12,576 results match your criteria International journal of pharmaceutics[Journal]


Incorporation of benzoyl peroxide nanocrystals into adapalene-loaded solid lipid microparticles: Part I - Nanocrystalline benzoyl peroxide.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Institut für Pharmazeutische Technologie TU Braunschweig, Mendelssohnstraße 1, 38106 Braunschweig, Germany; Center of Pharmaceutical Engineering, Franz-Liszt-Str, 35a, 38106 Braunschweig, Germany. Electronic address:

Hair follicles are a promising target for the administration of drugs to treat diseases associated with the pilosebaceous unit, such as acne. For solid lipid microparticle dispersions a successful and selective delivery of adapalene via targeted erosion of the particles in sebum has been shown. By embedding nanoparticulate benzoyl peroxide in lipid microparticles, the therapeutic potency of adapalene can be further increased by improving follicular deposition of benzoyl peroxide and minimizing direct contact between benzoyl peroxide and stratum corneum, which is responsible for the irritating potential of this active agent. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.031DOI Listing

Inhalable co-amorphous budesonide-arginine dry powders prepared by spray drying.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark; Wuya College of Innovation, Shenyang Pharmaceutical University, Wenhua Road 103, 110016, Shenyang, China. Electronic address:

Spray drying is a well-established technology to produce inhalable dry powders. However, the amorphous nature of the particles typically obtained from the process can lead to physically and chemically unstable products. The purpose of this study was to investigate whether spray-drying could be used as a manufacturing method to produce co-amorphous drug amino acid powders with high physical stability and inhalable particulate properties. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.036DOI Listing
April 2019
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Development and pharmacokinetics of a combination vaginal ring for sustained release of dapivirine and the protein microbicide 5P12-RANTES.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, UK. Electronic address:

The past fifteen years have witnessed a resurgence of interest in vaginal ring technologies for drug delivery applications, mostly driven by the impetus for development of vaginally-administered antiretroviral microbicides to help reduce the high acquisition rates for human immunodeficiency virus (HIV) among Sub-Saharan African women. Currently, the lead candidate microbicide is a 28-day silicone elastomer vaginal ring releasing dapivirine (Ring-004), an experimental non-nucleoside reverse transcriptase inhibitor. The ring was tested in two pivotal Phase III clinical studies in 2016 and is currently undergoing review by the European Medicines Agency. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.040DOI Listing

Gold nanoparticles loaded with Cullin-5 DNA increase sensitivity to 17-AAG in Cullin-5 Deficient Breast Cancer Cells.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Department of Biological Sciences, Towson University, Towson, MD, United States. Electronic address:

HSP90 inhibitors have the potential to treat many types of cancer due to the dependence of tumor cells on HSP90 for cell growth and proliferation. The Cullin-5 (Cul5) E3 ubiquitin ligase is required for HSP90 inhibitors to induce client protein degradation and subsequent cell death. Cul5 is expressed at low levels in breast cancer cells compared to patient matched controls. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.022DOI Listing

Egg white coated alginate nanoparticles with electron sprayer for potential anticancer application.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Research Institute of Sun Yat-Sen University in Shenzhen, Shenzhen, 518057, PR China; Key Laboratory of Sensing Technology and Biomedical Instrument of Guangdong Province, School of Biomedical Engineering, Sun Yat-sen University, Guangzhou 510006, PR China. Electronic address:

To development biomimetic strategy for enhanced cancer therapy, the paclitaxel loaded egg white/sodium alginate nanoparticles were prepared by electronic spray method. Their appearance and particle size were observed by transmission electron microscope and particle size analyzer. The drug release behavior of nanoparticles was determined by high performance liquid chromatography (HPLC). Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.045DOI Listing

Formulation and processability screening for the rational design of ethylene-vinyl acetate based intra-vaginal rings.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

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

The application of ethylene-vinyl acetate (EVA) copolymers in reservoir-type intra-vaginal rings (IVRs) offers advantages over silicones including i) versatile properties, ii) absence of curing chemistry, and iii) continuous and flexible processing via co-extrusion. Thus, we investigated the capability of EVA based IVRs to deliver broad ranges of estradiol (E2) thereby, fulfilling the requirements of local and systemic hormone replacement therapy (HRT) and contraception. To circumvent the high material needs associated with co-extrusion, we implemented a small-scale screening procedure that accurately predicts the E2 release from IVRs comprising E2 below its solubility concentration in the core. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.041DOI Listing

Post-irradiation recovery time strongly influences fractional laser-facilitated skin absorption.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine, Chang Gung University of Science and Technology, Kweishan, Taoyuan, Taiwan; Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan; Department of Anesthesiology, Chang Gung Memorial Hospital, Kweishan, Taoyuan, Taiwan. Electronic address:

Fractional CO laser treatment has been used in some clinical trials to promote topical drug delivery. Currently, there is no standard for laser settings to achieve a feasible therapy. The cutaneous recovery following laser treatment and its influence on drug absorption have not been well explored. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.043DOI Listing

The Formation and Effect of Mannitol Hemihydrate on the Stability of Monoclonal Antibody in the Lyophilized state.

