Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach
Publication date: Available online 25 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sang Yeob Park, Zion Kang, Prakash Thapa, Yong Suk Jin, Joo Won Park, Hye Jung Lim, Jae Young Lee, Sa-Won Lee, Min-Hyo Seo, Min-Soo Kim, Seong Hoon JeongAbstractSorafenib, a potent anticancer drug, has low absorption in the gastrointestinal tract due to its poor aqueous solubility. The main purpose of this investigation was to design sorafenib nanoparticle using a newly developed technique, nanoparticulation using fat and supercritical fluid (NUFSTM) to improve the absorption of sorafenib. The quality by design (QbD) tool...
Source: International Journal of Pharmaceutics - May 26, 2019 Category: Drugs & Pharmacology Source Type: research

The NFL-TBS.40-63 peptide targets and kills glioblastoma stem cells derived from human patients and also targets nanocapsules into these cells
The objective of this study is to investigate the effect of this peptide on BTICs isolated from human glioblastoma.The uptake of this peptide alone or coupled to nanocapsules was analyzed by flow cytometry and immunochemistry. Its anti-tumor effect was studied using proliferation, adhesion and viability assays. Peptide-mediated effects were also evaluated on the BTIC self-renewal ability and by immunocytochemistry to investigate their cell shape and microtubule network.Here we show that the peptide enters massively in BTICs and demonstrates an anti-tumor effect by inhibiting their proliferation and inducing their death thr...
Source: International Journal of Pharmaceutics - May 26, 2019 Category: Drugs & Pharmacology Source Type: research

Solidified SNEDDS for the oral delivery of rifampicin: Evaluation, proof of concept, in vivo kinetics, and in silico GastroPlusTM simulation
Publication date: Available online 24 May 2019Source: International Journal of PharmaceuticsAuthor(s): Afzal Hussain, Faiyaz Shakeel, Sandeep Kumar Singh, Ibrahim A. Alsarra, Abdul Faruk, Fars K. Alanazi, G.V. Peter ChristoperAbstractThe present investigation was performed to develop a rifampicin (RIF)-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) (solidified RIF-OF1) for in vitro and in vivo evaluations. Optimized formulations were tested for their powder flow characteristics, loading efficiency, and in vitro dissolution (at pH-1.2, 6.8 and 7.4). Compatibility studies were also performed. The formul...
Source: International Journal of Pharmaceutics - May 26, 2019 Category: Drugs & Pharmacology Source Type: research

Amorphous solid dispersions of ketoprofen and poly-vinyl polymers prepared via electrospraying and spray drying: a comparison of particle characteristics and performance
Publication date: Available online 24 May 2019Source: International Journal of PharmaceuticsAuthor(s): Emer Browne, Romina Charifou, Zelalem Ayenew Worku, Ramesh P. Babu, Anne Marie HealyAbstractThe purpose of this work was to compare the particle characteristics and dissolution performance of amorphous solid dispersions (ASDs) of ketoprofen and vinyl-pyrrolidone based polymers prepared using electrospraying and spray drying methods. Solution characteristics (surface tension, viscosity and conductivity) were determined for ethanolic solutions containing different vinyl-pyrrolidone based polymers (PVP and PVPVA) and differe...
Source: International Journal of Pharmaceutics - May 26, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of disaccharide-polyol systems on the thermal stability of freeze-dried Mycobacterium bovis
Publication date: Available online 25 May 2019Source: International Journal of PharmaceuticsAuthor(s): Yi Zhen Tan, Yi Qi Chong, Emerlyn Khong, Yun Khoon Liew, Norman ChiengAbstractLive attenuated Mycobacterium bovis (M. bovis), marketed as Bacille Calmette-Guérin is the only FDA-approved vaccine against tuberculosis. The prerequisite of cold chain storage between 2 to 8 °C hinders the global vaccination effort. The study aims to investigate the effect of trehalose, sucrose and glycerol combinations in enhancing the stability of M. bovis. The bacilli were formulated in various ratios of trehalose-glycerol, sucro...
Source: International Journal of Pharmaceutics - May 26, 2019 Category: Drugs & Pharmacology Source Type: research

