Critical quality attributes, in vitro release and correlated in vitro skin permeation —in vivo tape stripping collective data for demonstrating therapeutic (non)equivalence of topical semisolids: A case study of “ready-to-use” vehicles
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Tanja Ilić, Ivana Pantelić, Dominique Lunter, Sanela Đorđević, Bojan Marković, Dragana Ranković, Rolf Daniels, Snežana Savić This work aimed to prove the ability of “ready-to-use” topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory efforts to establish alternative, scientific...
Source: International Journal of Pharmaceutics - June 13, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of rosmarinic acid across the blood –brain barrier for neuronal rescue using polyacrylamide-chitosan-poly(lactide-co-glycolide) nanoparticles with surface cross-reacting material 197 and apolipoprotein E
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Yung-Chih Kuo, Rajendiran Rajesh Rosmarinic acid-loaded polyacrylamide-chitosan-poly(lactide-co-glycolide) nanoparticles (RA-PAAM-CH-PLGA NPs) were grafted with cross-reacting material 197 (CRM197) and apolipoprotein E (ApoE) for targeting of the blood–brain barrier (BBB) and rescuing degenerated neurons. The polymeric nanocarriers were prepared by microemulsion, solvent diffusion, grafting, and surface modification, and CRM197-ApoE-RA-PAAM-CH-PLGA NPs were used to treat human brain-microvascular en...
Source: International Journal of Pharmaceutics - June 12, 2017 Category: Drugs & Pharmacology Source Type: research

Multivariate statistical process control of a continuous pharmaceutical twin-screw granulation and fluid bed drying process
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): A.F. Silva, M.C. Sarraguça, M. Fonteyne, J. Vercruysse, F. De Leersnyder, V. Vanhoorne, N. Bostijn, M. Verstraeten, C. Vervaet, J.P. Remon, T. De Beer, J.A. Lopes A multivariate statistical process control (MSPC) strategy was developed for the monitoring of the ConsiGma™-25 continuous tablet manufacturing line. Thirty-five logged variables encompassing three major units, being a twin screw high shear granulator, a fluid bed dryer and a product control unit, were used to monitor the process. T...
Source: International Journal of Pharmaceutics - June 12, 2017 Category: Drugs & Pharmacology Source Type: research

