Interactions between UV filters and active substances in emulsion: effect on microstructure, physicochemical and in-vivo properties
The objective of the present study was to develop, characterize and evaluate the clinical efficacy of topical formulations containing or not active substances and UV-filters, separate and in combination. To this end a stable formulation was developed to which four aqueous active substances and four lipophilic UV-filters were added. The formulations were then submitted to microscopic characterization by light microscopy, to particle size measurement, and to macroscopic characterization by rheology and texture analysis. Finally, a clinical efficacy study was conducted to determine the effect of the formulations on the skin a...
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of Curcuma comosa tablets using liquisolid techniques: In vitro and in vivo evaluation
This study aimed to investigate the use of liquisolid technique to prepare tablets containing oleoresin-like crude extract of C. comosa, and to improve the dissolution profiles of its major compounds, diarylheptanoids (DAs). Free flowing powders of C comosa extract were obtained by adsorption onto solid carriers, microcrystalline cellulose, with colloidal silica as coating material. FTIR results ruled out possible interactions between C. comosa extract and excipients. The results indicated that all of liquisolid tablets met the USP requirements. The release of DAs were significantly increased through liquisolid formulation...
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Preservation of exosomes at room temperature using lyophilizationγAuthor Names
In conclusion, lyophilization with trehalose is an effective method for the storage of exosomes for various applications.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Computational Modelling and Experimental Validation of Drug Entrainment in a Dry Powder Inhaler
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Thomas Kopsch, Darragh Murnane, Digby SymonsAbstractIn a passive dry powder inhaler (DPI) a patient inhales to entrain drug powder. The goal of this study is to demonstrate experimentally that an Eulerian-Eulerian (EE CFD) computational fluid dynamics (CFD) method can accurately predict the entrainment of the dry powder formulation in DPIs. A CFD method that makes accurate predictions of the entrainment process can be applied in DPI design and optimization processes. Three different DPI entrainment geometries were tes...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Advanced formulations for Intranasal Delivery of Biologics
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Julia Rohrer, Noemi Lupo, Andreas Bernkop-SchnürchAbstractIntroductionThe global biologics market has been ever increasing over the last decades and is predicted to top Euro 350 by 2020. Facing this scenario, the parenteral route of biologics administration as hitherto standard route is inconvenient for the future. Among the alternatives, the intranasal delivery of therapeutic biologicals seems to be most promising but researchers are still facing challenges as indicated by the scarce number of successfully marke...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Analytical aspects of printed oral dosage forms
We describe the different printing techniques and give an overview of film-based oral dosage forms produced using them. The main part of the review focuses on the non-destructive analytical methods used for evaluation of qualitative aspects of printed dosage forms, e.g., solid-state properties, as well as for quantification of the active pharmaceutical ingredient (API) in the printed dosage forms, with an emphasis on spectroscopic methods. Finally, the authors share their view on the future of printed dosage forms.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

