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Dendrimer-conjugated peptide vaccine enhances clearance of Chlamydia trachomatis genital infection
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Ingrid S. Ganda, Qian Zhong, Mirabela Hali, Ricardo L.C. Albuquerque, Francine F. Padilha, Sandro R.P. da Rocha, Judith A. Whittum-Hudson Peptide-based vaccines have emerged in recent years as promising candidates in the prevention of infectious diseases. However, there are many challenges to maintaining in vivo peptide stability and enhancement of peptide immunogenicity to generate protective immunity which enhances clearance of infections. Here, a dendrimer-based carrier system is proposed for peptide-ba...
Source: International Journal of Pharmaceutics - May 27, 2017 Category: Drugs & Pharmacology Source Type: research

Polymer coated mucoadhesive liposomes intended for the management of xerostomia
In this study three different types of liposomes (positively, negatively and neutrally charged) were coated with five different types of polymers: low-methoxylated pectin (LM-pectin), high-methoxylated pectin (HM-pectin), alginate, chitosan and hydrophobically modified ethyl hydroxyethyl cellulose (HM-EHEC). The particle size and the zeta potential of the obtained carriers were tested by measuring dynamic light scattering (DLS) and electrophoretic mobility. Later on, selected positively charged liposomes were deposited on a negatively charged mica surface and depicted by atomic force microscopy (AFM). The water sorption pr...
Source: International Journal of Pharmaceutics - May 26, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted co-delivery of polypyrrole and rapamycin by trastuzumab-conjugated liposomes for combined chemo-photothermal therapy
In this study, we aimed to present a strategy to combine chemo and phototherapy and targeted delivery via monoclonal antibody for enhanced anticancer effects. We co-loaded a chemotherapeutic agent, rapamycin, and a photosensitizer, polypyrrole, in trastuzumab-conjugated liposomes (LRPmAb) for combined chemo-photothermal therapy. LRPmAb had small size (172.2±9.6nm), narrow distribution, and negative ζ-potential (−12.0±0.3mV). In addition, LRPmAb showed pH- and temperature-dependent release profiles. LRPmAb showed significantly enhanced uptake in BT-474 cells, a natural HER2/neu expressing cell line....
Source: International Journal of Pharmaceutics - May 25, 2017 Category: Drugs & Pharmacology Source Type: research

Cucurbit[7]-assisted sustained release of human calcitonin from thermosensitive block copolymer hydrogel
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Hui Shang, Xiaobin Chen, Yanpeng Liu, Lin Yu, Jianshu Li, Jiandong Ding Conventional formulations of human calcitonin (hCT), a peptide drug, normally suffer from limited therapeutic efficacy with low stability and short half-life. We have found that the fibrillation of highly amyloidogenic hCT can be inhibited by cucurbit[7] (CB[7]), an amphiphilic small molecule. Meanwhile, a thermogelling copolymer was found to be a suitable candidate for sustained delivery of peptide/protein drugs. Herein, we report a l...
Source: International Journal of Pharmaceutics - May 25, 2017 Category: Drugs & Pharmacology Source Type: research

