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Pharmaceutics, Volume 11, Issue 3

2019 March - 47 articles

Cover Story: Drug Transport across Porcine Intestine Using an Ussing Chamber System: Regional Differences and the Effect of P-Glycoprotein and CYP3A4 Activity on Drug Absorption
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Articles (47)

  • Review
  • Open Access
34 Citations
8,310 Views
20 Pages

Pharmaceutical Vehicles for Vaginal and Rectal Administration of Anti-HIV Microbicide Nanosystems

  • Letícia Mesquita,
  • Joana Galante,
  • Rute Nunes,
  • Bruno Sarmento and
  • José das Neves

Prevention strategies play a key role in the fight against HIV/AIDS. Vaginal and rectal microbicides hold great promise in tackling sexual transmission of HIV-1, but effective and safe products are yet to be approved and made available to those in ne...

  • Article
  • Open Access
50 Citations
7,997 Views
22 Pages

Cabazitaxel-Loaded Nanocarriers for Cancer Therapy with Reduced Side Effects

  • Nagavendra Kommineni,
  • Shaheen Mahira,
  • Abraham J. Domb and
  • Wahid Khan

Jevtana® is a micellar cabazitaxel (CBZ) solution that was approved for prostate cancer in 2010, and recently, this drug has been reported for breast cancer. The purpose of this study is to evaluate the mediated delivery of CBZ via liposomes and...

  • Article
  • Open Access
12 Citations
5,991 Views
19 Pages

Combination of Zinc Hyaluronate and Metronidazole in a Lipid-Based Drug Delivery System for the Treatment of Periodontitis

  • Attila Léber,
  • Mária Budai-Szűcs,
  • Edit Urbán,
  • Péter Vályi,
  • Attila Gácsi,
  • Szilvia Berkó,
  • Anita Kovács and
  • Erzsébet Csányi

Background: Despite being a highly prevalent disease and a possible contributor to adult tooth loss, periodontitis possesses no well-established therapy. The aim of the recent study was the development and evaluation of a mucoadhesive monophase lipid...

  • Communication
  • Open Access
18 Citations
4,480 Views
9 Pages

Gold nanocages (AuNCs) are biocompatible and porous nanogold particles that have been widely used in biomedical fields. In this study, hyaluronic acid (HA) and peptide- modified gold nanocages (HA-AuNCs/T/P) loaded with 2-[(aminocarbonyl)amino]-5-(4-...

  • Article
  • Open Access
15 Citations
4,527 Views
13 Pages

A Recombinant Enolase-Montanide™ PetGel A Vaccine Promotes a Protective Th1 Immune Response against a Highly Virulent Sporothrix schenckii by Toluene Exposure

  • Damiana Téllez-Martínez,
  • Deivys Leandro Portuondo,
  • Maria Luiza Loesch,
  • Alexander Batista-Duharte and
  • Iracilda Zeppone Carlos

The effect of vaccination in fungal strains that suffered changes in their virulence by exposure to environmental contaminants is largely known. Growing reports of resistance to antifungal drugs and the emergence of new highly virulent strains, possi...

  • Article
  • Open Access
37 Citations
9,391 Views
23 Pages

Drug absorption across viable porcine intestines was investigated using an Ussing chamber system. The apparent permeability coefficients, Papp,pig, were compared to the permeability coefficients determined in humans in vivo, Peff,human. Eleven drugs...

  • Review
  • Open Access
403 Citations
18,238 Views
45 Pages

Mathematical Modeling of Release Kinetics from Supramolecular Drug Delivery Systems

  • Constantin Mircioiu,
  • Victor Voicu,
  • Valentina Anuta,
  • Andra Tudose,
  • Christian Celia,
  • Donatella Paolino,
  • Massimo Fresta,
  • Roxana Sandulovici and
  • Ion Mircioiu

Embedding of active substances in supramolecular systems has as the main goal to ensure the controlled release of the active ingredients. Whatever the final architecture or entrapment mechanism, modeling of release is challenging due to the moving bo...

