Deformation behavior of crystallized mannitol during compression using a rotary tablet press simulator
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Nicolas Tarlier, Ian Soulairol, Noelia Sanchez-Ballester, Gilles Baylac, Adrien Aubert, Philippe Lefevre, Bernard Bataille, Tahmer SharkawiAbstractMannitol is commonly used as a pharmaceutical excipient for tablets; the most widely used oral dosage form for drug delivery. For tableting, mannitol is provided in two different forms: native crystals and textured particles. In order to optimize its formulation, a good understanding of the mechanical behavior mechanism of mannitol is necessary. Thus, the aim of...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The effects of three absorption-modifying critical excipients on the in vivo intestinal absorption of six model compounds in rats and dogs
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): D. Dahlgren, C. Roos, P. Johansson, C. Tannergren, A. Lundqvist, P. Langguth, M. Sjöblom, E. Sjögren, H. LennernäsAbstractPharmaceutical excipients that may affect gastrointestinal (GI) drug absorption are called critical pharmaceutical excipients, or absorption-modifying excipients (AMEs) if they act by altering the integrity of the intestinal epithelial cell membrane. Some of these excipients increase intestinal permeability, and subsequently the absorption and bioavailability of the drug....
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-tumor and anti-metastasis efficacy against breast cancer with an intratumoral injectable phospholipids-based phase separation gel co-loaded with 5-fluotouracil and magnesium oxide by neutralizing acidic microenvironment
In conclusion, the novel 5FU + MgO-PPSG system might have a great potential to improve treatment method against breast metastasis.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of glycerol on the physical and mechanical properties of thin gellan gum films for oral drug delivery
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Patrizia Paolicelli, Stefania Petralito, Gabriele Varani, Martina Nardoni, Settimio Pacelli, Laura Di Muzio, Jacopo Tirillò, Cecilia Bartuli, Stefania Cesa, Maria Antonietta Casadei, Alessandra AdroverAbstractIn this work, deacylated gellan gum and the plasticizer glycerol were used as primary components for the preparation of thin films intended for the oral delivery of therapeutic molecules. The samples were prepared by a solvent casting method and characterized for their thickness, tensile proper...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Rapid paper based colorimetric detection of glucose using a hollow microneedle device
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Dean Nicholas, Keiran A. Logan, Yingjie Sheng, Jinhui Gao, Sian Farrell, Dorian Dixon, Bridgeen Callan, Anthony P. McHale, John F. CallanAbstractThe monitoring of blood glucose is a key aspect of diabetes care in limiting the negative effects of hyperglycaemia to both the microvasculature and macrovasculature. Self-monitoring of blood glucose (SMBG) gives an indication of blood glucose at a specific point in time and is recommended to be carried out four times daily. However, due to the inconvenience and a...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Immunogenicity of diphtheria toxoid and poly(I:C) loaded cationic liposomes after hollow microneedle-mediated intradermal injection in mice
In this study, we aimed to investigate the immunogenicity of cationic liposomes loaded with diphtheria toxoid (DT) and poly(I:C) after hollow microneedle-mediated intradermal vaccination in mice. The following liposomal formulations were studied: DT loaded liposomes, a mixture of free DT and poly(I:C)-loaded liposomes, a mixture of DT-loaded liposomes and free poly(I:C), and liposomal formulations with DT and poly(I:C) either individually or co-encapsulated in the liposomes. Reference groups were DT solution adjuvanted with or without poly(I:C) (DT/poly(I:C)). The liposomal formulations were characterized in terms of parti...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Phase transitions of antibiotic clarithromycin forms I, IV and new form VII crystals
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Masataka Ito, Rika Shiba, Miteki Watanabe, Yasunori Iwao, Shigeru Itai, Shuji NoguchiAbstractMetastable crystal form I of the antibiotic clarithromycin has a pharmaceutically valuable characteristic that its crystalline phase transition can be applied for its sustained release from tablets. The phase transition of form I was investigated in detail by single crystal and powder X-ray analyses, dynamic vapor sorption analysis and thermal analysis. The single crystal structure of form I revealed that form I wa...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Calcium enhances gene expression when using low molecular weight poly-l-lysine delivery vehicles