TPGS modified nanoliposomes as an effective ocular delivery system to treat glaucoma
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Quansheng Jin, Huili Li, Zhaohui Jin, Lingjing Huang, Fazhan Wang, Yang Zhou, Yongmei Liu, Chunling Jiang, James Oswald, Jinhui Wu, Xiangrong SongAbstractThe aim of this study is to investigate the potential of D-alpha-tocopheryl poly (ethylene glycol 1000) succinate (TPGS) modified nanoliposomes as an ophthalmic delivery system of brinzolamide (Brz) for glaucoma treatment. The Brz loaded nanoliposomes containing TPGS (T-LPs/Brz) were firstly developed by a thin-film dispersion method. The average particle size was 96...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of Surface Chemistry of Polymeric Nanoparticles on Cutaneous Penetration of Cholecalciferol
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Augustine Lalloz, Marie-Alexandrine Bolzinger, Jimmy Faivre, Pierre-Luc Latreille, Araceli Garcia Ac, Cyrielle Rakotovao, Jean-Michel Rabanel, Patrice Hildgen, Xavier Banquy, Stéphanie BriançonAbstractWe investigated the influence of nanoparticle (NP) surface composition on different aspects of skin delivery of a lipophilic drug: chemical stability, release and skin penetration. Cholecalciferol was chosen as a labile model drug. Poly(lactic acid) (PLA)-based NPs without surface coating, with a non-ionic ...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Development and functional characterization of composite freeze dried wafers for potential delivery of low dose aspirin for elderly people with dysphagia
This study involves the development, characterization and optimization of composite wafers for potential oral and buccal delivery of low dose aspirin to prevent thrombosis in elderly patients with dysphagia. Blank (BLK) wafers (no loaded drug) were initially formulated by dissolving combinations of metolose (MET) with carrageenan (CAR) and MET with low molecular weight chitosan (CS) in different weight ratios in water, to identify optimum polymer combinations. However, drug loaded (DL) wafers were prepared using 45% v/v ethanol to help complete solubilization of the aspirin. The formulations were characterized using textur...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Azithromycin-loaded liposomes for enhanced topical treatment of methicillin-resistant Staphyloccocus aureus (MRSA) infections
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Zora Rukavina, Maja Šegvić Klarić, Jelena Filipović-Grčić, Jasmina Lovrić, Željka VanićAbstractAntibiotic delivery via liposomal encapsulation represents a promising approach for the efficient topical treatment of skin infections. The present study aimed to investigate the potential of using different types of azithromycin (AZT)-loaded liposomes to locally treat skin infections caused by methicillin-resistant Staphylococcus aureus (MRSA) strains. Conventional liposomes (CLs), deformable liposomes (DLs), ...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Chemoresponsive Smart Mesoporous Silica Systems – an Emerging Paradigm for Cancer Therapy
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Baranya Murugan, Uma Maheswari KrishnanAbstractNanotechnology-based interventions have gained popularity in the past decade for cancer therapy owing to their ability to overcome several shortcomings encountered in conventional therapy. Among the various nanoparticles that have been explored as drug carriers, mesoporous silica possesses certain desirable properties such as regulated pore size, high surface area, chemical and thermal stability, amenability for surface modification and biocompatibility. These systems hav...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Post-insertion parameters of PEG-derivatives in phosphocholine-liposomes
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Rosario Mare, Donatella Paolino, Christian Celia, Roberto Molinaro, Massimo Fresta, Donato CoscoAbstractThe insertion of specific derivatives into pre-formed colloidal systems has been shown to be a useful method for modifying their pharmacokinetic characteristics and biodistribution profiles.In this experimental work the effect of the post-insertion of different PEG-derivatives into pre-formed 100-nm liposomes made up of various lipid mixtures (DMPC, DPPC, DOPC, DSPC and cholesterol at different molar ratios) was inv...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

