Log in to search using one of your social media accounts:

 

Aerosolizable gold nano-in-micro dry powder formulations for theragnosis and lung delivery
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): A. Sofia Silva, Ana M. Sousa, Renato P. Cabral, Marta C. Silva, Clarinda Costa, Sónia P. Miguel, Vasco D.B. Bonifácio, Teresa Casimiro, Ilídio J. Correia, Ana Aguiar-Ricardo Functionalized gold nanoparticles (AuNPs) have been widely investigated as promising multifunctional nanosystems for the theragnosis of lung cancer, the most common and prominent cause of cancer death worldwide. Nevertheless, nanoparticles are not in appropriate sizes for an accurate deep lung delivery and the lac...
Source: International Journal of Pharmaceutics - January 22, 2017 Category: Drugs & Pharmacology Source Type: research

A novel methodology to study polymodal particle size distributions produced during continuous wet granulation
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Carlota Mendez Torrecillas, Gavin W. Halbert, Dimitrios A. Lamprou It is important during powder granulation to obtain particles of a homogeneous size especially in critical situations such as pharmaceutical manufacture. To date, homogeneity of particle size distribution has been defined by the use of the d50 combined with the span of the particle size distribution, which has been found ineffective for polymodal particle size distributions. This work focuses on demonstrating the limitations of the span pa...
Source: International Journal of Pharmaceutics - January 22, 2017 Category: Drugs & Pharmacology Source Type: research

Simulation and evaluation of rupturable coated capsules by finite element method
The objective of this study was to simulate and evaluate the burst behavior of rupturable coated capsules by finite element method (FEM). Film and coated capsules were prepared by dip-coating method and their dimensions were determined by stereomicroscope. Mechanical properties of the film were measured by tensile test and used as material properties of FEM models. Swelling pressure was determined by restrained expansion method and applied to the internal surface of FEM models. Water uptake of coated capsules was determined to study the formation of internal pressure. Burst test and in vitro dissolution was used to verify ...
Source: International Journal of Pharmaceutics - January 22, 2017 Category: Drugs & Pharmacology Source Type: research

Amorphous solid dispersion of cyclosporine A prepared with fine droplet drying process: Physicochemical and pharmacokinetic characterization
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Hiroki Suzuki, Tatsuru Moritani, Tadahiko Morinaga, Yoshiki Seto, Hideyuki Sato, Satomi Onoue The present study aimed to develop an amorphous solid dispersion (ASD) of cyclosporine A (CsA) by a fine droplet drying (FDD) process for improvement in oral absorption of CsA. CsA and hydroxypropyl cellulose-SSL were dissolved in 1,4-dioxane, and the solution was powdered by the FDD process to obtain the ASD formulation of CsA (ASD/CsA). The ASD/CsA was characterized in terms of morphology, particle size distrib...
Source: International Journal of Pharmaceutics - January 21, 2017 Category: Drugs & Pharmacology Source Type: research

Use of the channel fill level in defining a design space for twin screw wet granulation
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): L.J. Gorringe, G.S. Kee, M.F. Saleh, N.H. Fa, R.G. Elkes Twin screw wet granulation is a key process in the continuous manufacture of oral solid dosage forms. Previous research has qualitatively suggested that the channel fill level influences the granules produced. In this paper a quantitative measure of the total volumetric fraction of the conveying element channels of the screw filled with powder (φ) was used. Experimental results are shown which demonstrate that very similar particle size distribu...
Source: International Journal of Pharmaceutics - January 19, 2017 Category: Drugs & Pharmacology Source Type: research

The importance of the molecular weight of ethyl cellulose on the properties of aqueous-based controlled release coatings
In this study, dispersions of EC with varying viscosity grades (which correspond to molecular weights), ranging from 4 to 100 cps, were produced and characterised. The dispersions showed particle sizes around 200nm and highly negative ζ-potentials (approx. −100mV), which indicated stable dispersions as confirmed by sedimentation studies. The different latexes were used to produce free-standing film coatings. We hypothesised that the different viscosity grades of EC would result in different properties of the films. We found that an increase in viscosity grade (and higher molecular weight) resulted in lower coale...
Source: International Journal of Pharmaceutics - January 19, 2017 Category: Drugs & Pharmacology Source Type: research

