AS1411 derivatives as carriers of G-quadruplex ligands for cervical cancer cells
Publication date: Available online 10 July 2019Source: International Journal of PharmaceuticsAuthor(s): Joana Figueiredo, Jéssica Lopes-Nunes, Josué Carvalho, Francisca Antunes, Márcia Ribeiro, Maria Paula Cabral Campello, António Paulo, Artur Paiva, Gilmar F. Salgado, João A. Queiroz, Jean-Louis Mergny, Carla CruzAbstractNucleic acid aptamers can specifically bind to target molecules on the cell membrane that mediate their entrance into the cells. Their small size, high binding affinity, specificity, good biocompatibility, stability and low immunogenicity make them ideal drug delivery sy...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of different aliphatic acid grafted N-trimethyl chitosan surface-modified nanostructured lipid carriers for improved oral kaempferol delivery
This study compared the in vitro and in vivo effects of different aliphatic acid grafted N-trimethyl chitosan (TMC) surface-modified nanostructured lipid carriers (NLC) by oral delivery. Medium-chain fatty acids, decylic acids (DA), and long-chain fatty acids, palmitic acids (PA) were selected as contrasting objects. TMC, DA grafted TMC (DA-TMC), and PA grafted TMC (PA-TMC) were successively synthesized. Kaempferol loaded NLC (KNLC), KNLC coated with DA-TMC (DA-TMC-KNLC) and PA-TMC (PA-TMC-KNLC) were fabricated, respectively. KNLC were subspherical in shape at nano-size limits. The particle size increased from 93.6 to 125....
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Quality attributes and evaluation of pharmaceutical glass containers for parenterals
Publication date: Available online 11 July 2019Source: International Journal of PharmaceuticsAuthor(s): Charudharshini Srinivasan, Youlong Ma, Yangping Liu, Yifan Wang, Leanna Hengst, Xiaofei Liu, Roxana Toth, Jason Rodriguez, Adil Mohammad, Bandaranayake M.B. Bandaranayake, David Simon, Christopher Beekman, Maxwell Korang-Yeboah, Shiril Sivan, Sau (Larry) Lee, Celia N. CruzAbstractPharmaceutical containers for parenterals have been predominantly manufactured using glass as a packaging material of choice, especially Type-I glass, since it has been regarded as a chemically inert and an effective container closure system (CC...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Oral delivery of imatinib through galactosylated polymeric nanoparticles to explore the contribution of a saccharide ligand to absorption
Publication date: 10 September 2019Source: International Journal of Pharmaceutics, Volume 568Author(s): Yan Li, Baohui Yang, Xingwang ZhangAbstractImatinib (IMT) is a selective tyrosine kinase inhibitor clinically used for treating chronic myeloid leukemia and malignant gastrointestinal stromal tumors. However, oral administration of IMT is challenged by its high oral dose, low intestinal solubility and adverse reactions. This work aimed to investigate the effect of galactose ligand on polymeric nanoparticles-facilitated oral absorption of IMT. N-oleoyl-D-galactosamine was synthesized for fabricating biomimetic galactose-m...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

3D printing of unique water-soluble polymer-based suppository shell for controlled drug release
Publication date: 10 September 2019Source: International Journal of Pharmaceutics, Volume 568Author(s): Tatsuaki Tagami, Naomi Hayashi, Norihito Sakai, Tetsuya OzekiAbstract3D printing technology holds promise for application to personalized pharmaceuticals. Mold fabrication is a common technique in industrial 3D printing to produce objects with complex structures and could be used in new applications in pharmaceutical production. The aim of the current study is the fabrication of unique suppository shell molds composed of a water-soluble polymer (polyvinylalcohol) using a fused deposition modeling-type 3D printer so that ...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

