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Eur J Pharm Biopharm 2019 Apr 13. Epub 2019 Apr 13.

Department of Pharmacy and Biotechnology, University of Bologna, Bologna, Italy. Electronic address:

Staphylococcus aureus is the major causative agent of skin and soft tissue infections, whose prevention and treatment have become more difficult due to the emergence of antibiotic-resistant strains. In this regard, the development of an effective treatment represents a challenge that can be overcome by delivering new antibiofilm agents with appropriate nanocarriers. In this study, a biosurfactant (BS) isolated from Lactobacillus gasseri BC9 and subsequently loaded in liposomes (LP), was evaluated for its ability to prevent the development and to eradicate the biofilm of different methicillin resistant S. Read More

Eur J Pharm Biopharm 2019 Apr 11. Epub 2019 Apr 11.

School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Rue Michel-Servet 1, 1211 Geneva, Switzerland. Electronic address:

Resiquimod (R848), a member of the imidazoquinoline family, is a Toll-like receptor 7/8 agonist with high potency for cancer immunotherapy. However, tolerance induction and adverse effects limit its development as a drug. Encapsulation in a polymer matrix can circumvent these limitations, as shown in our formerly published approach where R848 was loaded into polylactic acid (PLA)-based nanoparticles (NP). Read More

Eur J Pharm Biopharm 2019 Apr 11. Epub 2019 Apr 11.

Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA; Center for Dermal Research, Rutgers-The State University of New Jersey, 145 Bevier Road, Piscataway, NJ 08854, USA. Electronic address:

The transdermal route offers an attractive alternative route of drug administration especially for Alzheimer's disease patients through eliminating gastrointestinal side effects and ultimately improving compliance. In this study, we prepared an optimized matrix -type patches for the transdermal delivery of galantamine free base with ex vivo and in vitro evaluation. Four pressure sensitive adhesives with different functional groups, ten penetration enhancers and four drug loadings were tested to determine the optimized patch. Read More

Eur J Pharm Biopharm 2019 Apr 5. Epub 2019 Apr 5.

Biomedical Sciences Research Institute, University of Ulster, Coleraine, Northern Ireland, U.K. BT52 1SA.

Mastectomy is a common surgical treatment used in the management of breast cancer but has associated physical and psychological consequences for the patient. Breast conservation surgery (BCS) is an alternative to mastectomy but is only possible when the tumour is of an appropriate size. Neo-adjuvant chemotherapy has been successfully used to downstage tumours and increase the number of patients eligible for BCS. Read More

Eur J Pharm Biopharm 2019 Apr 4. Epub 2019 Apr 4.

Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense, Denmark.

An experimental/computational approach has been successfully applied in order to study the effect of solubilizing vehicles (cyclodextrins and liposomes) on the passive diffusion of four active pharmaceutical ingredients (API) of different nature (hydrophilic, ionizable and lipophilic) through an unstirred water layer (UWL) model. This approach allowed the measurement of flux changes through the UWL and the computational calculation of different parameters relevant to interpret the interplay within solubilizing vehicles and UWL diffusion. In the case of cyclodextrin, this approach allowed the determination of free drug diffusivity (D), bound drug diffusivity (D) and the equilibrium constant (K). Read More

Eur J Pharm Biopharm 2019 Apr 4. Epub 2019 Apr 4.

IBMM, Université de Montpellier, CNRS, ENSCM, Faculté de Pharmacie, 15 avenue Charles Flahault, BP14491, 34093 Montpellier cedex 5, France.

Fast in situ forming, chemically crosslinked hydrogels were prepared by the amidation reaction between N-succinimidyl ester end groups of multi-armed poly(ethylene glycol) (PEG) and amino surface groups of poly(amido amine) (PAMAM) dendrimer generation 2.0. To control the properties of the PEG/PAMAM hydrogels, PEGs were used with different arm numbers (4 or 8) as well as different linkers (amide or ester) between the PEG arms and their terminal N-succinimidyl ester groups. Read More

Eur J Pharm Biopharm 2019 Apr 2. Epub 2019 Apr 2.