Int J Pharm 2019 Apr 15. Epub 2019 Apr 15.

Lek d.d., Kolodvorska 27, 1234 Mengeš, Slovenia.

Crystalline bulking agent in lyophilized biopharmaceutical formulations provides an elegant lyophilized cake structure and allows aggressive primary drying conditions. The interplay between amorphous and crystalline state of excipients heavily influence the stability of lyophilized biological products and should be carefully evaluated in the formulation and process development phase. This study focuses on: (1) elucidating the influence of formulation and lyophilization process variables on the formation of different states of mannitol and (2) its impact on model monoclonal antibody stability when compared to sucrose. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.044DOI Listing
April 2019
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BR2 and CyLoP1 enhance in-vivo SN38 delivery using pegylated PAMAM dendrimers.

Int J Pharm 2019 Apr 13. Epub 2019 Apr 13.

Nanotechnology Research Center, Institute of Pharmaceutical Technology, Mashhad University of Medical Sciences, Mashhad, Iran. Electronic address:

The usage of 7-Ethyl-10-hydroxy-camptothecin (SN38) as the most biologically active member of camptothecin family is restricted because of its poor solubility in pharmaceutical solvents. Polyamidoamine (PAMAM) dendrimers, can be used as suitable drug delivery carrier for poorly water soluble molecules. In this study, we prepared two cell penetrating peptides (BR2 and CyLoP1) conjugated formulations of PEGylated PAMAM containing SN38. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193029
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http://dx.doi.org/10.1016/j.ijpharm.2019.04.037DOI Listing
April 2019
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Amorphous solid dispersions of weak bases with pH-dependent soluble polymers to overcome limited bioavailability due to gastric pH variability - An in-vitro approach.

Int J Pharm 2019 Apr 13. Epub 2019 Apr 13.

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

Several drugs are pH-dependent soluble weak bases with a poor solubility in the intestinal pH range. Additionally a variable gastric pH, which is a common issue in the population, potentially reduces the in-vivo performance due to reduced solubility at elevated pH. Aiming to avoid the influence of variable gastric pH on the dissolution performance, enteric polymers - hydroxypropylmethylcellulose acetate succinate (HPMCAS),hydroxypropylmethylcellulose phthalate (HP-55, HP-50) and methacrylic acid ethylacrylate copolymer (Eudragit L100-55) together with nevirapine as model drug were used for the preparation of solid dispersions by hot-melt extrusion. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.034DOI Listing
April 2019
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The roles of short and long chain fatty acids on physicochemical properties and improved cancer targeting of albumin-based fattigation-platform nanoparticles containing doxorubicin.

Int J Pharm 2019 Apr 13. Epub 2019 Apr 13.

College of Pharmacy, Ajou University, Suwon 16499, Republic of Korea. Electronic address:

The aim of this study was to investigate the impact of different chain length fatty acids on physicochemical properties and cancer targeting of fattigation-platform nanoparticles (NPs). Two different types of fatty acids (short chain, 2-hydroxybutyric acid, C4; long chain, oleic acid, C18:1) were successfully conjugated to human serum albumin (HSA) via simple 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) coupling reaction. These conjugates readily formed HSA-C4 and HSA-C18:1 NPs which showed good stability in serum and desirable biocompatibility with normal cell line (HEK293T). Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193030
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http://dx.doi.org/10.1016/j.ijpharm.2019.04.038DOI Listing
April 2019
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Mucin Binding To Therapeutic Molecules: The Case Of Antimicrobial Agents Used In Cystic Fibrosis.

Int J Pharm 2019 Apr 13. Epub 2019 Apr 13.

Molecular Biotechnology and Health Science Department, University of Torino, Via Gioachino Quarello 15, 10135 Torino, Italy. Electronic address:

Mucin is a complex glycoprotein consisting of a wide variety of functional groups that can interact with exogenous agents. The binding to mucin plays a crucial role in drug pharmacokinetics especially in diseases, such as cystic fibrosis (CF), where mucin is overexpressed. In this study, we have investigated the interaction between mucin and several drugs used in CF therapy. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.032DOI Listing
April 2019
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Adjustment of triple shellac coating for precise release of bioactive substances with different physico-chemical properties in the ileocolonic region.

Int J Pharm 2019 Apr 13. Epub 2019 Apr 13.

Division of Food Technology, Kiel University, Heinrich-Hecht-Platz 10, 24118 Kiel, Germany.

Formulations for the controlled release of substances in the human terminal ileum and colon are essential to target the gut microbiome and its interactions with the intestinal mucosa. In contrast to pharmaceutical enteric coatings, reliable food-grade alternatives are still scarce. Shellac coatings have been used for various active ingredients, but their stability is affected by the physicochemical properties of the encapsulated substances. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.039DOI Listing

Nanoporous CD-MOF particles with uniform and inhalable size for pulmonary delivery of budesonide.