The presence of PEG on nanoparticles presenting the c[RGDfK]- and/or ATWLPPR peptides deeply affects the RTKs-AKT-GSK3β-eNOS signaling pathway and endothelial cells survival
Publication date: 10 September 2019Source: International Journal of Pharmaceutics, Volume 568Author(s): Tao Jia, Jéremy Ciccione, Thibault Jacquet, Manon Maurel, Titouan Montheil, Ahmad Mehdi, Jean Martinez, Béatrice Eymin, Gilles Subra, Jean-Luc CollAbstractCovering the surface of a nanoparticle with polyethylene glycol (PEG) is a common way to prevent non-specific interactions but how its presence impacts on the activity of targeting ligands is still poorly documented. We synthesized a set of 9 silica nanoparticles grafted with c[RGDfK]-, a peptide targeting integrin αvß3 (cRGD), and/or with ATW...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis of carboxymethylated nanocellulose fabricated ciprofloxacine – Montmorillonite composite for sustained delivery of antibiotics
This study sought to synthesize an antibiotic delivery material with more sustained release properties. A ciprofloxacin (CIP)-MMT composite was fabricated using carboxymethylated nanocellulose (CMCNF). A simple adsorption reaction intercalated 31.1% of CIP molecules present into the MMT under optimized conditions (pH 5, CIP = 1000 mg/L, Reaction time = 3 h). The synthesized CIP-MMT composite was fabricated using 1.5, 2, or 3 wt% CMCNF. Increasing the CMCNF content delayed the erosion of the CMCNF matrix and prevented rapid dissolution of the CIP-MMT composite. In vitro release experiments revealed that the CI...
Source: International Journal of Pharmaceutics - July 11, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of ionic interactions on protein stability prediction using solid-state hydrogen deuterium exchange with mass spectrometry (ssHDX-MS)
Publication date: Available online 10 July 2019Source: International Journal of PharmaceuticsAuthor(s): Mohamed H.H. AbouGhaly, Jiali Du, Sajal M. Patel, Elizabeth M. ToppAbstractDeuterium incorporation in solid-state hydrogen deuterium exchange with mass spectrometry (ssHDX-MS) has been correlated with protein aggregation on storage in sugar-based solid matrices. Here, the effects of sucrose, arginine and histidine buffer on the rate of aggregation of a lyophilized monoclonal antibody (mAb) were assessed using design of experiments (DoE) and response surface methodology. Lyophilized formulations were characterized using s...
Source: International Journal of Pharmaceutics - July 10, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of submicron drug particles via spray drying from organic solvents
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Adrian Dobrowolski, Ramona Strob, Jan Felix Dräger-Gillessen, Damian Pieloth, Gerhard Schaldach, Helmut Wiggers, Markus ThommesAbstractManufacturing poorly water-soluble active pharmaceutical ingredients (API) with sufficient bioavailability is a significant challenge in pharmaceutical research. A higher bioavailability can reduce both the applied dosage and the side effects for the patient. One method of increasing the bioavailability is to reduce the particle size of the drug down to the nanoscale.An innovative proce...
Source: International Journal of Pharmaceutics - July 10, 2019 Category: Drugs & Pharmacology Source Type: research

A nano-sized gel-in-oil suspension for transcutaneous protein delivery
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Safrina Dyah Hardiningtyas, Seiya Nagao, Emiko Yamamoto, Nana Shirakigawa, Rie Wakabayashi, Masahiro Goto, Hiroyuki Ijima, Noriho KamiyaAbstractWe developed a new oil-based delivery system for transdermal protein delivery, a gel-in-oil (G/O) nanosuspension, where gelatin-based hydrogel was coated with hydrophobic surfactants. The high entrapment efficiency of a model protein, phycocyanin (PC), into nano-sized gelatin hydrogel particles was achieved. Spectroscopic evaluation of PC suggested that the G/O nanosuspension could ...
Source: International Journal of Pharmaceutics - July 10, 2019 Category: Drugs & Pharmacology Source Type: research

Synthesis of carboxymethylated nanocellulose fabricated ciprofloxacine - montmorillonite composite for sustained delivery of antibiotics
This study sought to synthesize an antibiotic delivery material with more sustained release properties. A ciprofloxacin(CIP)-MMT composite was fabricated using carboxymethylated nanocellulose(CMCNF). A simple adsorption reaction intercalated 31.1% of CIP molecules present into the MMT under optimized conditions(pH 5, CIP= 1000 mg/L, Reaction time=3 h). The synthesized CIP-MMT composite was fabricated using 1.5, 2, or 3 wt% CMCNF. Increasing the CMCNF content delayed the erosion of the CMCNF matrix and prevented rapid dissolution of the CIP-MMT composite. In vitro release experiments revealed that the CIP-MMT composite mate...
Source: International Journal of Pharmaceutics - July 10, 2019 Category: Drugs & Pharmacology Source Type: research

