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Hydrophobically modified polysaccharide-based on polysialic acid nanoparticles as carriers for anticancer drugs
This study presented the development of hydrophobically modified polysialic acid (HPSA) nanoparticles, a novel anticancer drug nanocarrier that increases therapeutic efficacy without causing nonspecific toxicity towards normal cells. HPSA nanoparticles were prepared by 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (EDC)/N-hydroxysuccinimide (NHS) coupling between N-deacetylated polysialic acid (PSA) and 5β-cholanic acid. The physicochemical characteristics of HPSA nanoparticles (zeta-potential, morphology and size) were measured, and in vitro cytotoxicity and cellular uptake of PSA and HPSA nanoparticles were tested ...
Source: International Journal of Pharmaceutics - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Asialoglycoprotein receptor-targeted liposomes loaded with a norcantharimide derivative for hepatocyte-selective targeting
In conclusion, N-14NCTDA with an ideal logP is a better alternative for the treatment of primary hepatic carcinoma. GAL-Lipo offers an attractive strategy to specifically target hepatocytes via caveolin-dependent and clathrin-dependent asialoglycoprotein receptor-mediated endocytosis resulting in higher anticancer activity and fewer side-effects. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Leaching of plasticizers from polyvinylchloride perfusion lines by different lipid emulsions for premature infants under clinical conditions
This study demonstrates that the leaching of DEHP by lipid emulsions in conditions of total parenteral nutrition is many times higher than should be accepted and higher when compared to the other plasticizers. There was no significant difference in leaching of plasticizers in relation to the type of lipid emulsion. The influence of tube diameter on the leaching rate of plasticizers should be taken into account especially in particular exposed patients. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Accelerated in vitro release testing method for naltrexone loaded PLGA microspheres
The objective of the present study was to develop a discriminatory and reproducible accelerated release testing method for naltrexone loaded parenteral polymeric microspheres. The commercially available naltrexone microsphere product (Vivitrol®) was used as the testing formulation in the in vitro release method development, and both sample-and-separate and USP apparatus 4 methods were investigated. Following an in vitro drug stability study, frequent media replacement and addition of anti-oxidant in the release medium were used to prevent degradation of naltrexone during release testing at “real-time” (37&d...
Source: International Journal of Pharmaceutics - February 8, 2017 Category: Drugs & Pharmacology Source Type: research

Stem cell-extracellular vesicles as drug delivery systems: New frontiers for silk/curcumin nanoparticles
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Sara Perteghella, Barbara Crivelli, Laura Catenacci, Milena Sorrenti, Giovanna Bruni, Vittorio Necchi, Barbara Vigani, Marzio Sorlini, Maria Luisa Torre, Theodora Chlapanidas The aim of this work was to develop a novel carrier-in-carrier system based on stem cell-extracellular vesicles loaded of silk/curcumin nanoparticles by endogenous technique. Silk nanoparticles were produced by desolvation method and curcumin has been selected as drug model because of its limited water solubility and poor bioavailabi...
Source: International Journal of Pharmaceutics - February 7, 2017 Category: Drugs & Pharmacology Source Type: research

Aerodynamic properties and in silico deposition of meloxicam potassium incorporated in a carrier-free DPI pulmonary system
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Anita Chvatal, Árpád Farkas, Imre Balásházy, Piroska Szabó-Révész, Rita Ambrus Dry powder inhalers (DPIs) have been among the fastest developing inhaler forms in the past decades. Researches are focusing on the formulation of carrier-free powders to obtain a higher deep-lung deposition and hereby to increase the effectiveness of the medicine. The aim of our study was to prepare a carrier-free dry powder formulation of meloxicam potassium (MP), a novel salt ...
Source: International Journal of Pharmaceutics - February 7, 2017 Category: Drugs & Pharmacology Source Type: research

Measurement of the Raman spectra and hygroscopicity of four pharmaceutical aerosols as they travel from pressurised metered dose inhalers (pMDI) to a model lung
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): N. Davidson, H.-J. Tong, M. Kalberer, P.C. Seville, A.D. Ward, M.K. Kuimova, F.D. Pope Particle inhalation is an effective and rapid delivery method for a variety of pharmaceuticals, particularly bronchodilation drugs used for treating asthma and COPD. Conditions of relative humidity and temperature inside the lungs are generally very different from the outside ambient air, with the lung typically being warmer and more humid. Changes in humidity, from inhaler to lung, can cause hygroscopic phase transitio...
Source: International Journal of Pharmaceutics - February 7, 2017 Category: Drugs & Pharmacology Source Type: research