The physiochemical, mechanical, and adhesive properties of solvent-cast Vitamin E/Soluplus® films
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Ahmad Salawi, Sami NazzalAbstractSoluplus® is an amphiphilic graft copolymer used in hot melt extrusion applications and electrospinning. Very little information is available on the use of Soluplus® as a film former and in the development of film-based formulations. The overall aim of this work was to study the mechanical and adhesive properties of Soluplus® films prepared by the solvent casting technique. More specifically, we discovered that vitamin E can serve as a plasticizer for the Soluplus® polym...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Pollen grains as a novel microcarrier for oral delivery of proteins
In conclusion, upon use of a protein-friendly solvent for Eudragit L100-55, proteins could be encapsulated in ragweed pollen without denaturing them, and the resulting formulation exhibited selective release of the proteins at intestinal pH suggesting that the ragweed pollen grain-based formulation could be promising for oral delivery of proteins.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Self-assembly of biotinylated poly(ethylene glycol)-poly(curcumin) for paclitaxel delivery
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Lijun Hu, Min Li, Zhipeng Zhang, Yuanyuan Shen, Shengrong GuoAbstractPaclitaxel (PTX), one of the most potent anticancer agents, has showed a remarkable activity against varieties of tumors. However, the bioavailability of PTX is quite low due to its poor aqueous solubility. Moreover, the emerging multidrug resistance (MDR) in cancer to PTX remains a major obstacle for successful chemotherapy. In order to address these problems, we developed self-assembly of biotinylated poly(ethylene glycol)-poly(curcumin) (Biotin-PEG...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Local delivery of a cancer-favoring oncolytic vaccinia virus via poly (lactic-co-glycolic acid) nanofiber for theranostic purposes
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Narayanasamy Badrinath, Young Il Jeong, Hyung Young Woo, Seo Young Bang, Chan Kim, Jeong Heo, Dae Hwan Kang, So Young YooAbstractLocal delivery of viruses via nanomaterials has been demonstrated in the treatment of colon cancer. A cancer-favoring oncolytic vaccinia virus (CVV), which is an evolutionary cancer-favoring engineered vaccinia virus carrying the green fluorescent protein (GFP) gene, has antitumor efficacy in drug-resistant colon cancer and metastatic liver cells. Here, we present the antitumor efficacy of a ...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Uniformly Sized Iron Oxide Nanoparticles for Efficient Gene Delivery to Mesenchymal Stem Cells
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Qianhao Xu, Tianyuan Zhang, Qiyue Wang, Xinchi Jiang, Ai Li, Ying Li, Ting Huang, Fangyuan Li, Ying Hu, Daishun Ling, Jianqing GaoAbstractRecent advances in nanomaterials have made iron oxide nanoparticles (IONPs) as an innovative approach for the delivery of genes. However, the effectiveness of IONPs-assisted gene delivery is currently suffering from their poor uniformity, which not only exhibits detrimental effect on the magnetic property, but also leads to the poor reproducibility to maintain the optimal gene delive...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

The impact of protein corona on the behavior and targeting capability of nanoparticle-based delivery system
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Wei Xiao, Huile GaoAbstractOnce introduced into physiological environment, nanoparticles (NPs) are immediately coated with proteins, resulting in formation of what is known as protein corona. The formation of protein corona can be affected by many factors. Likewise, the addition of protein corona can alter the physicochemical properties and biodistribution of NPs. NPs with the coating protein corona can be considered as a biological identity that recognized by cells in biological system. Thus, to understand and regulat...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced Uptake and Improved Anti-tumor Efficacy of Doxorubicin Loaded Fibrin Gel with Liposomal Apatinib in Colorectal Cancer
Publication date: Available online 8 October 2018Source: International Journal of PharmaceuticsAuthor(s): Yuzhu Hu, Cong Wu, Changhui Zhu, Qingyu Fu, Jiajun Guo, Lihong Deng, Yihong He, Daoke Yang, Yongzhong Cheng, Xiang GaoAbstractColorectal cancer (CRC) exhibited high incidence rate worldwide and the advanced CRC had a poor prognosis. Thereupon, seeking efficient treatment for CRC is critical. Apatinib is a novel vascular epithelial growth factor receptor (VEGFR) inhibitor with inspiring therapeutic effect in some malignant cancers. In our study, doxorubicin was mixed in fibrin gel and apatinib was encapsulated with self...
Source: International Journal of Pharmaceutics - October 8, 2018 Category: Drugs & Pharmacology Source Type: research

SPF enhancement provided by rutin in a multifunctional sunscreen
Publication date: Available online 8 October 2018Source: International Journal of PharmaceuticsAuthor(s): Letícia Costa Tomazelli, Mayara Munhóz de Assis Ramos, Rafael Sauce, Thalita Marcílio Cândido, Fernanda Daud Sarruf, Claudinéia Aparecida Sales de Oliveira Pinto, Camila Areias de Oliveira, Catarina Rosado, Maria Valéria Robles Velasco, André Rolim BabyAbstractUnprotected chronic exposure to solar radiation can contribute to premature skin cancer and sunscreens are a key factor to avoid those detrimental effects. Currently, there is a growing interest in the photoprotecto...
Source: International Journal of Pharmaceutics - October 8, 2018 Category: Drugs & Pharmacology Source Type: research