Comminution-amorphisation relationships during ball milling of lactose at different milling conditions
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Samaneh Pazesh, Johan Gråsjö, Jonas Berggren, Göran Alderborn The purpose of the study was to investigate the relationship between comminution and amorphisation of α-lactose monohydrate particles during ball milling under different milling conditions, including ball-to-powder mass ratio, milling time and ball diameter. The results revealed that at a constant ball filling ratio, ball-to-powder mass ratio of 25:1 resulted in the lowest minimum particle diameter of ∼5μm and the h...
Source: International Journal of Pharmaceutics - June 12, 2017 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of a dimensionless mechanistic pan coating model for the prediction of coated tablet appearance
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Daniel Niblett, Stuart Porter, Gavin Reynolds, Tomos Morgan, Jennifer Greenamoyer, Ronald Hach, Stephanie Sido, Kapish Karan, Ian Gabbott A mathematical, mechanistic tablet film-coating model has been developed for pharmaceutical pan coating systems based on the mechanisms of atomisation, tablet bed movement and droplet drying with the main purpose of predicting tablet appearance quality. Two dimensionless quantities were used to characterise the product properties and operating parameters: the dimensionl...
Source: International Journal of Pharmaceutics - June 12, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation, characterization, and cytotoxicity studies of niclosamide loaded mesoporous drug delivery systems
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Vishwas Pardhi, Rahul B Chavan, Rajesh Thipparaboina, Sowjanya Thatikonda, VGM Naidu, Nalini R Shastri Recent reports on the anticancer potential of niclosamide have opened new avenues for anticancer treatment. Niclosamide belongs to the BCS class II, which is indicative of poor solubility and dissolution rate limited absorption. The aim of this study was to improve the dissolution rate of the drug by mesoporous drug delivery system. Porous silica grades (ordered and nonordered) with different pore size, ...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Could clinical photochemical internalisation be optimised to avoid neuronal toxicity?
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Caitriona O’Rourke, Colin Hopper, Alexander J. MacRobert, James B. Phillips, Josephine H. Woodhams Photochemical Internalisation (PCI) is a novel drug delivery technology in which low dose photodynamic therapy (PDT) can selectively rupture endo/lysosomes by light activation of membrane-incorporated photosensitisers, facilitating intracellular drug release in the treatment of cancer. For PCI to be developed further, it is important to understand whether nerve damage is an impending side effect when t...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Paclitaxel loaded phospholipid-based gel as a drug delivery system for local treatment of glioma
In conclusion, this study developed a novel PG based local PTX delivery system with simple preparation method, good tolerability and high therapeutic efficacy. It has a great potential to improve the clinical management of glioma. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Dry powder formulation of kanamycin with enhanced aerosolization efficiency for drug-resistant tuberculosis
Conclusion l-leucine improved the aerosolization of kanamycin by surface modification, which may be helpful for the effective treatment of drug-resistant tuberculosis. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Evaluation of tacrolimus sorption to PVC- and non-PVC-based tubes in administration sets: Pump method vs. drip method
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Su-Eon Jin, Seungho Jeon, Hyo-Jin Byon, Sung-Joo Hwang Tacrolimus sorption to tubes was evaluated using pump and drip methods For tubes, polyvinylchloride (PVC)- and non-PVC-based (polyurethane [PU] and polyolefin [PO]) tubes were used. First, inner surface properties of tubes were analyzed using field emission scanning electron microscopy and X-ray photoelectron spectroscopy. Tacrolimus was quantitatively analyzed using high-performance liquid chromatography with UV detection. For kinetic sorption analys...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Liposomal andrographolide dry powder inhalers for treatment of bacterial pneumonia via anti-inflammatory pathway
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Miao Li, Tongtong Zhang, Lifei Zhu, Rui Wang, Yiguang Jin Andrographolide (AG) is a chemical entity from traditional Chinese herbs and its oral pills have been applied to the treatment of respiratory inflammation. Here we report pulmonary delivery of liposomal AG dry powder inhalers (LADPIs) for treatment of Staphylococcus aureus-induced pneumonia. AG liposomes were prepared with the injection method and then freeze-dried for preparation of LADPIs. AG liposomes were small and stable with a mean size of 77...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Reshaping antibiotics through hydrophobic drug-bile acid ionic complexation enhances activity against Staphylococcus aureus biofilms
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Stefano Giovagnoli, Donatella Pietrella, Lanfranco Barberini, Claudio Santi, Andrea Carotti, Alessandro di Michele, Maurizio Ricci The antibiotic era is on the verge of a profound change and facing a ground shaking crisis. The frequent failures of antibiotic treatments are often associated with biofilm formation, which is responsible for chronic infections, exacerbation as well as reinfection. So far, albeit the large number of valuable strategies employed to combat biofilm formation, little success has b...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Improved respirable fraction of budesonide powder for dry powder inhaler formulations produced by advanced supercritical CO2 processing and use of a novel additive
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Yuta Miyazaki, Naoki Aruga, Kazunori Kadota, Yuichi Tozuka, Hirofumi Takeuchi A budesonide (BDS) suspension was obtained via advanced supercritical carbon dioxide (scCO2) processing. Thereafter, the suspension was freeze-dried (FD) to produce BDS particles for dry powder inhaler formulations (scCO2/FD processing). The scCO2/FD processed BDS powder showed low crystallinity by powder X-ray diffraction and a rough surface by scanning electron microscopy. The respirable fraction of BDS was assessed using a tw...
Source: International Journal of Pharmaceutics - June 10, 2017 Category: Drugs & Pharmacology Source Type: research