Insights on in vitro models for safety and toxicity assessment of cosmetic ingredients
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Andreia Almeida, Bruno Sarmento, Francisca Rodrigues According to the current European legislation, the safety assessment of each individual cosmetic ingredient of any formulation is the basis for the safety evaluation of a cosmetic product. Also, animal testing in the European Union is prohibited for cosmetic ingredients and products since 2004 and 2009, respectively. Additionally, the commercialization of any cosmetic products containing ingredients tested on animal models was forbidden in 2009. In cons...
Source: International Journal of Pharmaceutics - January 19, 2017 Category: Drugs & Pharmacology Source Type: research

Synthesis, characterization, and in-vitro antitumor activity of the polyethylene glycol (350 and 1000) succinate derivatives of the tocopherol and tocotrienol isomers of Vitamin E
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Ahmed Abu-Fayyad, Sami Nazzal Vitamin E refers to a group of saturated tocopherol (T) isomers and the biologically more active unsaturated tocotrienol (T3) isomers. PEGylated α-tocopherol, commercially known as Vitamin E TPGS, has been used as an emulsifier and therapeutic agent for children with vitamin E deficiency. Limited information, however, is available about the PEG conjugates of the tocotrienol isomers of vitamin E. The current work was therefore undertaken to synthesize and characterize th...
Source: International Journal of Pharmaceutics - January 18, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro gastric survival of commercially available probiotic strains and oral dosage forms
This study underlines the chasm between the current opinion about probiotics protection needs and the products proposed by many companies in the dietary supplements area. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 18, 2017 Category: Drugs & Pharmacology Source Type: research

In vivo pharmacokinetic studies and intracellular delivery of methotrexate by means of glycine-tethered PLGA-based polymeric micelles
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Madhwi, Rajendra Kumar, Pramod Kumar, Bhupinder Singh, Gajanand Sharma, Om Prakash Katare, Kaisar Raza Methotrexate (MTX) is a widely used drug for the management of various kinds of cancers. However, numerous challenges are associated with MTX like poor aqueous solubility, dose-dependent side effects and poor-bioavailability. With an aim to explore the potential benefits in drug delivery of MTX, it was intended to fabricate glycine-PLGA-based polymeric micelles. Glycine was chemically linked to PLGA and ...
Source: International Journal of Pharmaceutics - January 18, 2017 Category: Drugs & Pharmacology Source Type: research

Docosahexaenoic acid loaded lipid nanoparticles with bactericidal activity against Helicobacter pylori
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Catarina Leal Seabra, Cláudia Nunes, Maria Gomez-Lazaro, Marta Correia, José Carlos Machado, Inês C. Gonçalves, Celso A. Reis, Salette Reis, M. Cristina L. Martins Docosahexaenoic acid (DHA), an omega-3 polyunsaturated fatty acid present in fish oil, has been described as a promising molecule to the treatment of Helicobacter pylori gastric infection. However, due to its highly unsaturated structure, DHA can be easily oxidized loosing part of its bioactivity. This work aims the n...
Source: International Journal of Pharmaceutics - January 18, 2017 Category: Drugs & Pharmacology Source Type: research

Gold nanostar –polymer hybrids for siRNA delivery: Polymer design towards colloidal stability and in vitro studies on breast cancer cells
In this study, AuNCs were prepared by coating Gold Nano Stars (GNS) with suitable functionalised polymers, to give new insight on the choice of the coating in order to obtain colloidal stability, satisfying in vitro transfection behaviour and reliability in terms of homogeneous results upon GNS type changing. For this goal, GNS synthesized with three different sizes and shapes were coated with two different polymers: i) α-mercapto-ω-amino polyethylene glycol 3000Da (SH-PEG3000-NH2), a hydrophilic linear polymer; ii) PHEA-PEG2000-EDA-LA (PPE-LA), an amphiphilic hydroxyethylaspartamide copolymer containing a PEG ...
Source: International Journal of Pharmaceutics - January 18, 2017 Category: Drugs & Pharmacology Source Type: research

