Characterization of mannitol granules and powder: A comparative study using two flowability testers
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Yoshiko Takeuchi, Tomoka Tomita, Junko Kuroda, Akihiro Kageyu, Chihiro Yonekura, Yukiyoshi Hiramura, Kohei Tahara, Hirofumi Takeuchi In the manufacture of tablets, especially in direct tableting processes, the flowability of excipient powders and formulated powders is one of the most important characteristics. In the past two decades, orally disintegrating tablets (ODTs) have been prepared as popular solid dosage forms for elderly patients. Many types of mannitol granules have been developed and marketed...
Source: International Journal of Pharmaceutics - June 1, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo evaluation of an oral sustained release hepatoprotective caffeine loaded w/o Pickering emulsion formula – Containing wheat germ oil and stabilized by magnesium oxide nanoparticles
The objective of this study was to innovate an effective oral sustained release hepatoprotective formula for – the water soluble drug – caffeine. Caffeine is rapidly absorbed and eliminated which dictates frequent administration to achieve adequate therapeutic effect. A w/o Pickering emulsion incorporating caffeine in the internal phase was primed. It contained wheat germ oil and was stabilized by synthesized magnesium oxide nanoparticles (MgO NPs). Components selection was based on their antioxidant, hepatoprotective and anticarcinogenic effects. The MgO NPs were prepared via sol-gel method, and then were char...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin-grafted poly(anhydride) nanoparticles for oral glibenclamide administration. In vivo evaluation using C. elegans
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): David Lucio, María Cristina Martínez-Ohárriz, Zhongwei Gu, Yiyan He, Paula Aranaz, José Luis Vizmanos, Juan M. Irache The aim of this work was to prepare and evaluate cyclodextrins-modified poly(anhydride) nanoparticles to enhance the oral administration of glibenclamide. A conjugate polymer was synthesized by incorporating hydroxypropyl-β-cyclodextrin to the backbone of poly(methylvinyl ether-co-maleic anhydride) via Steglich reaction. The degree of substitution of anhyd...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

A novel fusion protein attenuates collagen –induced arthritis by targeting interleukin 17A and tumor necrosis factor α
This study was undertaken to generate a novel dual targeting fusion protein (DTF), targeting tumor necrosis factor α (TNF-α) and interleukin 17A (IL-17A), and determine its anti-arthritis properties in vitro and in vivo. DTF consisted of an anti-IL-17A single chain variable fragment, a soluble TNF receptor 1, and an Fc fragment. Both clinical and histopathological evaluations suggest that DTF and etanercept can ameliorate collagen induced arthritis. However, the arthritis severity score of DTF-treated mice was lower than that of etanercept-treated mice. In addition, DTF was more potent than etanercept in decrea...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of high pressure homogenization and stirred bead milling for the production of nano-crystalline suspensions
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Mostafa Nakach, Jean-René Authelin, Marc-Antoine Perrin, Harivardhan Reddy Lakkireddy Currently, the two technologies primarily used for the manufacturing of nano-crystalline suspensions using top down process (i.e. wet milling) are high pressure homogenization (HPH) and stirred bead milling (SBM). These two technologies are based upon different mechanisms, i.e., cavitation forces for HPH and shear forces for stirred bead milling. In this article, the HPH and SBM technologies are compared in terms...
Source: International Journal of Pharmaceutics - May 28, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced cellular uptake and osteogenic differentiation efficiency of melatonin by inclusion complexation with 2-hydroxypropyl β-cyclodextrin
In this study, an inclusion complex of MLT with 2-hydroxypropyl β-cyclodextrin (HP-β-CD) was prepared to improve the water solubility, and the osteogenic differentiation ability of the inclusion complex was investigated in MC3T3-E1 cells. The formation of HP-β-CD/MLT inclusion complex was confirmed by 1H and 13C nuclear magnetic resonance spectroscopy and wide-angle X-ray diffraction. The water solubility of MLT increased linearly upon addition of HP-β-CD because of the formation of the inclusion complex. Additionally, treatment of the cells with HP-β-CD/MLT inclusion complex showed higher uptake a...
Source: International Journal of Pharmaceutics - May 27, 2018 Category: Drugs & Pharmacology Source Type: research

