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Fabrication of non-dissolving analgesic suppositories using 3D printed moulds
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Yuanyuan Sun, Xucong Ruan, Hairui Li, Himanshu Kathuria, Guang Du, Lifeng Kang Conventional suppositories sometimes fail in exerting their therapeutic activity as the base materials melt inside body cavities. Also they are not suitable to provide long term treatment. Biomedical grade silicone elastomers may be used to fabricate non-dissolvable suppositories to overcome these disadvantages. We kneaded 4 analgesics into the 2 kinds of silicone polymers at 1%, 5% and 10% drug loading, respectively, to tes...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Can Sophorolipids prevent biofilm formation on silicone catheter tubes?
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Cristiana Pontes, Marta Alves, Catarina Santos, Maria H. Ribeiro, Lídia Gonçalves, Ana F. Bettencourt, Isabel A.C. Ribeiro Given the impact of biofilms in health care environment and the increasing antibiotic resistance and/or tolerance, new strategies for preventing that occurrence in medical devices are obligatory. Thus, biomaterials surface functionalization with active compounds can be a valuable approach. In the present study the ability of the biosurfactants sophorolipids to prevent...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Comparison of breaking tests for the characterization of the interfacial strength of bilayer tablets
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Luca Castrati, Vincent Mazel, Virginie Busignies, Harona Diarra, Alessandra Rossi, Paolo Colombo, Pierre Tchoreloff The bilayer tableting technology is gaining more acceptance in the drug industry, due to its ability to improve the drug delivery strategies. It is currently assessed by the European Pharmacopoeia, that the mechanical strength of tablets can be evaluated using a diametral breaking tester. This device applies a force diametrically, and records the tablet breaking point. This approach has b...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Targeted release of transcription factors for cell reprogramming by a natural micro-syringe
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Lionel Berthoin, Bertrand Toussaint, Frédéric Garban, Audrey Le Gouellec, Benjamin Caulier, Benoît Polack, David Laurin Ectopic expression of defined transcription factors (TFs) for cell fate handling has proven high potential interest in reprogramming differentiated cells, in particular for regenerative medicine, ontogenesis study and cell based modelling. Pluripotency or transdifferentiation induction as TF mediated differentiation is commonly produced by transfer of genetic infor...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