Experimental studies on the effect of moisture content and volume resistivity on electrostatic behaviour of pharmaceutical powders
This study experimentally investigated the effect of moisture content (ranging from approximately 1.8 to 30wt.%) on tribocharging behaviour of pharmaceutical granules, as well as their apparent volume resistivity. The tribocharging behaviour of pharmaceutical granules was investigated using a rotating device and apparent volume resistivity was measured in a conventional volume resistivity test cell. Additional measurements were performed on individual ingredients, each having the same moisture content as that of the granules, in order to investigate the effect of each single ingredient on the apparent volume resistivity of...
Source: International Journal of Pharmaceutics - January 17, 2017 Category: Drugs & Pharmacology Source Type: research

Epidermal growth factor (EGF) fragment-guided anticancer theranostic particles for pH-responsive release of doxorubicin
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Myun Koo Kang, Wei Mao, Jun Bae Lee, Hyuk Sang Yoo EGF fragment (EGFfr) and doxorubicin were chemically co-decorated on single magnetic nanoparticles (MNPs) for concomitant cancer targeting and treatment. Magnetic nanoparticles were prepared by the precipitation of ferric chloride hydrates in an ammonia solution and subsequent surface-functionalization with amines. The terminal thiol group of the EGF fragment was first conjugated to surface amines of the MNPs using a heterofunctional crosslinker, and doxo...
Source: International Journal of Pharmaceutics - January 17, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring gastrointestinal variables affecting drug and formulation behavior: Methodologies, challenges and opportunities
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Bart Hens, Maura Corsetti, Robin Spiller, Luca Marciani, Tim Vanuytsel, Jan Tack, Arjang Talattof, Gordon L. Amidon, Mirko Koziolek, Werner Weitschies, Clive G. Wilson, Roelof J. Bennink, Joachim Brouwers, Patrick Augustijns Various gastrointestinal (GI) factors affect drug and formulation behavior after oral administration, including GI transfer, motility, pH and GI fluid volume and composition. An in-depth understanding of these physiological and anatomical variables is critical for a continued progress...
Source: International Journal of Pharmaceutics - January 16, 2017 Category: Drugs & Pharmacology Source Type: research

Synergistic antimicrobial potential of essential oils in combination with nanoparticles: Emerging trends and future perspectives
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Mahendra Rai, Priti Paralikar, Priti Jogee, Gauravi Agarkar, Avinash P. Ingle, Marcos Derita, Susana Zacchino The development of resistance to different antimicrobial agents by bacteria, fungi, viruses, parasites, etc. is a great challenge to the medical field for the treatment of infections caused by them, and therefore, there is a pressing need to search for new and novel antimicrobials. The antimicrobial activity of essential oils and biogenic nanoparticles is well known. Recent studies have demonstrat...
Source: International Journal of Pharmaceutics - January 15, 2017 Category: Drugs & Pharmacology Source Type: research

Evaluation of aggregate and silicone-oil counts in pre-filled siliconized syringes: An orthogonal study characterising the entire subvisible size range
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Maryam Shah, Zahra Rattray, Katie Day, Shahid Uddin, Robin Curtis, Christopher F. van der Walle, Alain Pluen Characterisation of particulates in therapeutic monoclonal antibody (mAb) formulations is routinely extended to the sub-visible size-range (0.1–10μm). Additionally, with the increased use of pre-filled syringes (PFS), particle differentiation is required between proteinaceous and non-proteinaceous particles such as silicone-oil droplets. Here, three orthogonal techniques: Raster Image Corr...
Source: International Journal of Pharmaceutics - January 14, 2017 Category: Drugs & Pharmacology Source Type: research

Charge-assisted bond N+H mediates the gelation of amorphous lurasidone hydrochloride during dissolution
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Shuai Qian, Shanshan Wang, Zhen Li, Xiaojie Wang, Di Ma, Shujun Liang, Yuan Gao, Jianjun Zhang, Yuanfeng Wei Lurasidone hydrochloride (LH), the hydrochloride form of lurasidone with a charge-assisted bond N+ H, is an atypical antipsychotropic agent for the treatment of schizophrenia. As a BCS class II drug, LH has a low oral bioavailability mainly due to its poor water solubility and low dissolution. In order to improve its solubility, amorphization of LH was performed and characterized. Unexpectedly, ...
Source: International Journal of Pharmaceutics - January 13, 2017 Category: Drugs & Pharmacology Source Type: research