Implementation of a Mathematical Model for the Photochemical Kinetics of a Solid Form Active Pharmaceutical Ingredient
We present here the development of a photochemical model used to quantify the risk to photo-degradation of a solid drug substance. A key feature of the proposed model development is streamlined estimation of the dependence of the absorption spectra and the quantum yield to the wavelength. A mathematical description of the relationship between the quantum yield and the wavelength enables estimation of photo-degradation kinetics under any light anticipated to be encountered in the manufacturing environment. The system studied here consisted of a first order irreversible transformation (A → B(1Φ)) and the formalism s...
Source: International Journal of Pharmaceutics - May 25, 2019 Category: Drugs & Pharmacology Source Type: research

Experimental Investigation of Aerosol Deposition through a Realistic Respiratory Airway Replica: An Evaluation for MDI and DPI Performance
ConclusionThe developed realistic respiratory airways model provided an opportunity to more accurately evaluate the performance of drug delivery devices and studying mechanisms of the drug deposition.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 25, 2019 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of performance characteristics of timolol-loaded composite ocular films as potential delivery platform for treatment of glaucoma
Publication date: Available online 23 May 2019Source: International Journal of PharmaceuticsAuthor(s): Mohammad Tighsazzadeh, John C. Mitchell, Joshua S. BoatengAbstractThin and erodible polymeric films were developed as potential ocular drug delivery systems to increase drug retention on the eye with the aim of improving bioavailability and achieving controlled drug release. Two biocompatible film forming polymers, hyaluronic acid (HA) and hydroxypropyl methylcellulose (HPMC), which are currently used as thickening agents in eye drops were employed. Two different films were prepared (i) as single polymer and (ii) as compo...
Source: International Journal of Pharmaceutics - May 25, 2019 Category: Drugs & Pharmacology Source Type: research

Swellable polymeric particles for the local delivery of budesonide in oral mucositis
Publication date: Available online 23 May 2019Source: International Journal of PharmaceuticsAuthor(s): João C Campos, Domingos C Ferreira, Sofia Lima, Salette Reis, Paulo J CostaAbstractTopical drug delivery in the oral mucosa has its set of challenges due to the unique anatomical and physiological features of the oral cavity. As such, the outcomes of local pharmacological treatments in oral disorders can fail due to unsuccessfully drug delivery. Oral mucositis, a severe inflammatory and ulcerative side effect of oncological treatments, is one of such diseases. Although the damaged tissue is within reach, no approve...
Source: International Journal of Pharmaceutics - May 25, 2019 Category: Drugs & Pharmacology Source Type: research

Solidification of carvedilol loaded SMEDDS by swirling fluidized bed pellet coating
Publication date: Available online 23 May 2019Source: International Journal of PharmaceuticsAuthor(s): J. Mandić, M. Luštrik, F. Vrečer, M. Gašperlin, A. Zvonar PobirkAbstractSelf-(micro)emulsifying drug delivery systems (S(M)EDDS) have emerged as effective vehicles for enhancing bioavailability of poorly water soluble drugs, however solidification of the systems represents a major challenge. Objective of this study was development of carvedilol loaded liquid SMEDDS and transformation into solid pellets employing fluid-bed coating technologies. Carvediol-loaded formulation of SMEDDS was comprised of Capmul&...
Source: International Journal of Pharmaceutics - May 25, 2019 Category: Drugs & Pharmacology Source Type: research

PTS micelles for the delivery of hydrophobic methotrexate
Publication date: Available online 22 May 2019Source: International Journal of PharmaceuticsAuthor(s): Patrícia Cerqueira, Jennifer Noro, Sofia Moura, Diana Guimarães, Carla Silva, Artur Cavaco-Paulo, Ana LoureiroAbstractPolyoxyethanyl-α-tocopheryl sebacate (PTS) is an amphiphilic compound with self-emulsifying properties known to form micelles. In this work, we report the production of PTS micelles for the encapsulation and delivery of a hydrophobic derivative of methotrexate, MTX di-ethylated (MTX-OEt). We optimized the micelles production by testing two different techniques: auxiliary solvent and son...
Source: International Journal of Pharmaceutics - May 23, 2019 Category: Drugs & Pharmacology Source Type: research

pH-activated Heat Shock Protein Inhibition and Radical Generation Enhanced NIR Luminescence Imaging-guided Photothermal Tumour Ablation
Publication date: Available online 23 May 2019Source: International Journal of PharmaceuticsAuthor(s): Shuang Wang, Lin Li, Xiaohui Ning, Peidong Xue, Yuxin LiuAbstractPhotothermal therapy had great potential in being a new approach of tumour ablation due to their high selectivity and low side effect. However, the shallow penetration depth of near-infrared (NIR) irradiation resulted in the limited curative effect. Herein, a novel nanomedicine was developed based on the indocyanine green-loaded vanadium oxide nanocomposites (VO2-ICG) for pH-activated NIR luminescence imaging-guided enhanced photothermal tumour ablation. In ...
Source: International Journal of Pharmaceutics - May 23, 2019 Category: Drugs & Pharmacology Source Type: research