LARETH-25 and β-CD improve central transitivity and central pharmacological effect of the GLP-2 peptide
We reported that intracerebroventricular administration of glucagon-like peptide-2 (GLP-2) exerts antidepressant-like effects treated with or without adrenocorticotropic hormone. In the present study, we developed a nasal formulation of GLP-2 containing 5% polyoxyethylene (25) lauryl ether and 1% β-cyclodextrin that enhanced the resistance of GLP-2 to inactivation by dipeptidyl peptidase-4. Intranasal administration of this formulation (60μg/kg) increased the delivery of GLP-2 to the brain and had antidepressant-like effects on rats. These results suggest the potential of the GLP-2 nasal formulation for use as a no...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Tunable doxorubicin release from polymer-gated multiwalled carbon nanotubes
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Alessandro Pistone, Daniela Iannazzo, Shabana Ansari, Candida Milone, Marina Salamò, Signorino Galvagno, Santa Cirmi, Michele Navarra Two pH and temperature controlled drug delivery systems for cancer therapy are here reported by using vapour phase and liquid phase functionalized multiwalled carbon nanotubes (MWCNT). Both oxidized MWCNT were functionalized at the carboxyl groups with a short hydrophilic polyethylene glycol (PEG) chain. The nanosystems were loaded with doxorubicin and covered wit...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Changes in apoptosis-related gene expression and cytokine release in breast cancer cells treated with CpG-loaded magnetic PAMAM nanoparticles
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Negar Taghavi Pourianazar, Ufuk Gunduz CpG-oligodeoxynucleotide (CpG-ODN) can function as an immune adjuvant. Previously, we showed that stimulation of breast cancer cells with CpG-ODN conjugated with PAMAM dendrimer-coated magnetic nanoparticles (DcMNPs) has induced apoptosis. The aim of the current study was to evaluate the expression levels of some apoptosis-regulating genes in several human breast cancer cells treated with CpG/DcMNPs. Treated MDA-MB231 cells showed an increase in Noxa and Bax gene ...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Application of RPMI 2650 as a cell model to evaluate solid formulations for intranasal delivery of drugs
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Vanessa S.S. Gonçalves, Ana A. Matias, Joana Poejo, Ana T. Serra, Catarina M.M. Duarte During the development of intranasal drug delivery systems for local/systemic effect or brain targeting, it is necessary to assess its cytotoxicity and drug transport through nasal epithelium. In order to avoid animal experiments or the use of excised tissues, in vitro cell models, such as RPMI 2650 cells, are being preferred during recent years. Nevertheless, the deposition of solid formulations into nasal ce...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Mechanisms of cellular uptake and endosomal escape of calcium-siRNA nanocomplexes
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Matan Goldshtein, Efrat Forti, Emil Ruvinov, Smadar Cohen Ca2+-siRNA nanocomplexes represent a simple yet an effective platform for siRNA delivery into the cell cytoplasm, with subsequent successful siRNA-induced target gene silencing. Herein, we aimed to elucidate the roles played by calcium ions in siRNA nanocomplex formation, cell uptake, and endosomal escape. We investigated whether the replacement of Ca2+in the nanocomplex by other bivalent cations would affect their cell entry and subsequent gene...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Colistin-entrapped liposomes driven by the electrostatic interaction: Mechanism of drug loading and in vivo characterization
The objective of this study is to investigate the loading mechanism and validity of applying electrostatic attraction for the colistin entrapment and delivery in liposomes. Anionic lipids with various structures were used for colistin entrapment, and the properties of resulting liposomes (i.e. zeta-potential, EE and release rate) were highly dependent on the structure of anionic lipids. Based on consideration of intermolecular interactions, the retention of electrostatically entrapped colistin is essentially determined by the balance of interfacial hydrophobic attraction and electrostatic repulsion. The liposomal colistin ...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research

Adaptation of pharmaceutical excipients to FDM 3D printing for the fabrication of patient-tailored immediate release tablets
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Muzna Sadia, Agata Sośnicka, Basel Arafat, Abdullah Isreb, Waqar Ahmed, Antonios Kelarakis, Mohamed A Alhnan This work aims to employ fused deposition modelling 3D printing to fabricate immediate release pharmaceutical tablets with several model drugs. It investigates the addition of non-melting filler to methacrylic matrix to facilitate FDM 3D printing and explore the impact of (i) the nature of filler, (ii) compatibility with the gears of the 3D printer and iii) polymer: filler ratio on the 3D print...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Reevaluation of the diametral compression test for tablets using the flattened disc geometry
In this study, the flattened disc geometry was used as an alternative to avoid contact problems. The diametral compression on both flattened and standard geometries was first studied using finite element method (FEM) simulation. It was found that, for the flattened geometry, both maximum tensile strain and stress were located at the center of the tablet, which was not the case for the standard geometry. Experimental observations using digital image correlation (DIC) confirmed the numerical results. The experimental tensile strength obtained using both geometries were compared and it was found that the standard geometry alw...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of rifampicin to tuberculosis-infected macrophages: design, in-vitro, and in-vivo performance of rifampicin-loaded poly(ester amide)s nanocarriers
In this study, biodegradable amino acid based poly(ester amide)s (PEAs) were synthesized by the poly condensation reaction and RF-loaded NPs were fabricated by the dialysis method. The surface morphology and in-vitro drug release efficiency were examined. The effect of time and temperature on the cellular uptake of PEA-RF-NPs in NR8383 cells was evaluated. Fluorescence microscopic results of PEA-RF-NPs from NR8383 cell lines suggest its potential application in treating TB. The antibacterial activity of RF against Mycobacterium smegmatis was also evaluated. Based on these results, this approach provides a new means for con...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

