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Dual roles of TPGS based microemulsion for tacrolimus: Enhancing the percutaneous delivery and anti-psoriatic efficacy
In this study, we demonstrate for the first time the dual roles of Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS) based microemulsion (ME) for tacrolimus (TAC) to enhance TAC percutaneous delivery and anti-psoriatic efficacy. The ME formulation was developed and optimized based on pseudo-ternary phase diagrams combined with in vitro permeation. The result of Fourier transform infrared spectroscopy (FTIR) demonstrated that TAC was completely solubilized in the TPGS-ME. In vitro permeation studies showed that TPGS-ME enhanced TAC permeation through and into the skin, and the enhanced deposition of TAC in the normal or ...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research

Self-micellizing solid dispersions enhance the properties and therapeutic potential of fenofibrate: Advantages, profiles and mechanisms
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Nian-Qiu Shi, Yong Zhang, Yan Li, Hong-Wei Lai, Xiao Xiao, Bo Feng, Xian-Rong Qi The goal of this work was to compare fenofibrate (FEN)-containing self-micellizing solid dispersion (SmSD) and non-self-micellizing solid dispersion (NsSD) systems. Exploration of underlying mechanisms to improve FEN dissolution/solubility profiles was conducted to understand the enhanced therapeutic potential. SmSD and NsSD of FEN systems (SmSD/FEN and NsSD/FEN) were fabricated using a fuse-quench cooling method. The self-mi...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research

A multi-technique characterization of the stability of surfactant containing solid dispersion based buccal patches prepared by hot melt injection moulding
This study investigates the stability of typically complex multi-component hydrophilic solid dispersions that could be used in a clinical application. Felodipine solid dispersions in two types of blends consisting of PEG, PEO and Tween 80 or Vit E TPGS were prepared by hot melt-injection moulding (HMIM) across a range of drug loadings and subjected to a range of storage conditions. Microscopy, thermal analysis, spectroscopy and powder X-ray diffraction were used to characterize the systems. The semi-solid surfactant TPGS showed a better solubilizing effect on the drug than the liquid surfactant Tween 80 in the fresh state ...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Anna Krupa, Oriane Cantin, Beata Strach, Elżbieta Wyska, Zbisław Tabor, Juergen Siepmann, Andrzej Wróbel, Renata Jachowicz Different types of ground hot-melt extrudates loaded with 10, 20 or 30 % of the poorly water-soluble drug tadalafil were prepared and characterized in vitro and in vivo (in rats). Soluplus was used as an amorphous carrier material, whereas mannitol and lactitol were studied as crystalline matrix formers. The systems were characterized using X-ray powder diffraction, thermogra...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring drug solubility in fasted human intestinal fluid aspirates: Impact of inter-individual variability, sampling site and dilution
This study reports the solubility of a series of 27 commonly used acidic, neutral and basic drugs in human intestinal fluid samples collected from the duodenum or jejunum of healthy volunteers under fasted state conditions. The interindividual variability as well as the impact of factors such as pH, sampling site and bile salts on the solubility in human intestinal fluids was investigated. The solubility measurements were evaluated using a statistical experimental design. Variability in solubility across volunteers and sampling sites was highly compound-specific and appeared to be substantial for weak acids and bases and f...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research

Gemcitabine-vitamin E conjugates: Synthesis, characterization, entrapment into nanoemulsions, and in-vitro deamination and antitumor activity
The objective of the present study was to test the in-vitro anticancer activity of gemcitabine conjugated to the γ-tocotrienol isomer of vitamin E against pancreatic tumor cells. This objective was based on reported studies in which it was demonstrated that free tocotrienol isomers of vitamin E can potentiate the anticancer activity of gemcitabine. To accomplish this objective, a full synthesis scheme for gemcitabine conjugation to fatty acids (stearic and linoleic) and the tocopherol and tocotrienol isomers of vitamin E (α-T and γ-T3) was presented. The conjugates were characterized by 1H NMR and mass sp...
Source: International Journal of Pharmaceutics - June 20, 2017 Category: Drugs & Pharmacology Source Type: research