Simultaneous penetration monitoring of oil component and active drug from fluorinated nanoemulsions
Publication date: Available online 8 October 2018Source: International Journal of PharmaceuticsAuthor(s): Lisa Binder, Johannes Jatschka, Eva Maria Kulovits, Simone Seeböck, Hanspeter Kählig, Claudia ValentaAbstractIn the field of dermal drug delivery, determining the penetration depth of actives is a standard procedure for the development of novel formulations. Regarding the vehicle components, respective penetration studies are rather scarce due to their often challenging analytics. However, an understanding of the interactions between drugs and additives during skin penetrating could help to develop promising ...
Source: International Journal of Pharmaceutics - October 8, 2018 Category: Drugs & Pharmacology Source Type: research

Injectable Long-acting Human Immunodeficiency Virus Antiretroviral Prodrugs with Improved Pharmacokinetic Profiles
Publication date: Available online 8 October 2018Source: International Journal of PharmaceuticsAuthor(s): Sai Archana Krovi, Matthew D. Gallovic, Austin M. Keller, Menakshi Bhat, Pamela Tiet, Naihan Chen, Michael A. Collier, Elizabeth G. Gurysh, Erica N. Pino, Monica M. Johnson, M. Shamim Hasan Zahid, Mackenzie L. Cottrell, Jason R. Pirone, Angela D. Kashuba, Jesse J. Kwiek, Eric M. Bachelder, Kristy M. AinslieAbstractWhile highly active antiretroviral therapy (HAART) has significantly reduced mortality rates in patients with human immunodeficiency virus type 1 (HIV-1), its efficacy may be impeded by emergence of drug resi...
Source: International Journal of Pharmaceutics - October 8, 2018 Category: Drugs & Pharmacology Source Type: research

Methodology to estimate the break force of pharmaceutical tablets with curved faces under diametrical compression
Publication date: Available online 8 October 2018Source: International Journal of PharmaceuticsAuthor(s): M. Al-Sabbagh, P. Polak, R.J. Roberts, G.K. Reynolds, I.C. SinkaAbstractThis paper develops a methodology to estimate the break force of curved faced tablets under diametrical compression. Common excipients used in pharmaceutical tablet formulations, including microcrystalline cellulose, calcium phosphate and mannitol as well as their mixtures were characterised. Compacts of different densities were manufactured and their compressive and tensile strength was measured. The break force of curved face tablets having a com...
Source: International Journal of Pharmaceutics - October 8, 2018 Category: Drugs & Pharmacology Source Type: research

Antitumor Effect of a Liposome-Encapsulated β1,4-Galactosyltransferase Inhibitor
In this study, 612 was introduced into a cationic liposome (LP) delivery system, and the anti-proliferative effects of both free and the LP-incorporated 612 (612-LP) were investigated in A549 lung cancer cells, which actively express anionic sialic acid moieties on the surfaces of cells. The anti-proliferative effects were evaluated via MTT assays. The results revealed that free 612 and empty LP impose neither anti-proliferative nor apoptotic effects on cancer cells at low doses, whereas the 612-LP system inhibited cancer cell growth at a concentration as low as 0.1 μg/mL after 3 days of incubation, suggesting that this...
Source: International Journal of Pharmaceutics - October 7, 2018 Category: Drugs & Pharmacology Source Type: research

Analysis of Pin Milling of Pharmaceutical Materials
Publication date: Available online 6 October 2018Source: International Journal of PharmaceuticsAuthor(s): Tina Bonakdar, Mojtaba GhadiriAbstractMilling is an important process for tailoring the particle size distribution for enhanced dissolution, content uniformity, tableting, etc., specially for active pharmaceutical ingredients and excipient in pharmaceutical industries. Milling performance of particulate solids depends on the equipment operating conditions (geometry, process conditions and input energy etc.) as well as material properties (particle size, shape, and mechanical properties, such as Young's modulus, hardnes...
Source: International Journal of Pharmaceutics - October 7, 2018 Category: Drugs & Pharmacology Source Type: research