A comparative study between melt granulation/compression and hot melt extrusion/injection molding for the manufacturing of oral sustained release thermoplastic polyurethane matrices
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): G. Verstraete, P. Mertens, W. Grymonpré, P.J. Van Bockstal, T. De Beer, M.N. Boone, L. Van Hoorebeke, J.P. Remon, C. Vervaet During this project 3 techniques (twin screw melt granulation/compression (TSMG), hot melt extrusion (HME) and injection molding (IM)) were evaluated for the manufacturing of thermoplastic polyurethane (TPU)-based oral sustained release matrices, containing a high dose of the highly soluble metformin hydrochloride. Whereas formulations with a drug load between 0 and 70% (w...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Photosensitizer-conjugated tryptophan-containing peptide ligands as new dual-targeted theranostics for cancers
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Jisu Kim, Jihyun Chae, Jun Soo Kim, Sung-Ho Goh, Yongdoo Choi Here we report that new dual-targeted theranostic anti-cancer agents can be produced by simple conjugation of photosensitizers with tryptophan-containing peptide ligands via cyclic disulfide linkages. In the proof-of-concept study, photosensitizers conjugated with EGFR-targeting peptide GE11 (C-EGFR) were in close proximity with tryptophan residues in the conjugate, resulting in quenching of its fluorescence and singlet oxygen generation. C-...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Paclitaxel loaded magnetic nanocomposites with folate modified chitosan/carboxymethyl surface; a vehicle for imaging and targeted drug delivery
This study validate that NFs-BSA–CS–FA or NFs-BSA–CMC–FA and PTX-NFs-BSA–CS–FA or PTX-NFs-BSA–CS–FA are suitable systems for tumor diagnosis and therapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Application of 13C NMR cross-polarization inversion recovery experiments for the analysis of solid dosage forms
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Dariusz Maciej Pisklak, Monika Zielińska-Pisklak, Łukasz Szeleszczuk Solid-state nuclear magnetic resonance (ssNMR) is a powerful and unique method for analyzing solid forms of the active pharmaceutical ingredients (APIs) directly in their original formulations. Unfortunately, despite their wide range of application, the ssNMR experiments often suffer from low sensitivity and peaks overlapping between API and excipients. To overcome these limitations, the crosspolarization inversion recovery method w...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

HMDSO-plasma coated electrospun fibers of poly(cyclodextrin)s for antifungal dressings
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Alejandro Costoya, Florencia Montini Ballarin, Jose Llovo, Angel Concheiro, Gustavo A. Abraham, Carmen Alvarez-Lorenzo Electrospun mats containing cyclodextrin polymers (poly-αCD or poly-βCD) were developed to act as wound dressings showing tunable release rate of the antifungal agent fluconazole incorporated forming inclusion complexes. Poly-αCD and poly-βCD were prepared via cross-linking with epichlorohydrin (EPI) as water-soluble large molecular weight polymers. Then, polyCDs ...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Permeation of topically applied caffeine from a food by —product in cosmetic formulations: Is nanoscale in vitro approach an option?
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Francisca Rodrigues, Ana Catarina Alves, Claudia Nunes, Bruno Sarmento, M. Helena Amaral, Salette Reis, M. Beatriz P.P. Oliveira The aim of the present work was to develop and evaluate the potential of nanostructured lipid carriers associated with caffeine extracted from Coffee Silverskin (NLC-CS), a food by-product, as a new possible topical therapy of cellulitis. Caffeine gain increasing research interest due to their cosmetic potential, particularly in gynoid lipodystrophy, commonly known as celluli...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Triclosan loaded electrospun nanofibers based on a cyclodextrin polymer and chitosan polyelectrolyte complex
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Safa Ouerghemmi, Stéphanie Degoutin, Nicolas Tabary, Frédéric Cazaux, Mickaël Maton, Valérie Gaucher, Ludovic Janus, Christel Neut, Feng Chai, Nicolas Blanchemain, Bernard Martel This work focuses on the relevance of antibacterial nanofibers based on a polyelectrolyte complex formed between positively charged chitosan (CHT) and an anionic hydroxypropyl betacyclodextrin (CD)-citric acid polymer (PCD) complexing triclosan (TCL). The study of PCD/TCL inclusion complex and ...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