Development and characterization of nanobubbles containing paclitaxel and survivin inhibitor YM155 against lung cancer
Publication date: Available online 23 May 2019Source: International Journal of PharmaceuticsAuthor(s): Yücel Başpınar, Gülşah Erel-Akbaba, Mustafa Kotmakçı, Hasan AkbabaAbstractLung cancer remains 23% of cancer-related death worldwide, ranking on first place for men and second place for women. Almost each cancer type has a great deal in common, overexpression of the apoptosis inhibitor survivin. Chemotherapy with anticancer drugs is leading to side effects. Drug targeting by the use of nanobubbles is a useful strategy to reduce side effects. Nanobubbles in cancer are one of the most investigated carrie...
Source: International Journal of Pharmaceutics - May 23, 2019 Category: Drugs & Pharmacology Source Type: research

Naturally-derived electrospun wound dressings for target delivery of bio-active agents
Publication date: Available online 21 May 2019Source: International Journal of PharmaceuticsAuthor(s): Shohreh Fahimirad, Fatemeh AjalloueianAbstractElectrospun nanofibers are known as the advanced means for wound dressing. They have represented remarkable potency to encapsulate and deliver of biomolecules promoting wound healing process. Compared to synthetic polymers, naturally derived polymers (NDP) are more qualified candidates for fabrication of biomedical electrospun scaffolds. Not only nanofibers of NDP illustrate higher biocompatibility and biodegradability rates, but also they mimic the native extracellular matrix...
Source: International Journal of Pharmaceutics - May 22, 2019 Category: Drugs & Pharmacology Source Type: research

Design and evaluation of ionizable peptide amphiphiles for siRNA delivery
Publication date: Available online 22 May 2019Source: International Journal of PharmaceuticsAuthor(s): Patrick Neuberg, Alain Wagner, Jean-Serge Remy, Antoine KichlerAbstractSmall interfering RNAs (siRNAs) can down-regulate the expression of a target mRNA molecule in a sequence-specific manner, making them an attractive new class of drugs with broad potential for the treatment of diverse human diseases. Here, we report the synthesis of a series of cationic amphiphiles which were obtained by the coupling of amino acids and dipeptides onto a lipidic double chain. The new amphiphiles presenting a peptidic motif on a short hyd...
Source: International Journal of Pharmaceutics - May 22, 2019 Category: Drugs & Pharmacology Source Type: research

An enhanced charge-driven intranasal delivery of nicardipine attenuates brain injury after intracerebral hemorrhage
Publication date: Available online 20 May 2019Source: International Journal of PharmaceuticsAuthor(s): Tingwang Guo, Yuanyuan Guo, Yuhua Gong, Jingou Ji, Shilei Hao, Jia Deng, Bochu WangAbstractIntranasal drug delivery provided an alternative and effective approach for the intervention of an intracerebral hemorrhage (ICH). However, the short retention time at the absorption site and slow drug transport in intranasal gel influence the drug bioavailability and outcome of ICH. Herein, we fabricated a novel intranasal gel with oriented drug migration utilizing a charge-driven strategy to attenuate brain injury after ICH. Nicar...
Source: International Journal of Pharmaceutics - May 22, 2019 Category: Drugs & Pharmacology Source Type: research

Nonionic surfactants modulate the transport activity of ATP-binding cassette (ABC) transporters and solute carriers (SLC): Relevance to oral drug absorption
Publication date: Available online 21 May 2019Source: International Journal of PharmaceuticsAuthor(s): Ahmed A. Abdulhussein Al-Ali, Rasmus Blaaholm Nielsen, Bente Steffansen, René Holm, Carsten Uhd NielsenAbstractRecently, it has become evident that pharmaceutical excipients may interfere with the activity of ATP-binding cassette (ABC) transporters and solute carriers (SLC). The present review aims to provide an overview of surfactants shown to modulate substrate transport via SLCs and ABCs, and to discuss the relevance for oral drug absorption. In vitro, more than hundred surfactants have been suggested to decreas...
Source: International Journal of Pharmaceutics - May 22, 2019 Category: Drugs & Pharmacology Source Type: research