Polysaccharide-based film loaded with vitamin C and propolis: A promising device to accelerate diabetic wound healing
Publication date: Available online 6 October 2018Source: International Journal of PharmaceuticsAuthor(s): Guilherme T. Voss, Matheus S. Gularte, Ane G. Vogt, Janice L. Giongo, Rodrigo A. Vaucher, Joanna V.Z. Echenique, Mauro P. Soares, Cristiane Luchese, Ethel A. Wilhelm, André R. FajardoAbstractWound healing can be a painful and time-consuming process in patients with diabetes mellitus. In light of this, the use of wound healing devices could help to accelerate this process. Here, cellulose-based films loaded with vitamin C (VitC) and/or propolis (Prop), two natural compounds with attractive properties were enginee...
Source: International Journal of Pharmaceutics - October 7, 2018 Category: Drugs & Pharmacology Source Type: research

Polysorbate degradation in biotherapeutic formulations: Identification and discussion of current root causes
Publication date: Available online 6 October 2018Source: International Journal of PharmaceuticsAuthor(s): Mridula Dwivedi, Michaela Blech, Ingo Presser, Patrick GaridelAbstractBiotherapeutic protein formulations are often high concentration liquid protein solutions, which are required to be stable under pharmaceutically relevant storage conditions and presence of external stress. Non-ionic detergents like polysorbate have been the most commonly used excipient to maintain formulation stability. Recently, particle formation in polysorbate containing biotherapeutic formulations has arisen as a major quality concern and potent...
Source: International Journal of Pharmaceutics - October 7, 2018 Category: Drugs & Pharmacology Source Type: research

Improved oral bioavailability of notoginsenoside R1 with sodium glycocholate-mediated liposomes: preparation by supercritical fluid technology and evaluation in vitro and in vivo
Publication date: Available online 4 October 2018Source: International Journal of PharmaceuticsAuthor(s): Qiangyuan Fan, Yongtai Zhang, Xuefeng Hou, Zhe Li, Kai Zhang, Qun Shao, Nianping FengAbstractThe chief objective of this research was to appraise liposomes embodying a bile salt, sodium glycocholate (SGC), as oral nanoscale drug delivery system to strengthen the bioavailability of a water-soluble and weakly penetrable pharmaceutical, notoginsenoside R1 (NGR1). NGR1-loaded liposomes were prepared with the improved supercritical reverse evaporation (ISCRPE) method and the preparation conditions were optimized with respon...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

An Application of Deep Learning to Detect Process Upset during Pharmaceutical Manufacturing using Passive Acoustic Emissions
Publication date: Available online 22 September 2018Source: International Journal of PharmaceuticsAuthor(s): Allan Carter, Lauren BriensAbstractThe multivariate nature of a fluidized bed system creates process complexity that increases the risk of production upset. This research explores the use of passive acoustic emissions monitoring paired with an artificial neural network to detect fluidized bed distributor plate blockage. In many cases, early process failure detection can allow for immediate intervention, thus lowering operation costs. Blockages were simulated by actively covering portions of a top-spray fluidized bed...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Physicochemical and Biopharmaceutical Characterization of Celecoxib Nanoparticle: Avoidance of Delayed Oral Absorption Caused by Impaired Gastric Motility
Publication date: Available online 22 September 2018Source: International Journal of PharmaceuticsAuthor(s): Keisuke Yakushiji, Mizuki Ogino, Hiroki Suzuki, Yoshiki Seto, Hideyuki Sato, Satomi OnoueAbstractThe present study aimed to develop a celecoxib (CEL) nanoparticle with improved dissolution/dispersion and consistent absorption even in the presence of impaired gastric motility. CEL was pulverized by a wet-milling with hydroxypropyl cellulose (HPC), and the prepared nanoparticles were physicochemically characterized after freeze-drying. CEL nanoparticle with HPC-SSL (NP/CEL) exhibited better dissolution/dispersion beha...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