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Sheng-Xue Xie, Abdulgader A. Baoum, Nabil A. Alhakamy, Cory J. BerklandAbstractFour molecular weights of poly-l-lysine (PLL) [1000–5000 Da, 1500–8000 Da, 4000–15,000 Da and 15,000–30,000 Da] and three molecular weights of polyethyleneimine (PEI) [800 Da, 2,000 Da, and 25,000 Da] were used to systematically study the effect of calcium (Ca2+) to improve transfection efficiency of polyelectrolyte complexes. Complexes made using different molecular weights of PLL or PEI po...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of lidocaine forms (salt vs. freebase) on properties of drug–eudragit® L100-55 extrudates prepared by reactive melt extrusion
This study examines the preparation of sustained-release lidocaine polyelectrolyte complex using reactive melt extrusion. Eudragit L100-55 was selected as the ionic polymer. The influence of drug forms (freebase vs. hydrochloride salt) on lidocaine–Eudragit L100-55 interactions, physical stability, and dissolution properties of extrudates was investigated. It was confirmed by DSC, FT-IR and Raman spectroscopy that polyelectrolyte could only form via the acid–base reaction between Eudragit L100-55 and lidocaine freebase. Due to this ionic interaction, the lidocaine extrudate was physically more stable than the l...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Self-assembled liposome from multi-layered fibrous mucoadhesive membrane for buccal delivery of drugs having high first-pass metabolism
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Jianting Chen, Hao Pan, Yining Yang, Shihang Xiong, Hongliang Duan, Xinggang Yang, Weisan PanAbstractA novel delivery system based on self-assembled liposome from multi-layered fibrous mucoadhesive membrane has been developed to improve the bioavailability of Carvedilol (Car). This system consisted of an electrospun layer (enable self-assembly of liposome once contacting with water), an adhesive layer (prolong the retention period in the mouth) and a backing layer. SEM, DSC and FTIR were applied to charact...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of pixantrone to neutrophils by poly(sialic acid)-p-octadecylamine conjugate modified liposomes with improved antitumor activity
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Xiang Luo, Mingqi Liu, Ling Hu, Qiujun Qiu, Xinrong Liu, Cong Li, Mei Lu, Yang Liu, Ting Zhang, Songlei Zhou, David Julian McClements, Xian Jia, Yihui Deng, Yanzhi SongAbstractBased on the knowledge that poly(sialic acid) is a critical element for tumour development and that the receptors for its monomer are expressed on neutrophils, which play important roles in the progression and invasion of tumours, a poly(sialic acid)-p-octadecylamine conjugate (PSA-p-ODA) was synthesised and used to modify the surfac...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Laser based thermo-conductometry as an approach to determine ribbon solid fraction off-line and in-line
This study showed the potentials of this new technique and is a starting point for additional work that has to be done to overcome these challenges.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Isoniazid-loaded orodispersible strips: Methodical design, optimization and in vitro-in silico characterization
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Oluwatoyin A. Adeleke, Pei-Chin Tsai, Krizia M. Karry, Nkwe O. Monama, Bozena B. Michniak-KohnAbstractDrug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol-polyethylene glycol based orodispersible strip containing isoniazid, a first-line anti-tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and charac...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Real-time feedback control of twin-screw wet granulation based on image analysis
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Lajos Madarász, Zsombor Kristóf Nagy, István Hoffer, Barnabás Szabó, István Csontos, Hajnalka Pataki, Balázs Démuth, Bence Szabó, Kristóf Csorba, György MarosiAbstractThe present paper reports the first dynamic image analysis-based feedback control of continuous twin-screw wet granulation process. Granulation of the blend of lactose and starch was selected as a model process. The size and size distribution of the obtained particles ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Hot melt extrusion of ion-exchange resin for taste masking
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): David Cheng Thiam Tan, Jeremy Jianming Ong, Rajeev Gokhale, Paul Wan Sia HengAbstractTaste masking is important for some unpleasant tasting bioactives in oral dosage forms. Among many methods available for taste-masking, use of ion-exchange resin (IER) holds promise. IER combined with hot melt extrusion (HME) may offer additional advantages over solvent methods. IER provides taste masking by complexing with the drug ions and preventing drug dissolution in the mouth. Drug-IER complexation approaches describ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Strat-M® synthetic membrane: Permeability comparison to human cadaver skin