Biodegradable lipid nanoparticles induce a prolonged RNA interference-mediated protein knockdown and show rapid hepatic clearance in mice and nonhuman primates
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Yuta Suzuki, Kenji Hyodo, Takuya Suzuki, Yohei Tanaka, Hiroshi Kikuchi, Hiroshi Ishihara Lipid nanoparticles based on ionizable lipids have been clinically validated as a means of delivery for RNA interference (RNAi) therapeutics. The ideal properties of RNAi carriers are efficient delivery of oligonucleotides into target cells and rapid elimination after the function is performed. Here, we report that degradable lipid nanoparticles are effective carriers of small interfering RNA (siRNA) and have a high t...
Source: International Journal of Pharmaceutics - January 13, 2017 Category: Drugs & Pharmacology Source Type: research

A rational approach towards development of amorphous solid dispersions: Experimental and computational techniques
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Paroma Chakravarty, Joseph W. Lubach, Jonathan Hau, Karthik Nagapudi The purpose of this study was to determine the drug-polymer miscibility of GENE-A, a Genentech molecule, and hydroxypropyl methylcellulose-acetate succinate (HPMC-AS), a polymer, using computational and experimental approaches. The Flory-Huggins interaction parameter,χ, was obtained by calculating the solubility parameters for GENE-A and HPMC-AS over the temperature range of 25–100°C to obtain the free energy of mixing at d...
Source: International Journal of Pharmaceutics - January 13, 2017 Category: Drugs & Pharmacology Source Type: research

Methods to simulate rubbing of topical formulation for in vitro skin permeation studies
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Hiep X. Nguyen, Ashana Puri, Ajay K. Banga Rubbing a topical formulation on skin is generally assumed to enhance drug penetration. The aim of this study was to demonstrate different techniques such as using glass rod, rheometer, and gloved finger for rubbing a 2% salicylic acid gel on skin and investigate their effect on in vitro permeation of salicylic acid through dermatomed porcine ear skin. The studies included evaluation of the gel’s rheological properties, gel distribution on skin surface, in ...
Source: International Journal of Pharmaceutics - January 13, 2017 Category: Drugs & Pharmacology Source Type: research

Building parity between brand and generic peptide products: Regulatory and scientific considerations for quality of synthetic peptides
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Larisa C. Wu, Fu Chen, Sau L. Lee, Andre Raw, Lawrence X. Yu Peptides are a fast growing segment in the pharmaceutical industry. Consequently, the industry and regulatory agencies are increasing their focus on the regulatory path and quality considerations for peptide development and manufacturing. Although most peptides are synthetic, manufactured by solid phase synthesis, nevertheless they are complex molecules with challenging quality and regulatory aspects. This paper provides a structured overview...
Source: International Journal of Pharmaceutics - January 11, 2017 Category: Drugs & Pharmacology Source Type: research

Epothilone B-based 3-in-1 polymeric micelle for anticancer drug therapy
In this report, we showed that the combinational treatment of epothilone B (EpoB), 17-N-allylamino-17-demethoxygeldanamycin (17-AAG, Hsp90 inhibitor), and rapamycin (mTOR inhibitor) displays strong anticancer activity in vitro and in vivo. To address the poor water solubility of this 3 drug-combination, they were co-loaded into poly(ethylene glycol)-block-poly(d,l-lactic acid) (PEG-b-PLA) micelles, and the 3-in-1 loaded PEG-b-PLA micelle (m-EAR) was characterized in terms of drug loading efficiency, particle size, release kinetics. The m-EAR achieved high levels of all three drugs in water; formed micelles with hydrodynami...
Source: International Journal of Pharmaceutics - January 10, 2017 Category: Drugs & Pharmacology Source Type: research

