Effects of antibiotic component on in-vitro bacterial killing, physico-chemical properties, aerosolization and dissolution of a ternary-combinational inhalation powder formulation of antibiotics for pan-drug resistant Gram-negative lung infections
Publication date: Available online 21 February 2019Source: International Journal of PharmaceuticsAuthor(s): Sharad Mangal, Jiayang Huang, Nivedita Shetty, Heejun Park, Yu-wei Lin, Heidi H. Yu, Dmitry Zemlyanov, Tony Velkov, Jian Li, Qi Tony ZhouAbstractCombinational antibiotic formulations have emerged as an important strategy to combat antibiotic resistance. The main objective of this study was to examine effects of individual components on the antimicrobial activity, physico-chemical properties, aerosolization and dissolution of powder aerosol formulations when three synergistic drugs were co-spray dried. A ternary dry p...
Source: International Journal of Pharmaceutics - February 22, 2019 Category: Drugs & Pharmacology Source Type: research

3D printed chitosan dressing crosslinked with genipin for potential healing of chronic wounds
In this study, crosslinked chitosan (CH) based film matrices were prepared using 3D printing with genipin (GE) as a crosslinker, with glycerol (GLY) and poly ethylene glycol (PEG) as plasticiser. The 3D printed films were functionally characterized (tensile, fluid handling, mucoadhesion, drug dissolution, morphological properties and cell viability as well physico-chemical characterization using scanning electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction. CH-GE-PEG600 3D printed films having the ratio of 1:1 polymer: plasticizer was selected due to their appropriate flexibility. Fourier tran...
Source: International Journal of Pharmaceutics - February 22, 2019 Category: Drugs & Pharmacology Source Type: research

Buffer Solutions in Drug Formulation and Processing: How pKa values Depend on Temperature, Pressure and Ionic Strength
Publication date: Available online 22 February 2019Source: International Journal of PharmaceuticsAuthor(s): Lisa Samuelsen, René Holm, Audrey Lathuile, Christian SchönbeckAbstractSolution pH is an important factor during drug formulation and processing. Changes in pH present challenges. Regulation of pH is typically managed by using a buffer system, which must have a suitable pKa. The pKa of buffers depends on temperature, pressure and ionic strength. In addition, the pKa can also be affected by the polarity of the solvent, e.g., by the addition of a co-solvent. Theoretical considerations and accessible experim...
Source: International Journal of Pharmaceutics - February 22, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro antitumor potential of astaxanthin nanoemulsion against cancer cells via mitochondrial mediated apoptosis
Publication date: Available online 20 February 2019Source: International Journal of PharmaceuticsAuthor(s): Karuppusamy Shanmugapriya, Hyejin Kim, Hyun Wook KangAbstractAstaxanthin and alpha-tocopherol have various biological potential with induction of intracellular ROS production in cytosol, endoplasmic reticulum and mitochondrial site. The present study was performed to prepare nanoemulsion (NEs) formulation of astaxanthin and alpha-tocopherol with sodium caseinate (AS-AT/SC NEs) using spontaneous emulsification and ultrasonication for analyzing intracellular ROS production in apoptosis. NEs was characterized with stand...
Source: International Journal of Pharmaceutics - February 21, 2019 Category: Drugs & Pharmacology Source Type: research

Uptake and intracellular distribution of different types of nanoparticles in primary human myoblasts and myotubes
In this study we investigated the effects poly(lactide-co-glycolide) nanoparticles, mesoporous silica nanoparticles and liposomes, on the viability of primary human myoblasts and analyzed their cellular uptake and intracellular distribution in both primary human myoblasts and myotubes. Our data demonstrate that poly(lactide-co-glycolide) nanoparticles do not negatively affect myoblasts viability, contrarily to mesoporous silica nanoparticles and liposomes that induce a decrease in cell viability at the highest doses and longest incubation time. Poly(lactide-co-glycolide) nanoparticles and mesoporous silica nanoparticles ar...
Source: International Journal of Pharmaceutics - February 21, 2019 Category: Drugs & Pharmacology Source Type: research

Novel chitosan based nanoparticles as gene delivery systems to cancerous and noncancerous cells
This study indicated that chemical structure of these novel chitosan derivatives in the interaction with the cell type can lead to successful gene delivery.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 20, 2019 Category: Drugs & Pharmacology Source Type: research

