrain Y. Aymat, Elvin Almodovar, Gustavo Classe, Yleana Colón, Eric Sanchez, Rodolfo J. Romañach The implementation of process analytical technology and continuous manufacturing at an FDA approved commercial manufacturing site is described. In this direct compaction process the blends produced were monitored with a Near Infrared (NIR) spectroscopic calibration model developed with partial least squares (PLS) regressio...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 for sustained delivery of hydrophobic drugs
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Eneko Larrañeta, Laura Barturen, Michael Ervine, Ryan F. Donnelly Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 were prepared for hydrophobic drug delivery. The hydrogels were synthesized following a simple procedure carried out in solid state. The process did not require the use of any solvent and, as it is based on an esterification reaction, no toxic by-products were obtained. The resulting hydrogels contained Tween 85 inside the structure and due to the amphiphilic natu...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Performance of an acoustically mixed pharmaceutical dry powder delivered from a novel inhaler
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Ryoma Tanaka, Naoyuki Takahashi, Yasuaki Nakamura, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Semifluorinated alkane based systems for enhanced corneal penetration of poorly soluble drugs
This study evaluated the potential of two SFAs to act as vehicle for topical ocular drug delivery. After confirming ocular safety, an ex vivo corneal penetration model was developed to determine drug distribution and corneal bioavailability. Hydrophobic dye distribution in the different corneal layers was visualised under a confocal microscope. Corneal bioavailability of cyclosporine A (CsA) dissolved in perfluorobutylpentane (F4H5) or perfluorohexyloctane (F6H8) was compared to commercially available CsA ophthalmic emulsions, Restasis® and Ikervis®. Precorneal residence of the four test vehicles containing the hyd...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

A novel method for the production of core-shell microparticles by inverse gelation optimized with artificial intelligent tools
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Rosalia Rodríguez-Dorado, Mariana Landín, Ayça Altai, Paola Russo, Rita P. Aquino, Pasquale Del Gaudio Numerous studies have been focused on hydrophobic compounds encapsulation as oils. In fact, oils can provide numerous health benefits as synergic ingredient combined with other hydrophobic active ingredients. However, stable microparticles for pharmaceutical purposes are difficult to achieve when commonly techniques are used. In this work, sunflower oil was encapsulated in calcium-alg...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Molecular-level elucidation of saccharin-assisted rapid dissolution and high supersaturation level of drug from Eudragit ® E solid dispersion
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Keisuke Ueda, Harunobu Kanaya, Kenjirou Higashi, Keiji Yamamoto, Kunikazu Moribe In this work, the effect of saccharin (SAC) addition on the dissolution and supersaturation level of phenytoin (PHT)/Eudragit® E (EUD-E) solid dispersion (SD) at neutral pH was examined. The PHT/EUD-E SD showed a much slower dissolution of PHT compared to the PHT/EUD-E/SAC SD. EUD-E formed a gel layer after the dispersion of the PHT/EUD-E SD into an aqueous medium, resulting in a slow dissolution of PHT. Pre-dissolving SAC...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

In vivo controlled release of fenretinide from long-acting release depots for chemoprevention of oral squamous cell carcinoma recurrence
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Kari Nieto, Ping Pei, Daren Wang, Susan R. Mallery, Steven P. Schwendeman Local, long-acting release fenretinide (4HPR) millicylindrical implants were prepared and evaluated for their release kinetics in vivo and their ability to suppress oral cancer tumor explant growth. Poly(lactic-co-glycolic acid)(PLGA) implants were prepared as a function of drug loading and the presence of various excipients (pore-formers, solubilizers, crystallization inhibitors) to enhance release of the insoluble 4HPR. Release kin...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Characterisation of pore structures of pharmaceutical tablets: A review
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Daniel Markl, Alexa Strobel, Rüdiger Schlossnikl, Johan Bøtker, Prince Bawuah, Cathy Ridgway, Jukka Rantanen, Thomas Rades, Patrick Gane, Kai-Erik Peiponen, J. Axel Zeitler Traditionally, the development of a new solid dosage form is formulation-driven and less focus is put on the design of a specific microstructure for the drug delivery system. However, the compaction process particularly impacts the microstructure, or more precisely, the pore architecture in a pharmaceutical tablet. Besides t...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

An efficient PEGylated gene delivery system with improved targeting: Synergism between octaarginine and a fusogenic peptide
In this study, we describe the development of PEGylated CPP-based gene carrier with an improved targeting and a high transfection activity. The system was prepared by condensing DNA with a polycation followed by coating with a lipid envelope containing the octaarginine (R8) peptide as a model CPP. R8-modified nanoparticles produced high transfection activities, but the efficiency was reduced by PEG shielding. The reduced activity could be fully restored by the addition of a targeting ligand and a pH-sensitive fusogenic peptide. The efficiency of the proposed system is quite high, even in the presence of serum, and shows im...
Source: International Journal of Pharmaceutics - January 21, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of structural factors on release profiles of camptothecin from block copolymer conjugates with high load of drug
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Andrzej Plichta, Sebastian Kowalczyk, Ewa Olędzka, Marcin Sobczak, Marcin Strawski The aim of the present work was the synthesis and study the kinetics and profiles of camptothecin (CPT) release form block co- and ter-polymer conjugates comprising polylactide (PLA) segments and CPT moieties, structurally diverse by degrees of branching, content of d-PLA units and poly(ethylene glycol) methyl ether methacrylate (PEGMA). Six PLA, non-toxic macroinitiators (MIs), terminated with α-bromoester were synth...
Source: International Journal of Pharmaceutics - January 21, 2018 Category: Drugs & Pharmacology Source Type: research