Combined effects of the drug distribution and mucus diffusion properties of self-microemulsifying drug delivery systems on the oral absorption of fenofibrate
We present the absorption improvement mechanism of fenofibrate (FFB), a Biopharmaceutics Classification System (BCS) class II drug, from self-microemulsifying drug delivery systems (SMEDDS), centered on improving the diffusion of FFB through the unstirred water layer (UWL). Four SMEDDS formulations containing Labrafac™ lipophile WL 1349 (WL1349) or Labrafil® M 1944CS (M1944) oils and NIKKOL HCO-40 (HCO40) or NIKKOL HCO-60 (HCO60) surfactants were prepared. Every SMEDDS formulation formed microemulsion droplets of approximately 30 nm. In vitro tests showed that the microemulsion droplets containing M1944 had rel...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Improved delivery of PLGA microparticles and microparticle-cell scaffolds in clinical needle gauges using modified viscosity formulations
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Omar Qutachi, Emma J. Wright, Gemma Bray, Omar A. Hamid, Felicity R.A.J. Rose, Kevin M. Shakesheff, Derfogail Delcassian Polymer microparticles are widely used as acellular drug delivery platforms in regenerative medicine, and have emerging potential as cellular scaffolds for therapeutic cell delivery. In the clinic, PLGA microparticles are typically administered intramuscularly or subcutaneously, with the clinician and clinical application site determining the precise needle gauge used for delivery. Here,...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

The rheological and textural characterization of Soluplus ®/Vitamin E composites
In this study, Soluplus® was dissolved under heat in vitamin E at increasing concentrations from 0 to 40% (by weight). The flow behavior of the Soluplus®/Vitamin E composites was determined by applying shear stress using an advanced AR2000 rheometer. Under the linear viscoelastic region (LVR), the rheological properties of the blends such as dynamic viscosity (η′), storage modulus (G′), loss modulus (G″), and the phase angle tangent (tan δ) were measured. Hardness, adhesiveness, and cohesiveness of the blends were also measured with a TA.XT plus texture analyzer. Rheological analysis sho...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Model-based NIR spectroscopy implementation for in-line assay monitoring during a pharmaceutical suspension manufacturing process
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Maxim Verstraeten, Daan Van Hauwermeiren, Mario Hellings, Eline Hermans, Jeroen Geens, Chris Vervaet, Ingmar Nopens, Thomas De Beer The implementation of Process Analytical Technology (PAT) instruments is generally achieved stochastically. Sub-optimal PAT locations could introduce variation in the measurements which is not related to the analyte of interest. For this reason, rational approaches should be considered to establish an optimal sensor placement where relevant measurements are possible and the im...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

The effect of the composition of a fixed dose combination on bioequivalence results
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Jana Šalandová, Aleš Franc, Jiří Hofmann, Aleksandra Dumicic, Lenka Kukačková, Tereza Červená, Josef Beránek, Jan Srbek, Andrej Repický, Beata Vladovičová, David Vetchý The purpose of this work was to develop a new supergeneric product Meloxicam/Omeprazole. Such a combination brings a benefit in terms of decreasing side effects for the patients using meloxicam. The new combination is composed of a meloxicam powder blend (MPB) and ome...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of excipient properties, water activity, and water content on the disproportionation of a pharmaceutical salt
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Mitulkumar A. Patel, Suman Luthra, Sheri L. Shamblin, Kapildev K. Arora, Joseph F. Krzyzaniak, Lynne S. Taylor Excipients are crucial components of most pharmaceutical formulations. In the case of a solid oral dosage formulation containing the salt form of a weakly ionizable drug, excipient selection is critical, as some excipients are known to cause salt disproportionation (conversion of salt to the free form). Therefore, robust formulation design necessitates an in-depth understanding of the factors impa...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Toward smart Nebulization: Engineering acoustic airflow to penetrate maxillary sinuses in chronic rhinosinusitis
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Shima Jowhari Moghadam, Laurent Navarro, Lara Leclerc, Sophie Hodin, Jérémie Pourchez Treating chronic rhinosinusitis (CRS) by nebulization requires an airflow capable to deliver medication to deep target sites beyond the nasal valve. Fixed frequency acoustic airflow technology is currently available, mainly as post-surgical therapy, but still have not been able to realize the full potential of direct nose to paranasal sinuses delivery. Reported herein are the application of frequency sweep a...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Continuous inkjet printing of enalapril maleate onto orodispersible film formulations
In conclusion, it was feasible to print EM doses onto drug-free and HCT ODFs during an in-line continuous manufacturing process. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Lycopene loaded whey protein isolate nanoparticles: An innovative endeavor for enhanced bioavailability of lycopene and anti-cancer activity
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Ashay Jain, Gajanand Sharma, Gargi Ghoshal, Prashant Kesharwani, Bhupinder Singh, U.S. Shivhare, O.P. Katare The work entails a novel strategy of formulating the lycopene loaded whey protein isolate nanoparticles (LYC-WPI-NPs) solely using the rational blend of biomacromolecule without using equipment-intensive techniques. The LYC-WPI-NPs were fabricated as a substantial drug delivery platform, with maximum entrapment, spatial and controlled release manners, exceptional plasma concentration, and perspectiv...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