SEDDS for intestinal absorption of insulin: Application of Caco-2 and Caco-2/HT29 co-culture monolayers and intra-jejunal instillation in rats
In this study, insulin was complexed with phosphatidylcholine (SPC) to form an insulin-SPC complex (ins-SPC) with increased lipophilicity. The following three SEDDS: MCT(MAPC) (MC glycerides with MAPC and LAB), MCT(RH40) (MC glycerides with Kolliphor® RH40) and LCT(MAPC) (long-chain glycerides with MAPC and LAB) were loading with ins-SPC (4% or 8% w/w SPC). Three SEDDSs generated emulsions with droplet sizes between 50 to 470 nm and zeta potentials between -5 to -25 mV in a simulated intestinal medium. Mucus-secreting Caco-2/HT29-MTX-E12 co-culture and Caco-2 monolayers were used as in vitro cell transport models to in...
Source: International Journal of Pharmaceutics - February 18, 2019 Category: Drugs & Pharmacology Source Type: research

Tocophersolan stabilized lipid nanocapsules with high drug loading to improve the permeability and oral bioavailability of curcumin
Publication date: Available online 15 February 2019Source: International Journal of PharmaceuticsAuthor(s): Pradnya Bapat, Rohan Ghadi, Dasharath Chaudhari, Sameer S. Katiyar, Sanyog JainAbstractThe present investigation highlights the development of D-α-Tocopheryl polyethylene glycol 1000 succinate (Tocophersolan; TPGS) stabilized lipid nanocapsules for enhancing the oral bioavailability and permeability of curcumin (CUR). Lipid nanocapsules were optimized for different lipids, different concentrations of TPGS and different drug: lipid ratio and were further lyophilized. Subsequently, they were characterized by powd...
Source: International Journal of Pharmaceutics - February 16, 2019 Category: Drugs & Pharmacology Source Type: research

Characterisation and optimisation of diclofenac sodium orodispersible thin film formulation
Publication date: Available online 14 February 2019Source: International Journal of PharmaceuticsAuthor(s): Ibrahim Khadra, Mohammad A. Obeid, Claire Dunn, Stewart Watts, Gavin Halbert, Steve Ford, Alexander MullenAbstractOral Thin Film (OTF) is a newly emerging drug delivery system which has many benefits for patients. Although there has been some formulation of OTF products, these have mainly been as confectionary or dental health products. The most significant benefit of this dosage format will only be realised once more pharmaceutical products become available. Within this paper, OTF strips containing Diclofenac Sodium...
Source: International Journal of Pharmaceutics - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Chitosan and Chitosan Coating Nanoparticles for the Treatment of Brain Disease
This article gives a comprehensive review on the advantages and recent progresses in the treatment of brain disease by chitosan nanoparticles.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Combination of microneedles and microemulsions to increase celecoxib topical delivery for potential application in chemoprevention of breast cancer
Publication date: Available online 14 February 2019Source: International Journal of PharmaceuticsAuthor(s): Gabriela Mojeiko, Moacir de Brito, Giovanna C. Salata, Luciana B. LopesAbstractIn spite of the high incidence of breast cancer worldwide, there are few strategies for its chemoprevention, and they have limited adherence mainly due to their serious adverse effects. As a new approach for local breast cancer chemoprevention, we developed and optimized microemulsions for topical delivery of celecoxib to the breast skin, and evaluated their combination with microneedles to improve drug penetration for localization in the ...
Source: International Journal of Pharmaceutics - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Time scale based analysis of in-situ crystal formation in droplet undergoing rapid dehydration
Publication date: 5 April 2019Source: International Journal of Pharmaceutics, Volume 560Author(s): S. Shakiba, S. Mansouri, C. Selomulya, M.W. WooAbstractThe surface structure of crystalline particles affects the functionality of the particles in drug delivery. Prediction of the final structure of particles that crystallize easily within the spray drying process is of interests for many applications. A theoretical framework was developed for the prediction of crystal structure precipitating on the surface of the particle. This model was based on the dimensionless Damkohler number (Da), to be an indicator of final particle ...
Source: International Journal of Pharmaceutics - February 15, 2019 Category: Drugs & Pharmacology Source Type: research

Self-association of cyclodextrins and cyclodextrin complexes in aqueous solutions
Publication date: Available online 13 February 2019Source: International Journal of PharmaceuticsAuthor(s): Thorsteinn Loftsson, Phennapha Saokham, André Rodrigues Sá CoutoAbstractCyclodextrins (CDs) are oligosaccharides that self-assemble in aqueous solutions to form transient clusters, nanoparticles and small microparticles. The critical aggregation concentration (cac) of the natural αCD, βCD and γCD in pure aqueous solutions was estimated to be 25, 8 and 9 mg/ml, respectively. The cac of 2-hydroxypropyl-β-cyclodextrin (HPβCD), that consists of mixture of isomers, was estimated to...
Source: International Journal of Pharmaceutics - February 14, 2019 Category: Drugs & Pharmacology Source Type: research