INSERM, U1059, Dysfonction Vasculaire et Hémostase, Saint-Etienne, France; Université de Lyon, Saint-Etienne, F-42023, France; Laboratoire de Pharmacologie Toxicologie Gaz du sang, CHU de Saint-Etienne, Saint-Etienne, France. Electronic address:

The preclinical evaluation of nasally administered drug candidates requires screening studies based on in vitro models of the nasal mucosa. The aim of this study was to evaluate the morpho-functional characteristics of the 3D MucilAir™ nasal model with a pharmacological focus on [ATP]-binding cassette (ABC) efflux transporters. We initially performed a phenotypic characterization of the MucilAir™ model and assessed its barrier properties by immunofluorescence (IF), protein mass spectrometry and examination of histological sections. Read More

Eur J Pharm Biopharm 2019 Apr 2. Epub 2019 Apr 2.

Translational PKPD Research Group, Department of Pharmaceutical Biosciences, Associate Member of SciLife Lab, Uppsala University, Uppsala, Sweden. Electronic address:

The purpose of this study was to quantitatively investigate how conjugation of GSH to different liposomal formulations influence the brain delivery of methotrexate (MTX) in rats. GSH-PEG liposomal MTX based on hydrogenated soy phosphatidylcholine (HSPC) or egg yolk phosphatidylcholine (EYPC) and their corresponding PEG control liposomes were prepared. The brain delivery of MTX after intravenously administering free MTX, four liposomal formulations or free MTX + empty GSH-PEG-HSPC liposomes was evaluated by performing microdialysis in brain interstitial fluid and blood. Read More

Eur J Pharm Biopharm 2019 Apr 1. Epub 2019 Apr 1.

Department of Pharmaceutical Technology, Eberhard Karls University, Auf der Morgenstelle 8, Tuebingen, Germany. Electronic address:

Orodispersible tablets (ODTs) are a convenient dosage form and a recent trend in formulation development. The fast disintegration is accompanied by rapid removal of the active principle and the excipients from the mouth due to saliva flow and swallowing. Probiotic bacteria are a promising strategy to fight disease with bacterial aetiology in the mouth, but a certain residence time in the oral cavity is inevitable to exert their positive effects. Read More

Eur J Pharm Biopharm 2019 Mar 30. Epub 2019 Mar 30.

Ludwig-Maximilians-Universität München, Department of Pharmacy, Pharmaceutical Technology and Biopharmaceutics, 81377 Munich, Germany. Electronic address:

The number of antibody-drug conjugates (ADCs) on the market is expected to multiply in the upcoming years. The main reason: this novel drug delivery system combines the benefits of the selectivity of the antibody and the potency of the cytotoxic agent. The interplay of the antibody, linker and payload, however, calls for a stable and unique formulation. Read More

Eur J Pharm Biopharm 2019 Mar 22. Epub 2019 Mar 22.

Department of Pharmacy and BioTechnology, PharmTech Lab, University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy. Electronic address:

The current study proposes an original oral delivery system for the bioavailability enhancement of indomethacin (IND), a BCS class II drug, with the aim to overcome the common limitations of amorphous solid dispersion. In fact, the potential risk of drug re-crystallization is a serious concern for the stability of amorphous systems and represents, despite the great bioavailability, one of the primary causes of their limited clinical applications. IND-loaded microparticles (MPs) were prepared by spray congealing using oral-approved excipients (Gelucire 50/13 and the recently marketed Gelucire 48/16). Read More

Eur J Pharm Biopharm 2019 Mar 21. Epub 2019 Mar 21.