Co-delivery of evodiamine and rutaecarpine in a microemulsion-based hyaluronic acid hydrogel for enhanced analgesic effects on mouse pain models
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Yong-Tai Zhang, Zhe Li, Kai Zhang, Hong-Yu Zhang, Ze-Hui He, Qing Xia, Ji-Hui Zhao, Nian-Ping Feng The aim of this study was to improve the analgesic effect of evodiamine and rutaecarpine, using a microemulsion-based hydrogel (ME-Gel) as the transdermal co-delivery vehicle, and to assess hyaluronic acid as a hydrogel matrix for microemulsion entrapment. A microemulsion was formulated with ethyl oleate as the oil core to improve the solubility of the alkaloids and was loaded into a hyaluronic acid-structur...
Source: International Journal of Pharmaceutics - June 8, 2017 Category: Drugs & Pharmacology Source Type: research

Dendrimer encapsulated and conjugated delivery of berberine: A novel approach mitigating toxicity and improving in vivo pharmacokinetics
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Lokesh Gupta, Ashok Kumar Sharma, Avinash Gothwal, Mohammed Shahid Khan, Mahaveer Prasad Khinchi, Arem Qayum, Shashank Kumar Singh, Umesh Gupta Berberine (BBR) is a nitrogenous cyclic natural alkaloid with potential anticancer activity. However it has been less explored due to its poor pharmacokinetic profile. Dendrimers (e.g. PAMAM) have promising potential to deliver anticancer drugs/bio-actives because of their well-defined architecture, monodispersity and tailor-made surface functionality. In the pres...
Source: International Journal of Pharmaceutics - June 8, 2017 Category: Drugs & Pharmacology Source Type: research

Exenatide-loaded microsphere/thermosensitive hydrogel long-acting delivery system with high drug bioactivity
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Puxiu Wang, Xuezhi Zhuo, Wei Chu, Xing Tang A series of mixed hydrogels of PLGA-PEG-PLGA and PCLA-PEG-PCLA were synthesized, and investigated in terms of their critical micelle concentration, stability and thermosensitive properties. Also, some mixed hydrogel was selected to prepare Depot-gel-in-Ms-in-Matrix-gel system for the treatment of type 2 diabetes mellitus. Briefly, Exenatide (EXT) loaded hydrogels was encapsulated in PLGA microspheres (Ms) and further encapsulated into blank hydrogel. The mechani...
Source: International Journal of Pharmaceutics - June 8, 2017 Category: Drugs & Pharmacology Source Type: research

Antibacterial and antifungal properties of dendronized silver and gold nanoparticles with cationic carbosilane dendrons
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Cornelia E. Peña-González, Elzbieta Pedziwiatr-Werbicka, Tania Martín-Pérez, Eligia M. Szewczyk, José L. Copa-Patiño, Juan Soliveri, Jorge Pérez-Serrano, Rafael Gómez, Maria Bryszewska, Javier Sánchez-Nieves, F. Javier de la Mata Water soluble silver nanoparticles (AgNPs) capped with cationic carbosilane dendrons have been synthesized by direct reaction in water of dendrons, silver precursor and a reducing agent. These nanoparticles have been ...
Source: International Journal of Pharmaceutics - June 8, 2017 Category: Drugs & Pharmacology Source Type: research

Comparison of different zeolite framework types as carriers for the oral delivery of the poorly soluble drug indomethacin
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Christina Karavasili, Elsa P. Amanatiadou, Eleni Kontogiannidou, Georgios K. Eleftheriadis, Nikolaos Bouropoulos, Eleni Pavlidou, Ioanna Kontopoulou, Ioannis S. Vizirianakis, Dimitrios G. Fatouros Microporous zeolites of distinct framework types, textural properties and crystal morphologies namely BEA, ZSM and NaX, have been employed as carriers to assess their effect on modulating the dissolution behavior of a BCS II model drug (indomethacin). Preparation of the loaded carriers via the incipient wetness ...
Source: International Journal of Pharmaceutics - June 8, 2017 Category: Drugs & Pharmacology Source Type: research