In-line agglomeration degree estimation in fluidized bed pellet coating processes using visual imaging
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Andraž Mehle, Domen Kitak, Gregor Podrekar, Boštjan Likar, Dejan Tomaževič Agglomeration of pellets in fluidized bed coating processes is an undesirable phenomenon that affects the yield and quality of the product. In scope of PAT guidance, we present a system that utilizes visual imaging for in-line monitoring of the agglomeration degree. Seven pilot-scale Wurster coating processes were executed under various process conditions, providing a wide spectrum of process outcomes. Images of pellets we...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

New perspectives of starch: Synthesis and in vitro assessment of novel thiolated mucoadhesive derivatives
Conclusion In terms of these results, thiolated starch is a new, promising, polymer in the field of mucoadhesive drug delivery systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Novel excipients – Regulatory challenges and perspectives – The EU insight
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Piotr Kozarewicz, Thorsteinn Loftsson Novel excipients are indispensable in development of modern, advanced drug delivery systems and biotechnology-derived drugs. Although numerous novel excipients are developed for pharmaceutical use, they are not frequently seen in medicinal products due to the strict regulatory requirements and perception that their use makes new product evaluation more complex with risk of delays in the approval process. Regulators regard novel excipients as new substances and whenever...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Poly (amidoamine) (PAMAM) dendrimer mediated delivery of drug and pDNA/siRNA for cancer therapy
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Jun Li, Huamin Liang, Jing Liu, Ziyuan Wang Poly (amidoamine) (PAMAM) dendrimers are well-defined, highly branched macromolecules with numerous active amine groups on the surface. Because of their unique properties, PAMAM dendrimers have steadily grown in popularity in drug delivery, gene therapy, medical imaging and diagnostic application. This review focuses on the recent developments on the application in PAMAM dendrimers as effective carriers for drug and gene (pDNA, siRNA) delivery in cancer therapy, ...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Nano spray drying for encapsulation of pharmaceuticals
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Cordin Arpagaus, Andreas Collenberg, David Rütti, Elham Assadpour, Seid Mahdi Jafari Many pharmaceuticals such as pills, capsules, or tablets are prepared in a dried and powdered form. In this field, spray drying plays a critical role to convert liquid pharmaceutical formulations into powders. In addition, in many cases it is necessary to encapsulate bioactive drugs into wall materials to protect them against harsh process and environmental conditions, as well as to deliver the drug to the right place...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

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

Nanoparticle-based delivery of carbamazepine: A promising approach for the treatment of refractory epilepsy
This study investigates the effect of the Pgp inhibitor verapamil on the anticonvulsant effect of CBZ and its nanoparticulate formulation in the rat model of isoniazid-induced epilepsy. Verapamil significantly increased the anticonvulsant effect of CBZ and reduced its effective dose by at least 30% (from 30 mg/kg to 20 mg/kg). Binding of carbamazepine to the poloxamer 188-coated PLGA nanoparticles enabled a 30-fold increase of its anticonvulsive effect, as compared to the free drug. The inhibition of Pgp did not influence the effectivity of carbamazepine encapsulated in nanoparticles. Graphical abstract (Source: Intern...
Source: International Journal of Pharmaceutics - May 25, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoemulsion containing 8-methoxypsoralen for topical treatment of dermatoses: Development, characterization and ex vivo permeation in porcine skin
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Catarina Amorim Oliveira, Marcos Martins Gouvêa, Gabriel Ramos Antunes, Zaida Maria Faria de Freitas, Flávia Ferreira de Carvalho Marques, Eduardo Ricci-Junior Oral therapy with 8-methoxypsoralen (8-MOP) may cause major side effects, whereas the topical treatment might not be much effective due to the low penetration induced by typical formulations. Therefore, the objectives of this work are the development and characterization of a nanoemulsion (NE) containing 8-MOP together with an ex vivo...
Source: International Journal of Pharmaceutics - May 25, 2018 Category: Drugs & Pharmacology Source Type: research