University of Graz, Institute of Pharmaceutical Sciences, Department of Pharmaceutical Technology and Biopharmacy, Universitätsplatz 1, 8010 Graz, Austria; Research Center Pharmaceutical Engineering, Inffeldgasse 13, 8010 Graz, Austria. Electronic address:

The development of lipid nanoparticles requires knowledge on the crystalline structure, polymorphic transitions and lipid-drug interactions. This study aimed at introducing advanced techniques to characterize nanostructured lipid carriers (NLC) comprising palmitic acid, oleic acid, stabilizer and Domperidone. Crystallinity of single components and mixtures was investigated by laboratory Small Angle X-ray Scattering (SAXS). Read More

Eur J Pharm Biopharm 2019 Mar 21. Epub 2019 Mar 21.

Technical Development Biosimilars, Global Drug Development Novartis, Hexal AG, Keltenring 1+3, 82041, Oberhaching, Germany.

N-glycosylation is a common post-translational modification of biopharmaceutical products. Certain types of N-glycans have been shown to influence important properties of monoclonal antibody products including pharmacokinetics and effector functions. Complex biopharmaceuticals e. Read More

Eur J Pharm Biopharm 2019 Mar 21. Epub 2019 Mar 21.

Department of Pharmacy and Pharmacology, University of Bath, Bath, UK. Electronic address:

Characterization of controlled release formulations used for intra-articular (IA) drug administration is challenging. Bio-relevant synovial fluids (BSF), containing physiologically relevant amounts of hyaluronic acid, phospholipids and proteins, were recently proposed to simulate healthy and osteoarthritic conditions. This work aims to evaluate the performance of different controlled release formulations of methylprednisolone (MP) for IA administration, under healthy and disease states simulated conditions. Read More

Eur J Pharm Biopharm 2019 Mar 19. Epub 2019 Mar 19.

Institute of Pharmacy, Faculty of Biosciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, D-06120 Halle (Saale), Germany. Electronic address: http://pharmtech.pharmazie.uni-halle.de.

Nifedipine and nicardipine loaded PLGA extrudates have a great potential to prevent cerebral vasospasms after subarachnoid hemorrhage or surgical clipping of aneurysm. A constant release over approx. two weeks is desired. Read More

Eur J Pharm Biopharm 2019 Mar 19. Epub 2019 Mar 19.

Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, 55128, Mainz, Germany.

Food induced viscosity in the gastrointestinal tract is reported to reduce the bioavailability of tablets containing BCS class 3 drugs, mainly by retarding their disintegration and dissolution of the active pharmaceutical ingredient. The role of formulation factors in minimizing this negative food effect is largely unknown. Combinations of disintegrants were studied together with soluble and insoluble fillers and trospium chloride as model drug substance. Read More

Eur J Pharm Biopharm 2019 Mar 18. Epub 2019 Mar 18.

Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria. Electronic address:

Aim: The aim of the study was to establish a novel type of covalently mucus-binding polymers by targeting selectively amino groups within mucus glycoproteins.

Methods: N-Hydroxysuccinimide (NHS) was attached to carboxylic groups of polyacrylic acid (PAA). The reaction was mediated by the coupling reagent N,N'-dicyclohexylcarbodiimide (DCC) achieving polymeric NHS esters being able to form amide bonds with free amino groups. Read More

Eur J Pharm Biopharm 2019 Mar 13. Epub 2019 Mar 13.

Department of Dermatology, Venereology and Allergology, Center of Experimental and Applied Cutaneous Physiology (CCP), Charité - Universitätsmedizin Berlin, corporate member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health. Electronic address:

Topical retinoids are frequently applied for therapeutic and cosmeceutical reasons although their bioavailability is low due to their chemical and photochemical instability. Moreover, skin irritation is a common side effect. Therefore, proretinal nanoparticles (PRN) as a novel formulation of topical retinoids, which are based on chitosan grafted with retinal through reversible linkage, were developed and their skin penetration behavior was studied. Read More

Eur J Pharm Biopharm 2019 Mar 13. Epub 2019 Mar 13.