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Anika Haq, Benjamin Goodyear, Dina Ameen, Vivek Joshi, Bozena Michniak-KohnAbstractThe aim of this work was to investigate the correlation of permeation behavior of transdermal formulations through a novel synthetic membrane (Strat-M® EMD Millipore, MA) and human cadaver skin. Strat-M® membranes were designed with the intent to share similar structural and chemical characteristics found in the human skin however, omitting any biological behavior due to the absence of viable cells. Both human skin a...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of photo-degradation on the structure, stability, aggregation, and function of an IgG1 monoclonal antibody
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Dinen D. Shah, Jingming Zhang, Haripada Maity, Krishna M.G. MallelaAbstractPhotostability testing of therapeutic proteins is a critical requirement in the development of biologics. Upon exposure to light, pharmaceutical proteins may undergo a change in structure, stability, and functional properties that could have a potential impact on safety and efficacy. In this work, we studied how exposure to light, according to ICH guidelines, leads to photo-oxidation of a therapeutic IgG1 mAb. We also tested the abi...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

RTD-based material tracking in a fully-continuous dry granulation tableting line
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): M.C. Martinetz, A-P. Karttunen, S. Sacher, P. Wahl, J. Ketolainen, J.G. Khinast, O. KorhonenAbstractContinuous manufacturing (CM) offers quality and cost-effectiveness benefits over currently dominating batch processing. One challenge that needs to be addressed when implementing CM is traceability of materials through the process, which is needed for the batch/lot definition and control strategy. In this work the residence time distributions (RTD) of single unit operations (blender, roller compactor and ta...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of delayed pMDI actuation on the lung deposition of a fixed-dose combination aerosol drug
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Árpád Farkas, Alpár Horváth, Attila Kerekes, Attila Nagy, Szilvia Kugler, Lilla Tamási, Gábor TomisaAbstractLack of coordination between the beginning of the inhalation and device triggering is one of the most frequent errors reported in connection with the use of pMDI devices. Earlier results suggested a significant loss in lung deposition as a consequence of late actuation. However, most of our knowledge on the effect of poor synchronization is based on earlier w...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Chitosan based polymer-lipid hybrid nanoparticles for oral delivery of enoxaparin
In conclusion, GMO/CS based PLNs can provide a new insight to develop orally applicable delivery system for hydrophilic macromolecules. Their absorption can be enhanced with proposed PLNs and preparation of this PLNs was also found to be easy comparing to other similar methods.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Multivariate monitoring for the industrialisation of a continuous wet granulation tableting process
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Simeone Zomer, Jun Zhang, Sameer Talwar, Sayantan Chattoraj, Christopher HewittAbstractThe pharmaceutical industry is undergoing a significant change in product development and manufacturing strategies with the progressive shift from batch to continuous processes. These typically feature vast volumes of data generated by the numerous sensors connected to several unit operations running over the period of several hours or even days and that demand the application of increasingly efficient tools for process ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

A preliminary study for the development and optimization by experimental design of an in vitro method for prediction of drug buccal absorption
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Paola Mura, Serena Orlandini, Marzia Cirri, Francesca Maestrelli, Natascia Mennini, Giada Casella, Sandra FurlanettoAbstractThe work was aimed at developing an in vitro method able to provide rapid and reliable evaluation of drug absorption through buccal mucosa. Absorption simulator apparatus endowed with an artificial membrane was purposely developed by experimental design. The apparent permeation coefficient (Papp) through excised porcine buccal mucosa of naproxen, selected as model drug, was the target...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Lipidation of polyethylenimine-based polyplex increases serum stability of bioengineered RNAi agents and offers more consistent tumoral gene knockdown in vivo
