How to characterize a nasal product. The state of the art of in vitro and ex vivo specific methods
Publication date: 20 April 2019Source: International Journal of Pharmaceutics, Volume 561Author(s): Laurent Salade, Nathalie Wauthoz, Jonathan Goole, Karim AmighiAbstractNasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However, both t...
Source: International Journal of Pharmaceutics - March 4, 2019 Category: Drugs & Pharmacology Source Type: research

Subtle and unexpected role of PEG in tuning the penetration mechanisms of PLA-based nano-formulations into intact and impaired skin
We present a systematic study of the role of poly(ethylene glycol) (PEG) content in NPs on drug skin absorption. Cholecalciferol-loaded NPs of 100 nm of diameter were prepared by flash nanoprecipitation from PLA-b-PEG copolymers of various PEG lengths. As PEG content increased in the polymer, we observed a transition from a frozen solid particle structure to a more dynamic particle structure. Skin absorption studies showed that polymer composition influenced drug penetration depending on skin condition (intact or impaired). In intact skin, highly PEGylated NPs achieved the best skin absorption, even if the penetration diff...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Cascade therapy with doxorubicin and survivin-targeted tailored nanoparticles: an effective alternative for sensitization of cancer cells to chemotherapy
Publication date: Available online 27 February 2019Source: International Journal of PharmaceuticsAuthor(s): Cenk Daglioglu, Fatma Necmiye KaciAbstractChemotherapy frequently involves combination treatment protocols to maximize tumor cell killing. Unfortunately these intensive chemotherapeutic regimes, often show disappointing results due to the development of drug resistance and higher nonspecific toxicity on normal tissues. In cancer treatment, it is critically important to minimize toxicity while preserving efficacy. We have previously addressed this issue and proposed a nanoparticle-based combination therapy involving b...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Excipient Selection for Thermally Stable Enveloped and Non-Enveloped Viral Vaccine Platforms in Dry Powders
Publication date: Available online 28 February 2019Source: International Journal of PharmaceuticsAuthor(s): Steven P. Toniolo, Sam Afkhami, Ahmad Mahmood, Cécile Fradin, Brian D. Lichty, Matthew S. Miller, Zhou Xing, Emily D. Cranston, Michael R. ThompsonAbstractTwo enveloped viral vectors, vesicular stomatitis virus and influenza virus, and a non-enveloped viral vector, human adenovirus type 5, were encapsulated by spray drying to enhance thermal stability. Results with these candidates led to the hypothesis that stability performance of chosen excipients may be less virus-specific, as previously postulated in...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Linking carrier morphology to the powder mechanics of adhesive mixtures for dry powder inhalers via a blend-state model
Publication date: Available online 28 February 2019Source: International Journal of PharmaceuticsAuthor(s): Jonas Rudén, Göran Frenning, Tobias Bramer, Kyrre Thalberg, Junxue An, Göran AlderbornAbstractThe aim of this study was to investigate how the carrier morphology affects the expression of blend states in adhesive mixtures as a function of surface coverage ratio (SCR) and to identify where transitions between the different states occur. Adhesive mixtures of five lactose carriers with varying contents of lactose fines, corresponding to blends with different SCR ranging from 0-6, were produced by low-sh...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Carbon nanotubes significantly enhance the biological activity of CpG ODN in chickens
Publication date: Available online 28 February 2019Source: International Journal of PharmaceuticsAuthor(s): Jason Tomporowski, Jamille M. Heer, Brenda Allan, Susantha Gomis, Palok AichAbstractSynthetic unmethylated cytidine-phosphate-guanosine oligodeoxynucleotides (CpG ODN) is an effective immune stimulant in chicken. To be effective CpG dosage requirement is high. High dosage increases cost of treatment and introduces toxicity. A delivery system using multi-walled carbon nanotubes (MWCNT) is utilized in this study to aid in lowering the effective dose of the immune stimulant. CpG ODNs were attached non-covalently in diff...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Dissolution testing of oral film preparations: experimental comparison of compendial and non-compendial methods
Publication date: Available online 28 February 2019Source: International Journal of PharmaceuticsAuthor(s): Isabell Speer, Maren Preis, Jörg BreitkreutzAbstractIn vitro dissolution testing is one of the most frequently used tests in pharmaceutical quality control, since evaluation of the drug release profile and estimation of the dosage form performance is enabled. However, for oral film preparations no standardized compendial dissolution method or specifications are available worldwide.Therefore, four different dissolution methods described in the literature, namely the basket method, the paddle and glass disc (PGD) ...
Source: International Journal of Pharmaceutics - February 28, 2019 Category: Drugs & Pharmacology Source Type: research