Gelatin-based membrane containing usnic acid-loaded liposome improves dermal burn healing in a porcine model
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Paula Santos Nunes, Alessandra Silva Rabelo, Jamille Cristina Campos de Souza, Bruno Vasconcelos Santana, Thailson Monteiro Menezes da Silva, Mairim Russo Serafini, Paula dos Passos Menezes, Bruno dos Santos Lima, Juliana Cordeiro Cardoso, Júlio César Santana Alves, Luiza Abrahão Frank, Sílvia Stanisçuaski Guterres, Adriana Raffin Pohlmann, Malone Santos Pinheiro, Ricardo Luiz Cavalcanti de Albuquerque, Adriano Antunes de Souza Araújo There are a range of produ...
Source: International Journal of Pharmaceutics - October 5, 2016 Category: Drugs & Pharmacology Source Type: research

The development of medicines for older adults: A personal perspective from industry
Publication date: 30 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 2 Author(s): Linda Hakes (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 4, 2016 Category: Drugs & Pharmacology Source Type: research

Foreword: Special issue —geriatric drug therapy
Publication date: 30 October 2016 Source:International Journal of Pharmaceutics, Volume 512, Issue 2 Author(s): Mine Orlu Gul, Fang Liu, Carmel Hughes (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 4, 2016 Category: Drugs & Pharmacology Source Type: research

Dual effect of F-actin targeted carrier combined with antimitotic drug on aggressive colorectal cancer cytoskeleton: Allying dissimilar cell cytoskeleton disrupting mechanisms
This study suggests that employing such a suitable pair of drug-carriers with dissimilar sites of action, thus allying the different cell cytoskeleton disrupting mechanisms, may provide a more efficient cancer therapy approach. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 26, 2016 Category: Drugs & Pharmacology Source Type: research

Opsonisation of nanoparticles prepared from poly( β-hydroxybutyrate) and poly(trimethylene carbonate)-b-poly(malic acid) amphiphilic diblock copolymers: Impact on the in vitro cell uptake by primary human macrophages and HepaRG hepatoma cells
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Elise Vene, Ghislaine Barouti, Kathleen Jarnouen, Thomas Gicquel, Claudine Rauch, Catherine Ribault, Sophie M. Guillaume, Sandrine Cammas-Marion, Pascal Loyer The present work reports the investigation of the biocompatibility, opsonisation and cell uptake by human primary macrophages and HepaRG cells of nanoparticles (NPs) formulated from poly(β-malic acid)-b-poly(β-hydroxybutyrate) (PMLA-b-PHB) and poly(β-malic acid)-b-poly(trimethylene carbonate) (PMLA-b-PTMC) diblock copolymers, namel...
Source: International Journal of Pharmaceutics - September 23, 2016 Category: Drugs & Pharmacology Source Type: research

Cytotoxic and cytostatic side effects of chitosan nanoparticles as a non-viral gene carrier
In conclusion, treatment of different cell lines with CNs-pDNA showed that their biocompatibility was limited and the effects were cell type-dependent. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 23, 2016 Category: Drugs & Pharmacology Source Type: research