Design and development of multi-walled carbon nanotube-liposome drug delivery platforms
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Natassa Pippa, Demetrios D. Chronopoulos, Dimitris Stellas, Rodrigo Fernández-Pacheco, Raul Arenal, Costas Demetzos, Nikos Tagmatarchis The aim of this study is to design and develop delivery platforms made of liposomes and multi-walled carbon nanotubes (MWCNTs). We used different lipids with different main transition temperature (Tm) and differently functionalized MWCNTs with organic addends possessing either positive or negative charge. The phospholipids used for the formulations were 1,2-dipalmi...
Source: International Journal of Pharmaceutics - June 20, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of chemical and physical enhancement techniques on transdermal delivery of 3-fluoroamphetamine hydrochloride
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Ashana Puri, Kevin S. Murnane, Bruce E. Blough, Ajay K. Banga The present study investigated the passive transdermal delivery of 3-fluoroamphetamine hydrochloride (PAL-353) and evaluated the effects of chemical and physical enhancement techniques on its permeation through human skin. In vitro drug permeation studies through dermatomed human skin were performed using Franz diffusion cells. Passive permeation of PAL-353 from propylene glycol and phosphate buffered saline as vehicles was studied. Effect of o...
Source: International Journal of Pharmaceutics - June 20, 2017 Category: Drugs & Pharmacology Source Type: research

Novel salicylic acid-based chemically crosslinked pH-sensitive hydrogels as potential drug delivery systems
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Bahar Demirdirek, Kathryn E. Uhrich In this work, salicylic acid (SA), a non-steroidal anti-inflammatory, was chemically incorporated into hydrogel systems to achieve sustained SA release profiles. With its anti-inflammatory properties, sustained release of SA would be relevant for treating diseases such as diabetes and cancer. In this work, SA was chemically incorporated into hydrogel systems via covalent attachment to an itaconate moiety followed by UV-initiated crosslinking using acrylic acid and poly(...
Source: International Journal of Pharmaceutics - June 17, 2017 Category: Drugs & Pharmacology Source Type: research

How does secondary processing affect the physicochemical properties of inhalable salbutamol sulphate particles? A temporal investigation
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Joana T. Pinto, Snezana Radivojev, Sarah Zellnitz, Eva Roblegg, Amrit Paudel As pulmonary drug delivery is extended from low doses to high doses, physicochemical characteristics of the active pharmaceutical ingredient gain importance in the development of dry powder inhalers. Therefore, the present work aims to understand the impact of distinct engineering techniques on the process induced physicochemical characteristics of salbutamol sulphate particles over time. The particle engineering techniques chose...
Source: International Journal of Pharmaceutics - June 17, 2017 Category: Drugs & Pharmacology Source Type: research

Optimisation of HPMC ophthalmic inserts with sustained release properties as a carrier for thermolabile therapeutics
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Arnout Everaert, Yannick Wouters, Eline Melsbach, Nadia Zakaria, Annick Ludwig, Filip Kiekens, Wim Weyenberg A methodology was developed and optimised for the preparation of a new drug delivery system (DDS) with sustained release properties to allow ocular protein delivery and to limit destructive production steps during manufacturing. Elevated temperatures, shear forces and an oxidative environment should be avoided in order to prevent denaturation or oxidation of proteins. An aqueous HPMC solution was p...
Source: International Journal of Pharmaceutics - June 17, 2017 Category: Drugs & Pharmacology Source Type: research

Development of semisolid self-microemulsifying drug delivery systems (SMEDDSs) filled in hard capsules for oral delivery of aciclovir
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Ljiljana Djekic, Jovana Jankovic, Bojan Čalija, Marija Primorac The study aimed to develop semisolid self-microemulsifying drug delivery systems (SMEDDSs) as carriers for oral delivery of aciclovir in hard hydroxypropylmethyl cellulose (HPMC) capsules. Six self-dispersing systems (SD1-SD6) were prepared by loading aciclovir into the semisolid formulations consisting of medium chain length triglycerides (lipid), macrogolglycerol hydroxystearate (surfactant), polyglyceryl-3-dioleate (cosurfactant), glycero...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

Determination of the release mechanism of Theophylline from pellets coated with Surelease ®—A water dispersion of ethyl cellulose
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Jurgita Kazlauske, Maria Margherita Cafaro, Diego Caccavo, Mariagrazia Marucci, Gaetano Lamberti, Anna Angela Barba, Anette Larsson The aim of this study was to investigate the water transport over free standing films based on the aqueous ethyl cellulose (EC) coating Surelease® and the drug (Theophylline) release mechanism from coated pellets. It was found that the main drug release rate from pellets was controlled by a diffusion mechanism. However, the drug release rate was altered by addition of sod...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