Binder-free dry particulate coating process using a mild vibration field: effects of glass-transition temperature and powdering method of polymeric coating agents on coating performance
Publication date: Available online 26 February 2019Source: International Journal of PharmaceuticsAuthor(s): Toshiya Yasunaga, Kazukiyo Nakamura, Tooru Andoh, Hideki IchikawaAbstractWe employed a new dry coating process with mild-intensity vibration to prepare a 100-µm-sized microparticle capable of prolonged release of a drug. To accomplish this without using a binder, a series of laboratory-made acrylic latexes with different glass-transition temperatures (Tg) ranging from 30 °C to 80 °C were employed as coating agents, and the effects of Tg and powdering method of the coating agents on coating performance w...
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

CD44 targeted delivery of siRNA by using HA-decorated nanotechnologies for KRAS silencing in cancer treatment
In this study we developed ternary nanocomplexes to deliver an anti-KRAS siRNA to colorectal cancer cells, exploiting the interaction of hyaluronic acid (HA) with CD44 as a means to achieve selective targeting of CD44-positive cancer cells. Two different polycations, poly(hexamethylene biguanide) and chitosan, were complexed with siRNA and coated with HA. Physico-chemical properties and stability of nanoparticles were characterized, including size, surface charge, and degree of siRNA protection. We demonstrate nanoparticle internalization (flow cytometry), siRNA cytosolic release (confocal microscopy) and KRAS silencing (R...
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

How to characterize a nasal product. The state of the art of in-vitro and ex-vivo specific methods
Publication date: Available online 26 February 2019Source: International Journal of PharmaceuticsAuthor(s): Laurent Salade, Nathalie Wauthoz, Jonathan Goole, Karim AmighiAbstractNasal delivery offers many benefits over other conventional routes of delivery (e.g. oral or intravenous administration). Benefits include, among others, a fast onset of action, non-invasiveness and direct access to the central nervous system. The nasal cavity is not only limited to local application (e.g. rhinosinusitis) but can also provide direct access to other sites in the body (e.g. the central nervous system or systemic circulation). However...
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

Mechanistic Elucidation of Formation of Drug-Rich Amorphous Nanodroplets by Dissolution of the Solid Dispersion Formulation
Publication date: Available online 26 February 2019Source: International Journal of PharmaceuticsAuthor(s): Keisuke Ueda, Kenjirou Higashi, Kunikazu MoribeAbstractDrug-rich amorphous nanodroplets have great potential to improve intestinal absorption of poorly water-soluble drugs. Spray-dried samples (SPDs) of glibenclamide (GLB) with hypromellose (HPMC) or hypromellose acetate succinate (HPMC-AS, grade AS-LF and AS-HF) were prepared to investigate how GLB-rich amorphous nanodroplets form during the dissolution of solid dispersions. The co-spray drying of AS-LF significantly enhanced GLB dissolution from the SPD, leading to...
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 25 March 2019Source: International Journal of Pharmaceutics, Volume 559Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

Erratum to ‘Preservation of exosomes at room temperature using lyophilization’ [International Journal of Pharmaceutics 553 (2018) 1–7]
Publication date: 25 March 2019Source: International Journal of Pharmaceutics, Volume 559Author(s): Chonlada Charoenviriyakul, Yuki Takahashi, Makiya Nishikawa, Yoshinobu Takakura (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 27, 2019 Category: Drugs & Pharmacology Source Type: research

Involvement of metabolism-permeability in enhancing the oral bioavailability of curcumin in excipient-free solid dispersions co-formed with piperine
This study demonstrates that the developed co-amorphous CUR-PIP can enhance the bioavailability of CUR by increasing its dissolution, inhibiting metabolic processes, and facilitating membrane permeability.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 26, 2019 Category: Drugs & Pharmacology Source Type: research