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Qian-Yu Zhang, Pui Yan Ho, Mei-Juan Tu, Joseph L. Jilek, Qiu-Xia Chen, Su Zeng, Ai-Ming YuAbstractRecently we have established a novel approach to produce bioengineered noncoding RNA agents (BERAs) in living cells that carry target RNAi molecules (e.g., siRNA and miRNA) and thus act as “prodrugs”. Using GFP-siRNA-loaded BERA (BERA/GFP-siRNA) as a model molecule, this study was to define the in vitro and in vivo knockdown efficiency of BERAs delivered by liposome-polyethylenimine nanocomplex (li...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

All-atomistic molecular dynamics (AA-MD) studies and pharmacokinetic performance of PAMAM-dendrimer-furosemide delivery systems
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Daniel P. Otto, Melgardt M. de VilliersAbstractImprovement of problematic dissolution and solubility properties of a model drug, furosemide, was investigated for poly(amidoamine) (PAMAM) dendrimer complexes of the drug. Full and half generation dendrimers with amino and ester terminals respectively, were studied. In vitro release performance of these complexes was investigated at drug loads ranging 5–60% using simulated gastric fluids. Full generation dendrimers accommodated higher drug loads, outper...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Development of orally-deliverable DNA hydrogel by microemulsification and chitosan coating
In this study, we aimed to develop DNA hydrogel microspheres (Dgel-MS) coated with chitosan to improve their stability. Chitosan-coated Dgel-MS (Cs-Dgel-MS) was prepared by emulsifying Dgel to obtain the D-gel core, followed by mixing with microemulsions of chitosan for electrostatic coating. Fluorescence imaging of Cs-Dgel-MS labeled with fluorescent dyes showed that Dgel-MS (approximately 30 μm) was coated with chitosan. The recovery efficiency of Alexa Fluor 488-DNA was 87.4 ± 7.5%. To load a phosphorothioate CpG oligodeoxynucleotide into Dgel, a modified Dgel (mDgel) was designed and fluorescein isothio...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Amino acid conjugated chitosan nanoparticles for the brain targeting of a model dipeptidyl peptidase-4 inhibitor
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Jessica Fernandes, M. Vivek Ghate, Sanchari Basu Mallik, Shaila A. LewisAbstractSaxagliptin (SAX) is a dipeptidyl peptidase-4 enzyme inhibitor molecule now explored for its activity in the therapy of Alzheimer’s disease. Being extremely hydrophilic, it is unable to permeate the blood-brain barrier by the conventional therapy modalities. Further repurposing the drug, SAX is associated with a reduction in the blood sugar level in the periphery. In the present study, the chitosan-l-valine conjugate was ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced nanoparticle uptake into virus infected cells: Could nanoparticles be useful in antiviral therapy?
In this study, a fluorescently-labelled polymeric nanoparticle was prepared and used to track NP uptake into Huh7.5, human hepatoma cells transfected with replicating HCV genomes, compared with non-transfected cells as a model representing hepatocyte uptake. Confocal microscopy and flow cytometry of virus transfected Huh7.5 cells unexpectedly demonstrated two-fold increase in uptake of NP compared to non-transfected cells. Therefore, virus transfection enhanced NP uptake into Huh7.5 cells and NP could be considered as a promising delivery system for targeted treatment of hepatitis viruses.Graphical abstract (Source: Intern...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Combination of PLGA nanoparticles with mucoadhesive guar-gum films for buccal delivery of antihypertensive peptide
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Pedro M. Castro, Patrícia Baptista, Ana Raquel Madureira, Bruno Sarmento, Manuela E. PintadoAbstractOral administration of proteins and peptides still is a challenging task to overcome due to low permeability through absorptive epithelia, degradation and metabolism that lead to poor bioavailability. Attempting to overcome such limitations, an antihypertensive peptide derived from whey protein, with KGYGGVSLPEW sequence, was incorporated for the first time into polymeric nanoparticles. An experimenta...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Immunomodulatory and enhanced antitumor activity of a modified thymosin α1 in melanoma and lung cancer
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Fanwen Wang, Bin Li, Pengcheng Fu, Qingqing Li, Heng Zheng, Xingzhen LaoAbstractTumor-targeted therapy is an attractive strategy for cancer treatment. Peptide hormone thymosin α1 (Tα1) has been used against several diseases, including cancer, but its activity is pleiotropic. Herein, we designed a fusion protein Tα1-iRGD by introducing the tumor homing peptide iRGD to Tα1. Results show that Tα1-iRGD can promote T-cell activation and CD86 expression, thereby exerting better effe...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Physico-chemical properties of co-formulated fast-acting insulin with pramlintide
