Engineering of pharmaceutical cocrystals in an excipient matrix: spray drying versus hot melt extrusion
In conclusion, in order to reduce the number of unit operations required to produce a final pharmaceutical product, spray drying showed higher feasibility over HME to produce cocrystals within a carrier excipient.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 15, 2018 Category: Drugs & Pharmacology Source Type: research

Application of a chromatic confocal measurement system as new approach for in-line wet film thickness determination in continuous oral film manufacturing processes
Publication date: Available online 14 September 2018Source: International Journal of PharmaceuticsAuthor(s): Svenja Niese, Julian QuodbachAbstractThe key parameter of the oral film production process is the wet film thickness since it regulates the active pharmaceutical ingredient (API) content of the finished product. There is no general recommendation on how to adjust the gap height of the coating knife during the film manufacturing process to obtain the target content. Therefore, trial and error approaches are common to determine the surplus of drug for every newly developed formulation. This wastes resources, money and...
Source: International Journal of Pharmaceutics - September 15, 2018 Category: Drugs & Pharmacology Source Type: research

Synergy of nebulized phage PEV20 and ciprofloxacin combination against Pseudomonas aeruginosa
In conclusion, nebulized phage PEV20 and ciprofloxacin combination shows promising antimicrobial and aerosol characteristics for potential treatment of respiratory tract infections caused by drug-resistant P. aeruginosa.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

Facile Marriage of Gd3+ to Polymer-coated Carbon Nanodots with Enhanced Biocompatibility for Targeted MR/Fluorescence Imaging of Glioma
Publication date: Available online 14 September 2018Source: International Journal of PharmaceuticsAuthor(s): Yilin Du, Min Qian, Chengyi Li, Huiling Jiang, Yafeng Yang, Rongqin HuangAbstractOvercoming blood-brain barrier (BBB) for precise glioma diagnosis remains an urgent challenge due to its peculiar location in central nervous system (CNS). Herein, polymer-coated carbon nanodots with high hydrophilicity were facilely married with Gd-DTPA to construct a dual-modal imaging system (NCDDG). This system was demonstrated with obviously decreased toxicity and enhanced magnetic resonance imaging (MRI) ability compared to tradit...
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

The mechanism behind the biphasic pulsatile drug release from physically mixed poly(DL-lactic(-co-glycolic) acid)-based compacts
Publication date: Available online 14 September 2018Source: International Journal of PharmaceuticsAuthor(s): Max Beugeling, Niels Grasmeijer, Philip A. Born, Merel van der Meulen, Renée S. van der Kooij, Kevin Schwengle, Lieven Baert, Katie Amssoms, Henderik W. Frijlink, Wouter L.J. HinrichsAbstractSuccessful immunization often requires a primer, and after a certain lag time, a booster administration of the antigen. To improve the vaccinees’ comfort and compliance, a single-injection vaccine formulation with a biphasic pulsatile release would be preferable. Previous work has shown that such a release profile c...
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

Investigations on the interactions between curcumin loaded Vitamin E TPGS coated nanodiamond and Caco-2 cell monolayer
This study aimed at investigating the potential mechanism of improved transportation of the curcumin loaded D-α-tocopherol polyethylene glycol 1000 succinate coated nanodiamonds system (NDs/CUR/TPGS complexes) using an in vitro Caco-2 cell monolayer model. The core-shell structured NDs/CUR/TPGS nanocomplexes were 196.32 ± 5.76 nm in size, with a high loading efficiency of 81.59±3.42 %. Cytotoxicity results suggested that the blank NDs did not induce any serious toxicity on Caco-2 cells even after incubated for 72h. The cell viability for all the series of CUR loaded preparations was found to follow the ...
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

Reconstituted spray-dried phenytoin-loaded nanocapsules improve the in vivo phenytoin anticonvulsant effect and the survival time in mice
This study evaluated the in vivo anticonvulsant effect of a spray-dried powder for reconstitution containing phenytoin-loaded lipid-core nanocapsules. The effect of chitosan coating on redispersibility, gastrointestinal stability, and drug release from nanoparticles was evaluated during the development of the powders. Maltodextrin was used as adjuvant in the spray-drying process. Chitosan coating played an important role in redispersibility, and large particles (> 100 μm) were obtained using the highest concentration of solids in the feed. However, after aqueous redispersion, volume-based particle size was reduced to...
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