Gel in core carbosomes as novel ophthalmic vehicles with enhanced corneal permeation and residence
In conclusion, novel gel-core carbosomes could successfully be used as a promising delivery system for chronic ocular diseases. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 22, 2018 Category: Drugs & Pharmacology Source Type: research

Rapid automated process development of a continuous capsule-filling process
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Bernhard Wagner, Thomas Brinz, Stephanie Otterbach, Johannes Khinast This paper introduces a rapid automated process-development approach for a continuous capsule-filling process. In our proposed method, both the material attributes and the critical process parameters were varied to understand and to optimize the overall process. Using our approach a statistical process model can be generated with unprecedented speed (2 days), which is the prerequisite for effectively developing and operating continuous ...
Source: International Journal of Pharmaceutics - May 21, 2018 Category: Drugs & Pharmacology Source Type: research

Photocurable poly(ethylene glycol) as a bioink for the inkjet 3D pharming of hydrophobic drugs
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Giovanny F. Acosta-Vélez, Timothy Z. Zhu, Chase S. Linsley, Benjamin M. Wu Binder jetting and material extrusion are the two most common additive manufacturing techniques used to create pharmaceutical tablets. However, their versatility is limited since the powder component is present throughout the dosage forms fabricated by binder jet 3D printing and material extrusion 3D printing requires high operating temperatures. Conversely, material jetting allows for compositional control at a voxel level a...
Source: International Journal of Pharmaceutics - May 19, 2018 Category: Drugs & Pharmacology Source Type: research

New prediction methods for solubility parameters based on molecular sigma profiles using pharmaceutical materials
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Andreas Niederquell, Nicole Wyttenbach, Martin Kuentz Solubility parameters have been applied extensively in the chemical and pharmaceutical sciences. Particularly attractive is calculation of solubility parameters based on chemical structure and recently, new in silico methods have been proposed. Thus, screening charge densities of molecular surfaces (i.e. so-called σ-profiles) are used by the conductor-like screening model for real solvents (COSMO-RS) and can be employed in a quantitative structure...
Source: International Journal of Pharmaceutics - May 19, 2018 Category: Drugs & Pharmacology Source Type: research

Surface engineered excipients: II. Simultaneous milling and dry coating for preparation of fine-grade microcrystalline cellulose with enhanced properties
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Liang Chen, Xiaoyi Ding, Zizhou He, Siqi Fan, Kuriakose T. Kunnath, Kai Zheng, Rajesh N. Davé A solventless process for simultaneously milling and dry coating microcrystalline cellulose (MCC) was investigated for producing fine excipients in five different sizes (∼20, 25, 30, 35, 40 µm) having high bulk density (BD), good flow function coefficient (FFC), and excellent compaction. Avicel PH-102, used as the starting material, was milled and coated with two grades of silicas, hydrophobic a...
Source: International Journal of Pharmaceutics - May 18, 2018 Category: Drugs & Pharmacology Source Type: research