  • Article
  • Open Access
48 Citations
10,656 Views
20 Pages

Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

  • Somchai Sawatdee,
  • Apichart Atipairin,
  • Attawadee Sae Yoon,
  • Teerapol Srichana,
  • Narumon Changsan and
  • Tan Suwandecha

Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was...

  • Article
  • Open Access
4 Citations
3,320 Views
18 Pages

P-glycoprotein (P-gp)-mediated efflux of docetaxel in the gastrointestinal tract mainly impedes its oral chemotherapy. Recently, LC478, a novel di-substituted adamantyl derivative, was identified as a non-cytotoxic P-gp inhibitor in vitro. Here, we a...

  • Article
  • Open Access
38 Citations
7,031 Views
13 Pages

Development and Evaluation of Poorly Water-Soluble Celecoxib as Solid Dispersions Containing Nonionic Surfactants Using Fluidized-Bed Granulation

  • Hyeok Jin Kwon,
  • Eun-Ji Heo,
  • Young-Hwan Kim,
  • Sarah Kim,
  • Young-Ha Hwang,
  • Ji-Mi Byun,
  • Se Hyeop Cheon,
  • Sang Yeob Park,
  • Dong Yun Kim and
  • Dong-Jin Jang
  • + 2 authors

The purpose of this study is to develop a solid dispersion system with improved dissolution, absorption, and patient compliance of poorly water-soluble celecoxib (CXB). Instead of sodium lauryl sulfate (SLS), an anionic surfactant used in the markete...

  • Article
  • Open Access
24 Citations
4,997 Views
20 Pages

Tenofovir Hot-Melt Granulation using Gelucire® to Develop Sustained-Release Vaginal Systems for Weekly Protection against Sexual Transmission of HIV

  • Fernando Notario-Pérez,
  • Raúl Cazorla-Luna,
  • Araceli Martín-Illana,
  • Roberto Ruiz-Caro,
  • Juan Peña and
  • María-Dolores Veiga

Hot-melt granulation is a technique used to obtain granules by dispersing a drug in polymers at a high temperature. Tenofovir, an antiretroviral drug with proven activity as a vaginal microbicide, was dispersed in melted Gelucire® (or a mixture o...

  • Article
  • Open Access
80 Citations
7,030 Views
17 Pages

In Vitro Enhanced Skin Permeation and Retention of Imiquimod Loaded in β-Cyclodextrin Nanosponge Hydrogel

  • Monica Argenziano,
  • Adam Haimhoffer,
  • Chiara Bastiancich,
  • László Jicsinszky,
  • Fabrizio Caldera,
  • Francesco Trotta,
  • Sara Scutera,
  • Daniela Alotto,
  • Mara Fumagalli and
  • Roberta Cavalli
  • + 2 authors

Imiquimod (IMQ) is an immune response modifier clinically used for the treatment of various topical diseases. However, its poor aqueous solubility and skin penetration capability make the topical delivery of IMQ a challenging task. This work aims at...

  • Article
  • Open Access
42 Citations
8,163 Views
10 Pages

Evaluation of a Methylcellulose and Hyaluronic Acid Hydrogel as a Vehicle for Rectal Delivery of Biologics

  • Andreea Aprodu,
  • Julia Mantaj,
  • Bahijja Raimi-Abraham and
  • Driton Vllasaliu

Biologics have changed the management of Inflammatory Bowel Disease (IBD), but there are concerns regarding unexpected systemic toxicity and loss of therapeutic response following administration by injection. Local delivery of biologics directly to t...

  • Review
  • Open Access
161 Citations
14,045 Views
14 Pages

The Digital Pharmacies Era: How 3D Printing Technology Using Fused Deposition Modeling Can Become a Reality

  • Maisa R. P. Araújo,
  • Livia L. Sa-Barreto,
  • Tais Gratieri,
  • Guilherme M. Gelfuso and
  • Marcilio Cunha-Filho

The pharmaceutical industry is set to join the fourth industrial revolution with the 3D printing of medicines. The application of 3D printers in compounding pharmacies will turn them into digital pharmacies, wrapping up the telemedicine care cycle an...