pH sensitive dexamethasone encapsulated laponite nanoplatelets: Release mechanism and cytotoxicity
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): M. Roozbahani, M. Kharaziha, R. Emadi The purpose of this study was to develop an efficient strategy to use laponite (LAP) nanoplates as a platform for the efficient release of anionic dexamethasone (DEX). Results revealed that DEX was encapsulated into the interlayer space of LAP nanodisks through an intercalation process with a high loading efficiency of 95.10±0.80%. X-Ray diffraction (XRD) patterns and Fourier transform infrared (FTIR) spectra of the hybrid LAP/DEX nanoplates (LD-NPs) indicat...
Source: International Journal of Pharmaceutics - January 10, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Rajneet Kaur Khurana, Arvind K. Bansal, Sarwar Beg, Andrea Julie Burrow, O.P. Katare, Kamalinder K. Singh, Bhupinder Singh Mangiferin (Mgf), largely expressed out from the leaves and stem bark of Mango, is a potent antioxidant. However, its in vivo activity gets tremendously reduced owing to poor aqueous solubility and inconsistent gastrointestinal absorption, high hepatic first-pass metabolism and high P-gp efflux. The current research work, therefore, was undertaken to overcome the biopharmaceutical ...
Source: International Journal of Pharmaceutics - January 10, 2017 Category: Drugs & Pharmacology Source Type: research

Apoferritin nanocage as streptomycin drug reservoir: Technological optimization of a new drug delivery system
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): B. Ruozi, P. Veratti, M.A. Vandelli, A. Tombesi, M. Tonelli, F. Forni, F. Pederzoli, D. Belletti, G. Tosi The aim of this study is to formulate and characterize streptomycin-loaded apoferritin nanoparticles (ApoStrep NPs) for their potential therapeutic use in bacterial resistant infections (i.e. tuberculosis). ApoStrep NPs were prepared by disassembly/reassembly process via pH method and changing apoferritin/drug molar ratio, purified by dialyses process also associated with gel filtration chromatogra...
Source: International Journal of Pharmaceutics - January 9, 2017 Category: Drugs & Pharmacology Source Type: research

Design and characterization of a magnetite/PEI multifunctional nanohybrid as non-viral vector and cell isolation system
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Raúl Megías, Maialen Arco, Jesús Ciriza, Laura Saenz del Burgo, Gustavo Puras, Margarita López-Viota, Ángel V. Delgado, Jon P. Dobson, José L. Arias, José L. Pedraz It is described the reproducible formulation and complete physicochemical characterization of nanohybrids based on magnetite (Fe3O4) cores embedded within a polyethylenimine (PEI) matrix. Particle size, surface electrical charge, X-ray diffraction and Fourier transform infrared spectroscopy (...
Source: International Journal of Pharmaceutics - January 9, 2017 Category: Drugs & Pharmacology Source Type: research

Layer-by-layer assembly of hierarchical nanoarchitectures to enhance the systemic performance of nanoparticle albumin-bound paclitaxel
We report for the first time the application of LbL functional architectures for improving the systemic performance of nab-PTX with a view toward its clinical translation for cancer therapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 9, 2017 Category: Drugs & Pharmacology Source Type: research

Distinct biodistribution of doxorubicin and the altered dispositions mediated by different liposomal formulations
This study aims to investigate the drug tissue distribution and the driving force for tissue distribution from doxorubicin solution and two liposomal delivery systems, Doxil and Myocet. These three formulations were intravenously administered to mice at a single dose of 5mg/kg. Eleven organs, plasma and blood were collected at different time points. Total doxorubicin concentrations in each specimen were measured with LC–MS/MS. Compared to doxorubicin solution, both Doxil and Myocet produced distinct doxorubicin tissue exposure in all 11 tissues. Interestingly, the tissue exposure by Myocet was drastically different f...
Source: International Journal of Pharmaceutics - January 9, 2017 Category: Drugs & Pharmacology Source Type: research

Assessment of new-generation high-power electronic nicotine delivery system as thermal aerosol generation device for inhaled bronchodilators
Conclusion New generation high-power ENDS are very efficient to generate carrier-droplets in the submicron range containing drug molecules with a constant drug concentration whatever the size-fractions. ENDS appear to be highly patient-adaptive. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 8, 2017 Category: Drugs & Pharmacology Source Type: research

Application of aluminum chloride phthalocyanine-loaded solid lipid nanoparticles for photodynamic inactivation of melanoma cells
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Patrícia L. Goto, Marigilson P. Siqueira-Moura, Antonio C. Tedesco Cutaneous melanoma is the most aggressive skin cancer and is particularly resistant to current therapeutic approaches. Photodynamic therapy (PDT) is a well-established photoprocess that is employed to treat some cancers, including non-melanoma skin cancer. Aluminum chloride phthalocyanine (ClAlPc) is used as a photosensitizer in PDT; however, its high hydrophobicity hampers its photodynamic activity under physiological conditions...
Source: International Journal of Pharmaceutics - January 7, 2017 Category: Drugs & Pharmacology Source Type: research