Nano-precipitated curcumin loaded particles: effect of carrier size and drug complexation with (2-hydroxypropyl)- β-cyclodextrin on their biological performances
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Carla Serri, Mario Argirò, Linda Piras, Damiano Gustavo Mita, Antonina Saija, Luigi Mita, Maurizio Forte, Simona Giarra, Marco Biondi, Stefania Crispi, Laura Mayol In this work, curcumin (CURC)-encapsulating nanoparticles (NPs), made up of an amphiphilic blend of poloxamers and PLGA (PPC NPs) at different polymer concentrations, were prepared by nanoprecipitation. CURC was preliminarily complexed with (2-hydroxypropyl)-β-cyclodextrin (HPβCD) to improve its loading efficiency. The formatio...
Source: International Journal of Pharmaceutics - February 6, 2017 Category: Drugs & Pharmacology Source Type: research

Development of enteric-coated fixed dose combinations of amorphous solid dispersions of ezetimibe and lovastatin: Investigation of formulation and process parameters
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Manoela K. Riekes, Aswin Dereymaker, Philippe Berben, Patrick Augustijns, Hellen K. Stulzer, Guy Van den Mooter Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus®, top-coated with an enteric layer. The impact of different bead size, enteric polymers (Eudragit L...
Source: International Journal of Pharmaceutics - February 5, 2017 Category: Drugs & Pharmacology Source Type: research

Development of an injectable pseudo-bone thermo-gel for application in small bone fractures
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Pariksha J. Kondiah, Yahya E. Choonara, Pierre P.D. Kondiah, Pradeep Kumar, Thashree Marimuthu, Lisa C. du Toit, Viness Pillay A pseudo-bone thermo-gel was synthesized and evaluated for its physicochemical, mechanical and rheological properties, with its application to treat small bone fractures. The pseudo-bone thermo-gel was proven to have thermo-responsive properties, behaving as a solution in temperatures below 25°C, and forming a gelling technology when maintained at physiological conditions. Pol...
Source: International Journal of Pharmaceutics - February 4, 2017 Category: Drugs & Pharmacology Source Type: research

Statistical process control of cocrystallization processes: A comparison between OPLS and PLS
This study proposes an OPLS-based approach for BSPC of a cocrystallization process between hydrochlorothiazide and p-aminobenzoic acid monitored on-line with near infrared spectroscopy and compares the fault detection performance with the same approach based on PLS. A series of cocrystallization batches with imposed disturbances were used to test the ability to detect abnormal situations by OPLS and PLS-based BSPC methods. Results demonstrated that OPLS was generally superior in terms of sensibility and specificity in most situations. In some abnormal batches, it was found that the imposed disturbances were only detected w...
Source: International Journal of Pharmaceutics - February 4, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of PEG molecular weight and PEGylation degree on the physical stability of PEGylated lysozyme
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Josefine Morgenstern, Pascal Baumann, Carina Brunner, Jürgen Hubbuch During production, purification, formulation, and storage proteins for pharmaceutical or biotechnological applications face solution conditions that are unfavorable for their stability. Such harmful conditions include extreme pH changes, high ionic strengths or elevated temperatures. The characterization of the main influencing factors promoting undesired changes of protein conformation and aggregation, as well as the manipulation a...
Source: International Journal of Pharmaceutics - February 3, 2017 Category: Drugs & Pharmacology Source Type: research

Interaction of pharmaceutical excipients with organic cation transporters
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Sirima Soodvilai, Sunhapas Soodvilai, Varanuj Chatsudthipong, Tanasait Ngawhirunpat, Theerasak Rojanarata, Praneet Opanasopit Increasing evidences have shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on several transport function of uptake and efflux drug transporters. Herein, we investigated whether the excipients frequently used in many drug formulations affect transport function of organic cation transporters (OCTs) that are responsible for elimination...
Source: International Journal of Pharmaceutics - February 2, 2017 Category: Drugs & Pharmacology Source Type: research