Int J Pharm 2019 Apr 11. Epub 2019 Apr 11.

Center for Drug Delivery Systems, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203, China; Zhejiang Chinese University of Medicine, Hangzhou 310053, China. Electronic address:

It is essential to optimize a carrier of dry powder inhalation (DPI) for the aerodynamic deposition in vitro to achieve pulmonary delivery of drug molecules in vivo. In this study, neutralized nanoporous γ-cyclodextrin metal-organic framework (CD-MOF) crystals with cubic morphology and uniform inhalation size were developed and modified as a DPI carrier for budesonide (BUD). Cholesterol (CHO) and leucine (LEU)-poloxamer were used to modify the CD-MOF powder for the improvement of flowability and particle aerodynamic behaviour, for which the particle size distribution, Carr's index and in vitro pulmonary deposition were assessed. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.030DOI Listing
April 2019
2 Reads

In vitro evaluation of intravesical mucoadhesive self-emulsifying drug delivery systems.

Int J Pharm 2019 Apr 11. Epub 2019 Apr 11.

Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, Innsbruck, Austria.

Intravesical mucoadhesive self-emulsifying drug delivery system (SEDDS) have been developed via synthesis and incorporation of S-protected chitosan CS-MNA into SEDDS. N-acetyl cysteine-6-mercaptonicotinamide (NAC-6-MNA) was synthetized via disulphide exchange reaction between N-acetyl cysteine and 6-mercaptonicotinamide dimer. NAC-6-MNA was attached to chitosan (CS) via carbodiimide mediated amide bond formation. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.035DOI Listing
April 2019
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Effect of molecular weight of hypromellose on mucin diffusion and oral absorption behavior of fenofibrate nanocrystal.

Int J Pharm 2019 Apr 11. Epub 2019 Apr 11.

Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.

We investigated the effect of variation in the molecular weight of hypromellose (HPMC) on the oral absorption of fenofibrate (FFB) nanocrystal. Four types of HPMC with different molecular weights and sodium dodecyl sulfate (SDS) were used as dispersion stabilizers for FFB nanocrystal suspension. Wet-milling of FFB crystal with HPMC and SDS formed diamond-shaped FFB nanocrystals with approximately 150 nm diameter. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.033DOI Listing

Determination of mechanical and rheological properties of a cell-loaded peptide gel during ECM production.

Int J Pharm 2019 Apr 10. Epub 2019 Apr 10.

Pharmaceutical Technology, Department of Chemistry and Chemical Engineering, Chalmers University of Technology, Gothenburg, Sweden; SuMo BIOMATERIALS, VINN Excellence Center, Chalmers University of Technology, Gothenburg, Sweden. Electronic address:

The development of an injectable biomaterial that supports cell survival and maintains or promotes nucleus pulposus (NP) phenotype could aid delivery of cells to degenerated NPs causing low back pain. Mesenchymal cells were loaded and grown in a synthetic peptide gel, PuraMatrix®. Cells were observed within the gels over 0-28 days, and accumulation of glycosaminoglycans were detected by histological staining. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.028DOI Listing

Study of naproxen in some aqueous solutions of choline-based deep eutectic solvents: Solubility measurements, volumetric and compressibility properties.

Int J Pharm 2019 Apr 10. Epub 2019 Apr 10.

Department of Physical Chemistry, University of Tabriz, Tabriz, Iran.

Naproxen (NAP) is a widely used drug for the treatment of pain and inflammatory conditions. However, the physicochemical information about properties such as solubility, apparent molar volume, and apparent molar isentropic compressibility for this drug is not abundant especially in the presence of deep eutectic solvents (DES) as a new class of green solvents to overcome the low solubility of drugs. In this work, the solubility of NAP is studied in the solutions containing some choline chloride (ChCl) based DES at temperature ranges (298. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.029DOI Listing

Time-temperature superposition principle for the kinetic analysis of destabilization of pharmaceutical emulsions.

Int J Pharm 2019 Apr 9;563:406-412. Epub 2019 Apr 9.

Department of Pharmaceutical Technology, Graduate School of Medical and Pharmaceutical Science, University of Toyama, 2630 Sugitani, Toyama-shi, Toyama 930-0194, Japan. Electronic address:

The time-temperature superposition principle (TTSP) was applied to the destabilization kinetics of a pharmaceutical emulsion. The final goal of this study is to predict precisely the emulsion stability after long-term storage from the short-period accelerated test using TTSP. As the model emulsion, a cream preparation that is clinically used for the treatment of pruritus associated with chronic kidney disease was tested. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.020DOI Listing

Encapsulation and release of doxycycline from electrospray-generated PLGA microspheres: Effect of polymer end groups.