Determination of intestinal permeability using in situ perfusion model in rats: challenges and advantages to BCS classification applied to digoxin
Publication date: Available online 13 September 2018Source: International Journal of PharmaceuticsAuthor(s): Tamires Guedes Caldeira, Alejandro Ruiz-Picazo, Isabel Lozoya-Agullo, Dênia Antunes Saúde-Guimarães, Marta González-Álvarez, Jacqueline de Souza, Isabel González-Álvarez, Marival BermejoAbstractThe purpose of this work was to describe the closed loop in situ perfusion method in rats and to compare the difficulties and advantages with other methods proposed by regulatory agencies for BCS classification and finally to illustrate its application to evaluate the permeabili...
Source: International Journal of Pharmaceutics - September 14, 2018 Category: Drugs & Pharmacology Source Type: research

Polyvinylpyrrolidone affects thermal stability of drugs in solid dispersions
Publication date: Available online 11 September 2018Source: International Journal of PharmaceuticsAuthor(s): Yasmine Ben Osman, Tatsiana Liavitskaya, Sergey VyazovkinAbstractThe present study explores the hypothesis that a polymer can affect the thermal stability of a drug in solid polymer-drug dispersions. The hypothesis is tested in a systematic fashion by combining isoconversional kinetic analysis with thermogravimetric measurements on several solid dispersions. Experimental systems involve three drugs: indomethacin (IMC), felodipine (FD), and nifedipine (ND) and their solid dispersions with polyvinylpyrrolidone (PVP). ...
Source: International Journal of Pharmaceutics - September 12, 2018 Category: Drugs & Pharmacology Source Type: research

Potential Role of Stromal Collagen in Cystine Crystallization in Cystinosis Patients
Publication date: Available online 12 September 2018Source: International Journal of PharmaceuticsAuthor(s): Phillip Dixon, Keith Christopher, Anuj ChauhanAbstractCystinosis is a genetic disease that leads to the accumulation of intracellular cystine crystals in all organs including cornea due to the loss of cystine efflux transporters in the lysosome of the cells. While the mechanism for formation of intracellular cystine is well understood for most organs, it does not explain many observations for crystal accumulation in the cornea of cystinosis patients. First, the crystals in cornea are extracellular and needle-like wi...
Source: International Journal of Pharmaceutics - September 12, 2018 Category: Drugs & Pharmacology Source Type: research

Directing the nanoparticle formation by the combination with small molecular assembly and polymeric assembly for topical suppression of ocular inflammation
Publication date: Available online 10 September 2018Source: International Journal of PharmaceuticsAuthor(s): Jinhai Huang, Xinxin Yu, Yanfang Zhou, Renshu Zhang, Qianqian Song, Qinmei Wang, Xingyi LiAbstractIn this paper, we presented a simple yet versatile strategy to generate a high drug payload nanoparticles by the combination with small molecular assembly and polymeric assembly for topical suppression of ocular inflammation. Upon physical mixing of the succinated triamcinolone acetonide (TA-SA) supramolecular hydrogel with the poly (ethylene glycol)-poly (ɛ-caprolactone)-poly (ethylene glycol) (PECE) aqueous solution ...
Source: International Journal of Pharmaceutics - September 11, 2018 Category: Drugs & Pharmacology Source Type: research

Prevention of corneal neovascularization by subconjunctival injection of avastin® loaded thermosensitive hydrogels in rabbit model
Publication date: Available online 11 September 2018Source: International Journal of PharmaceuticsAuthor(s): Xu Xu, Jing Yu, Hui Shi, Jie Zhang, Xingyi LiAbstractThe antibody avastin® (Ava) has been clinically to treat various intraocular neovascular diseases, but suffering from the rapid clearance and short shelf-life of Ava in the requirement of frequent administration. In the present study, we reports the sustained release of Ava from a thermosensitive hydrogel based on poly(ethylene glycol)-poly(ɛ-caprolactone)-poly(ethylene glycol) (PECE) copolymer for the control of corneal neovascularization in rabbit model. Av...
Source: International Journal of Pharmaceutics - September 11, 2018 Category: Drugs & Pharmacology Source Type: research

