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2.538 Aktuelle Fachpublikationen in Molecular Pharmaceutics


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Mutual Impact of Phase Separation/Crystallization and Water Sorption in Amorphous Solid Dispersions

19.01.2018 | Christian Luebbert; Maximilian Wessner; Gabriele Sadowski, Molecular Pharmaceutics, 2018

The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ...


Design, Synthesis, and Biological Evaluation of 68Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

19.01.2018 | Fei Liu; Teli Liu; Xiaoxia Xu; Xiaoyi Guo; Nan Li; Chiyi Xiong; Chun Li; Hua Zhu; Zhi Yang, Molecular Pharmaceutics, 2018

Most of the radiolabeled somatostatin analogues (SSAs) are specific for subtype somatostatin receptor 2 (SSTR2). Lack of ligands targeting other subtypes of SSTRs, especially SSTR1, SSTR3, and SSTR5, limited their applications in tumors of low SSTR2 expression, including lung tumor. In this ...


Incorporation of mRNA in Lamellar Lipid Matrices for Parenteral Administration

18.01.2018 | Antje Ziller; Sara S. Nogueira; Eva Hühn; Sergio S. Funari; Gerald Brezesinski; Hermann Hartmann; Ugur Sahin; Heinri ..., Molecular Pharmaceutics, 2018

Insertion of high molecular weight messenger RNA (mRNA) into lyotropic lipid phases as model systems for controlled release formulations for the mRNA was investigated. Low fractions of 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) were used as an anchor to load the mRNA into a lamellar lipid ...


Engineered Cellular Uptake and Controlled Drug Delivery Using Two Dimensional Nanoparticle and Polymer for Cancer Treatment

18.01.2018 | Sudipta Senapati; Rashmi Shukla; Yamini Bhusan Tripathi; Arun Kumar Mahanta; Dipak Rana; Pralay Maiti, Molecular Pharmaceutics, 2018

Two major problems in chemotherapy, poor bioavailability of hydrophobic anticancer drug and its adverse side effects causing nausea, are taken into account by developing a sustained drug release vehicle along with enhanced bioavailability using two-dimensional layered double hydroxides (LDHs) ...


Gastric Emptying and Small Bowel Water Content after Administration of Grapefruit Juice Compared to Water and Isocaloric Solutions of Glucose and Fructose: A Four-Way Crossover MRI Pilot Study in Healthy Subjects

18.01.2018 | Michael Grimm; Mirko Koziolek; Marwa Saleh; Felix Schneider; Grzegorz Garbacz; Jens-Peter Kühn; Werner Weitschies, Molecular Pharmaceutics, 2018

Grapefruit juice (GFJ) is known to affect the bioavailability of drugs in different ways. Despite the influence on gastrointestinal enzymes and transporters, the influence on gastrointestinal fluid kinetics is regarded to be relevant for the absorption of several drugs. Thus, it was the aim of ...


Low-Density Lipoproteins and Human Serum Albumin as Carriers of Squalenoylated Drugs: Insights from Molecular Simulations

17.01.2018 | Semen O. Yesylevskyy; Christophe Ramseyer; Mariia Savenko; Simona Mura; Patrick Couvreur, Molecular Pharmaceutics, 2018

We have studied the interaction of three clinically promising squalenoylated drugs (gemcitabine-squalene, adenine-squalene, and doxorubicin-squalene) with low-density lipoproteins (LDL) by means of atomistic molecular dynamics simulations. It is shown that all studied squalenoylated drugs ...


Evaluation of the Active Targeting of Melanin Granules after Intravenous Injection of Dendronized Nanoparticles

17.01.2018 | C. Bordeianu; A. Parat; S. Piant; A. Walter; C. Zbaraszczuk-Affolter; F. Meyer; S. Begin-Colin; S. Boutry; R. N. Mul ..., Molecular Pharmaceutics, 2018

The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized ...


Millisecond Self-Assembly of Stable Nanodispersed Drug Formulations

17.01.2018 | Vikram J. Pansare; Aditya Rawal; Aaron Goodwin; Ron Beyerinck; Robert K. Prud’homme; Dwayne T. Friesen; Michael Gras ..., Molecular Pharmaceutics, 2018

We report the development of a new spray-drying and nanoparticle assembly process (SNAP) that enables the formation of stable, yet rapidly dissolving, sub-200 nm nanocrystalline particles within a high Tg glassy matrix. SNAP expands the class of drugs that spray-dried dispersion (SDD) processing ...


Comparison of the Expression Kinetics and Immunostimulatory Activity of Replicating mRNA, Nonreplicating mRNA, and pDNA after Intradermal Electroporation in Pigs

17.01.2018 | Bregje Leyman; Hanne Huysmans; Séan Mc Cafferty; Francis Combes; Eric Cox; Bert Devriendt; Niek N. Sanders, Molecular Pharmaceutics, 2018

Synthetic mRNA is becoming increasingly popular as an alternative to pDNA-based gene therapy. Currently, multiple synthetic mRNA platforms have been developed. In this study we investigated the expression kinetics and the changes in mRNA encoding cytokine and chemokine levels following ...


A d-Peptide Ligand of Integrins for Simultaneously Targeting Angiogenic Blood Vasculature and Glioma Cells

16.01.2018 | Yachao Ren; Changyou Zhan; Jie Gao; Mingfei Zhang; Xiaoli Wei; Man Ying; Zining Liu; Weiyue Lu, Molecular Pharmaceutics, 2018

The current prognosis of glioma patients remains poor after intensive multimodal treatments, which is partially due to the existence of the blood–brain tumor barrier (BBTB). In the present study, a novel “bifunctional ligand” (termed DVS) was developed by retro-inverso isomerization. DVS is a ...


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