Free paclitaxel-loaded E-selectin binding peptide modified micelle self-assembled from hyaluronic acid-paclitaxel conjugate inhibit breast cancer metastasis in a murine model
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Xiaofeng Han, Xuerong Dong, Jing Li, Manyuan Wang, Lei Luo, Zhaoxia Li, Xuran Lu, Rui He, Rongsong Xu, Muxin Gong The present work seeks to construct a nanovehicle for the efficient suppression of breast cancer metastasis through targeting E-selectin on tumor vascular endothelial cells and hyaluronic acid-receptor on tumor cells. Herein, a new ligand-PEG-lipid conjugate, E-selectin binding peptide-polyethene glycol-1-octadecylamine (Esbp-PEG-OA), was used as the targeting molecule of micelle self-assemble...
Source: International Journal of Pharmaceutics - June 5, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical characterization of pH-responsive and fusogenic self-assembled non-phospholipid vesicles for a potential multiple targeting therapy
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Martina Di Francesco, Christian Celia, Rosita Primavera, Nicola D’Avanzo, Marcello Locatelli, Massimo Fresta, Felisa Cilurzo, Cinzia Anna Ventura, Donatella Paolino, Luisa Di Marzio In order to obtain nanocarriers suitable for the delivery of drugs in the treatment of cancer, pH-responsive nanovesicles capable of facilitating fusion (fusogenic nanovesicles) were synthesized and then their physicochemical characteristics were modified. These nanovesicles were made by combining polysorbates having dif...
Source: International Journal of Pharmaceutics - June 5, 2017 Category: Drugs & Pharmacology Source Type: research

Extremely small-sized globular poly(ethylene glycol)-cyclic RGD conjugates targeting integrin αvβ3 in tumor cells
In this study, we report an extremely small-sized globular poly(ethylene glycol) (gPEG) conjugated with cyclic arginine-glycine-aspartic acid (cRGD) peptide and chlorin e6 (Ce6). This nanoparticle design takes advantage of the biocompatible functional gPEG (3–4nm in diameter) as an extremely small-sized drug carrier, the tumor targeting ability of cRGD, and the photodynamic tumor ablation ability of Ce6. We found that gPEG conjugated with cRGD and Ce6 (cRGD-gPEG-Ce6) exhibited much higher phototoxicity in SKOV-3 tumor cells (which have a very high density of integrin αvβ3 receptors) than in KB cells (which...
Source: International Journal of Pharmaceutics - June 5, 2017 Category: Drugs & Pharmacology Source Type: research

PLGA nanoparticles introduction into mitoxantrone-loaded ultrasound-responsive liposomes: In vitro and in vivo investigations
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Yuxuan Xin, Qi Qi, Zhenmin Mao, Xiaoping Zhan A novel ultrasound-responsive liposomal system for tumor targeting was prepared in order to increase the antitumor efficacy and decrease serious side effects. In this paper, PLGA nanoparticles were used ultrasound-responsive agents instead of conventional microbubbles. The PLGA-nanoparticles were prepared by an emulsion solvent evaporation method. The liposomes were prepared by a lipid film hydration method. Particle size, zeta potential, encapsulation efficie...
Source: International Journal of Pharmaceutics - June 5, 2017 Category: Drugs & Pharmacology Source Type: research

Argpyrimidine-tagged rutin-encapsulated biocompatible (ethylene glycol dimers) nanoparticles: Application for targeted drug delivery in experimental diabetes (Part 2)
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Abhishek Bhattacherjee, Abhay Sankar Chakraborti Diabetes mellitus is characterized by hyperglycemia and associated complications. However, long-term diabetes control is not often sustained by currently available therapeutic approaches. Research on nanoparticle-mediated drug delivery systems is in progress. Here we have tested a ligand (argpyrimidine)-tagged drug (rutin)-encapsulated biocompatible (ethylene glycol dimers) nanoparticle for targeted drug delivery in streptozotocin-induced diabetic rats. Arg...
Source: International Journal of Pharmaceutics - June 5, 2017 Category: Drugs & Pharmacology Source Type: research

