Complex amorphous solid dispersions based on poly(2-hydroxyethyl methacrylate): study of drug release from a hydrophilic insoluble polymeric carrier in the presence and absence of a porosity increasing agent
Publication date: Available online 16 May 2019Source: International Journal of PharmaceuticsAuthor(s): Melissa Everaerts, Guy Van den MooterAbstractAmorphous solid dispersions are nowadays typically made up of a drug compound and a water-soluble polymer. However, recently it has been demonstrated that amorphous solid dispersions based on insoluble polymers have a different and more delayed drug release profile, resulting in a prolonged duration of supersaturation. In this paper, binary and ternary amorphous solid dispersions based on poly(2-hydroxyethyl methacrylate) were prepared through spray drying to further investigat...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

A Biocompatible and Easy-to-make Polyelectrolyte Dressing with Tunable Drug Delivery Properties for Wound Care
The objective of this study is to address these problems by developing a tunable, biocompatible, and biodegradable CS-based dressing for wound treatment. The dressing is fabricated via electrostatic interactions between CS and carmellose (CM). Its swelling properties, erosion behavior, loading efficiency and drug release sustainability can be tuned by simply changing the CS/CM mass-to-mass ratio. Upon loaded with minocycline, the dressing effectively protects the wounds in mice from infection and enhances wound closure. Regarding its high tunability and promising in vivo performance, our dressing warrants further developme...
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 10 June 2019Source: International Journal of Pharmaceutics, Volume 564Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 16, 2019 Category: Drugs & Pharmacology Source Type: research

Improved oral bioavailability of the anticancer drug catechin using chitosomes: Design, in-vitro appraisal and in-vivo studies
This study aimed to elaborate catechin loaded chitosan-tethered liposomes (chitosomes) to enhance catechin oral bioavailability. Nanocarriers were optimized via ethanol injection method followed by physicochemical, ex vivo and biological appraisal in male Wistar albino rats. Results demonstrated that chitosomes possessed excellent nanosize of 137 nm, monodispersity (PDI
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

In-vitro evaluation of solid lipid nanoparticles: ability to encapsulate, release and ensure effective protection of peptides in the gastrointestinal tract
The objective of this study was to encapsulate a model water-soluble peptide in biodegradable and biocompatible solid lipid-based nanoparticles, i.e. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) in order to protect it from metabolic degradation. Leuprolide (LEU) and a LEU-docusate Hydrophobic Ion Pair (HIP) were encapsulated in SLN and NLC by High Pressure Homogenization. The particles were characterized regarding their Encapsulation Efficiency (EE), size, morphology, peptide release in FaSSIF-V2, and protective effect towards proteases. Nanoparticles of 120 nm with platelet structures were obtai...
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

Correlation between the solid state of lipid coating and release profile of API from hot melt coated microcapsules
Publication date: Available online 14 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sharareh Salar-Behzadi, Carolina Corzo, Lisa Schaden, Peter Laggner, Andreas ZimmerAbstractSolvent-free hot melt coating (HMC) provides a safer and more economic process compared to the conventional solvent coating techniques. However, drug release instability and the lack of fundamental understanding on it are limiting factors for application of HMC for industrial productions. In this work, we investigated glyceryl dibehenate, glyceryl monostearate and behenoyl polyoxyl-8 glyceride as HMC materials. The microstructure an...
Source: International Journal of Pharmaceutics - May 15, 2019 Category: Drugs & Pharmacology Source Type: research