Design of magnetic gene complexes as effective and serum resistant gene delivery systems for mesenchymal stem cells
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Tian-Yuan Zhang, Jia-He Wu, Qian-Hao Xu, Xia-Rong Wang, Jingxiong Lu, Ying Hu, Jun-ichiro Jo, Masaya Yamamoto, Daishun Ling, Yasuhiko Tabata, Jian-Qing Gao Gene engineered mesenchymal stem cells (MSCs) have been proposed as promising tools for their various applications in biomedicine. Nevertheless, the lack of an effective and safe way to genetically modify these stem cells is still a major obstacle in the current studies. Herein, we designed novel magnetic complexes by assembling cationized pullulan der...
Source: International Journal of Pharmaceutics - February 2, 2017 Category: Drugs & Pharmacology Source Type: research

Continuous direct compression as manufacturing platform for sustained release tablets
This study presents a framework for process and product development on a continuous direct compression manufacturing platform. A challenging sustained release formulation with high content of a poorly flowing low density drug was selected. Two HPMC grades were evaluated as matrix former: standard Methocel CR and directly compressible Methocel DC2. The feeding behavior of each formulation component was investigated by deriving feed factor profiles. The maximum feed factor was used to estimate the drive command and depended strongly upon the density of the material. Furthermore, the shape of the feed factor profile allowed d...
Source: International Journal of Pharmaceutics - February 1, 2017 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin-mediated self-associating chitosan micro-platelets act as a drug booster against Candida glabrata mucosal infection in immunocompetent mice
This study reports design and evaluation of chitosan-based microparticle activity against Candida glabrata in vitro and in vivo in immunocompetent mice model artificially maintained in oestrus state. Because their flattened shape, chitosan microparticles are called here micro-platelets. They were obtained by self-association of oleoyl chitosan and α-cyclodextrin in water. A mixture of amphotericin B-deoxycholate (Fungizone®, AmB-DOC) and chitosan micro-platelets gelified with pluronic® F127 (20wt%) completely cured C. glabrata vaginal infection. Colony factor unit counting and mycological analysis of mice vag...
Source: International Journal of Pharmaceutics - February 1, 2017 Category: Drugs & Pharmacology Source Type: research

Characterization and biocompatibility evaluation of cutaneous formulations containing lipid nanoparticles
In this study, we prepared a hydrogel based on NLC containing vitamin E (HG-NLCVE) and evaluated its suitability for cutaneous application. The experiments started with the HG-NLCVE characterization (organoleptic analysis, accelerated stability, particle size, morphology, pH, texture and rheology). Afterwards, in vitro experiments were carried out, evaluating the formulation biocompatibility (MTT and Neutral Red) and irritant potential (Hen’s egg test on the chorioallantoic membrane, HET-CAM) for cutaneous application. The results showed that the HG-NLCVE has adequate features for skin application, is biocompatible a...
Source: International Journal of Pharmaceutics - February 1, 2017 Category: Drugs & Pharmacology Source Type: research

Design of spray dried ternary solid dispersions comprising itraconazole, soluplus and HPMCP: Effect of constituent compositions
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Mark T. Davis, Catherine B. Potter, Maryam Mohammadpour, Ahmad B. Albadarin, Gavin M. Walker A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40°C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were...
Source: International Journal of Pharmaceutics - February 1, 2017 Category: Drugs & Pharmacology Source Type: research

Smart AS1411-aptamer conjugated pegylated PAMAM dendrimer for the superior delivery of camptothecin to colon adenocarcinoma in vitro and in vivo
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Mona Alibolandi, Seyed Mohammad Taghdisi, Pouria Ramezani, Fazileh Hosseini Shamili, Sara Amel Farzad, Khalil Abnous, Mohammad Ramezani In the current study camptothecin-loaded pegylated PAMAM dendrimer were synthesized and were functionalized with AS1411 anti-nucleolin aptamers for site-specific targeting against colorectal cancer cells which over expresses nucleolin receptors. The morphological properties and size dispersity of the prepared nanoparticles were evaluated using transmission electron micros...
Source: International Journal of Pharmaceutics - January 26, 2017 Category: Drugs & Pharmacology Source Type: research

Injection of SDF-1 loaded nanoparticles following traumatic brain injury stimulates neural stem cell recruitment
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Laura N. Zamproni, Mayara V. Mundim, Marimelia A. Porcionatto, Anne des Rieux Recruiting neural stem cell (NSC) at the lesion site is essential for central nervous system repair. This process could be triggered by the local delivery of the chemokine SDF-1. We compared two PLGA formulations for local brain SDF-1 delivery: SDF-1 loaded microspheres (MS) and SDF-1 loaded nanoparticles (NP). Both formulations were able to encapsulate more than 80% of SDF-1 but presented different release profiles, with 100% o...
Source: International Journal of Pharmaceutics - January 26, 2017 Category: Drugs & Pharmacology Source Type: research