Lipid core peptide/poly(lactic-co-glycolic acid) as a highly potent intranasal vaccine delivery system against Group A streptococcus
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Nirmal Marasini, Zeinab G. Khalil, Ashwini Kumar Giddam, Khairunnisa Abdul Ghaffar, Waleed M. Hussein, Robert J. Capon, Michael R. Batzloff, Michael F. Good, Mariusz Skwarczynski, Istvan Toth Rheumatic heart disease represents a leading cause of mortality caused by Group A Streptococcus (GAS) infections transmitted through the respiratory route. Although GAS infections can be treated with antibiotics these are often inadequate. An efficacious GAS vaccine holds more promise, with intranasal vaccination ...
Source: International Journal of Pharmaceutics - September 23, 2016 Category: Drugs & Pharmacology Source Type: research

Statistical analysis of industrial-scale roller compactor ‘Freund TF-MINI model’
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): M. Sajjia, Ahmad B. Albadarin, Gavin Walker The aim of this study is to perform a statistical analysis on a pharmaceutical roller compaction process using an industrial-scale roller compactor “Freund TF-MINI model”. The process was modelled using response surface methodology (RSM) to better understand and control the process in order to produce ribbons and granules with optimised quality. The significant process parameters were determined to be (i) the screw speed to roll speed ratio and (i...
Source: International Journal of Pharmaceutics - September 23, 2016 Category: Drugs & Pharmacology Source Type: research

Biophysical evaluation of hybrid Fc fusion protein of hGH to achieve basal buffer system
In conclusion, GXD-9 was found to be most stable at pH 7.0. The investigation of the biophysical stability of a hyFc-fusion protein has demonstrated a positive feasibility of developing more stable formulations to facilitate the initial drug development process for further clinical trials. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 23, 2016 Category: Drugs & Pharmacology Source Type: research

Alginate nanoparticles protect ferrous from oxidation: Potential iron delivery system
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Nuwanthi P. Katuwavila, A.D.L.C. Perera, Damayanthi Dahanayake, V. Karunaratne, Gehan A.J. Amaratunga, D. Nedra Karunaratne A novel, efficient delivery system for iron (Fe2+) was developed using the alginate biopolymer. Iron loaded alginate nanoparticles were synthesized by a controlled ionic gelation method and was characterized with respect to particle size, zeta potential, morphology and encapsulation efficiency. Successful loading was confirmed with Fourier Transform Infrared spectroscopy and Therm...
Source: International Journal of Pharmaceutics - September 22, 2016 Category: Drugs & Pharmacology Source Type: research

A comparison between conventional liposome and drug-cyclodextrin complex in liposome system
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Wen-Xi Wang, Shi-Sen Feng, Cai-Hong Zheng A drug-cyclodextrin complex in liposome system was prepared in order to make a comparison with conventional risperidone-loaded liposome. Thin film hydration, reverse phase evaporation and ethanol injection methods were taken as preparation means to obtain the two types of liposome. Differential thermal analysis (DTA) and transmission electron microscopy (TEM) were used to investigate the thermal characters of inclusion complexes and morphology of liposome, resp...
Source: International Journal of Pharmaceutics - September 20, 2016 Category: Drugs & Pharmacology Source Type: research

Low density lipoprotein receptor targeted doxorubicin/DNA-Gold Nanorods as a chemo- and thermo-dual therapy for prostate cancer
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Nan Zhang, Shasha Li, Haiying Hua, Dan Liu, Lili Song, Pengchao Sun, Weiwei Huang, Yafang Tang, Yongxing Zhao As drug vehicles and therapeutics, Gold Nanorods (GNRs) have various merits such as easy preparation and modification, passive accumulation to tumor tissues, effective intracellular delivery of therapeutics, and thermal responses to laser radiation. Doxorubicin (DOX) has been the standard chemotherapy for cancer. To enhance the anti-cancer efficacy, chemotherapy and thermotherapy were combined ...
Source: International Journal of Pharmaceutics - September 20, 2016 Category: Drugs & Pharmacology Source Type: research