Poly(acrylic acid) microspheres loaded with superparamagnetic iron oxide nanoparticles for transcatheter arterial embolization and MRI detectability: In vitro and in vivo evaluation
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Zi-Yuan Li, Xiao-Ya Qin, Li-Ying Guo, Huan Wang, Xiao-Xin Liu, Zhuo-Zhao Zheng, Hai-Tao Guan, Li Song, Ying-Hua Zou, Tian-Yuan Fan To develop embolic microspheres with MRI detectability, superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized and mixed with monomer of acrylic acid to prepare SPIONs-loaded polymerized microspheres (SPMs) by inverse suspension polymerization method. The SPMs were evaluated for the ability of embolization by investigating the morphology, particle size, elasticity...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Behaviour of silver nanoparticles in simulated saliva and gastrointestinal fluids
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Lucie Pinďáková, Věra Kašpárková, Kristina Kejlová, Markéta Dvořáková, Daniel Krsek, Dagmar Jírová, Lucie Kašparová Continuously increasing application of silver nanoparticles (AgNPs) requires information on their safety and performance under biological conditions. Assessment of AgNPs in biological systems is also related to availability of robust toxicological methods for evaluation of toxic potential of AgNPs an...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Characterization of new crystalline forms of hydroxyprogesterone caproate
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Jeffrey Caplette, Timothy Frigo, Michael Jozwiakowski, Helene Shea, Mahmoud Mirmehrabi, Peter Müller A systematic polymorph screening process was conducted on the steroid hydroxyprogesterone caproate, which had only one previously described orthorhombic crystalline form (A), in order to fully elucidate its solid state properties. Cooling, anti-solvent and evaporative techniques largely reproduced the same polymorph, but slurries in various solvents over two days produced a new triclinic form (B). Expe...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Sertaconazole nitrate loaded nanovesicular systems for targeting skin fungal infection: In-vitro, ex-vivo and in-vivo evaluation
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Menna M. Abdellatif, Islam A. Khalil, Mahmoud A.F. Khalil The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin ...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Development of modified release 3D printed tablets (printlets) with pharmaceutical excipients using additive manufacturing
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Alvaro Goyanes, Fabrizio Fina, Annalisa Martorana, Daniel Sedough, Simon Gaisford, Abdul W. Basit The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into ent...
Source: International Journal of Pharmaceutics - May 24, 2017 Category: Drugs & Pharmacology Source Type: research

Evaluation of lipid-stabilised tripropionin nanodroplets as a delivery route for combretastatin A4
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Victoria Mico, Antonia Charalambous, Sally A. Peyman, Radwa H. Abou-Saleh, Alexander F. Markham, P. Louise Coletta, Stephen D. Evans Lipid-based nanoemulsions are a cheap and elegant route for improving the delivery of hydrophobic drugs. Easy and quick to prepare, nanoemulsions have promise for the delivery of different therapeutic agents. Although multiple studies have investigated the effects of the oil and preparation conditions on the size of the nanoemulsion nanodroplets for food applications, analogo...
Source: International Journal of Pharmaceutics - May 22, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted si-RNA with liposomes and exosomes (extracellular vesicles): How to unlock the potential
Publication date: 20 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 2 Author(s): Sophia Antimisiaris, Spyridon Mourtas, Konstantina Papadia The concept of RNA interference therapeutics has been initiated 18 years ago, and the main bottleneck for translation of the technology into therapeutic products remains the delivery of functional RNA molecules into the cell cytoplasm. In the present review article after an introduction about the theoretical basis of RNAi therapy and the main challenges encountered for its realization, an overview of the different types of delivery systems or carriers, used...
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Delivery of siRNAs
Publication date: 20 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 2 Author(s): Gaetano Lamberti (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Old drug, new wrapping − A possible comeback for chloramphenicol?
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Sveinung G. Ingebrigtsen, Alena Didriksen, Mona Johannessen, Nataša Škalko-Basnet, Ann Mari Holsæter The antimicrobial drug chloramphenicol (CAM) exhibits activity against resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA). However, its use has been limited due to its toxicity. As the threat of antibiotic resistance continues to grow, a promising approach might be to increase the use of historical antimicrobial agents that demonstrate clinical efficacy, but a...
Source: International Journal of Pharmaceutics - May 21, 2017 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers employing polyphenols as promising anticancer agents: Quality by design (QbD) approach
This article aims to review the science behind development of NLCs and role of polyphenols as promising anticancer agents. Principles of Quality by Design (QbD) have also been explained which are used in formulation-development of many nanoparticles, including NLCs, as reported in literature. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 20, 2017 Category: Drugs & Pharmacology Source Type: research