A stent film of paclitaxel presenting extreme accumulation of paclitaxel in tumor tissue and excellent antitumor efficacy after implantation beneath the subcutaneous tumor xenograft in mice
Publication date: Available online 26 September 2018Source: International Journal of PharmaceuticsAuthor(s): Keqin Wu, Jieying Liu, Lei lei, Yuanyuan Shen, Shengrong GuoAbstractAnti-tumor drug/stent combinations play a dual role of stent and local chemotherapy to cancer. Herein, a series of paclitaxel (PTX) loaded polylactic acid (PLA) stent films were studied on drug release characteristics and in vivo antitumor effects. The film was implanted beneath and released drug towards the subcutaneous PC-3 tumor xenograft in mice, which consisted of a PTX-loaded layer and a drug-free backing layer. The concentrations of PTX were ...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of topical formulations for a novel skin whitening agent (AP736) using Hansen solubility parameters and PEG-PCL polymers
In this study, we aimed to develop a new topical delivery system in which AP736 is not only physically stable, but also suitably delivered to the skin. By calculating each HSP (Hansen Solubility Parameters), ethylenedioxy moiety-containing compounds could be easily selected for the formulation ingredients of AP736. Although the highest solubility of AP736 in diethylene glycol monoethyl ether make AP736-incorporated water in oil emulsions well formed, the recrystallization of AP736 was observed in oil in water emulsions. Therefore, we fabricated polymeric nanoparticles (PNPs) in order to encapsulate AP736. Three different P...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Controlled Drug Delivery from 3D Printed Two-Photon Polymerized Poly(Ethylene Glycol) Dimethacrylate Devices
Publication date: Available online 27 September 2018Source: International Journal of PharmaceuticsAuthor(s): Anh-Vu Do, Kristan Worthington, Budd Tucker, Aliasger K. SalemAbstractControlled drug delivery systems have been utilized to enhance the therapeutic effects of many drugs by delivering drugs in a time-dependent and sustained manner. Here, with the aid of 3D printing technology, drug delivery devices were fabricated and tested using a model drug (fluorophore: rhodamine B). Poly(ethylene glycol) dimethacrylate (PEGDMA) devices were fabricated using a two-photon polymerization (TPP) system and rhodamine B was homogenou...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mucus-penetrating phage-displayed peptides for improved transport across a mucus-like model
The objective of this work is to use phage display libraries as a screening tool to identify peptides that facilitate transport across the mucus barrier. Mucus is a complex selective barrier to particles and molecules, limiting penetration to the epithelial surface of mucosal tissues. In mucus-associated diseases such as cystic fibrosis (CF), mucus has increased viscoelasticity and a higher concentration of covalent and non-covalent physical entanglements compared to healthy tissues, which greatly hinders permeability and transport of drugs and particles across the mucosae for therapeutic delivery. Treatment of CF lung dis...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Detailed Modeling and Process Design of an Advanced Continuous Powder Mixer
Publication date: Available online 27 September 2018Source: International Journal of PharmaceuticsAuthor(s): Peter Toson, Eva Siegmann, Martina Trogrlic, Hermann Kureck, Johannes Khinast, Dalibor Jajcevic, Pankaj Doshi, Daniel Blackwood, Alexandre Bonnassieux, Patrick D Daugherity, Mary T. am EndeAbstractA vertical in-line continuous powder mixing device (CMT – Continuous Mixing Technology) has been modelled with the discrete element method (DEM) utilizing a calibrated cohesive contact model. The vertical design of the mixing device allows independent control of mean residence time (MRT) and shear rate. The hold-up m...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced dissolution of naproxen from pure-drug, crystalline nanoparticles: A case study formulated into spray-dried granules and compressed tablets
Publication date: Available online 29 September 2018Source: International Journal of PharmaceuticsAuthor(s): Veronika Braig, Christoph Konnerth, Wolfgang Peukert, Geoffrey LeeAbstractThis is a case study of the use of rapidly-dissolving naproxen crystalline nanoparticles to prepare compressed tablets. The dissolution rates of different formulations were determined: the crystalline pure-drug nanodispersion, a pure-drug microsuspension, a granule prepared by spray drying the nanodispersion with mannitol, and a tablet prepared by compressing the granule with a bulking agent and a disintegrant. The goal was to determine the in...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