TPP-dendrimer nanocarriers for siRNA delivery to the pulmonary epithelium and their dry powder and metered-dose inhaler formulations
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Elizabeth Bielski, Qian Zhong, Hamad Mirza, Matthew Brown, Ashura Molla, Teresa Carvajal, Sandro R.P. da Rocha The regulation of genes utilizing the RNA interference (RNAi) mechanism via the delivery of synthetic siRNA has great potential in the treatment of a variety of lung diseases. However, the delivery of siRNA to the lungs is challenging due to the poor bioavailability of siRNA when delivered intraveneously, and difficulty in formulating and maintaining the activity of free siRNA when delivered direc...
Source: International Journal of Pharmaceutics - June 1, 2017 Category: Drugs & Pharmacology Source Type: research

An investigation into the ability of alendronate ion pairs to increase oral absorption
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Nasim Samiei, Seyed Mohsen Foroutan, Fattaneh Razipour, Afshin Zarghi, Alireza Shafaati The purpose of this study is to increase oral absorption of the highly charged drug alendronate using an ion pair strategy. Ion pairing is a formulation approach in drug delivery that is performed to improve the lipophilicity of ionized drugs. Cationic counter ions, such as arginine, phenazopyridine, hyoscine and pyridostigmine, were selected to enhance the lipophilicity and permeability of alendronate. Data obtained fr...
Source: International Journal of Pharmaceutics - June 1, 2017 Category: Drugs & Pharmacology Source Type: research

Patient-specific 3D scanned and 3D printed antimicrobial polycaprolactone wound dressings
This study shows that 3D scanning and 3D printing, which are becoming simpler and more affordable, have the potential to offer solutions to produce personalised wound dressings. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 31, 2017 Category: Drugs & Pharmacology Source Type: research

Quality by Design approach for studying the impact of formulation and process variables on product quality of oral disintegrating films
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Sonal Mazumder, Naresh Pavurala, Prashanth Manda, Xiaoming Xu, Celia N. Cruz, Yellela S.R. Krishnaiah The present investigation was carried out to understand the impact of formulation and process variables on the quality of oral disintegrating films (ODF) using Quality by Design (QbD) approach. Lamotrigine (LMT) was used as a model drug. Formulation variable was plasticizer to film former ratio and process variables were drying temperature, air flow rate in the drying chamber, drying time and wet coat thic...
Source: International Journal of Pharmaceutics - May 31, 2017 Category: Drugs & Pharmacology Source Type: research

PEG coated and doxorubicin loaded multimodal Gadolinium oxide nanoparticles for simultaneous drug delivery and imaging applications
We report water-in-oil microemulsion mediated synthesis of PEG 1 1 Polyethylene glycol coated Gd2O3 NPs 2 2 Nanoparticles loaded with fluorescent anti-cancer drug dox 3 3 Doxorubicin for synchronous drug delivery, optical and MR 4 4 Magnetic resonance imaging applications. These PEG covered Gd2O3 NPs loaded with dox (Gd-PEG-dox NPs) were found to possess spherical morphology with 13nm size as measured from TEM and the hydrodynamic diameter comes out to be 37nm as determined from DLS. Fluorescence spectra and fluorescence microscopy images confirmed optical activity of the NPs. The paramagnetic nature of NPs was affirmed by...
Source: International Journal of Pharmaceutics - May 30, 2017 Category: Drugs & Pharmacology Source Type: research

Association of chitosan and aluminium as a new adjuvant strategy for improved vaccination
In conclusion, we established that CH-Al NPs, combining two immunostimulants to enhance both humoral and cellular immune responses, are a safe and promising system for antigen delivery. Our findings point towards their potential in future vaccination approaches. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 30, 2017 Category: Drugs & Pharmacology Source Type: research