Institute of Pharmacy, Biopharmaceutics and Pharmaceutical Technology, Center of Drug Absorption and Transport (C_DAT), University of Greifswald, Felix-Hausdorff-Straße 3, 17487 Greifswald, Germany. Electronic address:

Drug-eluting stents are often coated using single-stent coating techniques. In pharmaceutical industry, single-tablet coating is unthinkable. Instead large batches of tablets are coated in fluidized bed apparatuses or pan coaters. Read More

Eur J Pharm Biopharm 2019 Mar 11. Epub 2019 Mar 11.

College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, Michigan, 48109, USA.

Enteric coatings have shown in vivo dissolution rates that are poorly predicted by traditional in vitro tests, with the in vivo dissolution being considerably slower than in vitro. To provide a more mechanistic understanding of this, the dependence of the release properties of various enteric-coated (EC) products on bulk pH and bicarbonate molarity was investigated. It was found that, at presumably in vivo-relevant values, the bicarbonate molarity is a more significant determinant of the dissolution profile than bulk pH. Read More

Eur J Pharm Biopharm 2019 Mar 9. Epub 2019 Mar 9.

Department of Pharmacy, Uppsala University, Uppsala Biomedical Center P.O. Box 580, SE-75123 Uppsala, Sweden.

Intrinsic dissolution rate (IDR) is the surface specific dissolution rate of a drug. In early drug development, this property (among other parameters) is measured in order to compare different polymorphs and salt forms, guide formulation decisions, and to provide a quality marker of the active pharmaceutical ingredient (API) during production. In this review, an update on different methods and small-scale techniques that have recently evolved for determination of IDR is provided. Read More

Eur J Pharm Biopharm 2019 Mar 9. Epub 2019 Mar 9.

Inhalation Sciences, Stockholm, Sweden; Institute of Environmental Medicine, Karolinska Institutet, Stockholm, Sweden.

The surface area of the air/liquid interface in the lungs is substantial, so deposited doses of aerosol medicines per interface surface area when administered via the inhalation route is always quite low. However, in most in vitro systems used for dissolution testing of dry powder inhalables, the dose per surface area is generally much higher. The aim of this study was to investigate in one in vitro lung dissolution system, the DissolvIt, the manner in which the deposited dose per test surface area of drug particles influences the simulated dissolution- and absorption rate. Read More

Eur J Pharm Biopharm 2019 Mar 7. Epub 2019 Mar 7.

CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal; CIEPQPF - Departamento de Engenharia Química, Universidade de Coimbra, Rua Silvio Lima, 3030-790 Coimbra, Portugal. Electronic address:

Nowadays, despite the intensive research performed in the area of skin tissue engineering, the treatment of skin lesions remains a big challenge for healthcare professionals. In fact, none of the wound dressings currently used in the clinic is capable of re-establishing all the native features of skin. An ideal wound dressing must confer protection to the wound from external microorganisms, chemical, and physical aggressions, as well as promote the healing process by stimulating the cell adhesion, differentiation, and proliferation. Read More

Eur J Pharm Biopharm 2019 Mar 6. Epub 2019 Mar 6.

Department of Pharmaceutical Technology, Faculty of Chemistry and Pharmacy, University of Regensburg, 93040 Regensburg, Germany. Electronic address:

Lipid nanocapsules (LNCs) are extensively used as drug carrier systems, due to their small size distribution, biocompatibility and ease of preparation. They are especially useful for lipophilic drugs to overcome physicochemical constraints that limit their efficacy, such as low solubility in aqueous media. The aim of this work was to investigate the relationship between the intracellular availability of poorly soluble drugs delivered via LNCs and their biological efficacy in cells in vitro. Read More

Eur J Pharm Biopharm 2019 Apr 6;137:218-226. Epub 2019 Mar 6.

Department of Biochemistry and Molecular Biology, Bio21 Institute, University of Melbourne, 30 Flemington Road, Parkville 3052, Australia.