Int J Pharm 2019 Apr 9;564:1-9. Epub 2019 Apr 9.

Department of Biomaterials, Radboud University Medical Center, 6500 HB Nijmegen, the Netherlands. Electronic address:

The aim of this study was to investigate the influence of end group of poly(lactic-co-glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To this end, doxycycline hyclate (DOX) was selected as a model drug, and PLGA (molecular weight: 17 and 44 kDa) with either an acid or ester end group were electrosprayed with DOX. The processing parameters were optimized to obtain microspheres comparable in size. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.023DOI Listing

Eutexia for enhanced dissolution rate and anti-inflammatory activity of nonsteroidal anti-inflammatory agents: Caffeine as a melting point modulator.

Int J Pharm 2019 Apr 9;563:395-405. Epub 2019 Apr 9.

Department of Pharmaceutical Technology, College of Pharmacy, Tanta University, 4111 Tanta, Egypt. Electronic address:

Fast dissolution of nonsteroidal anti-inflammatory drugs (NSAIDs) is a prerequisite from patient perspective. However, most NSAIDs are slowly dissolving acidic compounds. Caffeine, a commonly used analgesic adjuvant with NSAIDs showed high potential as eutectic co-former for acidic compounds. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.024DOI Listing

Water-Based 3D Inkjet Printing of an Oral Pharmaceutical Dosage Form.

Int J Pharm 2019 Apr 9. Epub 2019 Apr 9.

Centre for Additive Manufacturing, Faculty of Engineering, University of Nottingham, Nottingham, NG7 2RD, UK.

Inkjet printing is a form of additive manufacturing where liquid droplets are selectively deposited onto a substrate followed by solidification. The process provides significant potential advantages for producing solid oral dosage forms or tablets, including a reduction in the number of manufacturing steps as well as the ability to tailor a unique dosage regime to an individual patient. This study utilises solvent inkjet printing to print tablets through the use of a Fujifilm Dimatix printer. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.026DOI Listing

A novel theranostic system of AS1411 aptamer-functionalized albumin nanoparticles loaded on iron oxide and gold nanoparticles for doxorubicin delivery.

Int J Pharm 2019 Apr 9. Epub 2019 Apr 9.

Cellular and Molecular Research Center, Yasuj University of Medical Sciences, Yasuj, Iran.

Recently DNA aptamers have attracted remarkable attention as possible targeting ligands since selective targeting of cancer cells is a critical step in cancer diagnosis and therapy. Here, the development of AS1411 aptamer-functionalized albumin nanoparticles loaded on iron oxide and gold nanoparticles is reported for target delivery of the well-known anticancer drug of doxorubicin (Dox). Iron oxide nanoparticles (IONPs) and gold nanoparticles (GNPs) were prepared by ultrasound-assisted and controlled seeded growth synthetic methods, respectively. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.025DOI Listing
April 2019
2 Reads

Leukocyte-mimetic liposomes possessing leukocyte membrane proteins pass through inflamed endothelial cell layer by regulating intercellular junctions.

Int J Pharm 2019 Apr 10;563:314-323. Epub 2019 Apr 10.

Graduate School of Biomedical Sciences, Tokushima University, Shomachi 1, Tokushima 770-8505, Japan.

Nanoparticles such as liposomes have been applied for the treatment of various diseases such as cancer and inflammatory diseases by utilizing the enhanced permeability and retention effect. However, their entry into inflammation sites is still limited since passive delivery of nanoparticles is often hampered by the presence of endothelial barriers. As leukocytes can pass through the inflamed endothelium via utilizing membrane protein functions, we hypothesized that incorporating leukocyte membrane proteins onto liposomal membranes may impart leukocyte-mimicking functions to liposomes, allowing for their adherence to and active passage through the inflamed endothelium. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.027DOI Listing

Additive Manufacturing of Personalized Orodispersible Warfarin Films.

Int J Pharm 2019 Apr 8. Epub 2019 Apr 8.

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Artillerigatan 6A, FI-20520 Åbo, Finland. Electronic address:

Warfarin is a narrow therapeutic index drug that requires personalized dosing which is currently not achieved by the marketed products. Further, pediatric and geriatric patients may face swallowing problems with solid oral dosage forms. To face these issues, the aim of the present study was to investigate semisolid extrusion 3D printing for production of warfarin containing orodispersible films. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.018DOI Listing

3D Printed Oral Theophylline Doses with Innovative 'Radiator-Like' Design: Impact of Polyethylene Oxide (PEO) Molecular Weight.

Int J Pharm 2019 Apr 8. Epub 2019 Apr 8.

Institute of Pharmaceutical Science, King's College London, London, UK.

