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International Journal of Pharmaceutics

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 property relationship (QSPR) to predict solubility parameters...
May 14, 2018: International Journal of Pharmaceutics
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 impacting salt disproportionation during processing or storage as this can negatively impact product quality and performance...
May 14, 2018: International Journal of Pharmaceutics
Lucas P Fonseca, Rafael B Trinca, Maria Isabel Felisberti
Amphiphilic hydrogels are widely reported as systems with great potential for controlled drug release. Nevertheless, the majority of studies make use of functionalization or attachment of drugs to the polymer chains. 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...
May 14, 2018: International Journal of Pharmaceutics
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, 40µm) 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 and hydrophilic (R972P and A200), using a fluid energy mill (FEM). Through judicious selection of the FEM feed rate, feeding pressure, and grinding pressure, five desired milled sizes were produced...
May 12, 2018: International Journal of Pharmaceutics
Yushi Sunazuka, Keisuke Ueda, Kenjirou Higashi, Yusuke Tanaka, Kunikazu Moribe
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 LabrafacTM 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...
May 12, 2018: International Journal of Pharmaceutics
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 tendency for them to become entrapped in the oil core of the emulsions. As anticipated, nano-sized, sterically stabilized oil-in-water lipid emulsions (LMs) of DTX-LA LMs and DTX LMs were successfully constructed...
May 12, 2018: International Journal of Pharmaceutics
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 the final polymer networks by introducing graphene oxide (0.5% w/w), gelatin or trypsin (10% w/w) in the polymerization feed. The physical chemical and mechanical characterization of hybrid materials was performed by means of determination of protein content, Raman spectroscopy, thermogravimetric analysis and measurement of tensile strength...
May 11, 2018: International Journal of Pharmaceutics
Max Jelkmann, Sonja Bonengel, Claudia Menzel, Svetislav Markovic, Andreas Bernkop-Schnürch
AIM: The purpose of this study was to develop a novel thiolated starch polymer with improved mucoadhesive properties by conjugation of cysteamine to starch as a natural polymer of restricted mucoadhesive properties. METHODS: Aldehyde substructures were integrated into starch via oxidative cleavage of vicinal diols by increasing amounts of sodium periodate followed by covalent attachment of cysteamine to oxidized starch via reductive amination. Thiol groups were quantified via Ellman's reaction and their impact on mucoadhesion was analyzed by rheological investigations, the rotating cylinder method and tensile studies on porcine mucosa...
May 11, 2018: International Journal of Pharmaceutics
Dahlgren David, Roos Carl, Johansson Pernilla, Tannergren Christer, Lundqvist Anders, Langguth Peter, Sjöblom Markus, Sjögren Erik, Lennernäs Hans
Pharmaceutical excipients that may affect gastrointestinal (GI) drug absorption are called critical pharmaceutical excipients (CPEs), or absorption-modifying excipients (AMEs) if they act by altering the integrity of the intestinal epithelial cell membrane. Some of these excipients increase intestinal permeability, and subsequently the absorption and bioavailability of the drug. This could have implications for both the assessment of bioequivalence and the efficacy of the absorption-enhancing drug delivery system...
May 11, 2018: International Journal of Pharmaceutics
Šalandová Jana, Franc Aleš, Hofmann Jiří, Dumicic Aleksandra, Kukačková Lenka, Červená Tereza, Beránek Josef, Srbek Jan, Repický Andrej, Vladovičová Beata, Vetchý David
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 omeprazole gastro-resistant pellets (OAP) in hard gelatin capsules. The main tasks were to select the excipients to keep the functional layer of OAP active and to prove the bioequivalence to the original products of meloxicam tablets together with omeprazole capsules...