Tumor-specific delivery of doxorubicin through conjugation of pH-responsive peptide for overcoming drug resistance in cancer
In this study, we prepared a peptide-Dox conjugate aimed at offering Dox molecules a tumor-specific functionality and improving the therapeutic effects of Dox against resistant tumor cells. A slightly acidic pH-sensitive peptide (SAPSP) with high selectivity for cancer cells was attached to Dox to obtain SAPSP-Dox prodrug. The structures and properties of this prodrug were characterized, confirming several merits, including desirable pH-sensitive property, good serum stability and favorable release behavior. Cellular uptake studies demonstrated that SAPSP-Dox was preferably accumulated in cancer cells (Dox-sensitive MCF-7 ...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

Targeting integrin-rich tumors with temoporfin-loaded vitamin-E-succinate-grafted chitosan oligosaccharide/d- α-tocopheryl polyethylene glycol 1000 succinate nanoparticles to enhance photodynamic therapy efficiency
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Junru Wu, Shu Feng, Wenchao Liu, Feng Gao, Yanzuo Chen A major challenge in cancer photodynamic therapy (PDT) is the poor tumor selectivity of the photosensitizer. Therefore, temoporfin (mTHPC)-loaded nanoparticles, based on vitamin-E-succinate-grafted chitosan oligosaccharide and cyclic (arginine-glycine-aspartic acid-d-phenylalanine-lysine) (c[RGDfK])-modified d-α-tocopheryl polyethylene glycol 1000 succinate, were prepared (RGD-NPs) and were expected to enhance the accumulation of mTHPC in integr...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

Impact of droplet evaporation rate on resulting in vitro performance parameters of pressurized metered dose inhalers
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Poonam Sheth, Matthew R. Grimes, Stephen W. Stein, Paul B. Myrdal Pressurized metered dose inhalers (pMDIs) are widely used for the treatment of pulmonary diseases. The overall efficiency of pMDI drug delivery may be defined by in vitro parameters such as the amount of drug that deposits on the model throat and the proportion of the emitted dose that has particles that are sufficiently small to deposit in the lung (i.e., fine particle fraction, FPF). The study presented examines product performance of ten...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

The future of pharmaceutical quality and the path to get there
This article outlines an ambitious goal and is intended to be thought-provoking in spite of the challenging path to get there. This goal is envisioned because it is in the best interest of patients and consumers and is realizable with continued advances and investments in science and technology. The fundamental destination of pharmaceutical quality has been long envisioned: a maximally efficient, agile, flexible pharmaceutical manufacturing sector that reliably produces high quality drugs without extensive regulatory oversight. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

RTD modeling of a continuous dry granulation process for process control and materials diversion
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Julia Kruisz, Jakob Rehrl, Stephan Sacher, Isabella Aigner, Martin Horn, Johannes G. Khinast Disturbance propagation during continuous manufacturing processes can be predicted by evaluating the residence time distribution (RTD) of the specific unit operations. In this work, a dry granulation process was modelled and four scenarios of feeding events were simulated. We performed characterization of the feeders and developed RTD models for the blender and the roller compactor based on impulse-response measur...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

A comprehensive spectroscopic study of the polymorphs of diflunisal and their phase transformations
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Anuradha R. Pallipurath, Francesco Civati, Juraj Sibik, Clare Crowley, J. Axel Zeitler, Patrick McArdle, Andrea Erxleben Understanding phase transitions in pharmaceutical materials is of vital importance for drug manufacturing, processing and storage. In this paper we have carried out comprehensive high-resolution spectroscopic studies on the polymorphs of the non-steroidal anti-inflammatory drug diflunisal that has four known polymorphs, forms I–IV (FI–FIV), three of which have known crystal ...
Source: International Journal of Pharmaceutics - June 16, 2017 Category: Drugs & Pharmacology Source Type: research

Raman imaging of cellular uptake and studies of silver nanoparticles effect in BJ human fibroblasts cell lines
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Monika Perlovska Harvanova, Jana Jiravova, Jakub Malohlava, Katerina Barton Tomankova, Dagmar Jirova, Hana Kolarova Silver nanoparticles (AgNPs) have been widely studied for their beneficial antimicrobial effect and have been considered by some to be a safe ingredient, as penetration of metal nanoparticles through the skin in vivo has not been proven. However, AgNPs are becoming a commonly applied nanomaterial for surface modifications of medical products which come into contact with damaged skin. In our ...
Source: International Journal of Pharmaceutics - June 14, 2017 Category: Drugs & Pharmacology Source Type: research

3D printed tablets loaded with polymeric nanocapsules: An innovative approach to produce customized drug delivery systems
This study represents an original approach to convert nanocapsules suspensions into solid dosage forms as well as an efficient 3D printing method to produce novel drug delivery systems, as personalised nanomedicines. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 13, 2017 Category: Drugs & Pharmacology Source Type: research

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