Oral hesperidin —Amorphization and improved dissolution properties by controlled loading onto porous silica
In this study, the maximum achievable drug loading compared to the theoretical drug loading, and the effect of drug loading degree on the dissolution properties (solubility, dissolution velocity) were investigated. Hesperidin was used as the model active (having also practical relevance for e.g. nutraceutical products), loading was performed onto AEROPERL® 300 Pharma. Degree of successful drug loading could be easily followed by simple light microscopy (=useful tool for formulation optimization), and was in agreement with scanning electron microscopy. Amorphous versus crystalline state was followed by X-ray diffraction...
Source: International Journal of Pharmaceutics - January 7, 2017 Category: Drugs & Pharmacology Source Type: research

Orodispersible films based on amorphous solid dispersions of tetrabenazine
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Zoé Senta-Loys, Sandrine Bourgeois, Jean-Pierre Valour, Stéphanie Briançon, Hatem Fessi In this work, the formation and stability of amorphous solid dispersions (SDs) as orodispersible films (ODF) were investigated using tetrabenazine (TBZ) as a poorly water soluble drug. The influence of polymer nature and pH-modifier incorporation to form and maintain SDs was investigated. TBZ-loaded ODF were formulated using 4 different polymers (HPMC, PVP, Pullulan, and HEC). Binary systems (BS...
Source: International Journal of Pharmaceutics - January 7, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and properties evaluation of a novel pH-sensitive liposomes based on imidazole-modified cholesterol derivatives
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Liang Ju, Fang Cailin, Wu Wenlan, Yu Pinghua, Gao Jiayu, Li Junbo As a new kind of drug carries, pH-sensitive liposomes have been widely studied in tumor therapy for their advantages of target ability and sustained-release. Here, we synthesized a pH-sensitive material, N-(3-Aminopropyl)imidazole-cholesterol (IM-Chol) and prepared a novel pH-sensitive liposomes using IM-Chol and phosphatidylcholine. IM-Chol was synthesized through amidation reaction between the amino group of N-(3-Aminopropyl)imidazole ...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

Graphene quantum dots for cancer targeted drug delivery
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Daniela Iannazzo, Alessandro Pistone, Marina Salamò, Signorino Galvagno, Roberto Romeo, Salvatore V. Giofré, Caterina Branca, Giuseppa Visalli, Angela Di Pietro A biocompatible and cell traceable drug delivery system Graphene Quantum Dots (GQD) based, for the targeted delivery of the DNA intercalating drug doxorubicin (DOX) to cancer cells, is here reported. Highly dispersible and water soluble GQD, synthesized by acidic oxidation and exfoliation of multi-walled carbon nanotubes (MWCNT), ...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

Core-shell nanofibers of curcumin/cyclodextrin inclusion complex and polylactic acid: Enhanced water solubility and slow release of curcumin
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Zeynep Aytac, Tamer Uyar Core-shell nanofibers were designed via electrospinning using inclusion complex (IC) of model hydrophobic drug (curcumin, CUR) with cyclodextrin (CD) in the core and polymer (polylactic acid, PLA) in the shell (cCUR/HPβCD-IC-sPLA-NF). CD-IC of CUR and HPβCD was formed at 1:2 molar ratio. The successful formation of core-shell nanofibers was revealed by TEM and CLSM images. cCUR/HPβCD-IC-sPLA-NF released CUR slowly but much more in total than PLA-CUR-NF at pH 1 an...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

The evaluation of physical properties of injection molded systems based on poly(ethylene oxide) (PEO)
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Jari Pajander, Alexia Rensonnet, Sami Hietala, Jukka Rantanen, Stefania Baldursdottir The effect of product design parameters on the formation and properties of an injection molded solid dosage form consisting of poly(ethylene oxide)s (PEO) and two different active pharmaceutical ingredients (APIs) was studied. The product design parameters explored were melting temperature and the duration of melting, API loading degree and the molecular weight (Mw) of PEO. The solid form composition of the model APIs...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