Entry of therapeutics into the brain: influence of exposed polarity calculated in silico and measured in vitro by supercritical fluid chromatography
Publication date: Available online 14 February 2019Source: International Journal of PharmaceuticsAuthor(s): Giacomo Russo, Francesco Barbato, Lucia Grumetto, Laurence Philippe, Frederic Lynen, Gilles H. GoetzAbstractThe present work proposes a novel application of EPSA (not an acronym but found to be referred to by many as Exposed Polar Surface Area), a supercritical fluid chromatography (SFC) polarity readout for assisting in the prediction of the extent of drug permeation through the blood-brain barrier (BBB). For this purpose, EPSA values for 69 structurally unrelated acidic, basic, neutral and amphoteric compounds were...
Source: International Journal of Pharmaceutics - February 14, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanistic Study on Rapid Fabrication of Fibrous Films via Centrifugal Melt Spinning
The objective of the present study was to develop a high throughput and solventless fiber fabrication method via centrifugal melt spinning (CMS) technology. A mechanistic study on the rapid fabrication of drug-loaded fibrous films was conducted using different model drugs and polymers. It was observed that the formability, morphology, and yield of fibrous films were affected by melt rheological properties of film components, operation temperature, and plasticizers. Maintaining suitable fluidity of molten materials during the CMS process is critical for the fiber formation. The produced fibrous films had high drug loading, ...
Source: International Journal of Pharmaceutics - February 13, 2019 Category: Drugs & Pharmacology Source Type: research

Ratiometric co-encapsulation and co-delivery of doxorubicin and paclitaxel by tumor-targeted lipodisks for combination therapy of breast cancer
In this study, a tumor-targeting lipodisk nanoparticle formulation was developed for ratiometric loading and the transportation of two hydrophobic model drugs, doxorubicin (DOX) and paclitaxel (PTX), in one single platform. Furthermore, a slightly acidic pH-sensitive peptide (SAPSP) incorporated into lipodisks effectively enhanced the tumor-targeting and cell internalization. The obtained co-loaded lipodisks were approximately 30 nm with a pH-sensitive property. The ratiometric co-delivery of two drugs via lipodisks was confirmed in both the drug-resistant MCF-7/ADR cell line and its parental MCF-7 cell line in vitro, as w...
Source: International Journal of Pharmaceutics - February 13, 2019 Category: Drugs & Pharmacology Source Type: research

Lipoic Acid-derived Cross-linked Liposomes for Reduction-responsive Delivery of Anticancer Drug
In this study, a novel disulfide cross-linked liposomes (CLs) assembled from dimeric lipoic acid-derived glycerophosphorylcholine (di-LA-PC) conjugate was developed. The conjugate was synthesized by a facial esterification of lipoic acid (LA) and glycerophosphorylcholine (GPC) and characterized by MS, 1H NMR and 13C NMR. Featuring the enhanced serum-stability and intracellular drug release determined by in vitro stability and GSH-responsive behavior, CLs prepared with dried thin film technique following 10 mol.% DTT cross-linking can attain effective delivery of anticancer candidates. Notably, CLs stably encapsulated doxor...
Source: International Journal of Pharmaceutics - February 13, 2019 Category: Drugs & Pharmacology Source Type: research

Correlating Multidimensional Short-Term Empirical Protein Properties to Long-Term Protein Physical Stability Data Via Empirical Phase Diagrams
This study contributes to long-term protein phase behavior research by presenting a systematic, data-dependent, and multidimensional data evaluation workflow to create a comprehensive overview of short-term protein analytics in relation to long-term protein phase behavior.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 13, 2019 Category: Drugs & Pharmacology Source Type: research

Mucoadhesive olaminosomes: A novel prolonged release nanocarrier of agomelatine for the treatment of ocular hypertension
In conclusion, mucoadhesive olaminosomes succeeded in enhancing agomelatine bioavailability in rabbits' eyes confirming the development of a novel ocular nanocarrier for insoluble drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 12, 2019 Category: Drugs & Pharmacology Source Type: research

Assessment of blend uniformity in a continuous tablet manufacturing process
This study demonstrated a mixing effect within the feed frame, which contribute to a 60% decrease in the relative standard deviation of the drug concentration, when compared to the chute. Variographic analysis showed that the minimum sampling and analytical error was five times less in the feed frame than the chute. This study demonstrates that the feed frame is an ideal location for monitoring the drug concentration of powder blends for CM processes.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 12, 2019 Category: Drugs & Pharmacology Source Type: research