On the role of forces governing particulate interactions in pharmaceutical systems: A review
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Saurabh Sarkar, Raj Mukherjee, Bodhisattwa Chaudhuri Process understanding for designing, optimizing and scaling of pharmaceutical unit operations is fundamentally important to address concerns of high risks, monumental costs, and productivity decline in the pharmaceutical industry. This is especially important in the rapidly changing landscape of the pharmaceutical industry. Pharmaceutical processes majorly deal with multiphase, multicomponent flows, basics of which are discussed in terms of fundamental c...
Source: International Journal of Pharmaceutics - May 20, 2017 Category: Drugs & Pharmacology Source Type: research

A quality by design (QbD) twin —Screw extrusion wet granulation approach for processing water insoluble drugs
In this study, a Quality by Design (QbD) approach was used to identify the effect of formulation parameters in a twin screw wet extrusion granulation process for the manufacturing of ibuprofen (IBU) granules with increased dissolution rates. A fractional factorial Design of Experiment (DoE) was used to investigate the effect of the excipient composition, binder amount and liquid to solid (L/S) ratio (independent variables) on drug dissolution rates, median particle size diameter and specific surface area (dependent variables). The intra-granular addition of the binder in inorganic/polymer blends processed with ethanol as g...
Source: International Journal of Pharmaceutics - May 19, 2017 Category: Drugs & Pharmacology Source Type: research

Paclitaxel: What has been done and the challenges remain ahead
We present an overview of the preclinical and clinical data of these systems including their pharmacokinetics, dose and administration, adverse events and clinical efficacy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 18, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and characterization of isoniazid-loaded crude soybean lecithin liposomes
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Christian Isalomboto Nkanga, Rui Werner Krause, Xavier Siwe Noundou, Roderick Bryan Walker Tuberculosis (TB) is a poverty related infectious disease that is rapidly giving rise to public health concerns. Lengthy drug administration and frequent adverse side-effects associated with TB treatment make anti-tubercular drugs (ATDs) good candidates for drug delivery studies. This work aimed to formulate and prepare liposomes as a cost-effective option for ATD delivery. Liposomes were prepared by film hydration u...
Source: International Journal of Pharmaceutics - May 18, 2017 Category: Drugs & Pharmacology Source Type: research

Design of nonionic micelle-laden polysaccharide hydrogels for controlled delivery of hydrophobic drugs
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Silvia Zarate Munoz, Roman Zhadan, Edgar Acosta The incorporation of micelle self-assembly in hydrogels has been used to produce self-healing materials, materials with tunable mechanical properties, and hydrophilic or hydrophobic drug delivery systems. However, little is known about the connection among formulation – structure – properties (particularly transport) in these systems. This connection is explored in alkyl ethoxylate micelle-laden gellan gum hydrogels used as delivery system for the...
Source: International Journal of Pharmaceutics - May 18, 2017 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetic and screening studies of the interaction between mononuclear phagocyte system and nanoparticle formulations and colloid forming drugs
This study suggests the MPS profiling platform is an effective method to screen and differentiate the important characteristics of NPs and colloid-forming drugs that affect their in vivo clearance. Implications of these findings on preclinical prediction of human clearance are discussed. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 18, 2017 Category: Drugs & Pharmacology Source Type: research

Microemulsion utility in pharmaceuticals: Implications for multi-drug delivery
This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10–100nm diameter, that form spontaneously upon mixing of oil, water and emulsifier. This review is the first to address advantages and disadvantages, as well as considerations and challenges in multi-drug delivery. For the period 1 January 2011–30 April 2016, 431 publications related to microemulsion drug delivery were identified and screened according to microemulsion, drug classification, and surfactant t...
Source: International Journal of Pharmaceutics - May 17, 2017 Category: Drugs & Pharmacology Source Type: research