Transdermal iontophoretic delivery of tacrine hydrochloride: Correlation between in vitro permeation and in vivo performance in rats
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Niketkumar Patel, Shashank Jain, Senshang Lin The aim of present investigation is to evaluate the feasibility of transdermal iontophoretic delivery of tacrine hydrochloride in Sprague Dawley (SD) rats using anodal iontophoretic patches and to correlate plasma tacrine concentration profiles to in vitro tacrine permeation flux. In vitro skin permeation studies were carried out across artificial membrane CELGRAD® 2400, freshly excised SD rat abdominal skin, freshly excised hairless rat abdominal skin,...
Source: International Journal of Pharmaceutics - September 20, 2016 Category: Drugs & Pharmacology Source Type: research

Fast dissolution of poorly water soluble drugs from fluidized bed coated nanocomposites: Impact of carrier size
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Mohammad Azad, Jacqueline Moreno, Ecevit Bilgili, Rajesh Davé Formation of core-shell nanocomposites of Fenofibrate and Itraconazole, model poorly water soluble drugs, via fluidized bed (FB) coating of their well-stabilized high drug loaded nanosuspensions is investigated. Specifically, the extent of dissolution enhancement, when fine carrier particles (sub–50μm) as opposed to the traditional large carrier particles (>300μm) are used, is examined. This allows testing the hypot...
Source: International Journal of Pharmaceutics - September 19, 2016 Category: Drugs & Pharmacology Source Type: research

Combining gas-phase electrophoretic mobility molecular analysis (GEMMA), light scattering, field flow fractionation and cryo electron microscopy in a multidimensional approach to characterize liposomal carrier vesicles
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Carlos Urey, Victor U. Weiss, Andreas Gondikas, Frank von der Kammer, Thilo Hofmann, Martina Marchetti-Deschmann, Günter Allmaier, György Marko-Varga, Roland Andersson For drug delivery, characterization of liposomes regarding size, particle number concentrations, occurrence of low-sized liposome artefacts and drug encapsulation are of importance to understand their pharmacodynamic properties. In our study, we aimed to demonstrate the applicability of nano Electrospray Gas-Phase Electrophoret...
Source: International Journal of Pharmaceutics - September 19, 2016 Category: Drugs & Pharmacology Source Type: research

Long term performance evaluation of small-diameter vascular grafts based on polyvinyl alcohol hydrogel and dextran and MSCs-based therapies using the ovine pre-clinical animal model
In conclusion, PVA/Dx graft can be an excellent scaffold candidate for vascular reconstruction, including clinic mechanically challenging applications, such as SDVGs, especially when associated to MSCs-based therapies to promote higher endothelialization and lower fibrosis of the vascular prosthesis, but also higher PR values. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 19, 2016 Category: Drugs & Pharmacology Source Type: research

Statistical analysis and comparison of a continuous high shear granulator with a twin screw granulator: Effect of process parameters on critical granule attributes and granulation mechanisms
This study is concerned with identifying the design space of two different continuous granulators and their respective granulation mechanisms. Performance of a continuous high shear granulator and a twin screw granulator with paracetamol formulations were examined by face-centered cubic design, which focused on investigating key performance metrics, namely, granule size, porosity, flowability and particle morphology of granules as a function of essential input process parameters (liquid content, throughput and rotation speed). Liquid and residence time distribution tests were also performed to gain insights into the liquid...
Source: International Journal of Pharmaceutics - September 19, 2016 Category: Drugs & Pharmacology Source Type: research

Comparison in toxicity and solubilizing capacity of hydroxypropyl- β-cyclodextrin with different degree of substitution
In this study, solubilizing capacity of HP-β-CDs with three different D.S. (4.55, 6.16 and 7.76) for 16 drugs were measured and their toxicities were compared by a 7-day i.v. administration (q.d.) study in rats. Generally, HP-β-CD with high D.S. (7.76) showed weaker solubilizing capacity for steroids and BCS class II drugs, but lower hemolytic activity, compared with that of HP-β-CD with low (4.55) or medium (6.16) D.S. HP-β-CD with low D.S. resulted in more changes in hematological and biochemical parameters, but the effects were reversible after a 7-day recovery. Moreover, HP-β-CD with medium D.S...
Source: International Journal of Pharmaceutics - September 19, 2016 Category: Drugs & Pharmacology Source Type: research