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Dayana Cabral da Silva, Luís Maurício T.R. LimaAbstractSince the discovery of amylin its use has been discouraged by the inadequacy of the protocol involving multiple injections in addition to insulin. We aimed here to develop a combined fixed-dose formulation of pramlintide with fast-acting insulin. We have investigated the compatibility of regular and fast-acting insulin analogues (Aspart, AspB28, and LisPro, LysB28ProB29) with the amylin analogue pramlintide by using electrospray ionizatio...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Systematic modifications of amino acid-based organogelators for the investigation of structure-property correlations in drug delivery system
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Beibei Hu, Wei Sun, Haiting Li, Helin Sui, Sanming LiAbstractThermogels, used as multi-functional drug-loading materials, have properties that mainly rely on their gelator structure. Although a large variety of organogel systems are used as drug delivery carriers, relatively few have been investigated in terms of their structure-property correlations based on amino acid derivative gelators. Here, a series of amino acid based gelators were synthesized to explore the role of the gelator structure on function...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoparticle-based delivery of carbamazepine: A promising approach for the treatment of refractory epilepsy
This study investigates the effect of the Pgp inhibitor verapamil on the anticonvulsant effect of CBZ and its nanoparticulate formulation in the rat model of isoniazid-induced epilepsy. Verapamil significantly increased the anticonvulsant effect of CBZ and reduced its effective dose by at least 30% (from 30 mg/kg to 20 mg/kg). Binding of carbamazepine to the poloxamer 188-coated PLGA nanoparticles enabled a 30-fold increase of its anticonvulsive effect, as compared to the free drug. The inhibition of Pgp did not influence the effectivity of carbamazepine encapsulated in nanoparticles.Graphical abstract (Source: Interna...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Improving the therapeutic efficacy of prilocaine by PLGA microparticles: Preparation, characterization and in vivo evaluation
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Marco Bragagni, María Esther Gil-Alegre, Paola Mura, Marzia Cirri, Carla Ghelardini, Lorenzo Di Cesare MannelliAbstractA delivery system based on poly(lactic-co-glycolic acid) polymer (PLGA) microparticles has been developed for parenteral administration of the local anesthetic prilocaine in its free base form. Both drug-free and drug-loaded microparticles, prepared by a double-emulsion-evaporation method, were characterized for mean size by Laser Diffraction Analysis, while their morphology was inv...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo evaluation of an oral sustained release hepatoprotective caffeine loaded w/o Pickering emulsion formula – Containing wheat germ oil and stabilized by magnesium oxide nanoparticles
The objective of this study was to innovate an effective oral sustained release hepatoprotective formula for – the water soluble drug – caffeine. Caffeine is rapidly absorbed and eliminated which dictates frequent administration to achieve adequate therapeutic effect. A w/o Pickering emulsion incorporating caffeine in the internal phase was primed. It contained wheat germ oil and was stabilized by synthesized magnesium oxide nanoparticles (MgO NPs). Components selection was based on their antioxidant, hepatoprotective and anticarcinogenic effects. The MgO NPs were prepared via sol-gel method, and then were char...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Layer-by-layer nanocoating of antibacterial niosome on orthopedic implant
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Anupma Dwivedi, Anisha Mazumder, Norased NasongklaAbstractThe major clinical hindrance of orthopedic implants is the bacterial infection, which can lead to biofilm formation and ultimately results in implant rejection. In this research, layer-by-layer nanocoating consists of vancomycin/PLA/vancomycin-loaded niosomes was designed. Vancomycin-loaded niosomes were formulated by thin film hydration method and the attributes of niosomes in terms of size, zeta potential, drug loading and EE, were assessed. The s...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The use of low molecular weight protamine to enhance oral absorption of exenatide