Investigating drug absorption from the colon: Single-pass vs. Doluisio approaches to in-situ rat large-intestinal perfusion
In conclusion, the single-pass intestinal perfusion (SPIP) and the Doluisio (closed-loop) perfusion models were found to be equally convenient and useful for obtaining validated colon permeability values, although more human colonic Fabs data are needed for a better understanding of colonic drug permeability and absorption. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 30, 2017 Category: Drugs & Pharmacology Source Type: research

Synbiotic loaded chitosan-Ca-alginate microparticles reduces inflammation in the TNBS model of rat colitis
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Tanja Petreska Ivanovska, Kristina Mladenovska, Zoran Zhivikj, Maja Jurhar Pavlova, Ivica Gjurovski, Trpe Ristoski, Lidija Petrushevska-Tozi New therapeutic strategies against inflammatory bowel disease (IBD) consider the usage of probiotics, prebiotics and synbiotics as beneficial for the intestinal microbial balance. Limitations of such an approach are addressed into difference in survival, persistence, colonization and variable effects among different probiotic strains, lack in understanding of probioti...
Source: International Journal of Pharmaceutics - May 30, 2017 Category: Drugs & Pharmacology Source Type: research

Biodegradable PCL/fibroin/hydroxyapatite porous scaffolds prepared by supercritical foaming for bone regeneration
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Luis Diaz-Gomez, Carlos A. García-González, Jiamian Wang, Fang Yang, Salvador Aznar-Cervantes, Jose Luis Cenis, Ricardo Reyes, Araceli Delgado, Carmen Évora, Angel Concheiro, Carmen Alvarez-Lorenzo Regenerative medicine seeks advanced solutions for bone repair in the form of bioactive synthetic scaffolds by using simple and reproducible processing techniques. In this work, poly-ε-caprolactone (PCL)-based porous scaffolds with improved osteoconductive and osteoinductive properti...
Source: International Journal of Pharmaceutics - May 30, 2017 Category: Drugs & Pharmacology Source Type: research

Ciprofloxacin-loaded lipid-core nanocapsules as mucus penetrating drug delivery system intended for the treatment of bacterial infections in cystic fibrosis
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Afra Torge, Stefanie Wagner, Paula S. Chaves, Edilene G. Oliveira, Silvia S. Guterres, Adriana R. Pohlmann, Alexander Titz, Marc Schneider, Ruy C.R. Beck Treatment of bacterial airway infections is essential for cystic fibrosis therapy. However, effectiveness of antibacterial treatment is limited as bacteria inside the mucus are protected from antibiotics and immune response. To overcome this biological barrier, ciprofloxacin was loaded into lipid-core nanocapsules (LNC) for high mucus permeability, sustai...
Source: International Journal of Pharmaceutics - May 27, 2017 Category: Drugs & Pharmacology Source Type: research

Dendrimer-conjugated peptide vaccine enhances clearance of Chlamydia trachomatis genital infection
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Ingrid S. Ganda, Qian Zhong, Mirabela Hali, Ricardo L.C. Albuquerque, Francine F. Padilha, Sandro R.P. da Rocha, Judith A. Whittum-Hudson Peptide-based vaccines have emerged in recent years as promising candidates in the prevention of infectious diseases. However, there are many challenges to maintaining in vivo peptide stability and enhancement of peptide immunogenicity to generate protective immunity which enhances clearance of infections. Here, a dendrimer-based carrier system is proposed for peptide-ba...
Source: International Journal of Pharmaceutics - May 27, 2017 Category: Drugs & Pharmacology Source Type: research