Comparative study of the therapeutic effect of Doxorubicin and Resveratrol combination on 2D and 3D (spheroids) cell cultures models
In this study, the therapeutic effect and the synergistic potential of a particular drug-combination towards 2D and 3D cell cultures of pancreatic cancer were compared for the first time. Thus, the effect of Doxorubicin:Resveratrol (DOX:RES) combinations (at molar ratios ranging from 5:1 to 1:5) in the viability of PANC-1 cells cultured as 2D monolayers and as 3D spheroids was analyzed. The results showed that the cells’ viability was more affected when DOX:RES combinations containing higher contents of RES (1:2 to 1:5 molar ratios) were used. This can be explained by the ability of RES to reduce the P-glycoprotein (...
Source: International Journal of Pharmaceutics - September 11, 2018 Category: Drugs & Pharmacology Source Type: research

Dry powder inhaler formulations of poorly water-soluble itraconazole: A balance between in-vitro dissolution and in-vivo distribution is necessary
Publication date: Available online 11 September 2018Source: International Journal of PharmaceuticsAuthor(s): Zhengwei Huang, Ling Lin, Cushla Mc Goverin, Hu Liu, Lili Wang, Qi Tony Zhou, Ming Lu, Chuanbin WuGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2018 Category: Drugs & Pharmacology Source Type: research

Improved anticancer efficacy of doxorubicin mediated by human-derived cell-penetrating peptide dNP2
Publication date: Available online 8 September 2018Source: International Journal of PharmaceuticsAuthor(s): Yucheng Xiang, Wei shan, Yuan HuangAbstractAlthough cell penetrating peptides (CPPs) have been extensively studied as an approach to deliver anti-cancer drugs into the tumor cells for the last 30 years, no FDA-approved CPP-based drugs are available, implying that the existing CPPs may have less efficiency in human or have side effects such as toxicity. Herein, we established a tumor targeting drug delivery system by attaching a human-derived cell-penetrating peptide dNP2 (CKIKKVKKKGRKKIKKVKKKGRK) to N-(2- hydroxyprop...
Source: International Journal of Pharmaceutics - September 9, 2018 Category: Drugs & Pharmacology Source Type: research

Tocopherol-loaded transfersomes: in vitro antioxidant activity and efficacy in skin regeneration
Publication date: Available online 7 September 2018Source: International Journal of PharmaceuticsAuthor(s): Carla Caddeo, Maria Letizia Manca, Josè Esteban Peris, Iris Usach, Octavio Diez-Sales, Maria Matos, Xavier Fernàndez-Busquets, Anna Maria Fadda, Maria ManconiAbstractTransfersomes were prepared by using different polysorbates (i.e., Tween 20, 40, 60 and 80) and loaded with tocopherol acetate, a naturally-occurring phenolic compound with antioxidant activity. The vesicles showed unilamellar morphology, small size (∼85 nm), low polydispersity index (≤0.27), and high entrapment efficiency, which inc...
Source: International Journal of Pharmaceutics - September 8, 2018 Category: Drugs & Pharmacology Source Type: research

Personalized orodispersible films by hot melt ram extrusion 3d printing
Publication date: Available online 8 September 2018Source: International Journal of PharmaceuticsAuthor(s): Umberto M. Musazzi, Francesca Selmin, Marco A. Ortenzi, Garba Khalid Mohammed, Silvia Franzé, Paola Minghetti, Francesco CilurzoAbstractThis work demonstrated the feasibility of the extemporaneous preparation of maltodextrins orodispersible films (ODF) by hot-melt ram-extrusion 3D printing. This method consists of three simple technological operations which can be also implemented in a pharmacy setting. First, maltodextrins, drug, and other excipients are mixed in a mortar and wetted with the plasticizer (i.e....
Source: International Journal of Pharmaceutics - September 8, 2018 Category: Drugs & Pharmacology Source Type: research