HIV therapy with anti-retroviral drugs is limited by the poor exposure of viral reservoirs, such as lymphoid tissue, to these small molecule drugs. We therefore investigated the effect of PEGylation on the anti-retroviral activity and subcutaneous lymphatic pharmacokinetics of the peptide-based fusion inhibitor enfuvirtide in thoracic lymph duct cannulated rats. Both the peptide and the PEG were quantified in plasma and lymph via ELISA. Read More

Eur J Pharm Biopharm 2019 Mar 5. Epub 2019 Mar 5.

Physikalische Chemie, Freie Universität Berlin, Takustr. 3, 14195 Berlin, Germany.

The penetration of topically applied tacrolimus formulated in micelles into murine skin is reported, measured by X-ray microscopy. Tacrolimus and micelles are probed for the first time by this high spatial resolution technique by element-selective excitation in the C 1s- and O 1s-regimes. This method allows selective detection of the distribution and penetration depth of drugs and carrier molecules into biologic tissues. Read More

Eur J Pharm Biopharm 2019 Apr 2;137:209-217. Epub 2019 Mar 2.

Institute for Particle Technology, Technische Universität Braunschweig, Germany; PVZ - Center of Pharmaceutical Engineering, Technische Universität Braunschweig, Germany.

Orodispersible films (ODFs) have a high potential to accelerate the individualized medication. The films can be produced as drug-free templates and subsequently printed with an API (active pharmaceutical ingredient) solution or suspension according to the needs of the patient. While the printing technology already enables a precise dosing of fluids, there is still a high need of suitable, edible templates with elevated loading capacity. Read More

Eur J Pharm Biopharm 2019 Apr 2;137:227-232. Epub 2019 Mar 2.

LAQV, Requimte, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, Caparica 2829-516, Portugal. Electronic address:

The major challenge of the pharmaceutical industry is to find potential solvents for poorly water-soluble drug molecules. Ionic liquids (ILs) have attracted this industry as (co-) solvents due to their unique physicochemical and biological properties. Herein, a straightforward approach for the enhancement of the water solubility of paracetamol and sodium diclofenac is presented, using new biocompatible N-acetyl amino acid N-alkyl cholinium-based ionic liquids as co-solvents (0. Read More

Eur J Pharm Biopharm 2019 Mar 2. Epub 2019 Mar 2.

Department of Pharmaceutics and Biopharmaceutics, University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany. Electronic address:

Nanostructured coatings of dental implants have shown great potential in overcoming many challenges responsible for implant failure. In this study, nano spray drying technology was utilized to produce novel biocompatible nanocoatings with antibacterial activity. The experiments were applied on titanium discs, which were used as a model material for dental implants. Read More

Eur J Pharm Biopharm 2019 Apr 2;137:148-163. Epub 2019 Mar 2.

Department of Pharmacy, University of Huddersfield, Huddersfield HD1 3DH, UK.

This work explores the use of UV imaging in solid dispersion systems. Solid dispersions are one of the common strategies used in improving the dissolution of poorly soluble drugs. Three manufacturing techniques (spray drying (SD), freeze drying (FD) and homogenising (HG)) are investigated. Read More

Eur J Pharm Biopharm 2019 Apr 28;137:196-208. Epub 2019 Feb 28.

Department of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, Bonn, Germany. Electronic address:

The problem of many gastroretentive systems is the mechanistic connection of drug release and gastric retention control. This connection could be successfully separated by formulating hollow tubes via hot-melt extrusion and sealing both tube ends, which led to immediately floating devices. The tube wall consisted of metformin crystals embedded in an inert polymer matrix of Eudragit® RS PO and E PO. Read More

Eur J Pharm Biopharm 2019 Apr 28;137:164-174. Epub 2019 Feb 28.