Chemical synthesis of chitosan/silver nanocomposites films loaded with moxifloxacin: Their characterization and potential antibacterial activity
This article reports moxifloxacin (Mox)-loaded nanocomposite films (CSN) of chitosan and chemically reduced silver (Ag). The synthesis of silver nanoparticles was confirmed by specific surface plasmon resonance (SPR) peaks detected via UV-Visible spectroscopy at the wavelength range of 400-450 nm. The embedded Mox was chemically characterized and kinetically analyzed for in-vitro drug release and ex-vivo drug permeation through rat skin. The prepared films presented higher swelling ratio and lower tensile strength (TS) and better elongation at break (EB) than control formulation (pure chitosan film). All the prepared Mox-l...
Source: International Journal of Pharmaceutics - February 26, 2019 Category: Drugs & Pharmacology Source Type: research

Poly(Vinyl Alcohol) 3D printed tablets: the effect of polymer particle size on drug loading and process efficiency
Publication date: Available online 25 February 2019Source: International Journal of PharmaceuticsAuthor(s): Saviano Marilena, Aquino Rita Patrizia, Pasquale Del Gaudio, Francesca Sansone, Russo PaolaAbstractFused deposition modeling by 3D-printing is a rapid technique for the production of personalized drug dosage forms. One of the most delicate step of the whole process is the drug loading onto the thermoplastic polymer to obtain the drug-loaded filament used as feedstock for 3D FDM printers. With the aim of improving the drug loading, a systematic study on the influence of polymer size distribution on the quantity of dru...
Source: International Journal of Pharmaceutics - February 26, 2019 Category: Drugs & Pharmacology Source Type: research

Efficacy of budesonide-loaded mesoporous silica microparticles capped with a bulky azo derivative in rats with TNBS-induced colitis
Publication date: Available online 26 February 2019Source: International Journal of PharmaceuticsAuthor(s): Daniel Ferri, Ana M. Costero, Pablo Gaviña, Margarita Parra, Virginia Merino, Adrián H. Teruel, Félix Sancenón, Ramón Martínez-MáñezAbstractA colon targeted drug delivery system for inflammatory bowel diseases (IBD), consisting in budesonide loaded mesoporous silica microparticles functionalized with a selective azo-molecular gate (M-Bud), has been evaluated for in vivo efficacy. Experimental colitis in male Wistar rats was induced by rectal instillation of 2,4,...
Source: International Journal of Pharmaceutics - February 26, 2019 Category: Drugs & Pharmacology Source Type: research

Development of a PAT Tool for Monitoring the Wurster Coater Performance
This study demonstrated the applicability of pressure fluctuations for the prediction of the coating thickness. This method can be regarded as a new robust, fast and non-intrusive PAT approach for monitoring the coating process which can be easily used by engineers and practitioners.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of the concentration process on unloaded and doxorubicin loaded liposomal dispersions
Publication date: Available online 22 February 2019Source: International Journal of PharmaceuticsAuthor(s): Diego Romano Perinelli, Marco Cespi, Filippo Rendina, Giulia Bonacucina, Giovanni Filippo PalmieriAbstractLiposomes are unilamellar nanovesicles made of phospholipids of great interest as drug delivery carriers, able to encapsulate both hydrophilic and lipophilic compounds. Some liposomal formulations have reached the market, including the doxorubicin loaded PEGylated liposomal dispersion Doxil®. The aim of the work was to investigate the possibility of concentrating liposomes through the ultrafiltration process ...
Source: International Journal of Pharmaceutics - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

Investigation of the formation of drug-drug cocrystals and coamorphous systems of the antidiabetic drug gliclazide
Publication date: Available online 23 February 2019Source: International Journal of PharmaceuticsAuthor(s): Marwah Aljohani, Pól MacFhionnghaile, Patrick McArdle, Andrea ErxlebenAbstractThe antidiabetic drug gliclazide (GLZ) has a slow absorption rate and a low bioavailability due to its poor solubility. GLZ is often prescribed along with an antihypertensive, as many diabetic patients have coexistent hypertension. Cocrystallization and coamorphization are attractive strategies to enhance dissolution rates and to reduce the number of medications a patient has to take. In this work the formation of cocrystals and coam...
Source: International Journal of Pharmaceutics - February 23, 2019 Category: Drugs & Pharmacology Source Type: research

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