Polysorbate 20 non-ionic surfactant enhances retinal gene delivery efficiency of cationic niosomes after intravitreal and subretinal administration
Publication date: 25 October 2018Source: International Journal of Pharmaceutics, Volume 550, Issues 1–2Author(s): Ilia Villate-Beitia, Idoia Gallego, Gema Martínez-Navarrete, Jon Zárate, Tania López-Méndez, Cristina Soto-Sánchez, Edorta Santos-Vizcaíno, Gustavo Puras, Eduardo Fernández, José Luis PedrazAbstractThe success of non-viral vectors based on cationic niosomes for retinal gene delivery applications depends on the ability to achieve persistent and high levels of transgene expression, ideally from a single administration. In this work, we studied the effe...
Source: International Journal of Pharmaceutics - September 8, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-bilayer-coated nanogels allow for sustained release and enhanced internalization
In conclusion, by formulating the organogel into the lipid bilayers, gel-liposomes were developed, allowing for sustained drug release, improved internalization and the resultant enhancement of cytotoxicity of chemotherapy agent to cancer cells.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 7, 2018 Category: Drugs & Pharmacology Source Type: research

Investigation on the impact of powder arching in small die filling
In this study, die fill performance of coarse and free-flowing nonpareils was evaluated using a specially designed die filling device in order to investigate the impact of non-cohesive arching during die fill under gravity flow. Through evaluating die fill performance, the arching phenomenon during dynamic conditions of die fill could be captured. Nonpareils with large particle size increased the likelihood of arching and caused poorer die fill performance for narrow orifices. In contrast, die fill in large orifices was generally better with larger particles due to reduced inter-particulate friction. Both particle size and...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Manufacturing and Characterization of Long-Acting Levonorgestrel Intrauterine Systems
In this study, a twin-syringe method with a customized mold was developed to manufacture hollow cylindrical polydimethylsiloxane (PDMS)-based levonorgestrel intrauterine systems (LNG-IUSs). Different mold materials, curing temperatures and times were screened to fabricate PDMS-drug reservoirs with good quality characteristics (easy demolding, good appearance and appropriate physicochemical characteristics). The prepared PDMS-drug reservoirs were covered with the release rate controlling membrane to fabricate the LNG-IUSs. Physicochemical characterization (drug content and content uniformity, powder X-Ray diffraction (PXRD)...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Vaginal Bifidobacterium breve for preventing urogenital infections: development of delayed release mucoadhesive oral tablets
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): Barbara Giordani, Luz Maria Melgoza, Carola Parolin, Claudio Foschi, Antonella Marangoni, Angela Abruzzo, Francesco Dalena, Teresa Cerchiara, Federica Bigucci, Barbara Luppi, Beatrice VitaliAbstractBifidobacteria are predominant microorganisms in the intestinal flora, but at the same time represent a subdominant group of the vaginal microbiota. For this reason, oral administration of these probiotic bacteria can provide beneficial effect for both intestinal and urogenital ecosystems.The first aim of this study was to...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Downscaling of the tableting process: feasibility of miniaturized forced feeders on a high-speed rotary tablet press
Publication date: Available online 6 September 2018Source: International Journal of PharmaceuticsAuthor(s): W. Grymonpré, B. Blahova Prudilova, V. Vanhoorne, B. Van Snick, F. Detobel, J.P. Remon, T. De Beer, C. VervaetAbstractWith the current transformation of the pharmaceutical industry towards continuous manufacturing, there is an inherent need to embrace this concept already during the early stages of drug formulation. Therefore, this research paper investigated the feasibility of using miniaturized forced feeders on a high-speed rotary tablet press with the intention of downscaling the tableting process. Forced ...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of excipients on encapsulation and release of insulin from spray-dried solid lipid microparticles
In conclusion, spray drying a solution containing both lipids and protein-phospholipid complex is a promising method for encapsulating protein into solid lipid MP, which can be used for sustained delivery of protein drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Loading studies of the anticancer drug Camptothecin into dual stimuli-sensitive nanoparticles. Stability scrutiny
Publication date: Available online 6 September 2018Source: International Journal of PharmaceuticsAuthor(s): Nieves Iglesias, Elsa Galbis, M. Jesús Díaz-Blanco, M.-Violante de-Paz, Juan A. GalbisAbstractIn recent years, the preparation of valuable drug delivery systems (DDS) from self-assembled amphiphilic copolymers has attracted much attention since these nanomaterials provide new opportunities to solve problems such as the lack of solubility in water of lipophilic drugs, improve their bioavailability, prolong their circulation time and decrease the side effects associated with their administration. In the c...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Novel Drug Delivery Systems for Natural Extracts: The Case Study of Vitis Vinifera Extract-SiO2 Nanocomposites
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): A. Scano, F. Ebau, M.L. Manca, V. Cabras, F. Cesare Marincola, M. Manconi, M. Pilloni, A.M. Fadda, G. EnnasAbstractBall Milling technique has been used to prepare for the first time Vitis Vinifera extract-silica nanocomposites (VV- SiO2 NCs), which combine the pharmacological effects of the extract with the effectiveness of silica as drug delivery system and active component in the treatment of wound healing. Different contents (1.0, 9.0 and 33.0 wt%) of Vitis Vinifera ethanolic extract were loaded into the silica ma...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