Antibacterial and transfection activities of nebulized formulations incorporating long n-alkyl chain silver N-heterocyclic carbene complexes
Publication date: Available online 6 July 2019Source: International Journal of PharmaceuticsAuthor(s): Angélique Mottais, Mathieu Berchel, Tony Le Gall, Yann Sibiril, Frédérique d'Arbonneau, Véronique Laurent, Paul-Alain Jaffrès, Tristan MontierAbstractThe development of new antibacterial molecules is essential in view of the emergence of pathogenic strains resistant to multiple antibiotics. Among the infectious pathologies, pulmonary infections are particularly difficult to treat due to the complexity of lung anatomy and the presence of natural barriers such as mucus. At present, the aer...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

Conception of nanosized hybrid liposome/poloxamer particles to thicken the interior core of liposomes and delay hydrophilic drug delivery
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Shayan Ahmed, Yohann Corvis, Rabah Gahoual, Arlen Euan, Rene Lai-Kuen, Brice Martin Couillaud, Johanne Seguin, Khair Alhareth, Nathalie MignetAbstractLiposomes are nanocarriers composed of phospholipids, especially designed to potentially carry drugs. However, liposomes suffer in terms of leakage of small hydrophilic drugs. To control the release, a system with lipid shell and polymeric viscous core, namely Hybrid liposome/polymer inside (HLPin), has been designed. For this purpose, we setup a syringe pump apparatus equippe...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

Aptamers as the chaperones (Aptachaperones) of drugs-from siRNAs to DNA nanorobots
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Marimuthu Citartan, Harleen Kaur, Ravinderan Presela, Thean-Hock TangAbstractAptamers, nucleic acid ligands that are specific against their corresponding targets are increasingly employed in a variety of applications including diagnostics and therapeutics. The specificity of the aptamers against their targets is also used as the basis for the formulation of the aptamer-based drug delivery system. In this review, we aim to provide an overview on the chaperoning roles of aptamers in acting as the cargo or load carriers, deliv...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

A simple blending with α-glycosylated naringin produces enhanced solubility and absorption of pranlukast hemihydrate
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Hiromasa Uchiyama, Kazunori Kadota, Akihito Nakanishi, Mahamadou Tandia, Yuichi TozukaAbstractThe possibility of newly developed α-glycosylated naringin (Naringin-G) as a solubilizing agent was investigated against pranlukast hemihydrate (PLH), a model drug with extremely low water solubility. The physical mixtures (PMs) of PLH/Naringin-G increased the solubility of PLH compared with PLH crystals and PMs with other additives, such as α-glycosylated rutin (Rutin-G) and sodium dodecyl sulfate (SDS). Naringin-G did...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

Automated therapy preparation of isoleucine formulations using 3D printing for the treatment of MSUD: first single-centre, prospective, crossover study in patients
Publication date: Available online 4 July 2019Source: International Journal of PharmaceuticsAuthor(s): Alvaro Goyanes, Christine M. Madla, Aysha Umerji, Goretti Duran Piñeiro, Jose Maria Giraldez Montero, María Jesús Lamas Diaz, Miguel Gonzalez Barcia, Farhan Taherali, Paula Sánchez-Pintos, Maria-Luz Couce, Simon Gaisford, Abdul W. BasitAbstractMaple syrup urine disease (MSUD) is a rare metabolic disorder with a worldwide prevalence of 1 in every 185,000 live births. However, certain populations display a significant overexpression of the disorder where incidence is reported to be 1 in every 52,...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

The thermostated medical jet nebulizer: Aerosol characteristics
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): M. Ochowiak, A. Kasperkowiak, M. Doligalski, T.R. Sosnowski, M. Matuszak, S. Włodarczak, M. Markowska, A. Krupińska, K. JabłczyńskaAbstractThe sudden expansion of gas at the outlet of the jet (pneumatic) nebulizer significantly reduces the temperature of the solution, which may provoke bronchospasm, therefore it is recommended to use modern pneumatic inhalers equipped with a thermostat or a universal thermal attachment that allow to obtain a higher temperature aerosol, i.e. thermo-aerosol. The research was carried out f...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

Tunable vegetable oil/silica hybrid microparticles for poorly water-soluble drug delivery
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Koceïla Doufène, Vincent Lapinte, Philippe Gaveau, Gautier Félix, Thomas Cacciaguerra, Joël Chopineau, Jean-Jacques Robin, Jean-Marie Devoisselle, Anne Aubert-PouësselAbstractTo encapsulate and deliver poorly water-soluble drugs, castor oil/silica hybrid microparticles (HMP)s were synthesized. Green chemistries were used to silylate the oil and further cross-link it into solid microparticles by sol-gel reaction. Silylated castor oils (ICO)s at various silylation ratios were prepared and allowed ...
Source: International Journal of Pharmaceutics - July 7, 2019 Category: Drugs & Pharmacology Source Type: research