Tableting performance of various mannitol and lactose grades assessed by compaction simulation and chemometrical analysis
Publication date: Available online 13 May 2019Source: International Journal of PharmaceuticsAuthor(s): Shubhajit Paul, Pirjo Tajarobi, Catherine Boissier, Changquan Calvin SunAbstractMannitol and lactose are commonly used fillers in pharmaceutical tablets, available in several commercial grades that are produced using different manufacturing processes. These grades significantly differ in particulate and powder properties that impact tablet manufacturability. Choice of sub-optimum type or grade of excipient in tablet formulation can lead to manufacturing problems and difficulties, which are magnified during a continuous ma...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Predicting tablet tensile strength with a model derived from the gravitation-based high-velocity compaction analysis data
In this study it was finally concluded, that the data obtained by the method was of practical relevance in pharmaceutical formulation development.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Photochemically stabilized formulation of dacarbazine with reduced production of algogenic photodegradants
Publication date: 10 June 2019Source: International Journal of Pharmaceutics, Volume 564Author(s): Atsushi Uchida, Hiroto Ohtake, Yukiko Suzuki, Hideyuki Sato, Yoshiki Seto, Satomi Onoue, Toshio OguchiAbstractThe present study aimed to develop a photochemically stabilized formulation of dacarbazine [5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide; DTIC] for reducing the production of algogenic photodegradant (5-diazoimidazole-4-carboxamide; Diazo-IC). Photochemical properties of DTIC were characterized by UV-visible light spectral analysis, reactive oxygen species (ROS) assay, and photostability testing. A pharmacokinet...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Targeted drug delivery to the brain via intranasal nanoemulsion: available proof of concept and existing challenges
Publication date: Available online 13 May 2019Source: International Journal of PharmaceuticsAuthor(s): Bappaditya Chatterjee, Bapi Gorain, Keithanchali Mohananaidu, Pinaki Sengupta, Uttam Kumar Mandal, Hira ChoudhuryAbstractIntranasal delivery has shown to circumvent blood-brain-barrier (BBB) and deliver the drugs into the CNS at a higher rate and extent than other conventional routes. The mechanism of drug transport from nose-to-brain is not fully understood yet, but several neuronal pathways are considered to be involved. Intranasal nanoemulsion for brain targeting is investigated extensively. Higher brain distribution o...
Source: International Journal of Pharmaceutics - May 14, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization of miRNA Delivery by using a Polymeric Conjugate based on Deoxycholic Acid-Modified Polyethylenimine
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fatemeh Radmanesh, Hamid Sadeghi Abandansari, Sara Pahlavan, Mehdi Alikhani, Mahdi Karimi, Sarah Rajabi, Bahram Kazemi Demneh, Hossein BaharvandAbstractSafe and efficient delivery of microRNA (miRNA) molecules is essential for their successful transition from research to the clinic setting. In the present study, we have used a bile acid, deoxycholic acid (DA), to modify 1.8 kDa branched polyethylenimine (bPEI1.8) and subsequently investigated gene delivery features of the resultant conjugates (PEI-DAn). We found significa...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

The Development of an Inline Raman Spectroscopic Analysis Method as a Quality Control Tool for Hot Melt Extruded Ramipril Fixed-dose Combination Products
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): G.P. Andrews, D.S. Jones, Z. Senta-Loys, A. Almajaan, S. Li, O. Chevallier, C. Elliot, A.M. Healy, J.F. Kelleher, A.M. Madi, G.C. Gilvary, Y. TianAbstractCurrently in the pharmaceutical industry, continuous manufacturing is an area of significant interest. In particular, hot-melt extrusion (HME) offers many advantages and has been shown to significantly reduce the number of processing steps relative to a conventional product manufacturing line. To control product quality during HME without process interruption, integratio...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Prediction of dissolution profiles by non-destructive NIR spectroscopy in bilayer tablets
This study describes how near infrared (NIR) spectroscopy can be used to predict the dissolution of bilayer tablets as a non-destructive approach. Tablets in this study consist of two APIs physically separated in layers and manufactured under three levels of hardness. NIR spectra were acquired for each layer in diffuse reflectance mode. Reference dissolution profile values were obtained using dissolution apparatus & HPLC. A multivariate PLS calibration model was developed for each API relating its dissolution profile with to spectral data. This calibration model was used to predict dissolution profile of an independent...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Novel Polyurethane-based nanoparticles of infliximab to reduce inflammation in an in-vitro intestinal epithelial barrier model
In this study we examined the potential of novel biodegradable polymers of polyesterurethane (PU), and its PEGylated (PU-PEG) form as nanocarriers of Infliximab (INF), to treat inflammation in an in-vitro epithelial model. Nanoparticles (NPs) formulated were of average size of 200-287nm. INF loading of NPs (INF-NPs) resulted in an increase in size and zeta potential. No cytotoxicity was observed for any of the NPs. Cellular interaction and uptake of PU NPs were similar compared with polycaprolactone (PCL) NPs and significantly higher to Poly(lactic-co-glycolic) acid (PLGA) NPs. Cellular interaction was higher for correspon...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