Sustained and controlled release of herbal medicines: The concept of synchronized release
Publication date: Available online 10 February 2019Source: International Journal of PharmaceuticsAuthor(s): Zhongjian Chen, Quangang Zhu, Jianping Qi, Yi Lu, Wei WuAbstractSynchronized release, defined as simultaneous release of multiple components while keeping the inter-component ratios steady, is crucial to the design and development of sustained- or controlled-release delivery systems of herbal medicines. A theory of infinite dose dividing is proposed to interpret the rationale behind synchronized release. The key point of the mechanisms is to curb diffusion so as to offset the release divergence caused by differences ...
Source: International Journal of Pharmaceutics - February 11, 2019 Category: Drugs & Pharmacology Source Type: research

Simvastatin-loaded solid lipid nanoparticles for enhanced anti-hyperlipidemic activity in hyperlipidemia animal model
In conclusion, SIM-SLNs showed a great promise for improving the therapeutic outcomes of SIM via its effective oral delivery.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 11, 2019 Category: Drugs & Pharmacology Source Type: research

Tailoring Novel Soft Nano-vesicles ‘Flexosomes’ for Enhanced Transdermal Drug Delivery: Optimization, characterization and comprehensive ex vivo - in vivo evaluation
Publication date: Available online 10 February 2019Source: International Journal of PharmaceuticsAuthor(s): Hanaa A. Abdel-Messih, Rania A.H. Ishak, Ahmed S. Geneidi, Samar MansourAbstractThe transdermal route is a convenient non-invasive way for drug delivery, however, the hydrophobic compact nature of stratum corneum (SC) forms an obstacle hindering the diffusion of drugs particularly hydrophilic ones. Hence, the purpose of this study was to develop novel soft nano-vesicles, entitled Flexosomes, amalgamating two penetration enhancers, ethanol and one edge activator (EA) from various types and different hydrophilic-lipoph...
Source: International Journal of Pharmaceutics - February 11, 2019 Category: Drugs & Pharmacology Source Type: research

An overview on the mathematical modeling of hydrogels’ behavior for drug delivery systems
Publication date: Available online 11 February 2019Source: International Journal of PharmaceuticsAuthor(s): Diego CaccavoAbstractHydrogels-based systems (HBSs) for drug delivery are nowadays extensively used and the interest in modeling their behavior is dramatically increasing. In this review a critical overview on the modeling approaches is given, quantitatively and qualitatively analyzing the publications on the subject, the trend of the publications per year and the type of modeling approaches. It was found that, despite the drug release fitting models (i.e. Higuchi’s equation) are the most abundant, their use fo...
Source: International Journal of Pharmaceutics - February 11, 2019 Category: Drugs & Pharmacology Source Type: research

Non-aqueous formulations for ram and screen extrusion-spheronisation
Publication date: Available online 11 February 2019Source: International Journal of PharmaceuticsAuthor(s): M. Zhang, S.L. Rough, R. Ward, C. Seiler, D.I. WilsonAbstractThe use of non-aqueous cellulose-based formulations for extrusion-spheronisation (E-S) is investigated. A 10 wt% hydroxypropyl cellulose/isopropyl alcohol solution (HPC/IPA) was identified as a suitable sticky liquid binder for preparing non-aqueous pastes. Preliminary tests were performed on a series of pastes using a ram as well as a laboratory roller screen extruder, since the former is commonly used in batch testing and the latter replicates the shear r...
Source: International Journal of Pharmaceutics - February 11, 2019 Category: Drugs & Pharmacology Source Type: research

Type 1 Diabetes Mellitus reversal via implantation of magnetically purified microencapsulated pseudoislets
In this study, INS1E pseudoislets were microencapsulated within alginate (A) and alginate-poly-L-lysine-alginate (APA) microcapsules and purified through the microfluidic device. APA microcapsules demonstrated higher mechanical integrity and stability than A microcapsules, showing better pseudoislets viability and biological function. Importantly, we obtained a reduction of the graft volume of 77.5% for A microcapsules and 78.6% for APA microcapsules. After subcutaneous implantation of induced diabetic Wistar rats with magnetically purified APA microencapsulated pseudoislets, blood glucose levels were restored into normoglycemia (
Source: International Journal of Pharmaceutics - February 10, 2019 Category: Drugs & Pharmacology Source Type: research

Novel bicephalous heterolipid based self-microemulsifying drug delivery system for solubility and bioavailability enhancement of efavirenz
In conclusion, the BHL can be used effectively as an oil phase in SMEDDS to enhance solubility and bioavailability of BCS Class II drugs. Further, it holds, in general, a great promise as a new excipient for solubility and bioavailability enhancementsGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 10, 2019 Category: Drugs & Pharmacology Source Type: research