On the role of API in determining porosity, pore structure and bulk modulus of the skeletal material in pharmaceutical tablets formed with MCC as sole excipient
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Cathy Ridgway, Prince Bawuah, Daniel Markl, J. Axel Zeitler, Jarkko Ketolainen, Kai-Erik Peiponen, Patrick Gane The physical properties and mechanical integrity of pharmaceutical tablets are of major importance when loading with active pharmaceutical ingredient(s) (API) in order to ensure ease of processing, control of dosage and stability during transportation and handling prior to patient consumption. The interaction between API and excipient, acting as functional extender and binder, however, is little ...
Source: International Journal of Pharmaceutics - May 16, 2017 Category: Drugs & Pharmacology Source Type: research

Cubosomes post-loaded with antimicrobial peptides: characterization, bactericidal effect and proteolytic stability
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Lukas Boge, Anita Umerska, Nada Matougui, Helena Bysell, Lovisa Ringstad, Mina Davoudi, Jonny Eriksson, Katarina Edwards, Martin Andersson Novel antibiotics, such as antimicrobial peptides (AMPs), have recently attended more and more attraction. In this work, dispersed cubic liquid crystalline gel (cubosomes) was used as drug delivery vehicles for three AMPs (AP114, DPK-060 and LL-37). Association of peptides onto cubosomes was studied at two cubosome/peptide ratios using high performance liquid chromatogr...
Source: International Journal of Pharmaceutics - May 16, 2017 Category: Drugs & Pharmacology Source Type: research

A new chemotherapy agent-free theranostic system composed of graphene oxide nano-complex and aptamers for treatment of cancer cells
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Amirhossein Bahreyni, Rezvan Yazdian-Robati, Shirin Hashemitabar, Mohammad Ramezani, Pouria Ramezani, Khalil Abnous, Seyed Mohammad Taghdisi The common cancer treatment strategies like chemotherapy and radiotherapy are nonspecific and can trigger severe side effects by damaging normal cells. So, targeted cancer therapies, such as apoptosis induction, have attracted great attention in recent years. In this project, two nano-complexes, MUC1 aptamer-NAS-24 aptamer-Graphene oxide (GO) and MUC1 aptamer-Cytochro...
Source: International Journal of Pharmaceutics - May 16, 2017 Category: Drugs & Pharmacology Source Type: research

Mucopenetrating nanoparticles for enhancement of oral bioavailability of furosemide: In vitro and in vivo evaluation/sub-acute toxicity study
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Salma El-Sayed Radwan, Magda Samir Sokar, Doaa Ali Abdelmonsif, Amal Hassan El-Kamel The aim of this study was to formulate and evaluate chitosan (CS)/alginate (ALG) nanoparticles (NPs) loaded with furosemide (FSM) in an attempt to enhance its release, permeability and bioavailability. Non-everted gut sac method was used to evaluate the ex vivo permeation of FSM from its suspension and the selected CS/ALG NPs formulation. The pharmacokinetic parameters of FSM subsequent to oral administration of the select...
Source: International Journal of Pharmaceutics - May 16, 2017 Category: Drugs & Pharmacology Source Type: research

Organic-inorganic hybrid nanoparticles controlled delivery system for anticancer drugs
In this study, iron oxide nanoparticles were prepared then surface modified via diazonium chemistry and coated with chitosan, and its derivative chitosan-grafted polylactic acid. The purpose was to increase the stability of the nanoparticles in physiological solution, heighten drug-loading capacity, prolong the release, reduce the initial burst effect and improve in vitro cytotoxicity of the model drug doxorubicin. The materials were characterized by DLS, ζ-potential, SEM, TGA, magnetization curves and release kinetics studies. Results confirmed the spherical shape, the presence of the coat and the advantages of using...
Source: International Journal of Pharmaceutics - May 16, 2017 Category: Drugs & Pharmacology Source Type: research

Potential and future scope of nanoemulgel formulation for topical delivery of lipophilic drugs
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Pinaki Sengupta, Bappaditya Chatterjee The Nanoemulgel drug delivery system is a formulation related intervention to improve the systemic delivery and therapeutic profile of lipophilic drugs. Nanoemulgel is an amalgamated formulation of two different systems in which nanoemulsion containing drug is incorporated into a gel base. The fusion of the two systems makes this formulation advantageous in several ways. Lipophilic drugs can be easily incorporated and the skin permeability of the incorporated drugs ca...
Source: International Journal of Pharmaceutics - May 15, 2017 Category: Drugs & Pharmacology Source Type: research