Amorphization within the tablet: Using microwave irradiation to form a glass solution in situ
In this study, the feasibility of microwave irradiation to prepare amorphous solid dispersions (glass solutions) in situ was investigated. Indomethacin (IND) and polyvinylpyrrolidone K12 (PVP) were tableted at a 1:2 (w/w) ratio. In order to study the influence of moisture content and energy input on the degree of amorphization, tablet formulations were stored at different relative humidity (32, 43 and 54% RH) and subsequently microwaved using nine different power-time combinations up to a maximum energy input of 90kJ. XRPD results showed that up to 80% (w/w) of IND could be amorphized within the tablet. mDSC measurements r...
Source: International Journal of Pharmaceutics - January 26, 2017 Category: Drugs & Pharmacology Source Type: research

Spray dried hyaluronic acid microparticles for adhesion controlled aggregation and potential stimulation of stem cells
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Fabio S. Palumbo, Stefano Agnello, Calogero Fiorica, Giovanna Pitarresi, Roberto Puleio, Guido R. Loria, Gaetano Giammona Spray-dried microparticles of a derivative of hyaluronic acid (HA) have been engineered to obtain a controlled aggregation with Human Mesenchymal Stem Cells (hMSCs) into 3D constructs. We demonstrated the utility of chemical functionalization of a native constituent of the extracellular matrix to improve processing performances and to control on stem cell adhesion and differentiation. ...
Source: International Journal of Pharmaceutics - January 26, 2017 Category: Drugs & Pharmacology Source Type: research

A novel injectable formulation of 6-fluoro-l-DOPA imaging agent for diagnosis of neuroendocrine tumors and Parkinson ’s disease
In conclusion, [18F]F-l-DOPA, formulated as FA, constitutes a promising dosage form for PET-CT diagnosis of both neuroendocrine tumors and Parkinson’s disease. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 24, 2017 Category: Drugs & Pharmacology Source Type: research

Biocompatible polymersomes-based cancer theranostics: Towards multifunctional nanomedicine
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Marzieh Mohammadi, Mohammad Ramezani, Khalil Abnous, Mona Alibolandi Polymersomes are polymeric vesicles that have numerous advantages for theranostics, the integrated approach of therapeutics and diagnostics. Polymersomes possess core- shell structures which encapsulate hydrophilic molecules in the aqueous compartment and hydrophobic molecules in the bilayer of the vesicles. Polymersomes are made of different amphiphilic block copolymers. Thus, in the process of designing polymersomes, a variety of amphi...
Source: International Journal of Pharmaceutics - January 24, 2017 Category: Drugs & Pharmacology Source Type: research

Nanoaggregation of inclusion complexes of glibenclamide with cyclodextrins
This study tries to provide an explanation about the processes involved in the formation of GB-βCDs complexes, which have been interpreted in different ways by several authors. Among native cyclodextrins, βCD presents the most appropriate cavity to host glibenclamide molecules showing AL solubility diagrams (K1:1 ≈1700M−1). However, A L − solubility profiles were found for βCD derivatives, highlighting the coexistence of several phenomena involved in the drug solubility enhancement. At low CD concentration, the formation of inclusion complexes can be studied and the stability constants can...
Source: International Journal of Pharmaceutics - January 23, 2017 Category: Drugs & Pharmacology Source Type: research

Composite particles based on particle engineering for direct compaction
Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Zhe Li, Xiao Lin, Lan Shen, YanLong Hong, Yi Feng Direct compaction (DC) is the preferred method for tablet production. However, only a minority of the active pharmaceutical ingredients (APIs) can be truly manufactured into tablets by DC so far due to that most of APIs lack sufficient functional properties required for DC. Particle engineering with co-processing provides a promising way to obtain various composite API and/or excipient particles with markedly improved functional properties, which makes suc...
Source: International Journal of Pharmaceutics - January 23, 2017 Category: Drugs & Pharmacology Source Type: research

RGD conjugated liposome-hollow silica hybrid nanovehicles for targeted and controlled delivery of arsenic trioxide against hepatic carcinoma
In conclusion, the strategy of constructing a nanocarrier with targeted delivery and controlled release characteristics is prospective to enhance the antitumor effect of ATO. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 22, 2017 Category: Drugs & Pharmacology Source Type: research

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