Optimization and evaluation of Oridonin-loaded Soluplus ®-Pluronic P105 mixed micelles for oral administration
In this study, a new type of mixed micelles was developed using Soluplus® (SOL) and Pluronic® P105 (P105) for the encapsulation of Oridonin (ORN). Oridonin-loaded micelles (ORN-M) were simply prepared using solvent evaporation and characterized for particle size, particle morphology, encapsulation efficiency, and drug loading. In addition, the in vitro drug release behavior of ORN-M was assessed using the widely applied dialysis bag technique. The pharmacokinetic property of ORN was explored in rats after oral administration of ORN-M. Optimized ORN-M were of a small size (137.2±1.65nm) and spherical shape wh...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

Cancer therapeutics with epigallocatechin-3-gallate encapsulated in biopolymeric nanoparticles
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Nisha Tyagi, Ranjit De, Jakob Begun, Amirali Popat With the recent quantum leap in chemoprevention by dietary products, their use as cancer therapeutics is garnering worldwide attention. The concept of effortlessly fighting this deadly disease by gulping cups of green tea or swallowing green tea extract capsules is appreciated universally. Epigallocatechin-3-gallate (EGCG), a major polyphenol in green tea, has generated significant interest in controlling carcinogenesis due to its growth-inhibitory eff...
Source: International Journal of Pharmaceutics - January 6, 2017 Category: Drugs & Pharmacology Source Type: research

Dermal quercetin lipid nanocapsules: Influence of the formulation on antioxidant activity and cellular protection against hydrogen peroxide
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): T. Hatahet, M. Morille, A. Shamseddin, A. Aubert-Pouëssel, J.M. Devoisselle, S. Bégu Quercetin is a plant flavonoid with strong antioxidant and antiinflammatory properties interesting for skin protection. However, its poor water solubility limits its penetration and so its efficiency on skin. For this purpose, quercetin lipid nanocapsules were formulated implementing phase inversion technique wherein several modifications were introduced to enhance quercetin loading. Quercetin lipid nanocap...
Source: International Journal of Pharmaceutics - January 5, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical characterisation and investigation of the bonding mechanisms of API-titanate nanotube composites as new drug carrier systems
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Barbara Sipos, Klára Pintye-Hódi, Zoltán Kónya, András Kelemen, Géza Regdon, Tamás Sovány Titanate nanotube (TNT) has recently been explored as a new carrier material for active pharmaceutical ingredients (API). The aim of the present work was to reveal the physicochemical properties of API-TNT composites, focusing on the interactions between the TNTs and the incorporated APIs. Drugs belonging to different Biopharmaceutical Classification System (...
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

Carrier particle design for stabilization and isolation of drug nanoparticles
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Teresa Tierney, Katalin Bodnár, Åke Rasmuson, Sarah Hudson Nanoparticles of poorly water-soluble drugs were prepared in suspension via antisolvent precipitation in order to improve their dissolution behaviour. Insoluble, surface-functionalized, micron-range, clay carrier particles were employed for the dual purpose of stabilizing the nanoparticles in suspended state, and facilitating their unhindered isolation to solid state; often a challenging step in nanoparticle production. The carrier...
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

Continuous monitoring of API content, API distribution and crushing strength after tableting via near-infrared chemical imaging
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): P.R. Wahl, I. Pucher, O. Scheibelhofer, M. Kerschhaggl, S. Sacher, J.G. Khinast Near-infrared chemical imaging (NIR-CI) with high-speed cameras based on the push-broom acquisition principle is a rapidly-evolving and can be used for a variety of purposes, from classification (and sorting) of products to mapping spatial distribution of materials. The present study examined if NIR-CI is suitable for tablet manufacturing. To that end, the tablets were introduced into the CI system via a flat belt conveyor....
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and evaluation of a novel dosage form for onychomycosis
In this study novel dosage forms were prepared and evaluated for their suitability in treatment of onychomycosis. Films were prepared comprising polymeric excipients such as chitosan, (hydroxypropyl)methyl cellulose, hydroxyethyl-cellulose, carboxymethylcellulose according to solvent evaporation method. Developed formulations were evaluated in terms of physical appearance, stability and adhesiveness. Furthermore skin and nail irritation studies were conducted. Five potential formulations (F1–F5) were designed while F1 and F4 exhibited the most promising results in terms of stability with 26min and 40.67min, respectiv...
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