Predicting the Solubility Enhancement of Amorphous Drugs and Related Phenomena Using Basic Thermodynamic Principles and Semi-Empirical Kinetic Models
Publication date: Available online 4 July 2019Source: International Journal of PharmaceuticsAuthor(s): Peter J. Skrdla, Philip D. Floyd, Philip C. Dell'OrcoGraphical abstractThe accurate prediction of the solubility enhancement offered by neat amorphous drugs and amorphous solid dispersions, over their crystalline (API) counterparts, has been discussed in several landmark works dating back at least two decades. Against this backdrop, an assessment of the current state-of-the-art for rigorously, yet simply (circumventing computational methods), determining the amorphous:crystalline solubility ratio based on thermo-analytica...
Source: International Journal of Pharmaceutics - July 5, 2019 Category: Drugs & Pharmacology Source Type: research

Kinetic stability studies of HBV vaccine in a microneedle patch
This study systematically demonstrated the antigenicity kinetics of HBV vaccine microneedles (MNs) during the fabrication, application and storage. To improve the stability of HBsAg in a microneedle patch, several selected saccharides were added to the MN formulations as stabilizers. According to the experimental data, no significant decrease of the bio-activity of HBsAg antigen was found during the microneedle fabrication process. And then immune effects of HBsAg added with different sugars were tested. Chitosan and trehalose loaded HBsAg MNs enhanced the antibody levels to approximately 1.5-fold and 2-fold of the plain H...
Source: International Journal of Pharmaceutics - July 5, 2019 Category: Drugs & Pharmacology Source Type: research

Learning from Parkinson’s patients: Usability of the Cyclops dry powder inhaler
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): M. Luinstra, V. Isufi, L. de Jong, A.W.F. Rutgers, P. Hagedoorn, J. Puttenstein, T. van Laar, H.W. FrijlinkAbstractEffective inhaler therapy requires correct handling of the inhaler, including being able to prepare the inhaler for use. Motor function impairment and cognitive disabilities, may impose problems on patients with Parkinson’s disease when they have to prepare medication, such as inhalers, for use. The aim of the present study was to examine whether Parkinson’s patients are able to correctly prepare th...
Source: International Journal of Pharmaceutics - July 5, 2019 Category: Drugs & Pharmacology Source Type: research

The role of chitosan as coating material for nanostructured lipid carriers for skin delivery of fucoxanthin
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Leticia Malgarim Cordenonsi, Angela Faccendini, Michele Catanzaro, Maria Cristina Bonferoni, Silvia Rossi, Lorenzo Malavasi, Renata Platcheck Raffin, Elfrides Eva Scherman Schapoval, Cristina Lanni, Giuseppina Sandri, Franca FerrariAbstractFucoxanthin (FUCO) is a marine carotenoid characterized by antiproliferative properties against hyperproliferative cells. The aim of this work was to design and develop nanostructured lipidic carriers (NLCs) based on bacuri butter and tucumã oil and loaded with FUCO, intended for s...
Source: International Journal of Pharmaceutics - July 4, 2019 Category: Drugs & Pharmacology Source Type: research

Spatio-temporal control on the delivery of triamcinolone acetonide using polymeric nanoparticles reduces steroid induced cataract
In this study, we aimed to reduce the bioavailability of topically administered corticosteroid, triamcinolone acetonide (TA) in lens via controlled spatial distribution in order to minimize TA induced posterior subcapsular cataract (PSC). For this, a negatively charged polymeric core-shell nanoparticulate drug delivery system composed of polycaprolactone (PCL) core and pluronic® F-68 (PF68) shell was fabricated. For in vivo studies, coumarin-6 (COU) loaded nanoparticles (NPs) were fabricated and studied for their biodistribution after topical administration in mice eyes and compared with free COU biodistribution. The a...
Source: International Journal of Pharmaceutics - July 4, 2019 Category: Drugs & Pharmacology Source Type: research