SN38 conjugated hyaluronic acid gold nanoparticles as a novel system against metastatic colon cancer cells
In this study SN38, a highly potent cytotoxic agent, was conjugated to negatively charged hyaluronic acid (HA), which was deposited on the surface of the positively charged gold nanoparticles via electrostatic interaction. The drug conjugation and its interaction with gold nanoparticles were verified by 1H NMR and UV–vis spectroscopies, respectively. The prepared SN38-HA gold NPs are negatively charged spherical nanoparticles with an average size of 75±10nm. In vitro release study revealed that drug release in acidic conditions (pH 5.2) was faster than that in physiological pH. Red light emitting diode (LED, 6...
Source: International Journal of Pharmaceutics - May 14, 2017 Category: Drugs & Pharmacology Source Type: research

Dipicolinic acid as a novel spore-inspired excipient for antibody formulation
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Iris L. Batalha, Peng Ke, Esther Tejeda-Montes, Shahid Uddin, Christopher F. van der Walle, Graham Christie Ionic excipients are commonly used in aqueous therapeutic monoclonal antibody (mAb) formulations. Novel excipients are of industrial interest, with a recent focus on Arg salt forms and their application as viscosity reducing and stabilizing additives. Here, we report that the calcium salt of dipicolinic acid (DPA, pyridine-2,6-dicarboxylic acid), uniquely present in nature in the core of certain bact...
Source: International Journal of Pharmaceutics - May 14, 2017 Category: Drugs & Pharmacology Source Type: research

Fluorinated ionic liquids for protein drug delivery systems: Investigating their impact on the structure and function of lysozyme
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Márcia Alves, Nicole S.M. Vieira, Luís Paulo N. Rebelo, João M.M. Araújo, Ana B. Pereiro, Margarida Archer Since the approval of recombinant human insulin by FDA in 1982, more than 200 proteins are currently available for pharmaceutical use to treat a wide range of diseases. However, innovation is still required to develop effective approaches for drug delivery. Our aim is to investigate the potential use of fluorinated ionic liquids (FILs) as drug delivery systems (DDS) for the...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of nanocarriers and excipients for preparation of nanoembedded microparticles
In this study, different polymer nanocarriers (poly(lactide-co-glycolide), poly(styrene), chitosan and dendrimers) were used for preparing NEMs by spray-drying. Further, distinct matrix excipients were investigated including sugars (i.e., trehalose, sucrose, mannitol) and polymers (poly(vinyl pyrrolidone) and poly(ethylene glycol)), and the characteristics and performance of NEMs were studied in detail. It was found that with increasing hydrophilicity of the polymer nanocarriers, an increasing amount of excipient was necessary to stabilize the nanoparticles. NEMs containing polyplexes and nanogels required a matrix-to-nano...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Solid nanofoams based on cellulose nanofibers and indomethacin —the effect of processing parameters and drug content on material structure
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): J. Bannow, J.-W. Benjamins, J. Wohlert, K. Löbmann, A.J. Svagan The unique colloidal properties of cellulose nanofibers (CNF), makes CNF a very interesting new excipient in pharmaceutical formulations, as CNF in combination with some poorly-soluble drugs can create nanofoams with closed cells. Previous nanofoams, created with the model drug indomethacin, demonstrated a prolonged release compared to films, owing to the tortuous diffusion path that the drug needs to take around the intact air-bubbles. H...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Limited drug solubility can be decisive even for freely soluble drugs in highly swollen matrix tablets
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): F. Siepmann, Y. Karrout, M. Gehrke, F.K. Penz, J. Siepmann The aim of this study was to elucidate the importance of potential limited solubility effects for the control of drug release from hydrophilic matrix tablets loaded with a freely water-soluble drug. It is often assumed that the considerable amounts of water penetrating into this type of advanced drug delivery systems are sufficient to rapidly dissolve the entire drug loading, and that limited drug solubility is not playing a role for the control of...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Polysaccharides-based nanocomplexes for the prolonged delivery of enoxaparin: In-vitro and in-vivo evaluation
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Shaimaa S. Ibrahim, Rihab Osman, Gehanne A.S. Awad, Nahed D. Mortada, Ahmed-Shawky Geneidi Thromboprophylaxis and anticoagulant therapy face serious medical challenges in terms of how crucial it is to maintain therapeutic activity of the anticoagulant agent over the required period of time. Failure to do so will lead to an increased risk of clot propagation if a subtherapeutic drug level is reached. On the other hand, higher-than intended anticoagulation levels might lead to an enhanced risk of hemorrhagic...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Recent advances in use of silver nanoparticles as antimalarial agents
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Mahendra Rai, Avinash P. Ingle, Priti Paralikar, Indarchand Gupta, Serenella Medici, Carolina A. Santos Malaria is one of the most common infectious diseases, which has become a great public health problem all over the world. Ineffectiveness of available antimalarial treatment is the main reason behind its menace. The failure of current treatment strategies is due to emergence of drug resistance in Plasmodium falciparum and drug toxicity in human beings. Therefore, the development of novel and effective an...
Source: International Journal of Pharmaceutics - May 13, 2017 Category: Drugs & Pharmacology Source Type: research