MRP2-mediated transport of etoposide in MDCKII MRP2 cells is unaffected by commonly used non-ionic surfactants
In conclusion, etoposide transport across MDCKII MRP2 cells was modulated by cyclosporine A, an inhibitor of MRP2 and P-gp, but not by specific P-gp inhibitors (valspodar and zosuquidar), which suggests that etoposide transport is primarily influenced by MRP2. In addition, commonly used non-ionic surfactants did not decrease MRP2-mediated etoposide transport in MDCKII MRP2 cells. These results suggest that etoposide transport in MDCKII MRP2 cells is a model system to investigate MRP2 interactions, and that surfactants may not have a large potential for increasing oral bioavailability of drugs through inhibition of MRP2 tra...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluating the potential of drug eluting contact lenses for treatment of bacterial keratitis using an ex vivo corneal model
This study aims to investigate the effectiveness of ofloxacin-loaded contact lenses as prolonged release devices for the treatment of bacterial keratitis.Two silicone hydrogel contact lenses (SHCLs) Senofilcon A (ACUVUE OASYS®) and Narafilcon A (ACUVUE TRUEYE®) were modified by incorporation of ofloxacin alone or with vitamin E (VE). The drug uptake and in vitro release kinetics were investigated and the antibacterial efficacy was assessed against Staphylococcus aureus and Pseudomonas aeruginosa in an ex vivo rabbit corneal model.The in vitro studies showed a higher uptake (p≤ 0.05) and longer duration of releas...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Drug stability and product performance characteristics of a dapivirine-releasing vaginal ring under simulated real-world conditions
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Diarmaid J. Murphy, Clare F. McCoy, Peter Boyd, Tiffany Derrick, Patrick Spence, Brid Devlin, R. Karl MalcolmAbstractIn two recent Phase III clinical trials, use of a 25 mg dapivirine vaginal ring significantly reduced HIV acquisition rates. Post hoc analysis from one of the trials indicated higher rates of protection among women over the age of 21 years when compared to younger women, most likely due to reduced adherence in the latter group. There is currently no information available on how release of dapivirine from th...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Application of an automated small-scale in vitro transfer model to predict in vivo precipitation inhibition
Publication date: Available online 11 May 2019Source: International Journal of PharmaceuticsAuthor(s): Christian Jede, Christian Wagner, Holger Kubas, Christian Weber, Markus Weigandt, Mirko Koziolek, Werner WeitschiesAbstractThe majority of NCEs are weakly basic drugs. Consequently, their solubility is highly pH-dependent, with higher solubility in the acidic stomach and poor solubility in the neutral intestinal environment. The gastric emptying of dissolved drug can lead to the intestinal precipitation of the drug. One option of reducing this process is to formulate the drug together with a precipitation inhibitor (PI). ...
Source: International Journal of Pharmaceutics - May 12, 2019 Category: Drugs & Pharmacology Source Type: research