Fabrication of redox-responsive Bi(mPEG-PLGA)-Se2 micelles for doxorubicin delivery
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Yihenew Simegniew Birhan, Balkew Zewge Hailemeskel, Tefera Worku Mekonnen, Endiries Yibru Hanurry, Haile Fentahun Darge, Abegaz Tizazu Andrgie, Hsiao-Ying Chou, Juin-Yih Lai, Ging-Ho Hsiue, Hsieh-Chih TsaiAbstractStimuli-responsive polymeric nanostructures have emerged as potential drug carriers for cancer therapy. Herein, we synthesized redox-responsive diselenide bond containing amphiphilic polymer, Bi(mPEG-PLGA)-Se2 from mPEG-PLGA and 3,3′-diselanediyldipropanoic acid (DSeDPA) using DCC/DMAP as coupling agents. Due...
Source: International Journal of Pharmaceutics - July 4, 2019 Category: Drugs & Pharmacology Source Type: research

Cell cytotoxicity, immunostimulatory and antitumor effects of lipid content of liposomal delivery platforms in cancer immunotherapies. A comprehensive in-vivo and in-vitro study
Publication date: Available online 2 July 2019Source: International Journal of PharmaceuticsAuthor(s): Amin Reza Nikpoor, Mahmoud Reza Jaafari, Parvin Zamani, Manouchehr Teymouri, Hamed Gouklani, Ehsan Saburi, Shahrzad Amiri Darban, Ali Badiee, Ali Bahramifar, Mahdi Fasihi-Ramandi, Ramezan Ali TaheriAbstractLiposome is one of the promising technologies for antigen delivery in cancer immunotherapies. It seems that the phospholipid content of liposomes can act as immunostimulatory molecules in cancer immunotherapy. In the present study, the immunological properties of different phospholipid content of liposomal antigen deliv...
Source: International Journal of Pharmaceutics - July 2, 2019 Category: Drugs & Pharmacology Source Type: research

Microstructural characterization of carrier-based dry powder inhalation excipients: Insights and guidance
Publication date: Available online 28 June 2019Source: International Journal of PharmaceuticsAuthor(s): Mustafa M.A. ElsayedAbstractThe growing interest in development of dry powder inhalation (DPI) products raises a need for development of standard testing methods and specifications for DPI excipients. The pharmaceutical industry meanwhile yet lacks compendial guidance on this topic. Despite of the complexity of interactions taking place in DPI systems and the large number and variety of interplaying factors, understanding of key determinants of performance (critical quality attributes) of DPI excipients have considerably...
Source: International Journal of Pharmaceutics - July 1, 2019 Category: Drugs & Pharmacology Source Type: research

Development of microparticles for controlled release of resveratrol to adipose tissue and the impact of drug loading on particle morphology and drug release
In this study, resveratrol was encapsulated into poly(lactide-co-glycolide) microparticles using an oil-in-water emulsion/solvent evaporation technique. The oil phase consisted of resveratrol and poly(lactide-co-glycolide) dissolved in a mixture of dichloromethane and ethanol; meanwhile, the aqueous phase contained poly(vinyl alcohol) as the emulsifier. Increasing ethanol’s volume ratio increased resveratrol’s solubility in the oil phase and particle drug loading. The maximal loading achieved was 65 µg/mg (6.5 %) and occurred when the ethanol to dichloromethane ratio was 1:3. Under these conditions, parti...
Source: International Journal of Pharmaceutics - July 1, 2019 Category: Drugs & Pharmacology Source Type: research

Understanding the Motion of Hard-shell Capsules in Dry Powder Inhalers
Publication date: Available online 28 June 2019Source: International Journal of PharmaceuticsAuthor(s): Benedict Benque, Johannes G. KhinastAbstractThe delivery of small drug particles from a dry powder inhaler (DPI) into the patient’s peripheral airways requires the dispersion of the powder. In DPIs that contain a rotating pierced capsule, the capsule’s motion is paramount to powder dispersion. Previous studies have simplified the capsule motion in an Aerolizer® inhaler as a constant rotation around a fixed center. The present work examines deviations from this simplified motion and describes the capsule c...
Source: International Journal of Pharmaceutics - June 29, 2019 Category: Drugs & Pharmacology Source Type: research

Preclinical safety of topically administered nanostructure lipid carriers (NLC) for wound healing application: biodistribution and toxicity studies
Publication date: Available online 28 June 2019Source: International Journal of PharmaceuticsAuthor(s): C. Vairo, M. Collantes, G. Quincoces, S. Villullas, I. Peñuelas, M. Pastor, A.G. Gil, E. Gainza, R.M. Hernandez, M. Igartua, G. GainzaAbstractRe-activation of the healing process is a major challenge in the field of chronic wound treatment. For that purpose, lipid-nanoparticles, especially nanostructured lipid carriers (NLC), possess extremely useful characteristics such as biodegradability, biocompatibility and long-term stability, besides being suitable for drug delivery. Moreover, they maintain wound moisture d...
Source: International Journal of Pharmaceutics - June 29, 2019 Category: Drugs & Pharmacology Source Type: research