  • Review
  • Open Access
776 Citations
32,303 Views
29 Pages

Routes of drug administration and the corresponding physicochemical characteristics of a given route play significant roles in therapeutic efficacy and short term/long term biological effects. Each delivery method has favorable aspects and limitation...

  • Article
  • Open Access
42 Citations
6,548 Views
22 Pages

The Self-Assembly Phenomenon of Poloxamers and Its Effect on the Dissolution of a Poorly Soluble Drug from Solid Dispersions Obtained by Solvent Methods

  • Joanna Szafraniec,
  • Agata Antosik,
  • Justyna Knapik-Kowalczuk,
  • Krzysztof Chmiel,
  • Mateusz Kurek,
  • Karolina Gawlak,
  • Joanna Odrobińska,
  • Marian Paluch and
  • Renata Jachowicz

The self-assembly phenomenon of amphiphiles has attracted particular attention in recent years due to its wide range of applications. The formation of nanoassemblies able to solubilize sparingly water-soluble drugs was found to be a strategy to solve...

  • Article
  • Open Access
35 Citations
5,562 Views
16 Pages

Design and Characterization of a New Quercus Suber-Based Pickering Emulsion for Topical Application

  • Catarina Carriço,
  • Pedro Pinto,
  • Angélica Graça,
  • Lídia Maria Gonçalves,
  • Helena Margarida Ribeiro and
  • Joana Marto

Quercus Suber Bark from Quercus suber L. is a natural, renewable and biodegradable biomaterial with multifunctional proprieties. In this study, we used it as solid particles to stabilize a Pickering emulsion. The main goal was to produce an optimized...

  • Review
  • Open Access
298 Citations
20,629 Views
26 Pages

Approximately 40% of new chemical entities (NCEs), including anticancer drugs, have been reported as poorly water-soluble compounds. Anticancer drugs are classified into biologic drugs (monoclonal antibodies) and small molecule drugs (nonbiologic ant...

  • Article
  • Open Access
22 Citations
6,706 Views
10 Pages

Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban

  • Minsoo Kim,
  • Heebin Son,
  • Keumhan Noh,
  • Eunyoung Kim,
  • Beom Soo Shin and
  • Wonku Kang

Concomitant use of rivaroxaban with non-dihydropyridine calcium channel blockers (non-DHPs) might lead to an increase of systemic rivaroxaban exposure and anticoagulant effects in relation to the inhibition of metabolic enzymes and/or transporters by...

  • Communication
  • Open Access
21 Citations
5,431 Views
21 Pages

Fibromyalgia (FM) and myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) are diseases of unknown etiology presenting complex and often overlapping symptomatology. Despite promising advances on the study of miRNomes of these diseases, no vali...

  • Review
  • Open Access
25 Citations
7,558 Views
26 Pages

What Drives Innovation: The Canadian Touch on Liposomal Therapeutics

  • Ada W. Y. Leung,
  • Carolyn Amador,
  • Lin Chuan Wang,
  • Urmi V. Mody and
  • Marcel B. Bally

Liposomes are considered one of the most successful drug delivery systems (DDS) given their established utility and success in the clinic. In the past 40–50 years, Canadian scientists have made ground-breaking discoveries, many of which were su...

  • Review
  • Open Access
22 Citations
6,610 Views
32 Pages

This review explores the use of energy sources, including ultrasound, magnetic fields, and external beam radiation, to trigger the delivery of drugs from liposomes in a tumor in a spatially-specific manner. Each section explores the mechanism(s) of d...

  • Article
  • Open Access
60 Citations
7,339 Views
13 Pages

Functional Magnetic Core-Shell System-Based Iron Oxide Nanoparticle Coated with Biocompatible Copolymer for Anticancer Drug Delivery

  • Thai Thanh Hoang Thi,
  • Diem-Huong Nguyen Tran,
  • Long Giang Bach,
  • Hieu Vu-Quang,
  • Duy Chinh Nguyen,
  • Ki Dong Park and
  • Dai Hai Nguyen

Polymer coating has drawn increasing attention as a leading strategy to overcome the drawbacks of superparamagnetic iron oxide nanoparticles (SPIONs) in targeted delivery of anticancer drugs. In this study, SPIONs were modified with heparin-Poloxamer...