In Vivo Evaluation of Chitosan Based Local Delivery Systems for Atorvastatin in Treatment of Periodontitis
In this study, the effect of locally delivered atorvastatin (2% w/v) containing chitosan formulations in the treatment of periodontitis was evaluated in rats with ligature induced periodontitis. The levels of interleukin-1beta (IL-1β), IL-6, IL-8, IL-10, transforming growth factor-β1 (TGF-β1), TGF-β2 and TGF-β3 were measured after treatment with formulations. Histomorphometric analysis included the measurements of the area of alveolar bone and the distance between cemento-enamel junction (CEJ) and connective tissue attachment to tooth. Inflammatory and osteoclastic activity scores were given semiqu...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

A novel test system for the evaluation of oral mucoadhesion of fast disintegrating tablets
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): Anja Hoffmann, Rolf DanielsAbstractOromucosal drug delivery is necessary when a local effect in the oral cavity is required. Bioadhesive formulations should be advantageous because a larger fraction of the active principal is retained at the site of action allowing for an enhanced and prolonged effect. Despite a variety of mucoadhesion test systems being described in literature, none of these in-vitro tests does relate to physiological conditions in the oral cavity and suites for the testing of complete dosage forms,...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development of a skin-friendly microemulsion for dermal allergen-specific immunotherapy
We examined epidermal penetration of Alexa Fluor-647 labelled bee-venom phospholipase A2 (Api m 1) using the Franz diffusion cell set up and confocal laser-scanning microscopy. First results of an in-vivo Api m 1-allergic mouse model indicated the protective efficacy of dermal AIT with our newly developed microemulsion.Summarily, the developed microemulsion is a suitable, stable drug delivery system for the topical administration of proteogenic allergens into the epidermis and is able to reach dendritic cells in the skin.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