Despite the abundant use of polyethylene oxides (PEOs) and their integration as an excipient in numerous pharmaceutical products, there have been no previous reports of applying this important thermoplastic polymer species alone to fused deposition modelling (FDM) 3D printing. In this work, we have investigated the manufacture of oral doses via FDM 3D printing by employing PEOs as a backbone polymer in combination with polyethylene glycol (PEG). Blends of PEO (molecular weight 100K, 200K, 300K, 600K or 900K) with PEG 6K (plasticiser) and a model drug (theophylline) were hot-melt extruded. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.017DOI Listing

Direct compaction properties of Zingiberis Rhizoma extracted powders coated with various shell materials: improvements and mechanism analysis.

Int J Pharm 2019 Apr 8. Epub 2019 Apr 8.

Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.

Direct compaction (DC) attracts more and more attention for tablet manufacturing; however, its application in natural plant product (NPP) tablets is still extremely limited. In this study, 8 kinds of composite particles (CPs) based on the Zingiberis Rhizoma extracted powder (ZR) (a natural plant product powder with poor DC properties) were prepared with different shell materials, including hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), dextran, inulin, mannitol, silica, and their combinations. Their physical properties and compacting parameters were characterized comprehensively. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.021DOI Listing

An In Vitro Evaluation of Importance of Airway Anatomy in Sub-Regional Nasal and Paranasal Drug Delivery with Nebulizers Using Three Different Anatomical Nasal Airway Replicas of 2-, 5- and 50-Year Old Human Subjects.

Int J Pharm 2019 Apr 8. Epub 2019 Apr 8.

Department of Mechanical and Nuclear Engineering, Virginia Commonwealth University, Richmond, VA, United States. Electronic address:

Intranasal delivery of nebulized drugs with the consideration of the nasal anatomy is not adequately studied. The objective of this study was to evaluate nasal and paranasal drug delivery with nebulizers, with and without pulsating airflow, in three anatomically-different nasal models in different age groups, considering normal and bidirectional breathing techniques. Anatomically-accurate nasal models of 2-, 5-, and 50-year old subjects were developed and tested to quantify sub-regional deposition of an aqueous solution of a model drug, nebulized with PARI SinuStar and Sinus nebulizers. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.019DOI Listing

Dynamics of water and xanthan chains in hydrogels studied by NMR relaxometry and their influence on drug release.

Int J Pharm 2019 Apr 6;563:373-383. Epub 2019 Apr 6.

Jožef Stefan Institute, Ljubljana, Slovenia.

The dynamic properties of water and polymer molecules in xanthan hydrogels at different polymer mass fractions were investigated through the combination of conventional and fast-field cycling NMR relaxation to obtain the information about dynamics in different time scales. The results showed that water dynamics were faster in diluted than in concentrated hydrogels. However, the type of polymer-chain dynamics did not change for xanthan fractions from 0. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.014DOI Listing

Innovative sprayable in situ gelling fluticasone suspension: development and optimization of nasal deposition.

Int J Pharm 2019 Apr 6. Epub 2019 Apr 6.

University of Zagreb, Faculty of Pharmacy and Biochemistry, Department of Pharmaceutical Technology, Zagreb, Croatia. Electronic address:

The aim of this study was to develop an innovative in situ gelling suspension for effective nasal delivery of fluticasone. Pectin, gellan gum and sodium hyaluronate were used as gelling/thickening agents, and Tween 80 as a suspending agent. The influence of the formulation and/or administration parameters on formulation sprayability and nasal deposition was explored with an appropriate experimental design with the range for parameters in the design obtained from previous research and domain knowledge. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.015DOI Listing

Preparation of in situ hydrogels loaded with azelaic acid nanocrystals and their dermal application performance study.

Int J Pharm 2019 Apr 6;563:249-258. Epub 2019 Apr 6.

University of Zagreb, Faculty of Pharmacy and Biochemistry, A. Kovacica 1, 10000 Zagreb, Croatia. Electronic address:

Azelaic acid (AZA) is a dicarboxylic acid that is topically used in the treatment of acne and rosacea since it possesses antibacterial and keratolytic activity. The primary objective of this study was to develop an AZA nanocrystal suspension. It is expected that improved solubility and dissolution rate will result in advanced biopharmaceutical properties, primarily the dermal bioavailability. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.016DOI Listing
April 2019
3.650 Impact Factor

Characterization of acoustic emission analysis in applications for inhalation device performance assessment.

Int J Pharm 2019 Apr 5;563:304-313. Epub 2019 Apr 5.

AstraZeneca R&D, Pharmaceutical Technology & Development,Pepparedsleden 1, 431 83 Mölndal, Sweden. Electronic address:

Acoustic Emission (AE) measurement technology has gained wide appreciation in material sciences and process monitoring. In inhalation research, AE has been used for adherence indicating applications in clinical studies. Promising results from feasibility studies using AE combined with multivariate data analysis (AE-MVDA) in the analysis of devices for inhalation have prompted a broader study reported in this paper. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.011DOI Listing

Cyclodextrin-membrane interaction in drug delivery and membrane structure maintenance.