Diversity of β-cyclodextrin-based nanosponges for transformation of actives
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sandip Pawar, Pravin Shende, Francesco TrottaAbstractβ-Cyclodextrin-based nanosponges (β-CDNSs) play an important role in new arrays of agriculture, floriculture, cosmetics, medicine, high molecular weight proteins, novel flame retardants, gas carriers and water filters. In recent years, the field of advance nanostructured systems witnesses a rapid development due to miniaturization, dose-reduction, sustained and controlled release of actives and long-term stability of material. β-CDNSs are colloidal and cr...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of the solid state form of tadalafil in sub-micron thin films using nanomechanical infrared spectroscopy
Publication date: Available online 9 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fatemeh Samaeifar, Andrea Casci Ceccacci, Sanjukta Bose Goswami, Line Hagner Nielsen, Ahmad Afifi, Kinga Zór, Anja BoisenAbstractAssessing physical stability of drugs is important both in the development as well as in the production phase in the pharmaceutical industry. We used nanomechanical infrared (NAM-IR) spectroscopy based on photothermal response of a nanomechanical resonator, to investigate the solid state forms of tadalafil (TAD), under various storage conditions in sub-micron thin films. The amorphous TAD ...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Biodistribution/Biostability Assessment of siRNA after Intravenous and Intratracheal Administration to Mice, Based on Comprehensive Analysis of In Vivo/Ex Vivo/Polyacrylamide Gel Electrophoresis Fluorescence Imaging
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Tomoyuki Okuda, Yoko Toyoda, Takashi Murakami, Hirokazu OkamotoAbstractWe performed in vivo/ex vivo/polyacrylamide gel electrophoresis (PAGE) fluorescence imaging of near-infrared fluorescence (NIRF)-labeled siRNA (Cy5.5-siGL3) in mice to investigate the validity of each fluorescence imaging result as the biodistribution/biostability assessment of siRNA. Statistically significant correlations could be obtained between the in vivo and ex vivo fluorescence intensities of Cy5.5 in the relevant regions/tissues, except the lun...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Phase transition and release kinetics of polyphenols encapsulated lyotropic liquid crystals
Publication date: Available online 10 May 2019Source: International Journal of PharmaceuticsAuthor(s): Heng Zhang, Zhongni WangAbstractIn this paper, the lyotropic liquid crystals formed in SL/IP/H2O system were prepared as a drug carrier system to encapsulate polyphenols. The components and introduction of drug had influences in the structure and rheological properties of lyotropic liquid crystals. The structure underwent a phase transition from lamellar phase (Lα) to Lα+HII (reverse hexagonal phase) mixed phases and micelle by increasing its IP/H2O mass ratio from 5/35 to 20/20 and 35/5, consistent with the t...
Source: International Journal of Pharmaceutics - May 11, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of thermal and shear stresses in the spray drying process on the stability of siRNA dry powders
In conclusion, stable siRNA based particles for inhalation purposes could be produced using the spray drying technology.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