Polymer coated mucoadhesive liposomes intended for the management of xerostomia
In this study three different types of liposomes (positively, negatively and neutrally charged) were coated with five different types of polymers: low-methoxylated pectin (LM-pectin), high-methoxylated pectin (HM-pectin), alginate, chitosan and hydrophobically modified ethyl hydroxyethyl cellulose (HM-EHEC). The particle size and the zeta potential of the obtained carriers were tested by measuring dynamic light scattering (DLS) and electrophoretic mobility. Later on, selected positively charged liposomes were deposited on a negatively charged mica surface and depicted by atomic force microscopy (AFM). The water sorption pr...
Source: International Journal of Pharmaceutics - May 26, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted co-delivery of polypyrrole and rapamycin by trastuzumab-conjugated liposomes for combined chemo-photothermal therapy
In this study, we aimed to present a strategy to combine chemo and phototherapy and targeted delivery via monoclonal antibody for enhanced anticancer effects. We co-loaded a chemotherapeutic agent, rapamycin, and a photosensitizer, polypyrrole, in trastuzumab-conjugated liposomes (LRPmAb) for combined chemo-photothermal therapy. LRPmAb had small size (172.2±9.6nm), narrow distribution, and negative ζ-potential (−12.0±0.3mV). In addition, LRPmAb showed pH- and temperature-dependent release profiles. LRPmAb showed significantly enhanced uptake in BT-474 cells, a natural HER2/neu expressing cell line....
Source: International Journal of Pharmaceutics - May 25, 2017 Category: Drugs & Pharmacology Source Type: research

Cucurbit[7]-assisted sustained release of human calcitonin from thermosensitive block copolymer hydrogel
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Hui Shang, Xiaobin Chen, Yanpeng Liu, Lin Yu, Jianshu Li, Jiandong Ding Conventional formulations of human calcitonin (hCT), a peptide drug, normally suffer from limited therapeutic efficacy with low stability and short half-life. We have found that the fibrillation of highly amyloidogenic hCT can be inhibited by cucurbit[7] (CB[7]), an amphiphilic small molecule. Meanwhile, a thermogelling copolymer was found to be a suitable candidate for sustained delivery of peptide/protein drugs. Herein, we report a l...
Source: International Journal of Pharmaceutics - May 25, 2017 Category: Drugs & Pharmacology Source Type: research