Int J Pharm 2019 Apr 5. Epub 2019 Apr 5.

Bioactive Molecules Research Laboratory, Doctoral School of Sciences and Technologies, Faculty of Sciences, Section II, Lebanese University, Lebanon. Electronic address:

Cyclodextrins (CDs) are cyclic oligosaccharides able to improve drug water solubility and stability by forming CD/drug inclusion complexes. To further increase drug entrapment and delay its release, the CD/drug inclusion complex can be embedded in the aqueous phase of a liposome, a lipid vesicle composed of phospholipid bilayer surrounding an aqueous compartment. The resulting carrier is known as drug-in-cyclodextrin-in-liposome (DCL) system. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193025
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http://dx.doi.org/10.1016/j.ijpharm.2019.03.063DOI Listing
April 2019
6 Reads

Probing the interactions among sphingosine and phytosphingosine ceramides with non- and alpha-hydroxylated acyl chains in skin lipid model membranes.

Int J Pharm 2019 Apr 5;563:384-394. Epub 2019 Apr 5.

University of Chemistry and Technology Prague, Faculty of Chemical Technology, Department of Organic Technology, Technická 5, 166 28 Prague, Czech Republic; Charles University, Faculty of Pharmacy in Hradec Králové, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address:

Ceramides (Cers) are significant constituents of the stratum corneum (SC), the uppermost skin layer responsible for skin barrier properties. Cers are a heterogeneous group of lipids whose mutual interactions are still unclear. To better understand these interactions, we characterized model membranes containing stearic acid, cholesterol, cholesterol sulfate and one or more of the following ceramides: N-stearoyl-sphingosine (CerNS), N-stearoyl-phytosphingosine (CerNP) and N-(2-hydroxy)stearoyl-phytosphingosine (CerAP). Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.010DOI Listing

Highly bioactive, bevacizumab-loaded, sustained-release PLGA/PCADK microspheres for intravitreal therapy in ocular diseases.

Int J Pharm 2019 Apr 5;563:228-236. Epub 2019 Apr 5.

School of Life Sciences, Jilin University, Changchun, Jilin 130012, China. Electronic address:

Bevacizumab, a vascular endothelial growth factor (VEGF)-targeting drug, is widely used as an off-label therapeutic for age-related macular degeneration (AMD). To reduce the monthly administration frequency, this study investigated microspheres comprising a poly(d, l-lactide-co-glycolide)/poly(cyclohexane-1,4-diyl acetone dimethylene ketal) (PLGA/PCADK) blend that could be loaded with bevacizumab-dextran particles using solid-in-oil-in-water (S/O/W) emulsification. Control microspheres were also prepared through water-in-oil-in-water (W/O/W) emulsification. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.012DOI Listing
April 2019
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Lipid-nucleic acid nanoparticles of novel ionizable lipids for systemic BMP-9 gene delivery to bone-marrow mesenchymal stem cells for osteoinduction.

Int J Pharm 2019 Apr 5;563:324-336. Epub 2019 Apr 5.

Department of Pharmaceutics, Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Kalabhavan Campus, Vadodara 390001, Gujarat, India. Electronic address:

Rational design of novel ionizable lipids for development of lipid-nucleic acid nanoparticles (LNP) is required for safe and effective systemic gene delivery for osteoporosis. LNPs require suitable characteristics for intravenous administration and effective accumulation in bone marrow for enhanced transfection. Hence, lipids with C18 tail and ionizable headgroup (Boc-His-ODA/BHODA and His-ODA/HODA) were synthesized and characterized physicochemically. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.006DOI Listing
April 2019
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The roles of a surfactant in zein-HPMC blend solid dispersions for improving drug delivery.

Int J Pharm 2019 Apr 4;563:169-173. Epub 2019 Apr 4.

Department for Management of Science and Technology Development, Ton Duc Thang University, Ho Chi Minh City, Viet Nam; Faculty of Pharmacy, Ton Duc Thang University, Ho Chi Minh City, Viet Nam. Electronic address:

This study aimed to originally investigate the roles of a surfactant in hydrophilic-hydrophobic polymer blend solid dispersions (SDs) to enhance drug dissolution. Different formulations of SDs containing a hydrophilic polymer, a hydrophobic polymer or a hydrophilic-hydrophobic blend were prepared with/without surfactant, and the crystal changes, wettability, and molecular interactions were investigated. The wettability was investigated by analysing the contact angle. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.009DOI Listing

Novel contamination-free wet milling technique using ice beads for poorly water-soluble compounds.

Int J Pharm 2019 Apr 3;563:413-425. Epub 2019 Apr 3.

Department of Industrial Pharmacy, Faculty of Pharmacy, Meijo University, 150 Yagotoyama, Tempaku, Nagoya 468-8503, Japan. Electronic address:

The aim of this study is to establish a contamination-free milling method using ice beads instead of conventional hard beads such as metal or ceramics. Ice beads, which melt after the milling process to form water, would solve the contamination issue attributed to bead breakage or abrasion. The technique/method for preparing spherical ice beads of mono-dispersed size ranging from 150 to 3000 μm was newly developed. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.008DOI Listing

Dermal delivery of therapeutic DNAzymes via chitosan hydrogels.