Investigating the ability of nanoparticle-loaded hydroxypropyl methylcellulose and xanthan gum gels to enhance drug penetration into the skin
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): X.J. Cai, P. Mesquida, S.A. Jones Nanoparticle-loaded topical formulations can disrupt drug aggregation through controlled drug-nanoparticle interactions to enhance topical drug delivery. However, the complex relationship between the drug, nanoparticle and formulation vehicle requires further understanding. The aim of this study was to use nanoparticle-loaded hydroxypropyl methylcellulose (HPMC) and xanthan gum gels to probe how the drug, nanoparticle and formulation vehicle interactions influenced the...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Phytochemical-loaded mesoporous silica nanoparticles for nose-to-brain olfactory drug delivery
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Shital Lungare, Keith Hallam, Raj K.S. Badhan Central nervous system (CNS) drug delivery is often hampered due to the insidious nature of the blood-brain barrier (BBB). Nose-to-brain delivery via olfactory pathways have become a target of attention for drug delivery due to bypassing of the BBB. The antioxidant properties of phytochemicals make them promising as CNS active agents but possess poor water solubility and limited BBB penetration. The primary aim of this study was the development of mesoporou...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Targeting prostate cancer cells with genetically engineered polypeptide-based micelles displaying gastrin-releasing peptide
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Wei Zhang, Sanjay Garg, Preethi Eldi, Fiona Huan-huan Zhou, Ian R.D. Johnson, Doug A. Brooks, Frankie Lam, Grigori Rychkov, John Hayball, Hugo Albrecht In recent years G protein-coupled receptors (GPCRs) have emerged as crucial tumorigenic factors that drive aberrant cancer growth, metastasis and angiogenesis. Consequently, a number of GPCRs are strongly expressed in cancer derived cell lines and tissue samples. Therefore a rational anti-cancer strategy is the design of nano-medicines that specifically...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Hydrodynamic size characterization of a self-emulsifying lipid pharmaceutical excipient by Taylor dispersion analysis with fluorescent detection
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Joseph Chamieh, Vincent Jannin, Frédéric Demarne, Hervé Cottet In this work, the sizing of microemulsion droplets of a lipid-based pharmaceutical excipient (Labrasol® ALF) is performed by Taylor dispersion analysis (TDA) using fluorescent detection. An hydrophobic fluorescent marker is used to tag the microemulsion droplet and to increase the sensitivity of detection (compared to UV detection). Combined with the frontal TDA mode, fluorescent detection was mandatory for an accur...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Development of solidified self-microemulsifying delivery systems with enhanced stability of sirolimus and extended release
In this study, the formulation of the SMEDDS was further optimized by investigating the influence of the excipients including the media, antioxidant and organic acid. It was demonstrated that addition of 0.20% of citric acid in SMEDDS most efficiently promoted the stability of SRL under high temperature (40±2°C), high humidity (relative humidity 90±5%) or strong light irradiation (4500±500lx). SMEDDS absorbed by microcrystalline cellulose (MCC) was mixed with hydroxypropyl methylcellulose (HPMC) to prepare tablets. The optimal formulation composed of 15% of HPMC 100 LV with hardness of 120N, which ...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Comparison of different in vitro release methods used to investigate nanocarriers intended for dermal application
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Benjamin Balzus, Miriam Colombo, Fitsum Feleke Sahle, Gaith Zoubari, Sven Staufenbiel, Roland Bodmeier In vitro drug release measurement is one of the most important methods used to assess the quality of a nanocarrier and estimate it́s in vivo performance. Different in vitro drug release methods have been used to investigate the drug release from nanocarriers, however, little information is available with regard to a comparison of these methods (e.g. discriminative power, reproducibility). Thus, drug ...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Intravitreal injection of rapamycin-loaded polymeric micelles for inhibition of ocular inflammation in rat model
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Wei Wu, Zhifen He, Zhaoliang Zhang, Xinxin Yu, Zongming Song, Xingyi Li The therapeutic efficacy of rapamycin conjugated monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles (rapamycin micelles) was evaluated in a rat experimental autoimmune uveitis (EAU) model. Rapamycin micelles exhibited spherical morphology and had a mean particle size of 40nm and a zeta-potential of −0.89mv. The water solubility of rapamycin improved by more than 1000-fold in a micellar formulat...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Novel nanostructured enoxaparin sodium-PLGA hybrid carriers overcome tumor multidrug resistance of doxorubicin hydrochloride
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Jia Wang, Lei Wu, Longfa Kou, Meng Xu, Jin Sun, Yongjun Wang, Qiang Fu, Peng Zhang, Zhonggui He Novel enoxaparin sodium-PLGA hybrid nanocarries (EPNs) were successfully designed for sustained delivery of hydrophilic cationic doxorubicin hydrochloride (DOX) and to overcome multidrug resistance (MDR). By incorporation of the negative polymer of enoxaparin sodium (ES), DOX was highly encapsulated into EPNs with an encapsulation efficiency of 92.49%, and ES effectively inhibited the proliferation of HUVEC ...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