New Jersey Center for Engineered Particulates and Department of Chemical and Materials Engineering, New Jersey Institute of Technology, Newark, NJ, USA. Electronic address:

Drying is an important unit operation in the manufacturing of polymer strip films as it affects various film quality attributes. Optimal design and control of convective drying process require models that capture the impact of critical process parameters such as air temperature and velocity on the temporal evolution of film thickness and moisture. Here, a detailed transport model was presented to capture moisture diffusion, heat transfer and moving boundary in convective drying of polymer strip films loaded with griseofulvin (GF), a poorly water-soluble drug. Read More

Eur J Pharm Biopharm 2019 Feb 25. Epub 2019 Feb 25.

Institute of Pharmaceutical Science, Franklin-Wilkins Building, King's College London, 150 Stamford Street, London SE1 9NH, UK. Electronic address:

Designing nanomaterials to release their drug pay-load upon exposure to an exogenous trigger can help to direct drug delivery, but how the triggered release, which often modifies the nanomaterial properties, influences the biological fate of these systems is currently unknown. The aim of this study was to investigate how the triggered drug release from PEG coated, soft, 50 nm distensible lipid nanocapsules (LNC) influenced their diffusion across a mucus barrier. The translocation speed of the non-triggered LNC across a 35 µm thick purified gastric mucin (PGM) barrier was 3 times faster (30. Read More

Eur J Pharm Biopharm 2019 Apr 25;137:185-195. Epub 2019 Feb 25.

Department of Pharmaceutical Sciences, Utrecht Institute for Pharmaceutical Sciences (UIPS), Faculty of Science, Utrecht University, Utrecht, the Netherlands. Electronic address:

Niemann-Pick disease type B is a hereditary rare condition caused by deficiency of the acid sphingomyelinase (ASM) that is needed for lysosomal hydrolysis of sphingomyelin to ceramide and phosphocholine. This deficiency leads to a massive accumulation of sphingomyelin in cells throughout the body, predominantly in the liver, spleen and lungs. Currently, there is no effective treatment available. Read More

Eur J Pharm Biopharm 2019 Apr 25;137:140-147. Epub 2019 Feb 25.

Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China. Electronic address:

The purpose of this study was to apply the phenomenon of liquid jet breakup to the preparation of sustained-release microspheres. The mechanisms of liquid jet breakup in different jet states were investigated and the single factor method was used to study the effect of each process parameter on the particle size and size distribution of microspheres. Meantime, the prepared microspheres were characterized by morphology, drug loading, encapsulation efficiency and in vitro release. Read More

Eur J Pharm Biopharm 2019 Apr 25;137:131-139. Epub 2019 Feb 25.

Department of Pharmacy, Pharmaceutical Technology and Biopharmaceutics, Ludwig-Maximilians-University, Butenandtstrasse 5-13, Munich D-81377, Germany.

The formulation of novel therapeutic proteins is a challenging task which aims at finding formulation conditions that will minimize protein degradation during long-term storage. One particularly important and difficult-to-predict protein degradation pathway is the so-called non-native aggregation. The qualitative and quantitative prediction of the latter has been a subject of extensive research over the past two decades. Read More

Eur J Pharm Biopharm 2019 Apr 20;137:86-94. Epub 2019 Feb 20.

CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, 6200-506 Covilhã, Portugal; CIEPQPF - Departamento de Engenharia Química, Universidade de Coimbra, Rua Sílvio Lima, 3030-790 Coimbra, Portugal. Electronic address:

IR780 is a near infrared (NIR) dye with a huge potential to be applied in cancer phototherapy and imaging. However, IR780 poor water solubility and acute cytotoxicity limit its direct use in cancer theragnostic. Herein, a novel Hyaluronic acid (HA)-based amphiphilic polymer was used, for the first time, in the preparation of polymeric nanoparticles (HPN) encapsulating IR780 aimed to be applied in breast cancer therapy. Read More

Eur J Pharm Biopharm 2019 Apr 19;137:95-111. Epub 2019 Feb 19.

Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liege, Belgium.

Nucleic acids carried by non-viral nanovectors have demonstrated high potential as a therapeutic strategy for gene-related diseases. The dermal or transdermal gene delivery allow to target local skin diseases or to reach the blood stream. However, the skin is the first defense barrier of the body and must be overcome to distribute nucleic acids. Read More

Eur J Pharm Biopharm 2019 Apr 19;137:77-85. Epub 2019 Feb 19.

Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University, Universitaetstrasse 1, 40225 Duesseldorf, Germany. Electronic address:

In a previous publication, the development of an in-line Raman spectroscopic method for continuous API quantification during twin-screw wet granulation was presented. An in-line method was developed successfully and the developed method showed an acceptable prediction error. A disadvantage of the developed method was that a measurement was only possible in the dark since light influenced the Raman spectra and made a data interpretation impossible. Read More

Eur J Pharm Biopharm 2019 Apr 16;137:56-67. Epub 2019 Feb 16.

School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China. Electronic address:

Small interfering RNA (siRNA) has recently illustrated therapeutic potential for malignant disorders. However, the clinical application of siRNA-based therapeutics is significantly retarded by the paucity of successful delivery systems. Recently, multifunctional gold nanoparticles (AuNPs) as non-viral delivery carriers have shown promise for transporting chemotherapeutics, proteins/peptides, and genes. Read More

Eur J Pharm Biopharm 2019 Apr 16;137:112-121. Epub 2019 Feb 16.

School of Pharmacy, Jiangsu University, 301# Xuefu Road, Zhenjiang, Jiangsu, China. Electronic address:

Targeted delivery of bioactive compounds such as proteins to the colon has numerous advantages for the therapeutic treatment of inflammatory bowel disease. The present study sought to fabricate alginate/chitosan microcapsules containing IL-1Ra (Alg/Chi/IL-1Ra MC) via a single-step electrospraying method. Two important factors of efficacy were measured-the pH-responsiveness of the microcapsule and the in-vitro drug release profile. Read More

Eur J Pharm Biopharm 2019 Apr 16;137:23-36. Epub 2019 Feb 16.

Department of Oncology and Molecular Medicine, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy. Electronic address:

The use of nanomaterials is increasing but the real risk associated with their use in humans has to be defined. In fact, nanomaterials tend to accumulate in organs over a long period of time and are slowly degraded or eliminated by the body. Exosomes are nanovesicles actively shuttle molecules, including chemical products and metals, through the body. Read More

Eur J Pharm Biopharm 2019 Apr 15;137:175-184. Epub 2019 Feb 15.

Department of Biochemistry, Radboud Institute for Molecular Life Sciences (RIMLS), Radboud University Medical Center, PO Box 9101, 6500 HB Nijmegen, the Netherlands. Electronic address:

Elastin-like polypeptide (ELP) nanoparticles are a versatile platform for targeted drug delivery. As for any type of nanocarrier system, an important challenge remains the ability of deep (tumor) tissue penetration. In this study, ELP particles with controlled surface density of the cell-penetrating peptide (CPP) octa-arginine (R8) were created by temperature-induced co-assembly. Read More

Eur J Pharm Biopharm 2019 Apr 15;137:122-130. Epub 2019 Feb 15.

Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. Electronic address:

The tumor microenvironment is the cellular environment that is also described as the "soil" for supporting tumor growth, proliferation, invasion and metastasis, as well as protecting tumor cells from immunological recognition. Notably, tumor cells can grow much faster than other normal organs and invade surrounding tissues more easily, which results in abnormal expression of enzymes in the tumor microenvironment, including matrix metalloproteinases, cathepsins, phospholipases, oxidoreductases, etc. In opposite, due to the high selectivity and catalytic activity, these enzymes can promote nanoparticles to recognize tumor tissues more accurately, and the more accumulation of drugs at primal tumor sites will enhance therapeutic efficacy with lower systemic toxicity. Read More

Eur J Pharm Biopharm 2019 Apr 14;137:37-45. Epub 2019 Feb 14.