May 11, 2018: International Journal of Pharmaceutics
Yasmin Thabet, Dominique Lunter, Joerg Breitkreutz
Piezoelectric inkjet printing onto orodispersible films (ODFs) was proven to be a successful technique applying flexible doses of active pharmaceutical ingredients (APIs) onto edible substrates. The reported API printing and ODF production was conducted in a non-continuous production approach. Within this study, drug-free and hydrochlorothiazide (HCT) containing ODFs should be imprinted in-line with enalapril maleate (EM) ink during continuous ODF production. Macrogol inks based on various solvents and solvent-water mixtures were developed providing dynamic viscosities from 7 to 17 mPa∗s...
May 10, 2018: International Journal of Pharmaceutics
Omar Qutachi, Emma J Wright, Gemma Bray, Omar A Hamid, Felicity R A J Rose, Kevin 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 precice needle gauge used for delivery. Here, we explored the role of needle diameter in microparticle delivery yield, and develop a modified viscosity formulation to improve microparticle delivery across a range of clinically relevent needle diameters...
May 10, 2018: International Journal of Pharmaceutics
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 potential of -20.6 mV. The NPs were stable during 3 months of storage at different temperatures and did not aggregate in the presence of protein-enriched simulated lacrimal fluid...
May 10, 2018: International Journal of Pharmaceutics
M Frant, E Dayyoub, U Bakowsky, K Liefeith
Biomaterials for applications in the urinary tract are challenged with both biofilm formation and encrustation, two highly interconnected processes. While great effort has been achieved developing promising materials there is only a limited choice of sophisticated in vitro models that are available to analyse the performance of biomaterials prior to performing delicate and expensive in vivo studies. In this study we present a complex BioEncrustation model that imitates both the processes of multi-species biofilm formation and encrustation in vitro...
May 9, 2018: International Journal of Pharmaceutics
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 were acquired during the coating processes in a contactless manner through an observation window of the coating apparatus...
May 9, 2018: International Journal of Pharmaceutics
Rahman Md Moshikur, Chowdhury Md Raihan, 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 acid esters (AAEs) were synthesized and investigated as biocompatible counter cations for the poorly water-soluble drug salicylic acid (Sal) to form Sal-ILs...
May 8, 2018: International Journal of Pharmaceutics
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 the particles size could be well controlled with narrow distribution. Aerodynamic performance was determined using next generation impactor (NGI), and the mass median aerodynamic diameter (MMAD) ranged strictly 1-5 μm range with fine particle fraction (FPF) up to 63...
May 8, 2018: International Journal of Pharmaceutics
Ting Wang, Jianping Qi, Ning Ding, Xiaochun Dong, Weili Zhao, Yi Lu, Changhong Wang, Wei Wu
Nanocrystals hold great potential as parenteral delivery carrier systems for poorly water-soluble drugs. Elucidation of the in vivo fate of parenteral nanocrystals is of pharmacological, toxicological and mechanistic significance. However, it is of tremendous difficulty to monitor real-time translocation of nanocrystals in vivo owing to progressive dissolution of nanocrystals and a lack of workable tools to probe nanocrystals. 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...
May 8, 2018: International Journal of Pharmaceutics
Anna Zybina, Anastasiya Anshakova, Julia Malinovskaya, Pavel Melnikov, Vladimir Baklaushev, Vladimir Chekhonin, Olga Maksimenko, Sergey Titov, Vadim Balabanyan, Jörg Kreuter, Svetlana Gelperina, Kenul Abbasova
Resistance to antiepileptic drugs (AEDs) is a major clinical problem. The overexpression of P-glycoprotein (Pgp), one of the main transporters limiting the entry of xenobiotics into the brain, is among the factors contributing to the AED resistance. Presently, there is no consensus on the interaction of carbamazepine (CBZ) with the Pgp. 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...
May 8, 2018: International Journal of Pharmaceutics
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 1 HNMR spectroscopy, 2D-NMR ROESY and molecular-modelling techniques. Freeze-drying technique was used to formulate the inclusion complexes between DXM, DPH and LDC with HP-ß-CD (1:1 molar ratio) in solid state. Inclusion complex formation was initially characterized by Fourier transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) techniques...
May 7, 2018: International Journal of Pharmaceutics
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