Int J Pharm 2019 Apr 3;563:208-216. Epub 2019 Apr 3.

Institute of Bioprocess Engineering and Pharmaceutical Technology, University of Applied Sciences Mittelhessen, Wiesenstrasse 14, 35390 Giessen, Germany; Faculty of Biology and Chemistry, Justus-Liebig University Giessen, Heinrich-Buff-Ring 17, 35392 Giessen, Germany. Electronic address:

Biopharmaceutical development is progressing rapidly. It is imperative that novel drug delivery systems are designed to protect the integrity of the biopharmaceutical, and, at the same time, transport and distribute the drug efficaciously to the target site. Administration of highly specific and sensitive molecules, like therapeutic proteins or nucleic acid-based drugs, present distinct challenges. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.005DOI Listing
April 2019
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Peptide generated anisotropic gold nanoparticles as efficient siRNA vectors.

Int J Pharm 2019 Apr 3;563:198-207. Epub 2019 Apr 3.

School of Biotechnology, Kalinga Institute of Industrial Technology Deemed to be University, Campus 11, Patia, Bhubaneswar, Odisha 751024, India. Electronic address:

Based on the cell penetrating ability of tryptophan-containing peptides, eight linear hexapeptides have been designed, synthesized and explored their efficiency toward the synthesis of gold nanoparticles under sunlight. The peptide generated gold nanoparticles (LP-GNPs) have been characterized by UV-visible spectroscopy, Transmission Electron Microscopy (TEM) and Dynamic Light Scattering (DLS) techniques. The binding ability of LP-GNPs toward siRNA, evaluated by gel electrophoresis indicates that sequence-selective-GNPs without any surface modifications exhibit strong affinity toward negatively charged biomolecules. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.007DOI Listing
April 2019
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Comparative study of liposomes, ethosomes and transfersomes as carriers for enhancing the transdermal delivery of diflunisal: In vitro and in vivo evaluation.

Int J Pharm 2019 Apr 2;563:293-303. Epub 2019 Apr 2.

Pharmacology Department, National Research Centre, El- Buhouth St., Dokki, Cairo 12622, Egypt.

The current study aimed to develop an effective transdermal nanovesicular carrier of diflunisal that provides enhanced delivery through the skin. Two types of nanovesicles, ethosomes and transfersomes, were investigated and compared to conventional liposomes. Ethosomes with variable ethanol contents (10, 30 and 50%) and transfersomes using different edge activators, including sodium deoxycholate, sodium cholate and sodium taurocholate, were prepared and characterized. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.001DOI Listing

Data reconciliation in the Quality-by-Design (QbD) implementation of pharmaceutical continuous tablet manufacturing.

Int J Pharm 2019 Apr 3;563:259-272. Epub 2019 Apr 3.

Davidson School of Chemical Engineering, Purdue University, West Lafayette, IN 47907, United States. Electronic address:

Data provided by in situ sensors is always affected by some level of impreciseness as well as uncertainty in the measurements due to process operation disturbance or material property variance. In-process data precision and reliability should be considered when implementing active product quality control and real-time process decision making in pharmaceutical continuous manufacturing. Data reconciliation is an important strategy to address such imperfections effectively, and to exploit the data redundancy and data correlation based on process understanding. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.003DOI Listing

Amorphous pullulan trehalose microparticle platform for respiratory delivery.

Int J Pharm 2019 Apr 2;563:156-168. Epub 2019 Apr 2.

Department of Mechanical Engineering, University of Alberta, Edmonton, Canada. Electronic address:

Spray drying biologics and small-molecule drugs can increase their thermal stability relative to liquid dosage forms and allow for widespread distribution to developing countries without cold chain infrastructure. In this study, pullulan trehalose powder is spray dried for inhalation. The powder is characterized in terms of manufacturability, physical stability, device compatibility, and aerosol performance. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.04.004DOI Listing
April 2019
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Data analytics on raw material properties to accelerate pharmaceutical drug development.

Int J Pharm 2019 Apr 2;563:122-134. Epub 2019 Apr 2.

Product Development and Supply, GlaxoSmithKline Research & Development, Park Road, SG12 0DP Ware, UK.

Manufacturability of active pharmaceutical ingredients (APIs) is often evaluated by an empirical approach during development due to limited material availability. This brings challenges in designing flexible yet robust manufacturing processes under highly accelerated timelines. Hence, good utilisation of a limited material dataset is key to accelerate the delivery of high quality final drug product into the market at minimum cost and maximum process capacity. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193025
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http://dx.doi.org/10.1016/j.ijpharm.2019.04.002DOI Listing
April 2019
2 Reads

Formulation and optimization of lyophilized nanosuspension tablets to improve the physicochemical properties and provide immediate release of silymarin.