Efficient siRNA transfer to knockdown a placenta specific lncRNA using RGD-modified nano-liposome: A new preeclampsia-like mouse model
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Qianwen Yu, Yue Qiu, Xuhui Wang, Jiajing Tang, Yayuan Liu, Ling Mei, Man Li, Ming Yang, Li Tang, Huile Gao, Zhirong Zhang, Wenming Xu, Qin He Preeclampsia is one of the most serious pregnancy complications. Many animal models have already been developed by researchers to study the pathogenesis and treatment of preeclampsia. However, most of these animal models were established by systemic administration or by surgery in the uterine cavity, which could lead to unwanted systemic toxicity or operative wounds ...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Amphiphilic polyurethane hydrogels as smart carriers for acidic hydrophobic drugs
In this study, we propose a strategy of combining amphiphilic polyurethanes with pH-responsive drugs to develop smart drug carriers. While the amphiphilic character of the polymer imparts an efficient load of hydrophobic and hydrophilic drugs, the drug’s characteristics determine the selectivity of the medium delivery. Drug loading and release behavior as well as hydrolytic degradation of chemically crosslinked polyurethane hydrogels based on PEG and PCL-triol (PU (polyurethane) hydrogels) synthesized by an easy one-pot route were studied. PU hydrogels have been shown to successfully load the hydrophobic acidic drug ...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of a ureteral catheter coating by means of a BioEncrustation in vitro model
In this study we present a complex BioEncrustation model that imitates both the processes of multi-species biofilm formation and encrustation in vitro. The resulting crystalline biofilms are compared to the deposits found on explanted ureteral stent surfaces (in vivo situation) and to deposits formed in an experimental set up that does not contain bacteria (Encrustator®). Further focus of this study is dedicated to employing the developed BioEncrustation model to evaluate the effect multifunctional coatings impose on the processes of biofilm formation and encrustation under in vitro conditions. The investigated TANP co...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Therapeutic efficacy of lipid emulsions of docetaxel-linoleic acid conjugate in breast cancer
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Tao Zhang, Meng Li, Ruyi Yang, Dong Zhang, Jibin Guan, Jiang Yu, Bin Yang, Huicong Zhang, Shenwu Zhang, Dan Liu, Yongjun Wang Docetaxel (DTX) solution is among the most widely-used parenteral formulations used in advanced breast cancer therapy. However, severe side effects have been observed due to the use of ethanol and polysorbate 80. Herein, a novel DTX-based prodrug, docetaxel-linoleic acid conjugate (DTX-LA) was successfully synthesized. The high lipid solubility of DTX and DTX-LA resulted in a tenden...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Electro-responsive graphene oxide hydrogels for skin bandages: The outcome of gelatin and trypsin immobilization
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Mariagrazia di Luca, Orazio Vittorio, Giuseppe Cirillo, Manuela Curcio, Magdalena Czuban, Florida Voli, Annafranca Farfalla, Silke Hampel, Fiore Pasquale Nicoletta, Francesca Iemma A free radical polymerization method was adopted for the fabrication of hybrid hydrogel films based on acrylamide and polyethylene glycol dimethacrylate as plasticizing and crosslinking agents, respectively, to be employed as smart skin bandages. Electro-sensitivity, biocompatibility and proteolytic properties were conferred to ...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Tracking translocation of self-discriminating curcumin hybrid nanocrystals following intravenous delivery
In this study, self-discriminating hybrid nanocrystals (SDHNs) of a model drug curcumin (CUR) were developed by embedding traces of environment-responsive fluorescent dyes into the crystalline lattices of CUR. The SDHNs glow, but the released dyes aggregate and quench spontaneously due to the aggregation-caused quenching (ACQ) effect. Following intravenous administration into rats, a large fraction of CUR nanocrystals are cleared from blood rapidly and accumulate mainly in liver and lung. A small fraction circulate in blood for at least 48 h. Long circulating might be attributable to the surface coating with poloxamer 18...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization and cytotoxicity evaluation of biocompatible amino acid esters used to convert salicylic acid into ionic liquids
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Rahman Md. Moshikur, Md. Raihan Chowdhury, Rie Wakabayashi, Yoshiro Tahara, Muhammad Moniruzzaman, Masahiro Goto The technological utility of active pharmaceutical ingredients (APIs) is greatly enhanced when they are transformed into ionic liquids (ILs). API-ILs have better solubility, thermal stability, and the efficacy in topical delivery than solid or crystalline drugs. However, toxicological issue of API-ILs is the main challenge for their application in drug delivery. To address this issue, 11 amino a...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Comparative analyses of flow and compaction properties of diverse mannitol and lactose grades
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Shubhajit Paul, Shao-Yu Chang, Jiangnan Dun, Wei-Jhe Sun, Kunlin Wang, Pirjo Tajarobi, Catherine Boissier, Changquan Calvin Sun Appropriate selection of excipient grade during tablet formulation development depends on thorough knowledge in their compaction and flow properties. Each chemically unique pharmaceutical excipient is usually available in several commercial grades that are widely different in powder properties, which influence their performance for a specific formulation application. In this work,...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Sorbitan ester nanoparticles (SENS) as a novel topical ocular drug delivery system: Design, optimization, and in vitro/ex vivo evaluation
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Jesus Alvarez-Trabado, Antonio López-García, Manuel Martín-Pastor, Yolanda Diebold, Alejandro Sanchez We explored the potential of two types of sorbitan ester nanoparticles (SENS) as novel tools for topical ocular drug delivery. The optimized SENS formulation (SENS-OPT) consisted of nanoparticles (NPs) of 170.5 nm, zeta potential +33.9 mV, and cyclosporine loading of 19.66%. After hyaluronic acid (HA) coating, the resulting SENS-OPT-HA NPs had a particle size of 177.6 nm and zeta...
Source: International Journal of Pharmaceutics - May 17, 2018 Category: Drugs & Pharmacology Source Type: research