In vivo biocompatibility, pharmacokinetics, antitumor efficacy, and hypersensitivity evaluation of ionic liquid-mediated paclitaxel formulations
In this study, the stability of the IL-PTX formulation was monitored by quantitative HPLC analysis, which showed that IL-PTX was more stable at 4 °C than at room temperature. The in vivo study showed that the IL-PTX formulation could be used in a therapeutic application as a biocompatible component of a drug delivery system. To assess the in-vivo biocompatibility, IL or IL-mediated formulations were administered intravenously by maintaining physiological buffered conditions (neutral pH and isotonic salt concentration). From in vivo pharmacokinetics data, the IL-PTX formulation was found to have a similar systemic circu...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Surface conjugation of EP67 to biodegradable nanoparticles increases the generation of long-lived mucosal and systemic memory T-cells by encapsulated protein vaccine after respiratory immunization and subsequent T-cell-mediated protection against respiratory infection
Publication date: Available online 8 May 2019Source: International Journal of PharmaceuticsAuthor(s): Shailendra B. Tallapaka, Bala V.K. Karuturi, Pravin Yeapuri, Stephen M. Curran, Yogesh A. Sonawane, Joy A. Phillips, D. David Smith, Sam D. Sanderson, Joseph A. VetroAbstractEncapsulation of protein vaccines in biodegradable nanoparticles (NP) increases T-cell expansion after mucosal immunization but requires incorporating a suitable immunostimulant to increase long-lived memory T-cells. EP67 is a clinically viable, host-derived peptide agonist of the C5a receptor that selectively activates antigen presenting cells over ne...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Controlled release Ibu-cryobarriers for the prevention of post-operative adhesions: In-vitro/in-vivo comparative study
Publication date: 30 June 2019Source: International Journal of Pharmaceutics, Volume 565Author(s): Noha S. El-Salamouni, Mennatallah A. Gowayed, Gihan S. LabibAbstractPost-operative adhesion is a common cause of several complications including intestinal obstruction, chronic pelvic pain and/or infertility. Adhesions are fibrous bands that result from the inflammatory reactions due to peritoneum damage. The current study focused on designing an effective anti-inflammatory loaded barrier for the prevention of post-operative adhesions. The proposed method is based on the use of polyvinyl alcohol (PVA), cryobarrier loaded with...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Gold Nanoparticles Loaded into Polymeric Hydrogel for Wound Healing in Rats: Effect of Nanoparticles’ Shape and Surface Modification
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Nouf N. Mahmoud, Suhair Hikmat, Duaa Abu Ghith, Manar Hajeer, Lama Hamadneh, Duaa Qattan, Enam A. KhalilAbstractNanotechnology-based platforms have gained a growing interest in healing skin wounds. Herein, gold nanoparticles (AuNPs) of different shapes (rods and spheres) and surface modifications (neutral, cationic and anionic charged polymers) were synthesized, characterized and loaded into a thermosensitive hydrogel (poloxamer 407). AuNPs-hydrogels exhibited excellent colloidal stability and demonstrated slow and prolong...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Managing efficacy and toxicity of drugs: Targeted delivery and excretion
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Pronab Kundu, Sinjan Das, Nitin ChattopadhyayAbstractMedicine is a natural companion of mankind of the present era for mere survival from the deadly diseases in the ever-increasing polluted environments. Hence, in recent years, major focus of pharmaceutical, medicinal and biophysical research has been navigated in exploring and developing new and simple avenues to enhance the efficacy of the administered drugs on one hand and to get rid of, or at least reduce, the toxic side effects of the excess drugs accumulated in human...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Quantitation of trace amorphous solifenacin succinate in pharmaceutical formulations by transmission Raman spectroscopy
In this study, we aimed to quantify amorphous solid in API by transmission Raman spectroscopy (TRS) and transmission near-infra-red spectroscopy (NIRS). To quantify the amount of trace amorphous solids contained in the API of a formulation, calibration curves of tablets containing 40% or 3% solifenacin succinate (SLFS) in the pharmaceutical formulations were prepared. The tablets varied in the ratio of amorphous solids in the API. TRS and NIRS were carried out with the calibration tablets and partial least square regression (PLSR) analysis was performed. Good results were obtained by both TRS and NIRS with the calibration ...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Cationized hyaluronic acid coated spanlastics for cyclosporine A ocular delivery: Prolonged ocular retention, enhanced corneal permeation and improved tear production
Publication date: Available online 8 May 2019Source: International Journal of PharmaceuticsAuthor(s): Yang Liu, Yanan Wang, Jinlong Yang, Hua Zhang, Li GanAbstractThe aim of this work was to design and evaluate novel cationized hyaluronic acid coated spanlastics (CHASVs), with the immunosuppressive peptide cyclosporine A (CsA) as the model drug. CHASVs exhibited ideal size, zeta potential, pH, osmolarity and entrapment efficiency. The developed CHASVs provided a surface tension of 34.98±0.19 mN/m, a contact angle of 21.07±3.56° and a viscosity of 9-12 mPa·s, which reflected favorable wetting and bi...
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research