Int J Pharm 2019 Apr 1;563:217-227. Epub 2019 Apr 1.

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Tykistökatu 6A, 20520 Turku, Finland. Electronic address:

Silymarin (SLM) is a hepatoprotective herbal drug characterized by low aqueous solubility and, consequently, low oral bioavailability. The objective of this study was to enhance the physiochemical properties of SLM, through preparation and optimization of lyophilized nanosuspension tablets (LNTs). LNTs were prepared by sonoprecipitation technique followed by a freeze-drying process using both polyvinyl alcohol (PVA) as stabilizer and binder, and mannitol as cryoprotectant and disintegrating agent. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.064DOI Listing
April 2019
1 Read

Dispersibility of phospholipids and their optimization for the efficient production of liposomes using supercritical fluid technology.

Int J Pharm 2019 Mar 30;563:174-183. Epub 2019 Mar 30.

School of Pharmacy, The University of Queensland, Woolloongabba, Brisbane, QLD 4102, Australia. Electronic address:

Liposomes are promising delivery vehicles and offer the added drawcard of being able to be made functional to target tissues such as cardiac muscle and cancerous cells. Current methods to manufacture liposomes need to be improved and supercritical fluid (SCF) technologies may offer a solution. Herein, the dispersibility of six different phospholipids (PLs) was determined in supercritical carbon dioxide (scCO). Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.053DOI Listing
March 2019
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Nanometric ion pair complexes of tobramycin forming microparticles for the treatment of Pseudomonas aeruginosa infections in cystic fibrosis.

Int J Pharm 2019 Mar 29;563:347-357. Epub 2019 Mar 29.

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy. Electronic address:

Sustained pulmonary delivery of tobramycin from microparticles composed of drug/polymer nanocomplexes offers several advantages against traditional delivery methods. Namely, in patients with cystic fibrosis, microparticle delivery can protect the tobramycin being delivered from strong mucoadhesive interactions, thus avoiding effects on its diffusion toward the infection site. Polymeric ion-pair complexes were obtained starting from two synthetic polyanions, through impregnation of their solid dissociated forms with tobramycin in aqueous solution. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.060DOI Listing
March 2019
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Particle engineering of excipients: A mechanistic investigation into the compaction properties of lignin and [co]-spray dried lignin.

Int J Pharm 2019 Mar 29;563:237-248. Epub 2019 Mar 29.

Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick, Ireland. Electronic address:

In this work, lignin was spray dried with sodium lauryl sulphate (SLS) in order to improve the compaction properties of lignin. Bulk level and physicochemical properties of spray dried formulations were measured and compared to as-received lignin and lactose which was used as a reference excipient. Single component tablets from individual powders were prepared and the mechanical properties of these powders were investigated by analysing force-displacement curves recorded during tableting, using a series of compaction equations. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.061DOI Listing

Drug-carrier binding and enzymatic carrier digestion in amorphous solid dispersions containing proteins as carrier.

Int J Pharm 2019 Mar 29;563:358-372. Epub 2019 Mar 29.

Drug Delivery and Disposition, KU Leuven, Department of Pharmaceutical and Pharmacological Sciences, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000 Leuven, Belgium. Electronic address:

In order to further explain the ability of gelatin 50PS and bovine serum albumin (BSA) to generate supersaturation of a series of poorly soluble drugs (carbamazepine, cinnarizine, diazepam, itraconazole, nifedipine, indomethacin, darunavir (ethanolate), ritonavir, fenofibrate, griseofulvin, ketoconazole, naproxen, phenylbutazone and phenytoin), drug-polymer binding was investigated using solution NMR and equilibrium dialysis experiments. Binding characteristics of the biopolymers were compared to those of PVP, PVPVA and HPMC. Since both biopolymers are prone to enzymatic digestion, we evaluated the influence of proteolytic enzymes like pepsin and pancreatin on the dissolution properties of poorly soluble compounds when formulated as amorphous solid dispersions with gelatin 50PS and BSA. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.062DOI Listing
March 2019
5 Reads

Salmeterol Xinafoate (SX) loaded into mucoadhesive solid lipid microparticles for COPD treatment.

Int J Pharm 2019 May 29;562:351-358. Epub 2019 Mar 29.

Istituto di Biomedicina e Immunologia Molecolare (IBIM), CNR, Via Ugo La Malfa, 153, 90146 Palermo, Italy. Electronic address:

Chronic obstructive pulmonary disease (COPD) is one of the main health problems worldwide. It is characterised by chronic inflammation in the lungs that leads to progressive, chronic, largely irreversible airflow obstruction. The use of long-acting β agonists remain today the frontline treatment for COPD with the aim of minimizing side effects and enhancing therapeutic usefulness. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.03.059DOI Listing
May 2019
4 Reads