  • Article
  • Open Access
51 Citations
11,522 Views
19 Pages

A Mathematical Approach to Consider Solid Compressibility in the Compression of Pharmaceutical Powders

  • Isabell Wünsch,
  • Jan Henrik Finke,
  • Edgar John,
  • Michael Juhnke and
  • Arno Kwade

In-die compression analysis is an effective method for the characterization of powder compressibility. However, physically unreasonable apparent solid fractions above one or apparent in-die porosities below zero are often calculated for higher compre...

  • Article
  • Open Access
21 Citations
7,463 Views
18 Pages

Exploring Bioequivalence of Dexketoprofen Trometamol Drug Products with the Gastrointestinal Simulator (GIS) and Precipitation Pathways Analyses

  • Marival Bermejo,
  • Gislaine Kuminek,
  • Jozef Al-Gousous,
  • Alejandro Ruiz-Picazo,
  • Yasuhiro Tsume,
  • Alfredo Garcia-Arieta,
  • Isabel González-Alvarez,
  • Bart Hens,
  • Deanna Mudie and
  • Gordon L. Amidon
  • + 2 authors

The present work aimed to explain the differences in oral performance in fasted humans who were categorized into groups based on the three different drug product formulations of dexketoprofen trometamol (DKT) salt—Using a combination of in vitr...

  • Article
  • Open Access
52 Citations
4,390 Views
7 Pages

Epirubicin-capped silver nanoparticles (NPs) were synthesized through a one-pot method by using epirubicin as both the functional drug and the reducing agent of Ag+ to Ag0. The preparation process was accomplished in 1 h. In addition, the obtained ep...

  • Review
  • Open Access
116 Citations
10,542 Views
21 Pages

Epilepsy is the fourth most common global neurological problem, which can be considered a spectrum disorder because of its various causes, seizure types, its ability to vary in severity and the impact from person to person, as well as its range of co...

  • Review
  • Open Access
29 Citations
6,303 Views
28 Pages

Computational Approaches in Theranostics: Mining and Predicting Cancer Data

  • Tânia F. G. G. Cova,
  • Daniel J. Bento and
  • Sandra C. C. Nunes

The ability to understand the complexity of cancer-related data has been prompted by the applications of (1) computer and data sciences, including data mining, predictive analytics, machine learning, and artificial intelligence, and (2) advances in i...

  • Article
  • Open Access
12 Citations
4,888 Views
19 Pages

Contribution of Molecular Structure to Self-Assembling and Biological Properties of Bifunctional Lipid-Like 4-(N-Alkylpyridinium)-1,4-Dihydropyridines

  • Martins Rucins,
  • Pavels Dimitrijevs,
  • Klavs Pajuste,
  • Oksana Petrichenko,
  • Ludmila Jackevica,
  • Anita Gulbe,
  • Signe Kibilda,
  • Krisjanis Smits,
  • Mara Plotniece and
  • Aiva Plotniece
  • + 5 authors

The design of nanoparticle delivery materials possessing biological activities is an attractive strategy for the development of various therapies. In this study, 11 cationic amphiphilic 4-(N-alkylpyridinium)-1,4-dihydropyridine (1,4-DHP) derivatives...

  • Article
  • Open Access
32 Citations
6,085 Views
19 Pages

Sustained Release from Injectable Composite Gels Loaded with Silver Nanowires Designed to Combat Bacterial Resistance in Bone Regeneration Applications

  • Arianna De Mori,
  • Meena Hafidh,
  • Natalia Mele,
  • Rahmi Yusuf,
  • Guido Cerri,
  • Elisabetta Gavini,
  • Gianluca Tozzi,
  • Eugen Barbu,
  • Mariateresa Conconi and
  • Marta Roldo
  • + 1 author

One-dimensional nanostructures, such as silver nanowires (AgNWs), have attracted considerable attention owing to their outstanding electrical, thermal and antimicrobial properties. However, their application in the prevention of infections linked to...