High dose dry powder inhalers to overcome the challenges of tuberculosis treatment
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Mohammad A.M. Momin, Ian G. Tucker, Shyamal C. DasAbstractTuberculosis (TB) is a major global health burden. The emergence of the human immunodeficiency virus (HIV) epidemic and drug resistance has complicated global TB control. Pulmonary delivery of drugs using dry powder inhalers (DPI) is an emerging approach to treat TB. In comparison with the conventional pulmonary delivery for asthma and chronic obstructive pulmonary disease (COPD), TB requires high dose delivery to the lung. However, high dose delivery depends ...
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Multifunctional carbamazepine loaded nanostructured lipid carrier (NLC) formulation
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Mohammed Elmowafy, Khaled Shalaby, Mohamed M. Badran, Hazim M. Ali, Mohamed S. Abdel-Bakky, Hussein M. IbrahimAbstractCarbamazepine is a valuable pharmacological agent prescribed in treatment of epilepsy and trigeminal neuralgia. Poor bioavailability, successive dose adjustments and reported long term toxic effects are the main hurdles associated with carbamazepine oral administration. Bees wax containing NLC formulations were developed using high shear homogenization/sonication technique to overcome drug limitations...
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: physicochemical and in vitro peculiarities important for dermal application
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Ines Nikolic, Dominique Jasmin Lunter, Danijela Randjelovic, Ana Zugic, Vanja Tadic, Bojan Markovic, Nebojsa Cekic, Lada Zivkovic, Dijana Topalovic, Biljana Spremo-Potparevic, Rolf Daniels, Snezana SavicGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Characterizing Drug Product Continuous Manufacturing Residence Time Distributions of Major/Minor Excipient Step Changes using Near Infrared Spectroscopy and Process Parameters
Publication date: Available online 31 August 2018Source: International Journal of PharmaceuticsAuthor(s): Leo Manley, Zhenqi ShiAbstractThe material residence time distribution in a continuous manufacturing process can be utilized to develop, design and justify the process control strategy. This paper successfully demonstrates using both major and minor formulation component step changes to determine the system response using either Near Infrared Spectroscopy or process parameters. These options provide development flexibility to determine the system’s material residence time earlier in the development process and mo...
Source: International Journal of Pharmaceutics - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Material tracking in a continuous direct capsule-filling process via residence time distribution measurements
Publication date: Available online 30 August 2018Source: International Journal of PharmaceuticsAuthor(s): Julia Kruisz, Jakob Rehrl, Eva Faulhammer, Andreas Witschnigg, Johannes G. KhinastAbstractContinuous production of pharmaceuticals requires traceability from the raw material to the final dosage form. With that regard, understanding the residence time distribution (RTD) of the whole process and its unit operations is crucial. This work describes a structured approach to characterizing and modelling of RTDs in a continuous blender and a tamping pin capsule filling machine, including insights into data processing. The pa...
Source: International Journal of Pharmaceutics - August 31, 2018 Category: Drugs & Pharmacology Source Type: research

3D Printed Capsules for Quantitative Regional Absorption Studies in the GI Tract
Publication date: Available online 30 August 2018Source: International Journal of PharmaceuticsAuthor(s): Derrick Smith, Yash Kapoor, Andre Hermans, Rebecca Nofsinger, Filippos Kesisoglou, Tiffany Gustafson, Adam ProcopioAbstractDrug development is a long process which requires careful evaluation of the drug substance (active pharmaceutical ingredient, API), drug product (tablet, capsule etc.) and the bioperformance (both pre-clinical and clinical) before testing the efficacy of the final dosage form. The earliest assessment of a new drug substance requires an understanding of the safety and clinical performance (Phase 1) ...
Source: International Journal of Pharmaceutics - August 31, 2018 Category: Drugs & Pharmacology Source Type: research

Residence time and uptake of porous and cationic maltodextrin-based nanoparticles in the nasal mucosa: comparison with anionic and cationic nanoparticles
Publication date: Available online 29 August 2018Source: International Journal of PharmaceuticsAuthor(s): Minh Quan Le, Rodolphe Carpentier, Isabelle Lantier, Céline Ducournau, Isabelle Dimier-Poisson, Didier BetbederAbstractDifferent types of biodegradable nanoparticles (NP) have been studied as nasal mucosa cell delivery systems. These nanoparticles need to strongly interact with mucosa cells to deliver their payload. However, only a few simultaneous comparisons have been made and it is therefore difficult to determine the best candidate. Here we compared 5 types of nanoparticles with different surface charge (ani...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

Protein aggregation – Mechanisms, detection, and control
Publication date: 25 October 2018Source: International Journal of Pharmaceutics, Volume 550, Issues 1–2Author(s): Wei Wang, Christopher J. RobertsAbstractProtein aggregation has been recognized as one of the major challenges in the development and commercialization of successful protein-based drug products because of the inherent and high aggregation tendency during various manufacturing processes, storage, and administration. Protein aggregates may impact significantly the product quality, safety and/or efficacy. This review is intended to summarize four major aspects of protein aggregation – (1) aggregation m...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