University of Pavia, Department of Drug Sciences, 27100 Pavia, Italy; Pharmaexceed srl, 27100 Pavia, Italy.

This paper aims at demonstrating silk fibroin nanoparticles (SFNs) promote anti-inflammatory properties of celecoxib (CXB) or curcumin (CUR), and could be exploited for osteoarthritis (OA) treatment. Nanoparticles were prepared by desolvation method and physico-chemically characterized (FT-IR, DSC, TGA, SEM, size distribution and drug release); empty and drug loaded nanoparticles were tested for their ROS-scavenging activity, hemolytic properties, cytotoxicity, and anti-inflammatory potency in an OA in vitro model. Results indicate that a controlled drug release has been achieved by varying the drug loading. Read More

Eur J Pharm Biopharm 2019 Feb 13. Epub 2019 Feb 13.

Division of Advanced Materials and Healthcare Technologies, School of Pharmacy, The University of Nottingham, NG7 2RD, UK. Electronic address:

Basal cell carcinoma (BCC) is the most common skin cancer in humans. Topical treatment with imiquimod provides a non-invasive, self-administered treatment with relatively low treatment cost. Despite displaying excellent efficacy, imiquimod is only licensed by the FDA for superficial BCC. Read More

Eur J Pharm Biopharm 2019 Apr 14;137:46-55. Epub 2019 Feb 14.

Department of Pharmacy, Uppsala Biomedical Center, Uppsala University, 751 23 Uppsala, Sweden; Swedish Drug Delivery Forum (SDDF), Uppsala University, Sweden. Electronic address:

In this review we will discuss how computational methods, and in particular classical molecular dynamics simulations, can be used to calculate solubility of pharmaceutically relevant molecules and systems. To the extent possible, we focus on the non-technical details of these calculations, and try to show also the added value of a more thorough and detailed understanding of the solubilization process obtained by using computational simulations. Although the main focus is on classical molecular dynamics simulations, we also provide the reader with some insights into other computational techniques, such as the COSMO-method, and also discuss Flory-Huggins theory and solubility parameters. Read More

Eur J Pharm Biopharm 2019 Apr 12;137:68-76. Epub 2019 Feb 12.

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Sri-Ayutthaya Road, Rajathavee, Bangkok, Thailand; Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand. Electronic address:

The purpose of this study was to evaluate the effect of charge on the in vitro drug performances of clarithromycin nanocrystals. To prepare different charges of nanocrystals, media milling was employed with the use of different stabilizing systems. The uncharged nanocrystals were prepared from poloxamer 407. Read More

Eur J Pharm Biopharm 2019 Apr 7;137:1-8. Epub 2019 Feb 7.

Graduate School of Biomedical Sciences, Nagasaki University, 1-7-1 Sakamoto, Nagasaki-shi, Nagasaki 852-8588, Japan. Electronic address:

Aim: Intracerebroventricular (ICV) administration of ultrasound-responsive bubbles and cranial ultrasound irradiation is reported as a transfection system for the cerebroventricular region. This study aimed to characterize the transfection system with respect to transfection efficiency, spatial distribution of transgene expression, and safety.

Methods: Plasmid DNA was transfected to mouse brain by ICV injection of ultrasound-responsive nanobubbles, followed by ultrasound irradiation to brain. Read More

Eur J Pharm Biopharm 2019 Apr 5;137:9-22. Epub 2019 Feb 5.

Department of Pharmacy, University of Greifswald, 17489 Greifswald, Germany. Electronic address:

Accurate prediction of oral absorption of drugs relies on biorelevant methodology. Current methods are based on Western healthy adult populations. Malnourished children have many differences in their gastrointestinal anatomy and physiology compared to a healthy Western adult. Read More