Powder die filling under gravity and suction fill mechanisms
Publication date: Available online 10 February 2019Source: International Journal of PharmaceuticsAuthor(s): R. Baserinia, I.C. SinkaAbstractIn pharmaceutical tablet manufacturing, the powder formulation is filled into a die and compacted into a tablet using rigid punches. Die fill is important because it limits the productivity of tablet presses and determines key quality attributes of tablets including weight and content uniformity.Die fill occurs due to gravity and suction fill mechanisms. A model linear shoe-die filling system has been instrumented with pressure measurement devices for detailed characterisation of air p...
Source: International Journal of Pharmaceutics - February 10, 2019 Category: Drugs & Pharmacology Source Type: research

Biomaterials for local drug delivery in central nervous system
Publication date: Available online 10 February 2019Source: International Journal of PharmaceuticsAuthor(s): Jia-Chen Chen, Li-Ming Li, Jian-Qing GaoAbstractThe central nervous system (CNS) is a vital part of human body which coordinate the actions by transmitting signals. Because of the existence of the blood-brain barrier and the blood-spinal cord barrier, diseases in CNS can hardly be directly intervened by non-invasive methods. While systemic delivery usually requires extravagant drug dosage and leads into toxicity in unexpected tissues, local drug delivery in CNS tissues provides a solution for the problems of physiolo...
Source: International Journal of Pharmaceutics - February 10, 2019 Category: Drugs & Pharmacology Source Type: research

Fisetin loaded binary ethosomes for management of skin cancer by dermal application on UV exposed mice
Publication date: Available online 10 February 2019Source: International Journal of PharmaceuticsAuthor(s): Thasleem Moolakkadath, Mohd. Aqil, Abdul Ahad, Syed Sarim Imam, Arshiya Praveen, Yasmin Sultana, Mohd Mujeeb, Zeenat IqbalAbstractFisetin loaded binary ethosomes were prepared and optimized using Box-Behnken design for dermal application to alleviate skin cancer. The prepared formulations were evaluated for vesicle size, entrapment efficiency and flux of fisetin. Additionally, the optimized formulation was further evaluated by transmission electron microscopy, confocal laser microscopy, vesicles-skin interaction, der...
Source: International Journal of Pharmaceutics - February 10, 2019 Category: Drugs & Pharmacology Source Type: research

A Study on the Applicability of Multiple Process Analysers in the Production of Coated Pellets
Publication date: Available online 8 February 2019Source: International Journal of PharmaceuticsAuthor(s): Klemen Korasa, Franc VrečerAbstractProcess analytical technology (PAT) has become an important factor in design, analysis and control of complex technological processes. In the present study, pellet coating process was monitored using four different PAT approaches, i.e. near-infrared (NIR) spectroscopy, Raman spectroscopy, in-line image analysis, and spatial filtering technique (SFT).Robustness and accuracy of a novel in-line image analyser was studied during the active ingredient coating process on the pilot scale i...
Source: International Journal of Pharmaceutics - February 9, 2019 Category: Drugs & Pharmacology Source Type: research

Afatinib-loaded Immunoliposomes Functionalized with Cetuximab: a Novel Strategy Targeting the Epidermal Growth Factor Receptor for Treatment of Non-small-cell Lung Cancer
Publication date: Available online 8 February 2019Source: International Journal of PharmaceuticsAuthor(s): Xiaoyan Lu, Sha Liu, Meishan Han, Xiucheng Yang, Kaoxiang Sun, Hongbo Wang, Hongjie Mu, Yuan Du, Aiping Wang, Ling Ni, Chunyan ZhangAbstractAfatinib, a selective and irreversible inhibitor of tyrosine kinase, was approved for the treatment of advanced non-small-cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) overexpression in 2013. Cetuximab (CTX), an anti-EGFR monoclonal antibody, is co-administered with afatinib to improve efficacy. Unfortunately, dose-related adverse reactions caused by combin...
Source: International Journal of Pharmaceutics - February 9, 2019 Category: Drugs & Pharmacology Source Type: research

Chitosan ascorbate hydrogel improves water uptake capacity and cell adhesion of electrospun poly(epsilon-caprolactone) membranes
Publication date: Available online 6 February 2019Source: International Journal of PharmaceuticsAuthor(s): Robin Augustine, Pan Dan, Inbar Schlachet, Didier Rouxel, Patrick Menu, Alejandro SosnikAbstractThe most important prerequisites for wound coverage matrices are biocompatibility, adequate porosity, degradability and exudate uptake capacity. A moderate hydrophilicity and exudate uptake capacity can often favour cell adhesion and wound healing potential, however, most of the synthetic polymers like polycaprolactone (PCL) are hydrophobic. Hydrogels based on natural polymers can improve the hydrophilicity and exudate upta...
Source: International Journal of Pharmaceutics - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