Study on the therapeutic index and synergistic effect of Chitosan-Zinc Oxide nanomicellar composites for drug-resistant bacterial biofilm inhibition
Publication date: Available online 6 May 2019Source: International Journal of PharmaceuticsAuthor(s): Mausam Mehta, Diane Allen-Gipson, Shyam Mohapatra, Mark Kindy, Alya LimayemAbstractThe synergistic effectiveness of chitosan with zinc oxide nanomicelles (CZNPs) on broad spectrum of multidrug resistance (MDR) was previously evidenced in our labs, requiring elucidation of the therapeutic index (TI) for safe in vivo use. This in vitro assessment estimated the effective dose (ED50) of micellar CZNPs for eradication of the MDR Enterococcus faecium 1449 model and the corresponding cytotoxic dose (LD50) against rat small intest...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Antioxidant activity of quercetin in Eudragit-coated liposomes for intestinal delivery
Publication date: Available online 6 May 2019Source: International Journal of PharmaceuticsAuthor(s): Carla Caddeo, Morena Gabriele, Xavier Fernàndez-Busquets, Donatella Valenti, Anna Maria Fadda, Laura Pucci, Maria ManconiAbstractQuercetin, a natural polyphenol with strong antioxidant activity, was loaded in Eudragit-coated liposomes conceived for intestinal delivery. Eudragit was used to form a protective shell on the surface of liposomes to resist gastric environment and allow the delivery of quercetin to the intestine. The physico-chemical properties of the liposomes were assessed by light scattering and cryogen...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Fast Raman Chemical Imaging of Tablets with Non-Flat Surfaces
Publication date: Available online 6 May 2019Source: International Journal of PharmaceuticsAuthor(s): Slobodan Šašić, Tim PrusnickAbstractA curved area with embossment on an analgesic tablet with three APIs is imaged with a Raman instrument equipped with hardware options that allow for continuous focus adjustment and very fast acquisition of micro-Raman spectra, about sixty spectra per second in this study. Univariate, self-modelling curve resolution, and regression derived images via the pure component spectra are obtained for all three APIs. The quality of the images and reasons for thresholding are discus...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Investigation of the parameters used in fused deposition modeling of poly(lactic acid) to optimize 3D printing sessions
This study assesses the feasibility of printing implantable devices using 3D printing Fused deposition modeling (FDM) technology. The influence of the deposition temperature, the deposition rate and the layer thickness on the printing process and the physical properties of the devices were evaluated. The filaments were composed of neat poly(lactic acid) (PLA) and blends of different plasticizers (polyethylene glycol 400 (PEG 400), triacetine (TA), acetyltriethyl citrate (ATEC) and triethyl citrate (TEC)) at 10% (w/w). The assessment of thermomechanical characteristics and morphology of both filaments and devices (cylinders...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of Cell Membrane-Adhesive Soft Polymeric Nanovehicles for Noninvasive Visualization of Epidermal-Dermal Junction-Targeted Drug Delivery
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Sungjun Hong, Jaesung Park, Ji Eun Kim, Daehwan Park, Seulgi Kim, Jeong Yi Kang, Jin Yong Lee, Woo Jin Hong, Hyanghwa Jeon, Ho Lee, Jin Woong KimAbstractWe propose a polymeric nanovehicles (PNVs)-based enhanced transdermal delivery platform. A technical advance can be found in that delivery efficiency is significantly enhanced by effective adhesion of PNVs to the cell membrane, which is characterized noninvasively by using a confocal laser scanning microscopy (CLSM)-based skin visualization technique. To this end, the PNVs...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Predicting the critical quality attributes of ibuprofen tablets via modelling of process parameters for roller compaction and tabletting
In this study, for ibuprofen tablets with high drug loading (
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Nano spray dryer for vectorizing α-Galactosylceramide in polymeric nanoparticles: a single step process to enhance invariant Natural Killer T lymphocyte responses
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Michelangelo Bauwelz Gonzatti, Maria Eduarda Perrud Sousa, Ariane Simões Tunissi, Renato Arruda Mortara, Adriano Marim de Oliveira, Natália Neto Pereira Cerize, Alexandre de Castro KellerAbstractThe recognition of α-galactosylceramide (αGC), a high-affinity CD1d antigen, by the invariant Natural Killer T (iNKT) lymphocytes results in potent immunostimulatory responses that have been exploited in advanced cancer patients. Therefore, to improve αGC biological activity, several studies vectoriz...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Atorvastatin loaded PLGA microspheres: preparation, HAp coating, drug release and effect on osteogenic differentiation of ADMSCs
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fatemeh Shokrolahi, Khosrow Khodabakhshi, Parvin Shokrollahi, Roya Badiani, Zohreh Mansoori MoghadamAbstractPolymer/bioceramic composite micro-particles have been used for bone regeneration in order to address weak mechanical properties/bioactivity of polymers and to enable easy filling of irregular bone defects through minimally invasive injection procedure. The purpose of this study was to determine whether injectable apatite-coated atorvastatin (AT) loaded Poly (d,l-lactide-co-glycolide) (PLGA) micro-particles can suppo...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Nanoformulation for potential topical delivery of Vismodegib in skin cancer treatment
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Maria Natalia Calienni, Camilo Febres-Molina, Ramiro Esteban Llovera, Christian Zevallos-Delgado, María Eugenia Tuttolomondo, Donatella Paolino, Massimo Fresta, Haruna L. Barazorda-Ccahuana, Badhin Gómez, Silvia del Valle Alonso, Jorge MontanariAbstractVismodegib (Erivedge®, Genentech) is a first-in-class inhibitor of the hedgehog signaling pathway for the treatment of basal cell carcinoma (BCC). The treatment currently consists of the oral administration of Erivedge® capsules. Although it has shown t...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of an in-line NIR spectroscopic method for the determination of the residence time in a tablet press
Publication date: Available online 7 May 2019Source: International Journal of PharmaceuticsAuthor(s): Fien De Leersnyder, Valérie Vanhoorne, Ashish Kumar, Chris Vervaet, Thomas De BeerAbstractIn the current study, the ability to use in-line NIR inside the feed frame of a tablet press to monitor the residence time distribution inside the tablet press was investigated. Pulse-response experiments were performed. In-line measurements inside the feed frame were compared to measurements on the actual produced tablets and the influence of different tableting parameters on the concentration profiles were studied. Turret spe...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Potential of biocompatible polymeric ultra-thin films, nanosheets, as topical and transdermal drug delivery devices
Publication date: 30 June 2019Source: International Journal of Pharmaceutics, Volume 565Author(s): Tomomi Hatanaka, Takanori Saito, Takaaki Fukushima, Hiroaki Todo, Kenji Sugibayashi, Soichi Umehara, Tomoharu Takeuchi, Yosuke OkamuraAbstractThe aim of the present study was to assess the potential of biocompatible polymeric nanosheets as topical and transdermal drug-delivery devices. Nanosheets are two-dimensional nanostructures with a thickness in the nanometer order, and their extremely large aspect ratios result in unique properties, including high transparency, flexibility, and adhesiveness. Nanosheet formulations conta...
Source: International Journal of Pharmaceutics - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