Development of daidzein nanosuspensions: preparation, characterization, in vitro evaluation, and pharmacokinetic analysis
Publication date: Available online 21 May 2019Source: International Journal of PharmaceuticsAuthor(s): Hui Wang, Yi Xiao, Hai Wang, Zechun Sang, Xiaole Han, Shuzhen Ren, Ruofei Du, Xiufeng Shi, Yan XieAbstractThe purpose of this investigation was to improve the solubility and oral bioavailability of daidzein via preparing nanosuspensions (NS) with steric stabilizers, electrostatic stabilizers, or a combination of both. Based on particle size and zeta potential, daidzein NS stabilized by HP-β-CD, soy lecithin, HP-β-CD + soy lecithin, TPGS, TPGS + SBE-β-CD, SDS, or HPMC E5 + SDS were generated and characterize...
Source: International Journal of Pharmaceutics - May 22, 2019 Category: Drugs & Pharmacology Source Type: research

Development and validation of a novel UPLC-ELSD method for the assessment of lipid composition of nanomedicine formulation
Publication date: Available online 18 May 2019Source: International Journal of PharmaceuticsAuthor(s): Mathieu Varache, Mathieu Ciancone, Anne-Claude CouffinAbstractLipid nanocarriers incorporating glycerides, polyethylene glycol (PEG)-stearates and phospholipids have attracted great attention for in vivo diagnostic, in vivo imaging, activated or non-activated targeted drug delivery. For quality control purposes, the development of appropriate methods for the quantification of their lipid components is needed. In the present study, we developed an analytical method for lipid quantification in formulated nanoparticles. PEG-...
Source: International Journal of Pharmaceutics - May 20, 2019 Category: Drugs & Pharmacology Source Type: research

Anandamide-Nanoformulation Obtained by Electrospraying for Cardiovascular Therapy
Publication date: Available online 18 May 2019Source: International Journal of PharmaceuticsAuthor(s): Virna Margarita Martín Giménez, Patricia Díaz-Rodríguez, Raúl Lelio Sanz, María Vivero-López, Angel Concheiro, Emiliano Diez, Natalia Prado, Diego Enrique Kassuha, Carmen Alvarez-Lorenzo, Walter ManuchaAbstractAnandamide (AEA), an endogenous cannabinoid, has a relevant antihypertensive effect. However, its cardioprotective role has been barely explored due to unfavorable physico-chemical properties and, sometimes, undesirable psychoactive effects. In this context, drug enca...
Source: International Journal of Pharmaceutics - May 20, 2019 Category: Drugs & Pharmacology Source Type: research

The Biopharmaceutics Classification System (BCS) and the Biopharmaceutics Drug Disposition Classification System (BDDCS): Beyond guidelines
Publication date: Available online 17 May 2019Source: International Journal of PharmaceuticsAuthor(s): Aggelos Charalabidis, Maria Sfouni, Christel Bergström, Panos. MacherasAbstractThe recent impact of the Biopharmaceutics Classification System (BCS) and the Biopharmaceutics Drug Disposition Classification System (BDDCS) on relevant scientific advancements is discussed. The major advances associated with the BCS concern the extensive work on dissolution of poorly absorbed BCS class II drugs in nutritional liquids (e.g. milk, peanut oil) and biorelevant media for the accurate prediction of the rate and the extent of o...
Source: International Journal of Pharmaceutics - May 18, 2019 Category: Drugs & Pharmacology Source Type: research

Shedding Light on Coatings: Real-time Monitoring of Coating Quality at Industrial Scale
This study examines OCT’s applicability to an industrial-scale pan coating process. Automated layer detection, classification and thickness calculation were executed in real time. To evaluate the system’s performance, runs with various tablet size, coating solution concentration and operating parameters were carried out and monitored. Our results indicate that, in addition to correct end-point determination, OCT enables real-time monitoring of the coating processes (thickness, homogeneity and roughness) and can support active process control by supplying information about the coating thickness and quality.Graph...
Source: International Journal of Pharmaceutics - May 18, 2019 Category: Drugs & Pharmacology Source Type: research