Elucidation of the orientation of selected drugs with 2-hydroxylpropyl- β-cyclodextrin using 2D-NMR spectroscopy and molecular modeling
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Saugat Adhikari, Saloni Daftardar, Filip Fratev, Miguel Rivera, Suman Sirimulla, Kenneth Alexander, Sai H.S. Boddu This project aims to study the nature of interaction and orientation of selected drugs such as dexamethorphan HBr (DXM), diphenhydramine HCl (DPH), and lidocaine HCl (LDC) inclusion complexes with hydroxyl-propyl ß-cyclodextrin (HP-ß-CD) using 1HNMR spectroscopy, 2D-NMR ROESY and molecular-modeling techniques. Freeze-drying technique was used to formulate the inclusion complexes be...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Engineering fast dissolving sodium acetate mediated crystalline solid dispersion of docetaxel
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Albert Nguessan Ngo, Danielle Thomas, James Murowchick, Navid J. Ayon, Archana Jaiswal, Bi-Botti Celestin Youan It is hypothesized that a novel crystalline solid dispersion (CSD) of docetaxel (C-DXT) can be engineered by dispersing native docetaxel (DXT, a BCS class II drug) in sodium acetate crystal (SA). DXT is dissolved in glacial acetic/SA solution and freeze-dried. The resulting C-DXT is characterized by differential scanning calorimetry (DSC), powder X-ray analysis (PXRD), LC-MS/MS, scanning electron...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of rabies pDNA nanoparticulate vaccine in poloxamer 407 gel
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Amit Bansal, Xianfu Wu, Victoria Olson, Martin J. D'Souza Plasmid DNA (pDNA) vaccines have the potential for protection against a wide range of diseases including rabies but are rapid in degradation and poor in uptake by antigen-presenting cells. To overcome the limitations, we fabricated a pDNA nanoparticulate vaccine. The negatively charged pDNA was adsorbed onto the surface of cationic PLGA (poly (d, l-lactide-co-glycolide))-chitosan nanoparticles and were used as a delivery vehicle. To create a hydroge...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of in vitro and in vivo antitumor effects of gambogic acid-loaded layer-by-layer self-assembled micelles
This study aimed to develop a novel type of multilayer micelle using protamine (PRM) and hyaluronic acid (HA) for the delivery of gambogic acid (GA). GA-loaded micelles (GA-M) were simply andrapidly prepared using lecithin/solutol HS15 using a film-dispersion method. PRM and HA were added in sequence to form layer-by-layer self-assembled micelles (HA-PRM-GA-M), in which particle size, zeta potential, particle morphology, drug loading, encapsulation efficiency, and in vitro release were investigated. Surface charge reversal demonstrated that rapid HA detachment exposed PRM, leading to activation of a “proton sponge&rd...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of nanodispersions by solvent displacement using the Venturi tube
The objective of this study was to evaluate the potential of this device for preparing NP of poly-ε-caprolactone. Response Surface Methodology was used to determine the effect of the operating conditions and optimization. The NP produced by VT were characterized by Dynamic Light-Scattering to determine their particle size distribution (PS) and polydispersity index (PDI). Results showed that the Reynolds number (Re) has a strong effect on both PS and process yield (PY).The turbulence regime is key to the efficient formation of NP. The optimal conditions for obtaining NP were a polymer concentration of 1.6 w/v, a r...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Exploring gelatin nanoparticles as novel nanocarriers for Timolol Maleate: Augmented in-vivo efficacy and safe histological profile
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Miral Shokry, Rania M. Hathout, Samar Mansour The use of gelatin has been gaining recognition in ocular delivery for its safety profile and biocompatible properties. Timolol Maleate (TM) is an anti-glaucoma drug possessing poor corneal penetration while causing eye irritation making it an ideal candidate for novel nanoparticulate systems. Timolol Maleate loaded Gelatin Nanoparticles (GNPs) were prepared using the double desolvation method utilizing glutaraldehyde as the crosslinking agent. Optimization of ...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of the lubricating effect of magnesium stearate and glyceryl behenate solid lipid nanoparticles in a direct compression process
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Lizbeth Martínez-Acevedo, María de la Luz Zambrano-Zaragoza, Gustavo Vidal-Romero, Susana Mendoza-Elvira, David Quintanar-Guerrero The aim of this study was to develop solid lipid nanoparticles (SLN) and introduce them into a direct compression process to evaluate their lubricant properties. The study consisted of preparing glyceryl behenate SLN (Compritol® 888 ATO) by hot dispersion, and magnesium stearate SLN by a novel nanoprecipitation/ion exchange method. The ejection force was measu...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of micrometric powders of parathyroid hormone (PTH1 –34)-loaded chitosan oligosaccharide by supercritical fluid assisted atomization
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Dong-Xiao Hong, Yu-Long Yun, Yi-Xin Guan, Shan-Jing Yao Parathyroid hormone (PTH1–34)-loaded dry powders were fabricated from aqueous solution for pulmonary administration using supercritical fluid assisted atomization introduced by a hydrodynamic cavitation mixer (SAA-HCM). Herein, chitosan oligosaccharide (CSO) was selected as a carrier in an effort to enhance transmucosal absorption of the drug. Well-defined, separated and spherical PTH(1–34)/CSO composite microparticles were obtained, and t...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of drug-loaded small unilamellar liposomes and evaluation of their potential for the treatment of chronic respiratory diseases
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Vincenzo De Leo, Silvia Ruscigno, Adriana Trapani, Sante Di Gioia, Francesco Milano, Delia Mandracchia, Roberto Comparelli, Stefano Castellani, Angela Agostiano, Giuseppe Trapani, Lucia Catucci, Massimo Conese The aim of the present investigation was to evaluate the influence of liposome formulation on the ability of vesicles to penetrate a pathological mucus model obtained from COPD affected patients in order to assess the potential of such vesicles for the treatment of chronic respiratory diseases by inh...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Polysaccharides-based multiparticulated interpolyelectrolyte complexes for controlled benznidazole release
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Mónica C. García, Rubén H. Manzo, Alvaro Jimenez-Kairuz Polysaccharides-based delivery systems and interpolyelectrolyte complexes (IPECs) are interesting alternatives to control the release of drugs, thereby improving therapies. Benznidazole (BZ) is the selected drug for Chagas disease pharmacotherapy. However, its side effects limit its efficacy and safety. We developed novel multiparticulated BZ-loaded IPECs based on chitosan and alginic acid, and investigated their physicochemical a...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Antibacterial and antioxidant electrospun materials from poly(3-hydroxybutyrate) and polyvinylpyrrolidone containing caffeic acid phenethyl ester – “in” and “on” strategies for enhanced solubility
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Milena Ignatova, Nevena Manolova, Iliya Rashkov, Nadya Markova Caffeic acid phenethyl ester (CAPE) possesses a set of valuable biological properties: antioxidant, antibacterial, antitumor, anti-inflammatory, antiviral, etc. However, CAPE is poorly soluble in aqueous environment which is limiting its possible therapeutic applications. In the present study novel fibrous materials enhancing CAPE solubility and accelerating CAPE release were developed. The materials were prepared from poly(3-hydroxybutyrate) (...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