AgCa-PLGA submicron particles inhibit the growth and colonization of E. faecalis and P. gingivalis on dentin through infiltration into dentinal tubules
Publication date: Available online 29 September 2018Source: International Journal of PharmaceuticsAuthor(s): Wei Fan, Danfeng Liu, Yanyun Li, Qing Sun, Bing FanAbstractEliminating the infection from root canals and periodontal tissues of human teeth as well as the repair of infected periodontal bone has been a great challenge. Poly(lactide-co-glycolide) (PLGA) particles have been used for drug delivery due to their biodegradability, sustained drug release and nontoxic properties. As silver ions (Ag+) exhibit strong antibacterial ability and calcium ions (Ca2+) are essential for hard tissue regeneration, the Ag+ and Ca2+ we...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of preparation technique on co-amorphization of carvedilol with acidic amino acids
In this study the basic drug carvedilol (CAR) and the two acidic AAs, glutamic acid and aspartic acid, were used to explore the possibilities of producing co-amorphous formulations using BM, SD and liquid assisted grinding (LAG). X-ray powder diffraction, thermal analysis and Fourier-transform infrared spectroscopy were used to determine the solid state form of the various CAR-AA mixtures prepared. BM the CAR-AA mixtures for 60 min did not result in co-amorphization as XRPD revealed remaining crystallinity of both CAR and the AA. On the other hand, successful co-amorphous salt formation was obtained for all SD samples. Dif...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Novel ultra-small micelles based on rebaudioside A: A potential nanoplatform for ocular drug delivery
Publication date: Available online 3 October 2018Source: International Journal of PharmaceuticsAuthor(s): Kaichao Song, Meng Xin, Hongxia Yu, Zhou Zheng, Jun Li, Mengshuang Li, Huimin Guo, Youlan Tan, Xianggen WuAbstractWe investigated if the self-assembled micelles of rebaudioside A (RA) could potentially be utilized as an ocular drug-delivery system in this investigation. RA self-assembled into micelles with ultra-small particle sizes (
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

A Poloxamer-407 modified liposome encapsulating epigallocatechin-3-gallate in the presence of magnesium: characterization and protective effect against oxidative damage
In conclusion, the results demonstrated that the produced formulation enhances the efficacy of EGCG under stress conditions, thus representing a potential formulation for the intracellular delivery of EGCG in diseases caused by oxidative damage.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