Critical Process Parameters in Manufacturing of Liposomal Formulations Of Amphotericin B
This study investigated how multi-step production approaches and related manufacturing conditions may affect essential physico-chemical and toxicological properties of the final drug product. A key challenge in the manufacture and analysis of liposomal AMB was the drug substance’s propensity to aggregate, with associated poor solubility in water and organic solvents. This study identified three key CPPs in a four step manufacturing process: (i) proper acidification during formation of the drug-lipid complexes (Step 1), (ii) liposome heat curing following liposomal particle sizing (Step 3), and (iii) flash-freezi...
Source: International Journal of Pharmaceutics - May 6, 2019 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetic characterization of kalata B1 and related therapeutics built on the cyclotide scaffold
This study provides new data essential to the evaluation of cyclotides as therapeutics, validating them as a viable drug design scaffold with tunable pharmacokinetic properties.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 5, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of doxycycline-loaded electrospun PCL/PEO membranes for a potential drug delivery system
Publication date: Available online 4 May 2019Source: International Journal of PharmaceuticsAuthor(s): Ş. Melda Eskitoros-Togay, Y. Emre Bulbul, Serdar Tort, Funda Demirtaş Korkmaz, Füsun Acartürk, Nursel DilsizAbstractPotential usage of biodegradable and biocompatible polymeric nanofibers is the most attention grabbing topic for the drug delivery system. In order to fabricate ultrafine fibers, electrospinning, one of the well-known techniques, has been extensively studied in the literature. In the present study, the objective is to achieve the optimum blend of hydrophobic and hydrophilic polymers to be used as ...
Source: International Journal of Pharmaceutics - May 5, 2019 Category: Drugs & Pharmacology Source Type: research

Rapid development of API nano-formulations from screening to production combining dual centrifugation and wet agitator bead milling
Publication date: Available online 4 May 2019Source: International Journal of PharmaceuticsAuthor(s): Martin Hagedorn, Lena Liebich, Ansgar Bögershausen, Ulrich Massing, Sven Hoffmann, Stefan Mende, Matthias RischerAbstract:Various wet ball nanomilling-screening tools for poorly soluble APIs are available which differ in their milling principle, batch size and number of samples. Here, the transferability of results from screening (small to medium-scale) to pharmaceutical production (largescale) was investigated. Wet ball milling in a dual centrifuge (DC) (10 -100 mg API, 40 samples in parallel) was used to identify st...
Source: International Journal of Pharmaceutics - May 5, 2019 Category: Drugs & Pharmacology Source Type: research