Sensitivity of a Continuous Hot-Melt Extrusion and Strand Pelletization Line to Control Actions and Composition Variation
Publication date: Available online 16 May 2019Source: International Journal of PharmaceuticsAuthor(s): T.R. Hörmann, J. Rehrl, O. Scheibelhofer, L.M. Schaden, A. Funke, C. Makert, J.G. KhinastAbstractThe purpose of this work was to develop a robust hot-melt extrusion and strand pelletization process for manufacturing pellets with an immediate release (IR) of a poorly water-soluble active pharmaceutical ingredient (API), nimodipine. The robustness of pharmaceutical continuous manufacturing processes and of its control strategy is vital for competitiveness to traditional batch-manufacturing. Therefore, first the sensiti...
Source: International Journal of Pharmaceutics - May 17, 2019 Category: Drugs & Pharmacology Source Type: research

A human skin high-throughput formulation screening method using a model hydrophilic drug
Publication date: Available online 15 May 2019Source: International Journal of PharmaceuticsAuthor(s): Patricia P. Martins, Arnold D. Estrada, Hugh D.C. SmythAbstractFranz cell (FC) experiments in topical and transdermal drug development represent the gold standard in vitro method but require a relatively high quantity of human skin, are low-throughput, and are time-consuming to perform. To address these issues, we studied a micro-well plate-based screening method for permeability and retention that could enable the direct screening of large numbers of formulations simultaneously across human skin. Using freshly excised de...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Rapid and continuous accumulation of nitric oxide-releasing liposomes in tumors to augment the enhanced permeability and retention (EPR) effect
Publication date: Available online 15 May 2019Source: International Journal of PharmaceuticsAuthor(s): Takuma Yoshikawa, Yukina Mori, Haitao Feng, Khanh Quoc Phan, Akihiro Kishimura, Jeong-Hun Kang, Takeshi Mori, Yoshiki KatayamaAbstractThe modulation of blood flow to tumors is a prominent strategy for improving the tumor accumulation of nanomedicines, resulting from the enhanced permeability and retention (EPR) effect. We previously reported a promising EPR enhancer—a nitric oxide (NO) donor-containing liposome (NO-LP)—which showed enhanced accumulation in tumor tissue. Herein, we study NO-LP in greater detail...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Strategizing biodegradable polymeric nanoparticles to cross the biological barriers for cancer targeting
Publication date: Available online 15 May 2019Source: International Journal of PharmaceuticsAuthor(s): Hira Choudhury, Bapi Gorain, Manisha Pandey, Rajneet Kaur, Prashant KesharwaniAbstractThe biological barriers in the body have been fabricated by nature to protect the body from foreign molecules. The successful delivery of drugs is limited and being challenged by these biological barriers including gastrointestinal tract, brain, skin, lungs, nose, mouth mucosa and immune system. In this review article, we envisage to understand the functionalities of these barriers and revealing various drug-loaded biodegradable polymeri...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of Bioactive Rifampicin loaded κ-Car-MA-INH/Nano Hydroxyapatite Composite for Tuberculosis Osteomyelitis Infected Tissue Regeneration
Publication date: Available online 15 May 2019Source: International Journal of PharmaceuticsAuthor(s): Rajendran Amarnath Praphakar, Murugan Sumathra, Rajadas Sam Ebenezer, Sounderrajan Vignesh, Harshavardhan Shakila, Mariappan RajanAbstractBiocompatible polymers and ceramic materials have been identified as vital components to fabricate drug delivery and tissue engineering applications because of their high drug loading capability, sustained release and higher mechanical strength with remarkable in-vivo bioavailability. In the present work, initially we designed κ-carrageenan grafted with maleic anhydride and then r...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Influence of the feed frame design on the powder behavior and the residence time distribution
The objective of the present study was to investigate the effect of different feed frame designs of a production-scale rotary tablet press on the residence time distribution of two microcrystalline cellulose blends, one of them serving as a tracer blend and the other serving as a filling material. With these powder blends, the effect of a reduction of the filling volume of a three chamber feed frame on the powder residence time was investigated. It was shown, that the volume reduction of the three chamber feed frame equipped with three modified large hub wheels led to a decrease of the powder residence time as well as to l...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Complex amorphous solid dispersions based on poly(2-hydroxyethyl methacrylate): study of drug release from a hydrophilic insoluble polymeric carrier in the presence and absence of a porosity increasing agent
Publication date: Available online 16 May 2019Source: International Journal of PharmaceuticsAuthor(s): Melissa Everaerts, Guy Van den MooterAbstractAmorphous solid dispersions are nowadays typically made up of a drug compound and a water-soluble polymer. However, recently it has been demonstrated that amorphous solid dispersions based on insoluble polymers have a different and more delayed drug release profile, resulting in a prolonged duration of supersaturation. In this paper, binary and ternary amorphous solid dispersions based on poly(2-hydroxyethyl methacrylate) were prepared through spray drying to further investigat...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