Improving Glioblastoma Therapeutic Outcomes via Doxorubicin-Loaded Nanomicelles Modified with Borneol
In conclusion, DOX BO-PMs can improve the glioblastoma therapeutic outcomes and become a promising nanodrug candidate for the application of doxorubicin in the field of glioblastoma therapy.Graphical abstractBorneol (BO) was firstly conjugated with DSPE-PEG2000-COOH to synthesize a novel carrier DSPE-PEG2000-BO to enhance the delivery of doxorubicin (DOX) into brain for glioblastoma therapy. BO-modified nanomicelles loading doxorubicin (DOX BO-PMs) were prepared using DSPE-PEG2000-BO and investigated thoroughly. DOX BO-PMs significantly enhanced the transport efficiency of DOX across blood-brain barrier (BBB) and also show...
Source: International Journal of Pharmaceutics - June 29, 2019 Category: Drugs & Pharmacology Source Type: research

Hair removal and bioavailability of chemicals: Effect of physicochemical properties of drugs and surfactants on skin permeation ex vivo
Publication date: Available online 27 June 2019Source: International Journal of PharmaceuticsAuthor(s): Astrid Pany, Victoria Klang, Caroline Peinhopf, Angela Zecevic, Johanna Ruthofer, Claudia ValentaAbstractCosmetic hair removal procedures are everyday routines in our society. However, it is unclear if such routines lead to increased uptake of applied substances such as drugs or formulation compounds, potentially resulting in skin irritation or sensitization. The aim of this study was to elucidate the effect of common depilation and epilation methods on skin penetration of two surfactants and four model drugs of differen...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Corrigendum to ‘A surfactant-like chemotherapeutic agent as a nanocarrier for delivering photosensitizers against cancer: A facile drug-delivering-drug strategy’ [Int. J. Pharm. 562 (2019) 313–320]
Publication date: Available online 27 June 2019Source: International Journal of PharmaceuticsAuthor(s): Zhaomeng Wang, Mengchi Sun, Tian Liu, Xiao Tan, Haotian Zhang, Xiangyu Zhang, Zhonggui He, Jin Sun (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Qualitative and quantitative analysis of the uptake of lipoplexes by villous placenta explants
This study reports a method to visualize and quantify the uptake of liposomal formulations in placental tissue using florescent labelling and appropriate analytical tools. Lipoplexes were labelled with a fluorescent lipid, DOPE-NBD while the encapsulated siRNA was fluorescently labelled with rhodamine. Lipoplexes were incubated with villous placenta explants, explants were imaged with confocal microscopy, then DOPE-NBD was extracted from the explant and quantified by HPLC. Qualitative evaluation by confocal microscopy showed the presence of lipoplexes and siRNA into the outer layer of the placental explants, the syncytiotr...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Biomimetic PCL-Gelatin Based Nanofibers Loaded with Ciprofloxacin Hydrochloride and Quercetin: A Potential Antibacterial and Anti-oxidant Dressing Material for Accelerated Healing of a Full Thickness Wound
Publication date: Available online 28 June 2019Source: International Journal of PharmaceuticsAuthor(s): Gufran Ajmal, Gunjan Vasant Bonde, Pooja Mittal, Gayasuddin Khan, Vivek Kumar Pandey, Bharati V. Bakade, Brahmeshwar MishraAbstractAn open wound is highly susceptible to microbial infection leading to elevated level of inflammatory response. For prompt healing, a wound requires a biomimetic dressing material with ideal hydrophilicity and tensile strength, possessing antimicrobial and antioxidant property. Although PCL-based nanofibers have sufficient tensile strength and biocompatibility, it lacks in terms of optimum hyd...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Ensuring Tablet Quality via Model-based Control of a Continuous Direct Compaction Process
Publication date: Available online 28 June 2019Source: International Journal of PharmaceuticsAuthor(s): Martin Kirchengast, Selma Celikovic, Jakob Rehrl, Stephan Sacher, Julia Kruisz, Johannes Khinast, Martin HornAbstractSwitching from batch to continuous pharmaceutical production offers several advantages, such as an increased productivity, a steady product quality, and decreased costs. This paper presents a control strategy for direct compaction on a continuous tablet production line consisting of two feeders, one blender, and a tablet press (TP). A data-driven, linear modeling approach is applied in order to develop a S...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Direct powder extrusion 3D printing: Fabrication of drug products using a novel single-step process
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): Alvaro Goyanes, Nour Allahham, Sarah J. Trenfield, Edmont Stoyanov, Simon Gaisford, Abdul W. BasitAbstractThree-dimensional (3D) printing is revolutionising how we envision manufacturing in the pharmaceutical field. Here, we report for the first time the use of direct powder extrusion 3D printing: a novel single-step printing process for the production of printlets (3D printed tablets) directly from powdered materials. This new 3D printing technology was used to prepare amorphous solid dispersions of itraconazole using four...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Polymorphism versus devitrification mechanism: Low-wavenumber Raman investigations in sulindac
This study has shown the enantiotropic relationship between Forms I and IV and that both the temperature of crystallization and the physical stability of Form I prepared is dependent on the technique used for preparing amorphous sulindac.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Treatment for chemical burning using liquid crystalline nanoparticles as an ophthalmic delivery system for pirfenidone
Publication date: Available online 26 June 2019Source: International Journal of PharmaceuticsAuthor(s): Rummenigge Oliveira Silva, Bruna Lopes da Costa, Flavia Rodrigues da Silva, Carolina Nunes da Silva, Mayara Brandão de Paiva, Lays Fernanda Nunes Dourado, Ângelo Malachias, Adriano Antunes de Souza Araújo, Paula Santos Nunes, Armando da Silva-CunhaAbstractSome recent studies have shown that pirfenidone (PFD) has favorable results in the healing process of the cornea. However, PFD in solution exhibits short half-life after topical application, and in this context, a liquid crystal nanoparticle system c...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