A single-layer film coating for colon-targeted oral delivery
This study designed a single-coat pH-sensitive layer for colon-specific delivery with a potential biopolymer, namely, zein. The tablets were coated with a pH-sensitive film combining zein and Kollicoat® MAE 100P. A scanning electron microscope (SEM) was used to study the surface characteristics of the coating layers, and Fourier transform infrared spectroscopy (FTIR) was used to investigate the molecular interactions between these coating materials. The delivery system showed its potential to prevent the release of drug in gastric and small intestinal simulated media for the delayed release of drug at the expected pH o...
Source: International Journal of Pharmaceutics - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization of preparation conditions for CTAB-modified Polygonatum sibiricum polysaccharide cubosomes using the response surface methodology and their effects on splenic lymphocytes
This study aimed to optimize the preparation conditions for cetyltrimethylammonium bromide-modified Polygonatum sibiricum polysaccharide cubosomes (CTAB-modified PSP-Cubs) by response surface methodology (RSM). Glyceryl-monooleate (GMO) was used as the lipid base for the cubosomes. The optimal preparation conditions of CTAB-modified PSP-Cubs were as follows: the mass percentage of PSP to GMO (X1), Poloxamer 407 (F127) to GMO (X2) and water to GMO (X3) was 1.4%, 9% and 50%, respectively. The encapsulation efficiency (EE) of CTAB-modified PSP-Cubs under the experimental conditions was 62.4 ± 3.6%, which was close to o...
Source: International Journal of Pharmaceutics - February 7, 2019 Category: Drugs & Pharmacology Source Type: research

Melatonin loaded with bacterial cellulose nanofiber by Pickering-emulsion solvent evaporation for enhanced dissolution and bioavailability
The objective of the present work aimed to explore the potential of bacterial cellulose (BC) for oral delivery of melatonin (MLT), a natural hormone that faces problems of low solubility and oral bioavailability. BC was hydrolyzed by sulfuric acid followed by the oxidation to prepare bacterial cellulose nanofiber suspension (BCNs). Melatonin-loaded bacterial cellulose nanofiber suspension (MLT-BCNs) was prepared by emulsion solvent evaporation method. The properties of freeze-dried BCs and MLT-BCNs were studied by Fluorescence microscopy (FM), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), X–r...
Source: International Journal of Pharmaceutics - February 5, 2019 Category: Drugs & Pharmacology Source Type: research

An Evaluation of Inhaled Antibiotic Liposome versus Antibiotic Nanoplex in Controlling Infection in Bronchiectasis
Publication date: Available online 4 February 2019Source: International Journal of PharmaceuticsAuthor(s): The-Thien Tran, Hong Yu, Celine Vidaillac, Albert Y.H. Lim, John A. Abisheganaden, Sanjay H. Chotirmall, Kunn HadinotoAbstractInhaled antibiotic nanoparticles have emerged as an effective strategy to control infection in bronchiectasis lung owed to their mucus-penetrating ability. Using ciprofloxacin (CIP) as the model antibiotic, we evaluated dry powder inhaler (DPI) formulations of two classes of antibiotic nanoparticles (i.e. liposome and nanoplex) in their (1) physical characteristics (i.e. size, zeta potential, C...
Source: International Journal of Pharmaceutics - February 5, 2019 Category: Drugs & Pharmacology Source Type: research

Porous and highly dispersible voriconazole dry powders produced by spray freeze drying for pulmonary delivery with efficient lung deposition
This study aimed to develop porous and inhalable voriconazole dry powder with good lung deposition by spray freeze drying (SFD), using tert-butyl alcohol (TBA) as a co-solvent. A three-factor two-level full factorial design approach was used to investigate the effect of total solute concentration, drug content and co-solvent composition on the aerosol performance of the SFD powder. In general, the SFD voriconazole powder exhibited porous and spherical structure, and displayed crystalline characteristics. The analysis of factorial design indicated that voriconazole content was the most significant variable that could influe...
Source: International Journal of Pharmaceutics - February 5, 2019 Category: Drugs & Pharmacology Source Type: research

Separation and identification of acylated leuprorelin inside PLGA microspheres
Publication date: Available online 4 February 2019Source: International Journal of PharmaceuticsAuthor(s): Ningzi Guo, Qi Zhang, Yue Sun, Huaxin YangAbstractStudies have shown that the N-terminus and lysine side residue of peptides are prone to acylation in poly(D,L-lactide-co-glycolide) (PLGA) microspheres. Peptides such as leuprorelin lack a free N-terminus or lysine and only contain serine, arginine, and tyrosine as nucleophilic residues. The purpose of this study was to detect potential acylation impurities and determine their corresponding acylation sites in commercial leuprorelin-loaded PLGA microspheres. Commercial ...
Source: International Journal of Pharmaceutics - February 5, 2019 Category: Drugs & Pharmacology Source Type: research