  • Review
  • Open Access
157 Citations
7,472 Views
27 Pages

Effects of Silicon Compounds on Biomineralization, Osteogenesis, and Hard Tissue Formation

  • Werner Götz,
  • Edda Tobiasch,
  • Steffen Witzleben and
  • Margit Schulze

Bioinspired stem cell-based hard tissue engineering includes numerous aspects: The synthesis and fabrication of appropriate scaffold materials, their analytical characterization, and guided osteogenesis using the sustained release of osteoinducing an...

  • Review
  • Open Access
252 Citations
16,106 Views
20 Pages

Strategies to Enhance Drug Absorption via Nasal and Pulmonary Routes

  • Maliheh Ghadiri,
  • Paul M. Young and
  • Daniela Traini

New therapeutic agents such as proteins, peptides, and nucleic acid-based agents are being developed every year, making it vital to find a non-invasive route such as nasal or pulmonary for their administration. However, a major concern for some of th...

  • Review
  • Open Access
4 Citations
6,145 Views
18 Pages

Although current antiretroviral drug therapy can suppress the replication of human immunodeficiency virus (HIV), a lifelong prescription is necessary to avoid viral rebound. The problem of persistent and ineradicable viral reservoirs in HIV-infected...

  • Article
  • Open Access
59 Citations
6,505 Views
16 Pages

Drug Solubility Enhancement through the Preparation of Multicomponent Organic Materials: Eutectics of Lovastatin with Carboxylic Acids

  • Andrea Mariela Araya-Sibaja,
  • José Roberto Vega-Baudrit,
  • Teodolito Guillén-Girón,
  • Mirtha Navarro-Hoyos and
  • Silvia Lucia Cuffini

Lovastatin (LOV) is a drug used to treat hypercholesterolemia. Recent studies have identified its antioxidant effects and potential use in the treatment of some types of cancer. However, the low bioavailability related to its poor water solubility li...

  • Article
  • Open Access
38 Citations
6,467 Views
18 Pages

The impact of formulation and process variables on the in-vitro release of prednisone from a multiple-unit pellet system was investigated. Box-Behnken Response Surface Methodology (RSM) was used to generate multivariate experiments. The extrusion-sph...

  • Review
  • Open Access
71 Citations
8,964 Views
22 Pages

Liposomal formulations have been developed to improve the therapeutic index of encapsulated drugs by altering the balance of on- and off-targeted distribution. The improved therapeutic efficacy of liposomal drugs is primarily attributed to enhanced d...

  • Article
  • Open Access
18 Citations
6,374 Views
16 Pages

Mathematical Modelling of Intravenous Thrombolysis in Acute Ischaemic stroke: Effects of Dose Regimens on Levels of Fibrinolytic Proteins and Clot Lysis Time

  • Boram Gu,
  • Andris Piebalgs,
  • Yu Huang,
  • Colin Longstaff,
  • Alun D. Hughes,
  • Rongjun Chen,
  • Simon A. Thom and
  • Xiao Yun Xu

Thrombolytic therapy is one of the medical procedures in the treatment of acute ischaemic stroke (AIS), whereby the tissue plasminogen activator (tPA) is intravenously administered to dissolve the obstructive blood clot. The treatment of AIS by throm...

  • Article
  • Open Access
38 Citations
4,227 Views
16 Pages

Enhanced Oral Bioavailability, Anti-Tumor Activity and Hepatoprotective Effect of 6-Shogaol Loaded in a Type of Novel Micelles of Polyethylene Glycol and Linoleic Acid Conjugate

  • Huiyun Zhang,
  • Qilong Wang,
  • Congyong Sun,
  • Yuan Zhu,
  • Qiuxuan Yang,
  • Qiuyu Wei,
  • Jiaxin Chen,
  • Wenwen Deng,
  • Michael Adu-Frimpong and
  • Ximing Xu
  • + 1 author

6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were design...