The effect of device resistance and inhalation flow rate on the lung deposition of orally inhaled mannitol dry powder
In conclusion the resistance of Osmohaler™ did not significantly affect the total and regional lung deposition at 50–70L/min PIFR. Instead, the total and regional lung depositions are dependent on the particle size of the aerosol and inhalation flow rate, the latter itself affecting the particle size distribution. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

Drug-eluting biodegradable ureteral stent: New approach for urothelial tumors of upper urinary tract cancer
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Alexandre A. Barros, Shane Browne, Carlos Oliveira, Estevão Lima, Ana Rita C. Duarte, Kevin E. Healy, Rui L. Reis Upper urinary tract urothelial carcinoma (UTUC) accounts for 5–10% of urothelial carcinomas and is a disease that has not been widely studied as carcinoma of the bladder. To avoid the problems of conventional therapies, such as the need for frequent drug instillation due to poor drug retention, we developed a biodegradable ureteral stent (BUS) impregnated by supercritical fluid...
Source: International Journal of Pharmaceutics - September 17, 2016 Category: Drugs & Pharmacology Source Type: research

In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Nrupa Borkar, René Holm, Mingshi Yang, Anette Müllertz, Huiling Mu In the present study, the differences in oral absorption of apomorphine and its diester prodrugs and the effect of lipid-based formulations on the absorption of apomorphine or its prodrugs were investigated. Apomorphine, dilauroyl apomorphine (DLA) and dipalmitoyl apomorphine (DPA) were orally administered (0.24mmol/kg) to rats as: DLA-o/w emulsion, DPA-o/w emulsion, apomorphine-o/w emulsion, apomorphine aqueous suspension, ...
Source: International Journal of Pharmaceutics - September 13, 2016 Category: Drugs & Pharmacology Source Type: research

Design, fabrication and biomedical applications of zein-based nano/micro-carrier systems
Publication date: 20 November 2016 Source:International Journal of Pharmaceutics, Volume 513, Issues 1–2 Author(s): Yong Zhang, Lili Cui, Feng Li, Nianqiu Shi, Chunlei Li, Xianghui Yu, Yan Chen, Wei Kong Nano/micro-carrier systems have shown promising application in the biomedical field as various delivery carriers. The composite material and fabrication method determine their microstructures, properties and thus their potential applications. Since approved as tablet coating material by the U.S. Food and Drug Administration (US-FDA), zein has been widely investigated as one of protein-based materials in the past few...
Source: International Journal of Pharmaceutics - September 13, 2016 Category: Drugs & Pharmacology Source Type: research