A Biocompatible and Easy-to-make Polyelectrolyte Dressing with Tunable Drug Delivery Properties for Wound Care
The objective of this study is to address these problems by developing a tunable, biocompatible, and biodegradable CS-based dressing for wound treatment. The dressing is fabricated via electrostatic interactions between CS and carmellose (CM). Its swelling properties, erosion behavior, loading efficiency and drug release sustainability can be tuned by simply changing the CS/CM mass-to-mass ratio. Upon loaded with minocycline, the dressing effectively protects the wounds in mice from infection and enhances wound closure. Regarding its high tunability and promising in vivo performance, our dressing warrants further developme...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 10 June 2019Source: International Journal of Pharmaceutics, Volume 564Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Improved oral bioavailability of the anticancer drug catechin using chitosomes: Design, in-vitro appraisal and in-vivo studies
This study aimed to elaborate catechin loaded chitosan-tethered liposomes (chitosomes) to enhance catechin oral bioavailability. Nanocarriers were optimized via ethanol injection method followed by physicochemical, ex vivo and biological appraisal in male Wistar albino rats. Results demonstrated that chitosomes possessed excellent nanosize of 137 nm, monodispersity (PDI
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

In-vitro evaluation of solid lipid nanoparticles: ability to encapsulate, release and ensure effective protection of peptides in the gastrointestinal tract
The objective of this study was to encapsulate a model water-soluble peptide in biodegradable and biocompatible solid lipid-based nanoparticles, i.e. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) in order to protect it from metabolic degradation. Leuprolide (LEU) and a LEU-docusate Hydrophobic Ion Pair (HIP) were encapsulated in SLN and NLC by High Pressure Homogenization. The particles were characterized regarding their Encapsulation Efficiency (EE), size, morphology, peptide release in FaSSIF-V2, and protective effect towards proteases. Nanoparticles of 120 nm with platelet structures were obtai...
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

Correlation between the solid state of lipid coating and release profile of API from hot melt coated microcapsules
Publication date: Available online 14 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sharareh Salar-Behzadi, Carolina Corzo, Lisa Schaden, Peter Laggner, Andreas ZimmerAbstractSolvent-free hot melt coating (HMC) provides a safer and more economic process compared to the conventional solvent coating techniques. However, drug release instability and the lack of fundamental understanding on it are limiting factors for application of HMC for industrial productions. In this work, we investigated glyceryl dibehenate, glyceryl monostearate and behenoyl polyoxyl-8 glyceride as HMC materials. The microstructure an...
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

Tableting performance of various mannitol and lactose grades assessed by compaction simulation and chemometrical analysis
Publication date: Available online 13 May 2019Source: International Journal of PharmaceuticsAuthor(s): Shubhajit Paul, Pirjo Tajarobi, Catherine Boissier, Changquan Calvin SunAbstractMannitol and lactose are commonly used fillers in pharmaceutical tablets, available in several commercial grades that are produced using different manufacturing processes. These grades significantly differ in particulate and powder properties that impact tablet manufacturability. Choice of sub-optimum type or grade of excipient in tablet formulation can lead to manufacturing problems and difficulties, which are magnified during a continuous ma...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Predicting tablet tensile strength with a model derived from the gravitation-based high-velocity compaction analysis data
In this study it was finally concluded, that the data obtained by the method was of practical relevance in pharmaceutical formulation development.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Photochemically stabilized formulation of dacarbazine with reduced production of algogenic photodegradants
Publication date: 10 June 2019Source: International Journal of Pharmaceutics, Volume 564Author(s): Atsushi Uchida, Hiroto Ohtake, Yukiko Suzuki, Hideyuki Sato, Yoshiki Seto, Satomi Onoue, Toshio OguchiAbstractThe present study aimed to develop a photochemically stabilized formulation of dacarbazine [5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide; DTIC] for reducing the production of algogenic photodegradant (5-diazoimidazole-4-carboxamide; Diazo-IC). Photochemical properties of DTIC were characterized by UV-visible light spectral analysis, reactive oxygen species (ROS) assay, and photostability testing. A pharmacokinet...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Targeted drug delivery to the brain via intranasal nanoemulsion: available proof of concept and existing challenges
Publication date: Available online 13 May 2019Source: International Journal of PharmaceuticsAuthor(s): Bappaditya Chatterjee, Bapi Gorain, Keithanchali Mohananaidu, Pinaki Sengupta, Uttam Kumar Mandal, Hira ChoudhuryAbstractIntranasal delivery has shown to circumvent blood-brain-barrier (BBB) and deliver the drugs into the CNS at a higher rate and extent than other conventional routes. The mechanism of drug transport from nose-to-brain is not fully understood yet, but several neuronal pathways are considered to be involved. Intranasal nanoemulsion for brain targeting is investigated extensively. Higher brain distribution o...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization of miRNA Delivery by using a Polymeric Conjugate based on Deoxycholic Acid-Modified Polyethylenimine
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fatemeh Radmanesh, Hamid Sadeghi Abandansari, Sara Pahlavan, Mehdi Alikhani, Mahdi Karimi, Sarah Rajabi, Bahram Kazemi Demneh, Hossein BaharvandAbstractSafe and efficient delivery of microRNA (miRNA) molecules is essential for their successful transition from research to the clinic setting. In the present study, we have used a bile acid, deoxycholic acid (DA), to modify 1.8 kDa branched polyethylenimine (bPEI1.8) and subsequently investigated gene delivery features of the resultant conjugates (PEI-DAn). We found significa...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