Interactions of the antimicrobial peptide nisin Z with conventional antibiotics and the use of nanostructured lipid carriers to enhance antimicrobial activity
In this study, the interaction of the AMPs, nisin Z and melittin, with conventional antibiotics was investigated on Staphylococcus aureus, Staphylococcus epidermidis and Escherichia coli. The effectiveness of nanostructured lipid carriers (NLCs) for the entrapment of nisin Z was also evaluated. Findings revealed that nisin Z exhibited additive interactions with numerous conventional antibiotics. Notable synergism was observed for novobiocin-nisin Z combinations. The addition of the non-antibiotic adjuvant EDTA significantly improved the antimicrobial activity of free nisin Z towards E.coli. NLCs containing nisin Z were eff...
Source: International Journal of Pharmaceutics - May 11, 2017 Category: Drugs & Pharmacology Source Type: research

Angelica gigas Nakai extract-loaded fast-dissolving nanofiber based on poly(vinyl alcohol) and Soluplus for oral cancer therapy
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Suyeong Nam, Jeong-Jun Lee, Song Yi Lee, Jae Young Jeong, Wie-Soo Kang, Hyun-Jong Cho A poly(vinyl alcohol) (PVA) and Soluplus (SP)-based nanofiber (NF) mat was fabricated using an electrospinning method for the delivery of Angelica gigas Nakai (AGN) extract (ext) to oral cancers. AGN/SP NF (mean diameter: 75±26nm; entrapment efficiency: 84.6±18.6%) and AGN/PVA/SP NF (mean diameter: 170±35nm; entrapment efficiency: 81.0±10.1%) were fabricated using an electrospinning method. Amo...
Source: International Journal of Pharmaceutics - May 11, 2017 Category: Drugs & Pharmacology Source Type: research

Superior antitumor effect of extremely high drug loading self-assembled paclitaxel nanofibers
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Huae Xu, Xiaowei Lu, Jun Li, Dan Ding, Hong Wang, Xiaolin Li, Weiping Xie Recent studies focused on the nanodelivery system of paclitaxel (Ptx) to overcome the poor solubility and hypersensitivity of Ptx caused by the application of Cremophor EL as a solvent. Although many studies use different types of polymers as carriers to prepare Ptx-loaded polymeric nanoparticles, the relatively low loading efficiency of Ptx-loaded polymeric nanoparticles significantly limits its application. Here, we design and synt...
Source: International Journal of Pharmaceutics - May 11, 2017 Category: Drugs & Pharmacology Source Type: research