In this study, we constructed a zinc ion (Zn2+) and exenatide complex functionalized nanoparticle (NP) oral delivery system to overcome the above-mentioned issue. Polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) was used as a drug carrier to escape enzymatic degradation in the gastrointestinal tract, and low molecular weight protamine (LMWP) was used as a functional group to increase penetration of NPs into the intestinal epithelium. The functionalized NPs exhibited significantly improved penetration across the intestinal epithelium, as shown by cell uptake and transmembrane transport experiments. Moreover, a s...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Development of self-emulsifying drug delivery systems (SEDDS) for ciprofloxacin with improved mucus permeating properties
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Sergey Zaichik, Christian Steinbring, Claudia Menzel, Ludwig Knabl, Dorothea Orth-Höller, Helmut Ellemunter, Katharina Niedermayr, Andreas Bernkop-SchnürchAbstractThe aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the fluoroquinolone antibiotic ciprofloxacin (CIP) exhibiting highly mucus permeating properties and antimicrobial activity in in vitro models. Various SEDDS formulations were developed and evaluated regarding droplet size, polydispersity ind...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Roberto Gonzalez-Pizarro, Marcelle Silva-Abreu, Ana Cristina Calpena, María Antonia Egea, Marta Espina, María Luisa GarcíaAbstractThe main objective of this study was the development and optimization of fluorometholone-loaded PLGA nanoparticles for the treatment of inflammatory conditions of the eye. Design of experiments was used to obtain nanoparticles with the best physicochemical characteristics. The optimized nanoparticles containing 1.5 mg·mL−1 of fluorometholone s...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

A new therapeutic avenue for bronchiectasis: Dry powder inhaler of ciprofloxacin nanoplex exhibits superior ex vivo mucus permeability and antibacterial efficacy to its native ciprofloxacin counterpart
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): The-Thien Tran, Celine Vidaillac, Hong Yu, Valerie F.L. Yong, Dan Roizman, Ravishankar Chandrasekaran, Albert Y.H. Lim, Teck Boon Low, Gan Liang Tan, John A. Abisheganaden, Mariko Siyue Koh, Jeanette Teo, Sanjay H. Chotirmall, Kunn HadinotoAbstractNon-cystic fibrosis bronchiectasis (NCFB) characterized by permanent bronchial dilatation and recurrent infections has been clinically managed by long-term intermittent inhaled antibiotic therapy among other treatments. Herein we investigated dry powder inhaler (...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

pH-Responsive hyaluronated liposomes for docetaxel delivery
In this study, we report pH-responsive liposomes consisting of hydrogenated soy phosphatidylcholine (HSPC) as a lipid, hyaluronic acid (HA) grafted with functional 3-diethylaminopropyl (DEAP) groups (hereafter denoted as HA-g-DEAP) as a pH-responsive polymer, and docetaxel (DTX) as an antitumor drug. DTX-loaded HSPC liposomes were prepared via a conventional liposome manufacturing procedure and then were decorated with HA-g-DEAP (HA-g-DEAP0.15, HA-g-DEAP0.25, and HA-g-DEAP0.40, according to the molar conjugate ratio of DEAP to HA) in an aqueous solution (pH 7.4), by sonication. The liposomes with HA-g-DEAP0.40 allowed the ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Visual validation of the measurement of entrapment efficiency of drug nanocarriers
In conclusion, the ultrafiltration method is the method of choice for efficient separation and accurate measurement of EE.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

TEMPO-oxidized starch nanoassemblies of negligible toxicity compared with polyacrylic acids for high performance anti-cancer therapy
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Yumeng Jiang, Tao Li, Meiling Lu, Dan Li, Fazheng Ren, Huiying Zhao, Yuan LiAbstractThere is an urgent need for developing nanocarrier of excellent biocompatibility which can selectively release drugs at desired locations that can increase intratumoral drug concentration and reduce side effects. Herein, we developed a highly biocompatible nanocarrier made of oxidized starch in delivering doxorubicin (DOX) for enhanced anti-cancer therapy. The 30% oxidized starch can spontaneously self-assemble into 30&ndas...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Nrp-1 receptor targeting peptide-functionalized TPGS micellar nanosystems to deliver 10-hydroxycampothecin for enhanced cancer chemotherapy
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Anbu Mozhi, Israr Ahmad, Qari Muhammad Kaleem, Ruslan G. Tuguntaev, Ahmed Shaker Eltahan, Chen Wang, Rong Yang, Chan Li, Xing-Jie LiangAbstractMitochondria are considered the power house of cells where ATP is generated for cellular metabolism, and they also act as a crucial regulator of the intrinsic apoptosis pathway. During ATP synthesis, reactive oxygen species (ROS) are produced as secondary products. Overproduction of ROS can promote mitochondrial DNA mutation, dysfunction and depolarization of the mi...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Pentaglycine lipid derivates – rp-HPLC analytics for bioorthogonal anchor molecules in targeted, multiple-composite liposomal drug delivery systems