The Development of an Inline Raman Spectroscopic Analysis Method as a Quality Control Tool for Hot Melt Extruded Ramipril Fixed-dose Combination Products
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): G.P. Andrews, D.S. Jones, Z. Senta-Loys, A. Almajaan, S. Li, O. Chevallier, C. Elliot, A.M. Healy, J.F. Kelleher, A.M. Madi, G.C. Gilvary, Y. TianAbstractCurrently in the pharmaceutical industry, continuous manufacturing is an area of significant interest. In particular, hot-melt extrusion (HME) offers many advantages and has been shown to significantly reduce the number of processing steps relative to a conventional product manufacturing line. To control product quality during HME without process interruption, integratio...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Prediction of dissolution profiles by non-destructive NIR spectroscopy in bilayer tablets
This study describes how near infrared (NIR) spectroscopy can be used to predict the dissolution of bilayer tablets as a non-destructive approach. Tablets in this study consist of two APIs physically separated in layers and manufactured under three levels of hardness. NIR spectra were acquired for each layer in diffuse reflectance mode. Reference dissolution profile values were obtained using dissolution apparatus & HPLC. A multivariate PLS calibration model was developed for each API relating its dissolution profile with to spectral data. This calibration model was used to predict dissolution profile of an independent...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Novel Polyurethane-based nanoparticles of infliximab to reduce inflammation in an in-vitro intestinal epithelial barrier model
In this study we examined the potential of novel biodegradable polymers of polyesterurethane (PU), and its PEGylated (PU-PEG) form as nanocarriers of Infliximab (INF), to treat inflammation in an in-vitro epithelial model. Nanoparticles (NPs) formulated were of average size of 200-287nm. INF loading of NPs (INF-NPs) resulted in an increase in size and zeta potential. No cytotoxicity was observed for any of the NPs. Cellular interaction and uptake of PU NPs were similar compared with polycaprolactone (PCL) NPs and significantly higher to Poly(lactic-co-glycolic) acid (PLGA) NPs. Cellular interaction was higher for correspon...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