3D extrusion printing of high drug loading immediate release paracetamol tablets
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Shaban A. Khaled, Morgan R. Alexander, Ricky D. Wildman, Martin J. Wallace, Sonja Sharpe, Jae Yoo, Clive J. Roberts The manufacture of immediate release high drug loading paracetamol oral tablets was achieved using an extrusion based 3D printer from a premixed water based paste formulation. The 3D printed tablets demonstrate that a very high drug (paracetamol) loading formulation (80% w/w) can be printed as an acceptable tablet using a method suitable for personalisation and distributed manufacture. Parace...
Source: International Journal of Pharmaceutics - January 20, 2018 Category: Drugs & Pharmacology Source Type: research

Nanogel-DFO conjugates as a model to investigate pharmacokinetics, biodistribution, and iron chelation in vivo
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Yan Wang, Zhi Liu, Tien-Min Lin, Shaurya Chanana, May P. Xiong Deferoxamine (DFO) to treat iron overload (IO) has been limited by toxicity issues and short circulation times and it would be desirable to prolong circulation to improve non-transferrin bound iron (NTBI) chelation. In addition, DFO is currently unable to efficiently target the large pool of iron in the liver and spleen. Nanogel-Deferoxamine conjugates (NG-DFO) can prove useful as a model to investigate the pharmacokinetic (PK) properties and b...
Source: International Journal of Pharmaceutics - January 19, 2018 Category: Drugs & Pharmacology Source Type: research

Stability, biocompatibility and antioxidant activity of PEG-modified liposomes containing resveratrol
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Carla Caddeo, Laura Pucci, Morena Gabriele, Claudia Carbone, Xavier Fernàndez-Busquets, Donatella Valenti, Ramon Pons, Antonio Vassallo, Anna Maria Fadda, Maria Manconi The present investigation reports the development of PEG-modified liposomes for the delivery of naturally occurring resveratrol. PEG-modified liposomes were prepared by direct sonication of the phospholipid aqueous dispersion, in the presence of two PEG-surfactants. Small, spherical, unilamellar vesicles were produced, as demonstrate...
Source: International Journal of Pharmaceutics - January 13, 2018 Category: Drugs & Pharmacology Source Type: research

Probing the particulate microstructure of the aerodynamic particle size distribution of dry powder inhaler combination products
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): M.W. Jetzer, B.D. Morrical, M. Schneider, S. Edge, G. Imanidis The in-vitro aerosol performance of two combination dry powder inhaler (DPI) products, Foster® NEXThaler® and Seretide® Diskus® were investigated with single particle aerosol mass spectrometry (SPAMS). The in-vitro pharmaceutical performance is markedly different for both inhalers. Foster® NEXThaler® generates a higher fine particle fraction (FPF <5 μm) and a much higher relative extra fine particle fraction ...
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Controllable encapsulation of α-mangostin with quaternized β-cyclodextrin grafted chitosan using high shear mixing
In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized β-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex. Molecular dynamics simulations indicate that α-mangostin is included within the hydrophobic β-CD cavity and being absorbed on the QCD-g-CS surface, with these results being confirmed by Fourier transform infrared (FTIR) spectro...
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Optimized tableting for extremely oxygen-sensitive probiotics using direct compression
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Rania Allouche, Sébastien Dupont, Alexandre Charriau, Patrick Gervais, Laurent Beney, Odile Chambin Faecalibacterium prausnitzii was previously recognized for its intestinal anti-inflammatory activities and it has been shown less abundant in patients with chronic intestinal diseases. However, the main problems encountered in the use of this interesting anaerobic microorganism are firstly its high sensitivity to the oxygen and secondly, its ability to reach the large intestine alive as targeted site....
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Novel enzyme formulations for improved pharmacokinetic properties and anti-inflammatory efficacies
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Lan Yang, Shenglei Yan, Yonghong Zhang, Xueyuan Hu, Qi Guo, Yuming Yuan, Jingqing Zhang Anti-inflammatory enzymes promote the dissolution and excretion of sticky phlegm, clean the wound surface and accelerate drug diffusion to the lesion. They play important roles in treating different types of inflammation and pain. Currently, various formulations of anti-inflammatory enzymes are successfully prepared to improve the enzymatic characteristics, pharmacokinetic properties and anti-inflammatory efficacies...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Accelerated full-thickness wound healing via sustained bFGF delivery based on a PVA/chitosan/gelatin hydrogel incorporating PCL microspheres
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Amir Shamloo, Morteza Sarmadi, Zahra Aghababaie, Manouchehr Vossoughi Herein, a hybrid hydrogel/microsphere system is introduced for accelerated wound healing by sustained release of basic fibroblast growth factor (bFGF). The hydrogel is composed of a mixture of PVA, gelatin and chitosan. The double-emulsion-solvent-evaporation method was utilized to obtain microspheres composed of PCL, as the organic phase, and PVA, as the aqueous phase. Subsequently, various in-vitro and in-vivo assays were performed...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Zinc delivery from non-woven fibres within a therapeutic nipple shield
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Theresa Maier, Rebekah L. Scheuerle, Daniel Markl, Sylvaine Bruggraber, Axel Zeitler, Ljiljana Fruk, Nigel K.H. Slater A Therapeutic Nipple Shield (TNS) was previously developed to respond to the global need for new infant therapeutic delivery technologies. However, the release efficiency for the same Active Pharmaceutical Ingredient (API) from different therapeutic matrices within the TNS formulation has not yet been investigated. To address this, in-vitro release of elemental zinc into human milk fro...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhancing the solubility and bioavailability of poorly water-soluble drugs using supercritical antisolvent (SAS) process
This article also presents an overview of the main aspects of the SAS-assisted particle precipitation process, its mechanism, and parameters, as well as our own experiences, recent advances, and trends in development. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