Development of an Amorphous Nanosuspension by Sonoprecipitation-Formulation and Process Optimization using Design of Experiment methodology
Publication date: Available online 2 February 2019Source: International Journal of PharmaceuticsAuthor(s): Bhavin Y. Gajera, Dhaval A. Shah, Rutesh H. DaveAbstractA Design of Experiment (DoE) methodology was adopted to investigate and optimize process parameters and formulations variables for preparing an amorphous clotrimazole (CLT) nanosuspension by sonoprecipitation technique. The amorphous nanosuspension can provide a synergistic effect of increase in dissolution velocity and kinetic solubility which can be advantageously used to improve bioavailability of low-solubility drugs. A Box-Behnken design was utilized to stud...
Source: International Journal of Pharmaceutics - February 3, 2019 Category: Drugs & Pharmacology Source Type: research

Advances in nanocarriers enabled brain targeted drug delivery across blood brain barrier
Publication date: Available online 2 February 2019Source: International Journal of PharmaceuticsAuthor(s): Garima Sharma, Ashish R. Sharma, Sang-Soo Lee, Manojit Bhattacharya, Ju-Suk Nam, Chiranjib ChakrabortyAbstractThe blood brain barrier (BBB) offers protection to the central nervous system (CNS) by maintaining homeostasis. Besides restricting the entry of harmful xenobiotics and endogenous molecules to CNS, BBB also limits the entry of therapeutic agents. Nanotechnology offers the possibility to deliver small molecules/drugs against CNS disorders across BBB. Recently, due to excellent biocompatibility, functional versa...
Source: International Journal of Pharmaceutics - February 3, 2019 Category: Drugs & Pharmacology Source Type: research

Antibacterial drug release from a biphasic gel system: mathematical modelling
Publication date: Available online 2 February 2019Source: International Journal of PharmaceuticsAuthor(s): Michela Abrami, Samuel Golob, Fabio Pontelli, Gianluca Chiarappa, Gabriele Grassi, Beatrice Perissutti, Dario Voinovich, Nadia Halib, Luigi Murena, Gesmi Milcovich, Mario GrassiAbstractBacterial infections represent an important drawback in the orthopaedic field, as they can develop either immediately after surgery procedures or after some years. Specifically, in case of implants, they are alleged to be troublesome as their elimination often compels a surgical removal of the infected implant. A possible solution strat...
Source: International Journal of Pharmaceutics - February 2, 2019 Category: Drugs & Pharmacology Source Type: research

Handling forces for the use of different inhaler devices
Publication date: Available online 31 January 2019Source: International Journal of PharmaceuticsAuthor(s): Anna-Maria Ciciliani, Peter Langguth, Herbert WachtelAbstractAge and comorbidities can impact on the success of handling an inhaler. In this pilot study, we assessed finger strength in 62 participants (aged 5–17 years [n = 20], 18–65 years [n = 22] and> 65 years [n = 20]) by using different types of inhalers with integrated sensors (Respimat®, Breezhaler®, Aerolizer®, Genuair®, Diskus®, Ellipta®, HandiHaler®, Turbohaler® and a pressurized metered-dose inhaler [Atrovent&re...
Source: International Journal of Pharmaceutics - February 1, 2019 Category: Drugs & Pharmacology Source Type: research

Entecavir-loaded poly (lactic-co-glycolic acid) microspheres for long-term therapy of chronic hepatitis-B: preparation and in vitro and in vivo evaluation
Publication date: Available online 31 January 2019Source: International Journal of PharmaceuticsAuthor(s): Chunyan Zhang, Aiping Wang, Huiyun Wang, Maocai Yan, Rongcai Liang, Xiuting He, Fenghua Fu, Hongjie Mu, Kaoxiang SunAbstractTo avoid severe exacerbations in the load of hepatitis B virus (HBV) as a consequence of discontinuous use of anti-HBV drugs, entecavir (ETV), the first-line anti-HBV drug, was primally formulated as extended-release poly (lactic-co-glycolic acid) microspheres in the present study. Because ETV is slightly soluble in water and in some other organic solvents used for microsphere preparation, method...
Source: International Journal of Pharmaceutics - February 1, 2019 Category: Drugs & Pharmacology Source Type: research