Controlled release Ibu-cryobarriers for the prevention of post-operative adhesions: In-vitro / in-vivo comparative study
Publication date: Available online 2 May 2019Source: International Journal of PharmaceuticsAuthor(s): Noha S. El-Salamouni, Mennatallah A. Gowayed, Gihan S. LabibGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 3, 2019 Category: Drugs & Pharmacology Source Type: research

The effect of new compounds in stabilizing downstream monoclonal antibody (mAb) process intermediates
Publication date: Available online 3 May 2019Source: International Journal of PharmaceuticsAuthor(s): Irina Ramos, Eva C. Lourenço, Osvaldo S. Ascenso, Christopher D. Maycock, Madhukar Dasika, Matthew L. Dickson, M. Rita VenturaAbstractDetermining the stability of downstream process (DSP) intermediates is an extremely important parameter used to maintain product quality attributes within their acceptance ranges. The IgG4 monoclonal antibody studied (mAb1) showed aggregation under acidic conditions, inhibiting the use of low pH treatment to inactivate endogenous retroviruses, and poor virus filtration performance. Bo...
Source: International Journal of Pharmaceutics - May 3, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro evaluation of innovative light-responsive nanoparticles for controlled drug release in intestinal PDT
In this study, innovative light-sensitive NP were investigated for a photodynamic therapy (PDT) of gastrointestinal tumors. Nanoparticles based on a newly developed light-responsive polycarbonate (LrPC) and poly(lactic-co-glycolic-acid) (PLGA) were loaded with the approved photosensitizer 5,10,15,20-tetrakis(m-hydroxyphenyl)chlorin (mTHPC). Mucus penetrating properties were obtained by surface PEGylation of the nanoparticles either by using LrPC in combination with a PEGylated PLA (PEG-PLA) or by a combination with PEGylated LrPC (LrPC-PEG). Cytotoxic potential in dependency of a light-induced drug release was investigated...
Source: International Journal of Pharmaceutics - May 2, 2019 Category: Drugs & Pharmacology Source Type: research

Design and development of letrozole nanoemulsion: A comparative evaluation of brain targeted nanoemulsion with free letrozole against status epilepticus and neurodegeneration in mice
Publication date: Available online 30 April 2019Source: International Journal of PharmaceuticsAuthor(s): Ramsha Iqbal, Shakeeb Ahmed, Gaurav K. Jain, Divya VohoraAbstractThe target of the current study is to formulate letrozole loaded nanoemulsion (LET-NE) for the direct nose to brain delivery to reduce peripheral effects of letrozole (LET). LET-NE is compared against intraperitoneally administered free LET in kainic acid (KA) induced status epilepticus (SE) in mice. LET loaded nanoemulsion (LET-NE) was prepared by aqueous microtitration method using Triacetin, Tween 80 and PEG-400 as the oil phase, surfactant, and co-surf...
Source: International Journal of Pharmaceutics - May 2, 2019 Category: Drugs & Pharmacology Source Type: research

Liposome Mediated-CYP1A1 Gene Silencing Nanomedicine Prepared Using Lipid Film-Coated Proliposomes as a Potential Treatment Strategy of Lung Cancer
Publication date: Available online 30 April 2019Source: International Journal of PharmaceuticsAuthor(s): Mengtian Zhang, Qin Wang, Ka-Wai Wan, Waqar Ahmed, David A Phoenix, Zhirong Zhang, Mohamed A. Elrayess, Abdelbary Elhissi, Xun SunAbstractThe occurrence of lung cancer is linked with tobacco smoking, mainly through the generation of polycyclic aromatic hydrocarbons (PAHs). Elevated activity of cytochrome P4501A1 (CYP1A1) plays an important role in the metabolic processing of PAHs and its carcinogenicity. The present work aimed to investigate the role of CYP1A1 gene in PAH-mediated growth and tumor development in vitro a...
Source: International Journal of Pharmaceutics - May 2, 2019 Category: Drugs & Pharmacology Source Type: research