A novel lactoferrin-modified stealth liposome for hepatoma-delivery of triiodothyronine
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Rosa Pireddu, Monica Pibiri, Donatella Valenti, Chiara Sinico, Anna Maria Fadda, Gabriella Simbula, Francesco Lai Triiodothyronine (T3), a thyroid hormone synthesized and secreted by the thyroid gland, plays an essential role in morphogenesis and differentiation through interaction with its nuclear receptors (TRs). However, there are increasing evidences for its role in hepatocellular carcinoma (HCC) suppression. The aim of this work was to develop an effective hepatocellular carcinoma targeting drug d...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mucus adhesion- and penetration-enhanced liposomes for paclitaxel oral delivery
In conclusion, the dual functional CS-TGA-PF liposomes with mucus adhesion- and permeation-enhanced properties could be used as a promising nanodrug delivery system for PTX oral delivery. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mucus-PVPA (mucus Phospholipid Vesicle-based Permeation Assay): An artificial permeability tool for drug screening and formulation development
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Margherita Falavigna, Mette Klitgaard, Christina Brase, Selenia Ternullo, Nataša Škalko-Basnet, Gøril Eide Flaten The mucus layer covering all mucosal surfaces in our body is the first barrier encountered by drugs before their potential absorption through epithelial tissues, and could thus affect the drugs’ permeability and their effectiveness. Therefore, it is of key importance to have in vitro permeability models that can mimic this specific environment. For this purpose, t...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Loading of polymyxin B onto anionic mesoporous silica nanoparticles retains antibacterial activity and enhances biocompatibility
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Zahra Gounani, Mohammad A. Asadollahi, Rikke L. Meyer, Ayyoob Arpanaei Polymyxin B is a polycationic antibiotic used as the last line treatment against antibiotic-resistant Gram negative bacteria. However, application of polymyxin B is limited because of its toxicity effects. Herein, we used bare and surface modified mesoporous silica nanoparticles (MSNs) with an average diameter of 72.29 ± 8.17 nm as adsorbent for polymyxin B to improve its therapeutic properties. The polymyxin B adsorpti...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Notorious but not understood: How liquid-air interfacial stress triggers protein aggregation
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Ellen Koepf, Simon Eisele, Rudolf Schroeder, Gerald Brezesinski, Wolfgang Friess Protein aggregation is a major challenge in the development of biopharmaceuticals. As the pathways of aggregation are manifold, good understanding of the mechanisms behind is essential. Particularly, the presence of liquid-air interfaces has been identified to trigger the formation of large protein particles. Investigations of two monoclonal antibodies (IgGs) at the liquid-air interface exhibited the formation of a highly ...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Real-time process monitoring in a semi-continuous fluid-bed dryer – microwave resonance technology versus near-infrared spectroscopy
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Johanna Peters, Andreas Teske, Wolfgang Taute, Claas Döscher, Michael Höft, Reinhard Knöchel, Jörg Breitkreutz The trend towards continuous manufacturing in the pharmaceutical industry is associated with an increasing demand for advanced control strategies. It is a mandatory requirement to obtain reliable real-time information on critical quality attributes (CQA) during every process step as the decision on diversion of material needs to be performed fast and automatically. Where po...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Real time release testing of tablet content and content uniformity
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Daniel J. Goodwin, Sander van den Ban, Mike Denham, Ian Barylski A comprehensive commercial control strategy for tablet content and content uniformity focussed on the unit operation of compression is presented and is proposed to enable real time release for these critical quality attributes. The control strategy is based on process understanding, process control through compaction force weight control on the tablet press, periodic checks of mean and individual tablet weight combined with at-line testin...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

OAT1 and OAT3 also mediate the drug-drug interaction between piperacillin and tazobactam
In conclusion, piperacillin and tazobactam are the substrates of hOAT1/3, and OAT1/3 mediate the DDI between piperacillin and tazobactam. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research