Gastrointestinal behavior of itraconazole in humans – Part 2: The effect of intraluminal dilution on the performance of a cyclodextrin-based solution
In conclusion, this work demonstrates that variations in intraluminal dilution may have a drastic impact on the gastrointestinal behavior of lipophilic drugs in the presence of cyclodextrins. In the case of an AP-type interaction with cyclodextrins, the trade-off between solubility and permeability may be affected. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 11, 2017 Category: Drugs & Pharmacology Source Type: research

Structural description of the marketed form of valsartan: A crystalline mesophase characterized by nanocrystals and conformational disorder
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Yannick Guinet, Laurent Paccou, Florence Danède, Patrick Derollez, Alain Hédoux Valsartan is an antihypertensive drug, recognized to be marketed in an amorphous state, different from that obtained by quenching the liquid state below T g. This is an unusual and very original situation, given that the amorphous state is unstable. Low-wavenumber Raman spectroscopy and X-ray diffraction investigations were carried out on the various solid-state forms of valsartan. It was found that the marketed f...
Source: International Journal of Pharmaceutics - May 11, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro release testing method development for ophthalmic ointments
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Quanying Bao, Jie Shen, Rajan Jog, Carmen Zhang, Bryan Newman, Yan Wang, Stephanie Choi, Diane J. Burgess It is essential as well as challenging to develop a reliable in vitro release testing method for determining whether differences in release profiles exist between qualitatively and quantitatively equivalent ophthalmic ointment formulations. There is a lack of regulatory guidance on in vitro release testing methods for ophthalmic formulations. Three different in vitro release testing methods 1) USP appa...
Source: International Journal of Pharmaceutics - May 10, 2017 Category: Drugs & Pharmacology Source Type: research

Poly(glucono- δ-lactone) based nanocarriers as novel biodegradable drug delivery platforms
In this study, ring-opening polymerization of a carbohydrate-derived lactone, glucono-δ-lactone (GDL), generates a new highly branched polymer (PGDL) that can form stable nanoparticles through a w/o emulsification approach. The biodegradable and biocompatible particles can carry anticancer agent 5-fluorouracil (5-FU) effectively. The controlled release of 5-FU from the PGDL particles exhibits a non-Fickian mechanism without an initial burst, with an enhanced release exponent at tumoral pH. Cell viability studies by MTT assays indicate that ovarian carcinoma cells (OVCAR-3) and macrophage cells (raw 264.7) treated wit...
Source: International Journal of Pharmaceutics - May 10, 2017 Category: Drugs & Pharmacology Source Type: research

Development of nanostructured lipid carriers for intraoral delivery of Domperidone
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Carolin Tetyczka, Martin Griesbacher, Markus Absenger-Novak, Eleonore Fröhlich, Eva Roblegg The oral cavity displays one potentially attractive route that is not associated with gastric transit and hepatic first pass metabolism. However, poorly soluble active candidates require a drug delivery system to facilitate their transport through oral biological membranes. To this end, nanostructured lipid carriers (NLC) were loaded with Domperidone and produced with high pressure homogenization. NLC were char...
Source: International Journal of Pharmaceutics - May 9, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained delivery of siRNA poly- and lipopolyplexes from porous macromer-crosslinked gelatin gels
In this study, we systematically investigated cross-linked gelatin based hydrogel formulations (cGEL) as degradable controlled release matrices for siRNA. Aiming at the definition of correlations between cGEL composition, siRNA nanoparticle formulation, release kinetics of complexed siRNA and transfection efficiency, we combined five different cGEL formulations and three transfection systems, i.e. polyplexes with polyethyleneimine (PEI), PEI in combination with liposomes (lipopolyplexes) and polyplexes based on tyrosin-modified PEI (P10Y). It was found that the distribution of these poly-/lipopolyplexes, when applied onto ...
Source: International Journal of Pharmaceutics - May 9, 2017 Category: Drugs & Pharmacology Source Type: research