Poly(acrylic acid) microspheres loaded with superparamagnetic iron oxide nanoparticles for transcatheter arterial embolization and MRI detectability: In vitro and in vivo evaluation
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Zi-Yuan Li, Xiao-Ya Qin, Li-Ying Guo, Huan Wang, Xiao-Xin Liu, Zhuo-Zhao Zheng, Hai-Tao Guan, Li Song, Ying-Hua Zou, Tian-Yuan Fan To develop embolic microspheres with MRI detectability, superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized and mixed with monomer of acrylic acid to prepare SPIONs-loaded polymerized microspheres (SPMs) by inverse suspension polymerization method. The SPMs were evaluated for the ability of embolization by investigating the morphology, particle size, elasticity...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Behaviour of silver nanoparticles in simulated saliva and gastrointestinal fluids
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Lucie Pinďáková, Věra Kašpárková, Kristina Kejlová, Markéta Dvořáková, Daniel Krsek, Dagmar Jírová, Lucie Kašparová Continuously increasing application of silver nanoparticles (AgNPs) requires information on their safety and performance under biological conditions. Assessment of AgNPs in biological systems is also related to availability of robust toxicological methods for evaluation of toxic potential of AgNPs an...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Characterization of new crystalline forms of hydroxyprogesterone caproate
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Jeffrey Caplette, Timothy Frigo, Michael Jozwiakowski, Helene Shea, Mahmoud Mirmehrabi, Peter Müller A systematic polymorph screening process was conducted on the steroid hydroxyprogesterone caproate, which had only one previously described orthorhombic crystalline form (A), in order to fully elucidate its solid state properties. Cooling, anti-solvent and evaporative techniques largely reproduced the same polymorph, but slurries in various solvents over two days produced a new triclinic form (B). Expe...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Sertaconazole nitrate loaded nanovesicular systems for targeting skin fungal infection: In-vitro, ex-vivo and in-vivo evaluation
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Menna M. Abdellatif, Islam A. Khalil, Mahmoud A.F. Khalil The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin ...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Development of modified release 3D printed tablets (printlets) with pharmaceutical excipients using additive manufacturing
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Alvaro Goyanes, Fabrizio Fina, Annalisa Martorana, Daniel Sedough, Simon Gaisford, Abdul W. Basit The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into ent...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Evaluation of lipid-stabilised tripropionin nanodroplets as a delivery route for combretastatin A4
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Victoria Mico, Antonia Charalambous, Sally A. Peyman, Radwa H. Abou-Saleh, Alexander F. Markham, P. Louise Coletta, Stephen D. Evans Lipid-based nanoemulsions are a cheap and elegant route for improving the delivery of hydrophobic drugs. Easy and quick to prepare, nanoemulsions have promise for the delivery of different therapeutic agents. Although multiple studies have investigated the effects of the oil and preparation conditions on the size of the nanoemulsion nanodroplets for food applications, analogo...
Source: International Journal of Pharmaceutics - May 22, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted si-RNA with liposomes and exosomes (extracellular vesicles): How to unlock the potential
Publication date: 20 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 2 Author(s): Sophia Antimisiaris, Spyridon Mourtas, Konstantina Papadia The concept of RNA interference therapeutics has been initiated 18 years ago, and the main bottleneck for translation of the technology into therapeutic products remains the delivery of functional RNA molecules into the cell cytoplasm. In the present review article after an introduction about the theoretical basis of RNAi therapy and the main challenges encountered for its realization, an overview of the different types of delivery systems or carriers, used...
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Delivery of siRNAs
Publication date: 20 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 2 Author(s): Gaetano Lamberti (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Old drug, new wrapping − A possible comeback for chloramphenicol?
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Sveinung G. Ingebrigtsen, Alena Didriksen, Mona Johannessen, Nataša Škalko-Basnet, Ann Mari Holsæter The antimicrobial drug chloramphenicol (CAM) exhibits activity against resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA). However, its use has been limited due to its toxicity. As the threat of antibiotic resistance continues to grow, a promising approach might be to increase the use of historical antimicrobial agents that demonstrate clinical efficacy, but a...
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers employing polyphenols as promising anticancer agents: Quality by design (QbD) approach
This article aims to review the science behind development of NLCs and role of polyphenols as promising anticancer agents. Principles of Quality by Design (QbD) have also been explained which are used in formulation-development of many nanoparticles, including NLCs, as reported in literature. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 20, 2017 Category: Drugs & Pharmacology Source Type: research

On the role of forces governing particulate interactions in pharmaceutical systems: A review
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Saurabh Sarkar, Raj Mukherjee, Bodhisattwa Chaudhuri Process understanding for designing, optimizing and scaling of pharmaceutical unit operations is fundamentally important to address concerns of high risks, monumental costs, and productivity decline in the pharmaceutical industry. This is especially important in the rapidly changing landscape of the pharmaceutical industry. Pharmaceutical processes majorly deal with multiphase, multicomponent flows, basics of which are discussed in terms of fundamental c...
Source: International Journal of Pharmaceutics - May 20, 2017 Category: Drugs & Pharmacology Source Type: research

A quality by design (QbD) twin —Screw extrusion wet granulation approach for processing water insoluble drugs
In this study, a Quality by Design (QbD) approach was used to identify the effect of formulation parameters in a twin screw wet extrusion granulation process for the manufacturing of ibuprofen (IBU) granules with increased dissolution rates. A fractional factorial Design of Experiment (DoE) was used to investigate the effect of the excipient composition, binder amount and liquid to solid (L/S) ratio (independent variables) on drug dissolution rates, median particle size diameter and specific surface area (dependent variables). The intra-granular addition of the binder in inorganic/polymer blends processed with ethanol as g...
Source: International Journal of Pharmaceutics - May 19, 2017 Category: Drugs & Pharmacology Source Type: research

Paclitaxel: What has been done and the challenges remain ahead
We present an overview of the preclinical and clinical data of these systems including their pharmacokinetics, dose and administration, adverse events and clinical efficacy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 18, 2017 Category: Drugs & Pharmacology Source Type: research