Spontaneously formed porous structure and M1 polarization effect of Fe3O4 nanoparticles for enhanced antitumor therapy
In this study, we developed a novel Fe3O4 nanoparticles-doxorubicin (DOX)-Hyaluronic acid (HA) nanoparticles on the basis of firstly discovered “formed porous structure” in spontaneously assembled Fe3O4 nanoparticles. The Mechanism of Action (MOA) behind this porous DOX-loading cargo was tested and confirmed. A multi-functional Fe3O4-DOX+HA nanoparticle was further constructed by incorporating HA into our system. In vitro and in vivo studies exhibited that Fe3O4-DOX+HA owned enhanced antitumor efficacy with significantly prolonged survival time due to the combination of M1 polarization ability of Fe3O4 nanopart...
Source: International Journal of Pharmaceutics - February 1, 2019 Category: Drugs & Pharmacology Source Type: research

Micelle-solubilized axitinib for ocular administration in anti-neovascularization
In this study, axitinib, a class of tyrosine kinase inhibitors, was loaded via the amphiphilic copolymer MPEG-PCL, improving its dispersibility in water. Axitinib-loaded micelles showed low toxicity in concentration gradient assays. Additionally, multiple doses by scratch assay confirmed that axitinib had no significant effect on normal cell migration, and biosafety test results showed good cell compatibility. After we established the corneal neovascularization model after an alkali burn in rats, the anti-angiogenic efficacy was tested, with dexamethasone as a positive control. The results showed that axitinib-loaded micel...
Source: International Journal of Pharmaceutics - January 31, 2019 Category: Drugs & Pharmacology Source Type: research

Storage stability of inhalable phage powders containing lactose at ambient conditions
Publication date: Available online 31 January 2019Source: International Journal of PharmaceuticsAuthor(s): Rachel Yoon Kyung Chang, Martin Wallin, Elizabeth Kutter, Sandra Morales, Warwick Britton, Jian Li, Hak-Kim ChanAbstractThe aim of this study was to evaluate the storage stability of inhalable phage powders containing lactose and leucine as excipient. As an FDA-approved excipient for inhalation, lactose is preferred over other sugars. PEV phages active against antibiotic-resistant Pseudomonas aeruginosa was spray dried with lactose (55–90%) and leucine (45–10%). Produced powders were heat-sealed in an alum...
Source: International Journal of Pharmaceutics - January 31, 2019 Category: Drugs & Pharmacology Source Type: research

Enhancing analgesic and anti-inflammatory effects of capsaicin when loaded into olive oil nanoemulsion: an in-vivo study
Publication date: Available online 31 January 2019Source: International Journal of PharmaceuticsAuthor(s): Zahra Ghiasi, Fariba Esmaeli, Mahdi aghajani, Mahmoud Ghazi Khansari, Mohammad Ali Faramarzi, Amir AmaniAbstractTopical preparations of capsaicin, the major pungent ingredient of hot pepper, are being used for management of pain and inflammatory disorders. Purpose of this study was to use nanoemulsion as an effective topical drug carrier for in-vivo delivery of capsaicin. An oil-in-water nanoemulsion containing capsaicin was prepared by spontaneous emulsification method. Optimized formulation showed a median droplet d...
Source: International Journal of Pharmaceutics - January 31, 2019 Category: Drugs & Pharmacology Source Type: research

Retentive device for intravesical drug delivery based on water-induced shape memory response of poly(vinyl alcohol): design concept and 4D printing feasibility
Publication date: Available online 30 January 2019Source: International Journal of PharmaceuticsAuthor(s): A. Melocchi, N. Inverardi, M. Uboldi, F. Baldi, A. Maroni, S. Pandini, F. Briatico-Vangosa, L. Zema, A. GazzanigaAbstractThe use of shape memory polymers exhibiting water-induced shape recovery at body temperature and water solubility was proposed for the development of indwelling devices for intravesical drug delivery. These could be administered via catheter in a suitable temporary shape, retained in the bladder for a programmed period of time by recovery of the original shape and eliminated with urine following dis...
Source: International Journal of Pharmaceutics - January 30, 2019 Category: Drugs & Pharmacology Source Type: research

Pluronic F127-based micelles for tumor-targeted bufalin delivery
In this study, we developed novel thermal and redox-responsive micelles based on the Pluronic F127 tri-block copolymer and employed these for redox-responsive intratumor release of bufalin, an anti-cancer drug. Pluronic F127 was first functionalized with carboxylate groups, and then assembled into micelles. The HOOC-F127-COOH micelles are 20 ± 4 nm in size at 37 °C, but expand to 281 ± 5 nm when cooled to 4 °C. This allows for the free diffusion of bufalin into the micellar cores at low temperatures, while at 37 °C the micelles are much more compact and the drug molecules can be effectively held i...
Source: International Journal of Pharmaceutics - January 30, 2019 Category: Drugs & Pharmacology Source Type: research