A novel antibacterial agent based on AgNPs and Fe3O4 loaded chitin microspheres with peroxidase-like activity for synergistic antibacterial activity and wound-healing
In this study, a novel antibacterial agent was developed based on chitin nanofibrous microspheres loaded with AgNPs and Fe3O4 nanoparticles (Ag-Fe3O4-NMs) for synergistic antibacterial activity and wound healing. Ag-Fe3O4-NMs was prepared via an in situ synthetic method which showed an excellent porosity and wettability. Moreover, Ag-Fe3O4-NMs were capable of sustained release of Ag+ and catalysed the decomposition of low H2O2 concentrations to generate hydroxyl radical (·OH). The ·OH radicals and Ag+ showed higher antibacterial activity and exhibited the toxicity with high dose of AgNPs and H2O2. In vitro bi...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Prevention of rat liver fibrosis by selective targeting of hepatic stellate cells using hesperidin carriers
In conclusion, this newly developed carrier represents a potentially beneficial approach for HSCs specific targeting of hesperidin in a rat model with liver fibrosis.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Smart pH Responsive Drug Delivery System Based on poly(HEMA-co-DMAEMA) Nanohydrogel
Publication date: Available online 3 October 2018Source: International Journal of PharmaceuticsAuthor(s): Amir Roointan, Javad Farzanfar, Soliman Mohammadi-Samani, Abbas Behzad-Behbahani, Fatemeh FarjadianAbstractThe advent of smart nanohydrogel has revealed new opportunities for scientists to develop the most efficient anti-cancer vehicles with safe and biocompatible profile. In this experiment, using reversible addition–fragmentation chain transfer polymerization method as a novel, safe and smart pH responsive formulation of poly (hydroxyethyl methacrylate-co-N, N-dimethylaminoethyl methacrylate) and poly (ethylene...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Towards a better understanding of dry binder functionality
Publication date: Available online 4 October 2018Source: International Journal of PharmaceuticsAuthor(s): Oscar-Rupert Arndt, Peter KleinebuddeAbstractIt is of great importance to get a deeper understanding of the binding behaviour and functionality of different types of dry binders, since dry binders are crucial to ensure appropriate properties of dry granules and tablets. Based on previous studies, the most effective dry bindersof chemically different types have been chosen to apply a new approach analysing the compressibility of tablets made from pure dry binders. Therefore, tablets were compressed at different tabletin...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 15 November 2018Source: International Journal of Pharmaceutics, Volume 551, Issues 1–2Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Utilizing glutathione-triggered nanoparticles to enhance chemotherapy of lung cancer by reprograming the tumor microenvironment
Publication date: 1 December 2018Source: International Journal of Pharmaceutics, Volume 552, Issues 1–2Author(s): Tao Cui, Xiaohong Li, Yaqian Shu, Xianzhou Huang, Yan Wang, Wenli ZhangAbstractIn the present study, we have developed the robust nanoparticles (MGC-GNP/PTX), which are TAMs and tumor cells-dual recognizable, for targeting cancer therapy. Of great importance, the developed nano-platforms are glutathione (GSH)-activable, which means it remains structure intact under normal physiological condition and can be disrupted when exposed to certain concentration of GSH. As demonstrated by the drug release assay in...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Soluplus micelles for acyclovir ocular delivery: Formulation and cornea and sclera permeability
Publication date: 1 December 2018Source: International Journal of Pharmaceutics, Volume 552, Issues 1–2Author(s): Angela Varela-Garcia, Angel Concheiro, Carmen Alvarez-LorenzoAbstractNearly 20% of people affected by the herpes simplex virus (HSV) suffer from vision problems. The virus can infect all layers of the cornea or cause inflammatory diseases of the sclera. The aim of this work was to test whether encapsulation of acyclovir in Soluplus or Solutol polymeric micelles increases its solubility, corneal permeability and sclera penetration. The aqueous solubility of acyclovir is known to be low, and therefore appro...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Binding and structure-kinetic relationship analysis of selective TLR4-targeted immunosuppressive self-assembling heparin nanoparticles
In conclusion, the present study characterizes the immunosuppressive effect of aliphatic heparin derivatives and provides a promising strategy to develop selective immunosuppressants for acute and chronic inflammatory disorders.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro effect of mPEG2k-PCLx micelles on rat liver cytochrome P450 enzymes
In conclusion, mPEG2k-PCLx micelles can interfere with the normal metabolic function of CYP450s in vitro, indicating polymeric micelles as promising drug nano-carriers might cause micelle–drug interaction and the in vivo interaction deserves further investigation.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

A preclinical evaluation of cytarabine prodrug nanofibers assembled from cytarabine-lauric acid conjugate toward solid tumors
Publication date: 1 December 2018Source: International Journal of Pharmaceutics, Volume 552, Issues 1–2Author(s): Ruiling Liu, Yue Jiang, Xu Hu, Jilian Wu, Wei Jiang, Guoxia Jin, Yuxia LuanAbstractCytarabine (Ara-C) has become cornerstones for the treatment of hatmatological malignancies for several decades; however, it still faces serious challenges in clinical applications due to its side effects such as hand foot syndrome (HFS) and stomatitis. Therefore, considerable researchers have devoted to looking for the new derivative with desirable activity and low toxicity. A new prodrug based on the conjugation of cytara...
Source: International Journal of Pharmaceutics - October 5, 2018 Category: Drugs & Pharmacology Source Type: research