Design of PEI-conjugated bio-reducible polymer for efficient gene delivery
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Joung-Pyo Nam, Soyoung Kim, Sung Wan Kim The poly(cystaminebis(acrylamide)-diaminohexane) (poly(CBA-DAH)) was designed previously as a bio-reducible efficient gene delivery carrier. However, the high weight ratio required to form the polyplexes between poly(CBA-DAH) with pDNA is still a problem that needs to be addressed. To solve this problem and increase the transfection efficiency, poly(ethylenimine) (PEI, 1.8 kDa) was conjugated to poly(CBA-DAH) via disulfide bond. The PEI conjugated poly(CBA-DAH) (P...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research

From allergen to oral vaccine carrier: A new face of ragweed pollen
Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Md Jasim Uddin, Harvinder Singh Gill Oral delivery of vaccines is highly desirable, yet it has met with limited success. Previously we developed allergen-free pollen grains as a novel approach for oral vaccination. We showed that spores of Lycopodium clavatum can be used for oral vaccination. However, it is unknown if pollens of other species can be similarly used as an oral vaccine carrier. Therefore, in this study, we evaluated common ragweed (RW) pollen (Ambrosia elatior) for its oral vaccination potent...
Source: International Journal of Pharmaceutics - May 16, 2018 Category: Drugs & Pharmacology Source Type: research