The effect of administration media on palatability and ease of swallowing of multiparticulate formulations
Publication date: Available online 28 August 2018Source: International Journal of PharmaceuticsAuthor(s): Felipe L. Lopez, Terry B. Ernest, Mine Orlu, Catherine TuleuAbstractMultiparticulate formulations based on pellets, granules or beads, could be advantageous for paediatrics, geriatrics and patients with swallowing difficulties. However, these formulations may require suitable administration media to facilitate administration. The aim of this work was to investigate the effect of administration media properties on palatability and ease of swallowing of multiparticulates. A range of vehicles were developed using xanthan ...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

The combination of Nanomicelles with Terpenes for Enhancement of Skin Drug Delivery
Publication date: Available online 29 August 2018Source: International Journal of PharmaceuticsAuthor(s): Emine Kahraman, Neşet Neşetoğlu, Sevgi Güngör, Duri Şehvar Ünal, Yıldız ÖzsoyAbstractThe nanomicelles have recently drawn a great deal of attention for drug delivery into the skin. However, these carriers have only deposited in hair follicles and furrows, and drug in the micelles may not therapeutically reach into viable skin layers. The aim of this study was to formulate a combination of nanomicelles with terpenes to overcome this challenge and evaluate their potential for topical drug delive...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

Dendrimer as a new potential carrier for topical delivery of siRNA: a comparative study of dendriplex vs. lipoplex for delivery of TNF-α siRNA
Publication date: Available online 27 August 2018Source: International Journal of PharmaceuticsAuthor(s): Palpandi Pandi, Anjali Jain, Nagavendra Kommineni, Maksim Ionov, Maria Bryszewska, Wahid KhanAbstractTopical delivery of siRNA is challenging task due to complex barrier property of stratum corneum and cationic lipid based carriers have been widely explored for this purpose due to improved permeation through skin. For gene delivery application, dendrimers are considered as efficient carrier due to their cationic nature and well-defined surface groups. However, they are not well explored for topical delivery. This work ...
Source: International Journal of Pharmaceutics - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Diffusion through the ex vivo vitreal body – Bovine, porcine, and ovine models are poor surrogates for the human vitreous
In this study, the mechanical, physical and rheological properties of ovine, porcine, and bovine surrogates were investigated and compared to human vitreous. In addition, a bespoke Franz cell construct was used to compare the diffusion of a model drug (fluorescein) through vitreous samples. Despite the similarity in rheological properties between bovine, porcine and human vitreous samples, diffusion of fluorescein through the different vitreous samples revealed great differences in values of steady-state flux and diffusion coefficient. In addition, a first-generation vitreous mimic, composed of 4.5 mg/mL hyaluronic acid ...
Source: International Journal of Pharmaceutics - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Application of Box-Behnken experimental design for the formulation and optimisation of selenomethionine-loaded chitosan nanoparticles coated with zein for oral delivery
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Giuliana Vozza, Minna Danish, Hugh J. Byrne, Jesús M. Frías, Sinéad M. RyanAbstractSelenomethionine is an essential amino acid with a narrow therapeutic index and susceptibility to oxidation. Here it was encapsulated into a nanoparticle composed of chitosan cross-linked with tripolyphosphate for oral delivery. The formulation was optimised using a three-factor Box-Behnken experimental design. The chitosan:tripolyphosphate ratio, chitosan solvent pH, and drug load concentration were independently va...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Micro/nanostructured inhalable formulation based on polysaccharides: Effect of a thermoprotectant on powder properties and protein integrity
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Sonia Al-Qadi, Pablo Taboada, Carmen Remuñán-LópezAbstractCombined micro- and nanosystems are appealing for pulmonary protein delivery, fulfilling the specific physiological requirements for efficient outcomes in-vivo. However, fabrication of protein formulations may impose stresses perturbing protein conformational stability and, hence, biological activity. Herein, a protein, insulin (INS), was nanoencapsulated inside chitosan nanoparticles (CS NPs) by ionic gelation. By spray drying, the resultan...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of ring size and drug loading on the pharmacokinetics of a combination dapivirine-darunavir vaginal ring in cynomolgus macaques