  • Article
  • Open Access
11 Citations
5,935 Views
26 Pages

Previous observations demonstrated that cimetidine decreased the clearance of procainamide (PA) and/or N-acetylprocainamide (NAPA; the primary metabolite of PA) resulting in the increased systemic exposure and the decrease of urinary excretion. Despi...

  • Article
  • Open Access
25 Citations
4,443 Views
14 Pages

Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration

  • Maria Cristina Bonferoni,
  • Luca Ferraro,
  • Barbara Pavan,
  • Sarah Beggiato,
  • Elena Cavalieri,
  • Paolo Giunchedi and
  • Alessandro Dalpiaz

The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified...

  • Article
  • Open Access
4 Citations
3,980 Views
16 Pages

Renal impairment (RI) is a highly prevalent disease which can alter the pharmacokinetics (PK) of xenobiotics, including those that are predominately metabolized. The expression and activity of drug metabolizing enzymes (DMEs) and protein binding of c...

  • Article
  • Open Access
22 Citations
4,687 Views
19 Pages

Development of Novel EE/Alginate Polyelectrolyte Complex Nanoparticles for Lysozyme Delivery: Physicochemical Properties and In Vitro Safety

  • Sabrina Sepúlveda-Rivas,
  • Hans F. Fritz,
  • Camila Valenzuela,
  • Carlos A. Santiviago and
  • Javier O. Morales

The number of biologic drugs has increased in the pharmaceutical industry due to their high therapeutic efficacy and selectivity. As such, safe and biocompatible delivery systems to improve their stability and efficacy are needed. Here, we developed...

  • Article
  • Open Access
40 Citations
5,422 Views
20 Pages

The functional physicochemical properties of nicotine (NIC)-loaded composite freeze-dried wafers and solvent-evaporated films comprising hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA), stabilized with magnesium aluminium silicate (MAS),...

  • Article
  • Open Access
31 Citations
7,041 Views
16 Pages

Investigation of Crystallization and Salt Formation of Poorly Water-Soluble Telmisartan for Enhanced Solubility

  • Chulhun Park,
  • Nileshkumar M. Meghani,
  • Yongkwan Shin,
  • Euichaul Oh,
  • Jun-Bom Park,
  • Jing-Hao Cui,
  • Qing-Ri Cao,
  • Thao Truong-Dinh Tran,
  • Phuong Ha-Lien Tran and
  • Beom-Jin Lee

The crystal changes and salt formation of poorly water-soluble telmisartan (TEL) in various solvents were investigated for enhanced solubility, stability and crystallinity. Polymorphic behaviors of TEL were characterized by dispersing in distilled wa...

  • Perspective
  • Open Access
60 Citations
5,501 Views
16 Pages

Parenteral amphotericin B has been considered as first-line therapy in the treatment of systemic fungal and parasitic infections, however its use has been associated with a number of limitations including affordability, accessibility, and an array of...

  • Article
  • Open Access
25 Citations
5,215 Views
13 Pages

Three-Step Thermal Drawing for Rapid Prototyping of Highly Customizable Microneedles for Vascular Tissue Insertion

  • KangJu Lee,
  • Seung Hyun Park,
  • JiYong Lee,
  • Suho Ryu,
  • Chulmin Joo and
  • WonHyoung Ryu

Microneedles (MNs) have been extensively developed over the last two decades, and highly efficient drug delivery was demonstrated with their minimal invasiveness via a transdermal route. Recently, MNs have not only been applied to the skin but also t...

  • Review
  • Open Access
73 Citations
6,514 Views
23 Pages

Neuronanomedicine: An Up-to-Date Overview

  • Daniel Mihai Teleanu,
  • Cristina Chircov,
  • Alexandru Mihai Grumezescu and
  • Raluca Ioana Teleanu

The field of neuronanomedicine has recently emerged as the bridge between neurological sciences and nanotechnology. The possibilities of this novel perspective are promising for the diagnosis and treatment strategies of severe central nervous system...

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Pharmaceutics - ISSN 1999-4923