In-line monitoring and optimization of powder flow in a simulated continuous process using transmission near infrared spectroscopy
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Md Anik Alam, Zhenqi Shi, James K. Drennen, Carl A. Anderson In-line monitoring of continuous powder flow is an integral part of the continuous manufacturing process of solid oral dosage forms in the pharmaceutical industry. Specifically, monitoring downstream from loss-in-weight (LIW) feeders and/or continuous mixers provides important data about the state of the process. Such measurements support control of the process and thereby enhance product quality. Near Infrared Spectroscopy (NIRS) is a potential ...
Source: International Journal of Pharmaceutics - May 9, 2017 Category: Drugs & Pharmacology Source Type: research

Predicting drug loading in PLA-PEG nanoparticles
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): M. Meunier, A. Goupil, P. Lienard Polymer nanoparticles present advantageous physical and biopharmaceutical properties as drug delivery systems compared to conventional liquid formulations. Active pharmaceutical ingredients (APIs) are often hydrophobic, thus not soluble in conventional liquid delivery. Encapsulating the drugs in polymer nanoparticles can improve their pharmacological and bio-distribution properties, preventing rapid clearance from the bloodstream. Such nanoparticles are commonly made of no...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Limiting the level of tertiary amines on polyamines leads to biocompatible nucleic acid vectors
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Margarida Isabel Simão Carlos, Kai Zheng, Natalie Garrett, Natrah Arifin, David G. Workman, Ilona Kubajewska, Abdulrahman A. Halwani, Julian Moger, Qi Zhang, Andreas G. Schätzlein, Ijeoma F. Uchegbu We have designed an efficient, synthetic nucleic acid vector, which is relatively non-toxic. [N-(2-ethylamino)-6-O-glycolchitosan – EAGC] polymers were 10–50 fold less toxic than Lipofectamine 2000, able to complex DNA, mRNA and siRNA into positively charged (zeta potential=+40 − 5...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced adhesion and in situ photothermal ablation of cancer cells in surface-functionalized electrospun microfiber scaffold with graphene oxide
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Nicolò Mauro, Cinzia Scialabba, Giovanna Pitarresi, Gaetano Giammona The physicochemical characteristics of a biomaterial surface highly affect the interaction with living cells. Recently, much attention has been focused on the adhesion properties of functional biomaterials toward cancer cells, since is expected to control metastatic spread of a tumor, which is related to good probability containing the progression of disease burden. Here, we designed an implantable poly(caprolactone)-based electros...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Formulation and characterisation of dissolving microneedles for the transdermal delivery of therapeutic peptides
This study presents a dissolving MN system composed of polyvinylpyrrolidone (PVP) and trehalose to encapsulate active pharmaceutical peptides within the MN matrix. Rapid systemic delivery is then achieved once the needles have penetrated the SC and dissolved in the interstitial fluid of the skin. A variety of characterisation techniques were carried out to determine the optimum formulation. A model peptide, polymyxin B, was then incorporated into the MN system and delivered through porcine skin. In addition, the activity of the model drug was monitored during all stages of the formulation process. Graphical abstract (Sourc...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Montmorillonite-lipid hybrid carriers for ionizable and neutral poorly water-soluble drugs: Formulation, characterization and in vitro lipolysis studies
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Tahnee J. Dening, Shasha Rao, Nicky Thomas, Clive A. Prestidge Lipid-based formulations (LBFs) are a popular strategy for enhancing the gastrointestinal solubilization and absorption of poorly water-soluble drugs. In light of this, montmorillonite-lipid hybrid (MLH) particles, composed of medium-chain triglycerides, lecithin and montmorillonite clay platelets, have been developed as a novel solid-state LBF. Owing to the unique charge properties of montmorillonite, whereby the clay platelet surfaces carry a...
Source: International Journal of Pharmaceutics - May 5, 2017 Category: Drugs & Pharmacology Source Type: research