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Diarmaid J. Murphy, Delphine Desjardins, Peter Boyd, Nathalie Dereuddre- Bosquet, Lev Stimmer, Anna Caldwell, Roger Le Grand, Charles Kelly, Jens van Roey, R. Karl MalcolmAbstractThis work investigates the impact of vaginal ring size and drug loading on the in vitro release, safety, ease of fit, and pharmacokinetics in cynomolgus macaques of matrix-type silicone elastomer vaginal rings containing a combination of the non-nucleoside reverse transcriptase inhibitor dapivirine and the protease inhibitor darunavir. Drug-fr...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Targeted Efflux Transporter Inhibitors – A Solution to Improve Poor Cellular Accumulation of Anti-Cancer Agents
In this study, we prepared 5 LAT1-utilizing prodrugs of an efflux pump inhibitor, probenecid (PRB). All novel compounds were transported into human breast cancer cells (MCF-7) mainly via LAT1. The compounds also interacted with either multiresistant proteins (MRPs), P-glycoprotein (P-gp) or breast cancer resistant protein (BCRP) and increased significantly (3-4 -fold) the cellular accumulation of anti-cancer agent vinblastine (VBL). Consequently, this improved the anti-proliferative efficacy of VBL by decreasing the cell growth after 72 h from 100% (VBL treatment alone) to 48-75% (combination treatment). However, the same ...
Source: International Journal of Pharmaceutics - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Acrylic microparticles increase daptomycin intracellular and in vivo anti-biofilm activity against Staphylococcus aureus
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Anne-Kathrin Woischnig, Lidia M. Gonçalves, Maxime Ferreira, Richard Kuehl, Judith Kikhney, Annette Moter, Isabel A.C. Ribeiro, António J. Almeida, Nina Khanna, Ana Francisca BettencourtGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Freeze-drying of Monoclonal Antibody-Conjugated Gold Nanorods: Colloidal Stability and Biological Activity
Publication date: Available online 23 August 2018Source: International Journal of PharmaceuticsAuthor(s): Majd A. Hamaly, Samer R. Abulateefeh, Khaled M. Al-Qaoud, Alaaldin M. AlkilanyAbstractMaintaining colloidal stability of nanoparticles in suspensions is a major challenge. Therefore, freeze-drying (lyophilization) is recently proposed to preserve colloidal stability of nanoparticles through maintaining them in a solid state. However, freeze-drying would itself induce nanoparticle aggregation unless proper formulation with a careful selection of cryoprotectants is considered. Herein, we evaluate the colloidal stability ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

Protein Aggregation - Mechanisms, Detection, and Control
Publication date: Available online 23 August 2018Source: International Journal of PharmaceuticsAuthor(s): Wei Wang, Christopher J. RobertsAbstractProtein aggregation has been recognized as one of the major challenges in the development and commercialization of successful protein-based drug products because of the inherent and high aggregation tendency during various manufacturing processes, storage, and administration. Protein aggregates may impact significantly the product quality, safety and/or efficacy. This review is intended to summarize four major aspects of protein aggregation – (1) aggregation mechanisms,(2) ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

Self-emulsifying drug delivery systems changing their zeta potential via a flip-flop mechanism
Publication date: Available online 24 August 2018Source: International Journal of PharmaceuticsAuthor(s): Esmaeil Salimi, Bao Le-Vinh, Forouhe Zahir-Jouzdani, Barbara Matuszczak, Azadeh Ghaee, Andreas Bernkop-SchnürchAbstractTo overcome the mucus layer and cell membrane barrier, self-emulsifying drug delivery systems (SEDDS) exhibiting negative zeta potential, switching to positive values when having reached the cell membrane is a promising approach. Accordingly, a novel conjugate was synthesized by covalent attachment of phosphotyrosine to octadecylamine, which was incorporated into SEDDS. Generated system presented ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research