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Steffen Wöll, Stefan Schiller, Christopher Bachran, Lee Kim Swee, Regina ScherließAbstractThe quantification of lipids and assessment of lipid composition is an indispensable step during the pharmaceutical development of novel lipid based drug delivery systems such as liposomes. Broad excipient screenings of such formulations raise the need for versatile analytical methods. Even more demanding complexity is generated by introduction of targeted systems requiring functionalized lipids. We address...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Potential of the association of dodecyl gallate with nanostructured lipid system as a treatment for paracoccidioidomycosis: In vitro and in vivo efficacy and toxicity
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Junya de Lacorte Singulani, Liliana Scorzoni, Natália Manuela Strohmayer Lourencetti, Luana Rossi Oliveira, Rosana Silva Conçolaro, Patricia Bento da Silva, Ana Carolina Nazaré, Carlos Roberto Polaquini, Francesca Damiani Victorelli, Marlus Chorilli, Luis Octávio Regasini, Ana Marisa Fusco Almeida, Maria José Soares Mendes GianniniAbstractParacoccidioidomycosis (PCM) is a systemic mycosis endemic in Latin America, caused by Paracoccidioides spp. A limited number of antifu...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Practical aspects in size and morphology characterization of drug-loaded nano-liposomes
In this study, we compare two most commonly used approaches for assessing the size distribution and morphology of liposomal nano-drug systems, namely, dynamic light scattering (DLS) and cryogenic-transmission electron microscopy (cryo-TEM); an automated quantitative analysis method was developed for the latter method. We demonstrate the advantages and disadvantages of each of these two approaches for a commercial formulation of the anti-cancer drug doxorubicin - Doxil®, in which the drug is encapsulated, mostly in the form of nano-rod crystals. With increasing drug concentration, these nano-rods change the shape of the...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Incorporating platelet-rich plasma into coaxial electrospun nanofibers for bone tissue engineering
In conclusion, this study shows that the incorporation of PRP had positive effects on the bioactivity and osteogenic ability of coaxial nanofibrous mats. Such nanofibrous mats may prove beneficial in various applications of bone tissue engineering.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation and optimization of a dry powder for inhalation of second-line anti-tuberculosis drugs
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Rajeev Ranjan, Ashish Srivastava, Reena Bharti, Lipika Ray, Jyotsna Singh, Amit MisraAbstractA spray drying process was standardized to prepare an inhalable powder comprising d-cycloserine and ethionamide, two “second line” drugs employed for treating multi-drug resistant (MDR) tuberculosis (TB). The aim of the process development effort was to maximize product yield. Contour plots were generated using a small central composite design (CCD) with face centered (α = 1) to maximize the p...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation techniques for high dose dry powders
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Ashlee D. Brunaugh, Hugh D.C. SmythAbstractDelivery of drugs to the lungs via dry powder inhaler (DPI) is a promising approach for the treatment of both local pulmonary conditions and systemic diseases. Though DPIs are widely used for the pulmonary deposition of potent bronchodilators, anticholinergics, and corticosteroids, there is growing interest in the utilization of this delivery system for the administration of high drug doses to the lungs, as made evident by recent regulatory approvals for anti-micr...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical-grade oral films as substrates for printed medicine
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): M. Wimmer-Teubenbacher, C. Planchette, H. Pichler, D. Markl, W.K. Hsiao, A. Paudel, S. StegemannAbstractIn contact-less printing, such as piezo-electric drop on demand printing used in the study, the drop formation process is independent of the substrate. This means that having developed a printable formulation, printed pharmaceutical dosage forms can be obtained on any pharmaceutical grade substrate, such as polymer-based films. In this work we evaluated eight different oral films based on their suitabili...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research