A systematic review of the use of dosage form manipulation to obtain required doses to inform use of manipulation in paediatric practice
This study sought to determine whether there is an evidence base for drug manipulation to obtain the required dose, a common feature of paediatric clinical practice. A systematic review of the data sources, PubMed, EMBASE, CINAHL, IPA and the Cochrane database of systematic reviews, was used. Studies that considered the dose accuracy of manipulated medicines of any dosage form, evidence of safety or harm, bioavailability, patient experience, tolerability, contamination and comparison of methods of manipulation were included. Case studies and letters were excluded. Fifty studies were eligible for inclusion, 49 of which invo...
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

Influence of particle properties on powder bulk behaviour and processability
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Umang V. Shah, Vikram Karde, Chinmay Ghoroi, Jerry Y.Y. Heng Understanding interparticle interactions in powder systems is crucial to pharmaceutical powder processing. Nevertheless, there remains a great challenge in identifying the key factors affecting interparticle interactions. Factors affecting interparticle interactions can be classified in three different broad categories: powder properties, environmental conditions, and powder processing methods and parameters. Although, each of these three cat...
Source: International Journal of Pharmaceutics - January 4, 2017 Category: Drugs & Pharmacology Source Type: research

Raloxifene microsphere-embedded collagen/chitosan/ β-tricalcium phosphate scaffold for effective bone tissue engineering
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Ming-Lei Zhang, Ji Cheng, Ye-Chen Xiao, Ruo-Feng Yin, Xu Feng Engineering novel scaffolds that can mimic the functional extracellular matrix (ECM) would be a great achievement in bone tissue engineering. This paper reports the fabrication of novel collagen/chitosan/β-tricalcium phosphate (CCTP) based tissue engineering scaffold. In order to improve the regeneration ability of scaffold, we have embedded raloxifene (RLX)-loaded PLGA microsphere in the CCTP scaffold. The average pore of scaffold was ...
Source: International Journal of Pharmaceutics - January 2, 2017 Category: Drugs & Pharmacology Source Type: research

Development and characterization of anti-inflammatory activity of curcumin-loaded biodegradable microspheres with potential use in intestinal inflammatory disorders
Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): E. Blanco-García, F.J. Otero-Espinar, J. Blanco-Méndez, J.M. Leiro-Vidal, A. Luzardo-Álvarez This research addresses the development and in vitro evaluation of a microparticulate system intended for intestine-targeted delivery of curcumin (CRM), a natural polyphenol with anti-inflammatory properties. Microspheres (Ms) based on zein (ZN) and Gantrez® AN119 (PVMMA) were prepared by spray-drying and coated with a pH-sensitive polymer (Eudragit® FS30D). An experimental design w...
Source: International Journal of Pharmaceutics - January 2, 2017 Category: Drugs & Pharmacology Source Type: research

Efficient gene delivery to primary human retinal pigment epithelial cells: The innate and acquired properties of vectors
In this study, vectors with different characteristics differing in mixing orders of pDNA, PEI polymer, and PLGA/PEI or PLGA nanoparticles were prepared and characterized. Then, their characteristics and efficacy in gene delivery to RPE cells in the presence of vitreous or fetal bovine serum (FBS) were evaluated. All formulations showed no cytotoxicity and were able to protect pDNA from premature release and degradation in extracellular media. Also, the adsorption of vitreous or serum proteins onto the surface of vectors changed their properties and hence cellular uptake and transfection efficacy. Graphical abstract (Source...
Source: International Journal of Pharmaceutics - December 30, 2016 Category: Drugs & Pharmacology Source Type: research

Hydrophilic drug encapsulation in shell-core microcarriers by two stage polyelectrolyte complexation method
In this study a protocol exploiting the combination of the ultrasonic atomization and the complexation between polyelectrolytes was developed to efficiently encapsulate a hydrophilic chemotherapeutic agent essentially used in the treatment of colon cancer, 5-fluorouracil, in enteric shell-core alginate-based microcarriers. The atomization assisted by ultrasound allowed to obtain small droplets by supplying low energy and avoiding drug degradation. In particular microcarriers were produced in a home-made apparatus where both the core (composed of alginate, drug, and Pluronic F127) and shell (composed of only alginate) feed ...
Source: International Journal of Pharmaceutics - December 30, 2016 Category: Drugs & Pharmacology Source Type: research