BIND, a novel analytical approach for monitoring powder adhesion at the die wall with use of the surface replication method
Publication date: Available online 27 June 2019Source: International Journal of PharmaceuticsAuthor(s): Shinichi Saito, Takashi Osamura, Hiroaki Kikuoka, Tadatsugu Tanino, Satomi OnoueAbstractTableting failure due to binding is often caused by powder adhesion to the die wall. The present study was undertaken to develop a novel approach for analyzing the binding characteristics of various formulations and manufacturing methods, named “Binding Identification for Net Detriment” (BIND). Binding characteristics with raloxifene hydrochloride as a model preparation were evaluated by visual observation, ejection force ...
Source: International Journal of Pharmaceutics - June 28, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of Drying Method and Excipient on Structure and Stability of Protein Solids Using Solid-State Hydrogen/Deuterium Exchange Mass Spectrometry (ssHDX-MS)
Publication date: Available online 25 June 2019Source: International Journal of PharmaceuticsAuthor(s): Nathan E. Wilson, Elizabeth M. Topp, Qi Tony ZhouAbstractPowders containing one of four model proteins (myoglobin, bovine serum albumin, lysozyme, β-lactoglobulin) were formulated with either sucrose, trehalose, or mannitol and dried using lyophilization or spray-drying. The powders were characterized using solid-state Fourier transform infrared spectroscopy (ssFTIR), solid-state fluorescence spectroscopy, differential scanning calorimetry (DSC) and solid-state hydrogen/deuterium exchange mass spectrometry (ssHDX-MS...
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Efficacy of ketoconazole gel-flakes in treatment of vaginal candidiasis: Formulation, in vitro and clinical evaluation
In conclusion, flakes in situ gel could be considered as a highly promising KTZ delivery option for treatment of vaginal candidiasis.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Direct powder extrusion 3D printing: fabrication of drug products using a novel, single-step process
Publication date: Available online 25 June 2019Source: International Journal of PharmaceuticsAuthor(s): Alvaro Goyanes, Nour Allahham, Sarah J. Trenfield, Edmont Stoyanov, Simon Gasiford, Abdul W. BasitAbstractThree-dimensional (3D) printing is revolutionising how we envision manufacturing in the pharmaceutical field. Here, we report for the first time the use of Direct Powder Extrusion 3D printing: a novel, single-step printing process for the production of printlets (3D printed tablets) directly from powdered materials. This new 3D printing technology was used to prepare amorphous solid dispersions of itraconazole using ...
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Influence of the unloading conditions on capping and lamination: study on a compaction simulator
Publication date: Available online 25 June 2019Source: International Journal of PharmaceuticsAuthor(s): Vincent Mazel, Léo Desbois, Pierre TchoreloffAbstractCapping and lamination are classical industrial issues that can be challenging during the scale up of solid dosage forms. Previous publications showed that changing the unloading conditions (triaxial decompression, loaded ejection) made it possible to mitigate capping. In the present study, a systematic study of the effect of the unloading conditions on capping and lamination was performed using a compaction simulator.One model formulation for capping and one fo...
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Data fusion strategies for performance improvement of a Process Analytical Technology platform consisting of four instruments: An electrospinning case study
Publication date: Available online 26 June 2019Source: International Journal of PharmaceuticsAuthor(s): Tibor Casian, Attila Farkas, Kinga Ilyés, Balázs Démuth, Enikő Borbás, Lajos Madarász, Zsolt Rapi, Balázs Farkas, Attila Balogh, András Domokos, György Marosi, Ioan Tomută, Zsombor Kristóf NagyAbstractThe aim of this work was to develop a PAT platform consisting of four complementary instruments for the characterization of electrospun amorphous solid dispersions with meloxicam. The investigated methods, namely NIR spectroscopy, Raman spectroscopy, Colorimetry...
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 20 July 2019Source: International Journal of Pharmaceutics, Volume 566Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 26, 2019 Category: Drugs & Pharmacology Source Type: research