MRP2-mediated transport of etoposide in MDCKII MRP2 cells is unaffected by commonly used non-ionic surfactants
In conclusion, etoposide transport across MDCKII MRP2 cells was modulated by cyclosporine A, an inhibitor of MRP2 and P-gp, but not by specific P-gp inhibitors (valspodar and zosuquidar), which suggests that etoposide transport is primarily influenced by MRP2. In addition, commonly used non-ionic surfactants did not decrease MRP2-mediated etoposide transport in MDCKII MRP2 cells. These results suggest that etoposide transport in MDCKII MRP2 cells is a model system to investigate MRP2 interactions, and that surfactants may not have a large potential for increasing oral bioavailability of drugs through inhibition of MRP2 tra...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluating the potential of drug eluting contact lenses for treatment of bacterial keratitis using an ex vivo corneal model
This study aims to investigate the effectiveness of ofloxacin-loaded contact lenses as prolonged release devices for the treatment of bacterial keratitis.Two silicone hydrogel contact lenses (SHCLs) Senofilcon A (ACUVUE OASYS®) and Narafilcon A (ACUVUE TRUEYE®) were modified by incorporation of ofloxacin alone or with vitamin E (VE). The drug uptake and in vitro release kinetics were investigated and the antibacterial efficacy was assessed against Staphylococcus aureus and Pseudomonas aeruginosa in an ex vivo rabbit corneal model.The in vitro studies showed a higher uptake (p≤ 0.05) and longer duration of releas...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Drug stability and product performance characteristics of a dapivirine-releasing vaginal ring under simulated real-world conditions
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Diarmaid J. Murphy, Clare F. McCoy, Peter Boyd, Tiffany Derrick, Patrick Spence, Brid Devlin, R. Karl MalcolmAbstractIn two recent Phase III clinical trials, use of a 25 mg dapivirine vaginal ring significantly reduced HIV acquisition rates. Post hoc analysis from one of the trials indicated higher rates of protection among women over the age of 21 years when compared to younger women, most likely due to reduced adherence in the latter group. There is currently no information available on how release of dapivirine from th...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Application of an automated small-scale in vitro transfer model to predict in vivo precipitation inhibition
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Christian Jede, Christian Wagner, Holger Kubas, Christian Weber, Markus Weigandt, Mirko Koziolek, Werner WeitschiesAbstractThe majority of NCEs are weakly basic drugs. Consequently, their solubility is highly pH-dependent, with higher solubility in the acidic stomach and poor solubility in the neutral intestinal environment. The gastric emptying of dissolved drug can lead to the intestinal precipitation of the drug. One option of reducing this process is to formulate the drug together with a precipitation inhibitor (PI). ...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Diversity of β-cyclodextrin-based nanosponges for transformation of actives
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sandip Pawar, Pravin Shende, Francesco TrottaAbstractβ-Cyclodextrin-based nanosponges (β-CDNSs) play an important role in new arrays of agriculture, floriculture, cosmetics, medicine, high molecular weight proteins, novel flame retardants, gas carriers and water filters. In recent years, the field of advance nanostructured systems witnesses a rapid development due to miniaturization, dose-reduction, sustained and controlled release of actives and long-term stability of material. β-CDNSs are colloidal and cr...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of the solid state form of tadalafil in sub-micron thin films using nanomechanical infrared spectroscopy
Publication date: Available online 9 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fatemeh Samaeifar, Andrea Casci Ceccacci, Sanjukta Bose Goswami, Line Hagner Nielsen, Ahmad Afifi, Kinga Zór, Anja BoisenAbstractAssessing physical stability of drugs is important both in the development as well as in the production phase in the pharmaceutical industry. We used nanomechanical infrared (NAM-IR) spectroscopy based on photothermal response of a nanomechanical resonator, to investigate the solid state forms of tadalafil (TAD), under various storage conditions in sub-micron thin films. The amorphous TAD ...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Biodistribution/Biostability Assessment of siRNA after Intravenous and Intratracheal Administration to Mice, Based on Comprehensive Analysis of In Vivo/Ex Vivo/Polyacrylamide Gel Electrophoresis Fluorescence Imaging
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Tomoyuki Okuda, Yoko Toyoda, Takashi Murakami, Hirokazu OkamotoAbstractWe performed in vivo/ex vivo/polyacrylamide gel electrophoresis (PAGE) fluorescence imaging of near-infrared fluorescence (NIRF)-labeled siRNA (Cy5.5-siGL3) in mice to investigate the validity of each fluorescence imaging result as the biodistribution/biostability assessment of siRNA. Statistically significant correlations could be obtained between the in vivo and ex vivo fluorescence intensities of Cy5.5 in the relevant regions/tissues, except the lun...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Phase transition and release kinetics of polyphenols encapsulated lyotropic liquid crystals
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Heng Zhang, Zhongni WangAbstractIn this paper, the lyotropic liquid crystals formed in SL/IP/H2O system were prepared as a drug carrier system to encapsulate polyphenols. The components and introduction of drug had influences in the structure and rheological properties of lyotropic liquid crystals. The structure underwent a phase transition from lamellar phase (Lα) to Lα+HII (reverse hexagonal phase) mixed phases and micelle by increasing its IP/H2O mass ratio from 5/35 to 20/20 and 35/5, consistent with the t...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research