Microfibrillar Polymeric Ocular Inserts for Triamcinolone Acetonide Delivery
In this study, a well-known aliphatic polyester, poly(1,4-butylene succinate) (PBS), was used as starting material to produce hydrophobic microfibrillar scaffolds by means of electrospinning technique. Plasma-assisted chemical surface functionalization of the PBS scaffolds with appropriate biopolymers (inulin, α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide, heparin) was carried out to confer to the final ocular inserts ad hoc properties as wettability, mucoadhesion and cytocompatibility on human corneal epithelial cells, by improving surface hydrophilicity without modifying the bulk properties of the material. The l...
Source: International Journal of Pharmaceutics - June 25, 2019 Category: Drugs & Pharmacology Source Type: research

Phagocytosis of spherical and ellipsoidal micronetwork colloids from crosslinked poly(ε-caprolactone)
Publication date: Available online 24 June 2019Source: International Journal of PharmaceuticsAuthor(s): Fabian Friess, Toralf Roch, Barbara Seifert, Andreas Lendlein, Christian WischkeAbstractThe effect of non-spherical particle shapes on cellular uptake has been reported as a general design parameter to control cellular recognition of particulate drug carriers. Beside shape, also size and cell-particle ratio should mutually effect phagocytosis. Here, the capability to control cellular uptake of poly(ɛ-caprolactone) (PCL) based polymer micronetwork colloids (MNC), a carrier system that can be transferred to various shapes...
Source: International Journal of Pharmaceutics - June 25, 2019 Category: Drugs & Pharmacology Source Type: research

Blend of cellulose ester and enteric polymers for delayed and enteric coating of core tablets of hydrophilic and hydrophobic drugs
In conclusion, core tablets can be coated with cellulose ester and enteric polymers blend to impart both delayed and enteric release feature to the tablets containing hydrophilic or hydrophobic drug.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 25, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization of composition and obtainment parameters of biocompatible nanoemulsions intended for intraductal administration of piplartine (piperlongumine) and mammary tissue targeting
Publication date: Available online 24 June 2019Source: International Journal of PharmaceuticsAuthor(s): Vanessa F.M. Carvalho, Giovanna C. Salata, Jenyffer K.R. de Matos, Sandra Costa-Fernandez, Marlus Chorilli, Alexandre A. Steiner, Gabriel L.B. de Araujo, Edilberto R. Silveira, Leticia V. Costa-Lotufo, Luciana B. LopesAbstractAs a new strategy for treatment of ductal carcinoma in situ, biocompatible and bioadhesive nanoemulsions for intraductal administration of the cytotoxic agent piplartine (piperlongumine) were optimized in this study. To confer bioadhesive properties, the nanoemulsion was modified with chitosan or hy...
Source: International Journal of Pharmaceutics - June 25, 2019 Category: Drugs & Pharmacology Source Type: research

Transscleral sustained ranibizumab delivery using an episcleral implantable device: Suppression of laser-induced choroidal neovascularization in rats
In conclusion, the PEGDM/COL sheet device suppressed CNV via a transscleral administration route for 18 weeks, indicating that prolonged sustained ranibizumab release could reduce the burden of repeated intravitreal injections.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 25, 2019 Category: Drugs & Pharmacology Source Type: research