Improved metabolic stability and therapeutic efficacy of a novel molecular gemcitabine phospholipid complex
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Chander Parkash Dora, Varun Kushwah, Sameer S. Katiyar, Pradeep Kumar, Viness Pillay, Sarasija Suresh, Sanyog Jain The aim of the present research is to increase lipid solubility, metabolic stability and therapeutic efficacy of water soluble gemcitabine (GEM) via phospholipid complex (PC) formation. A novel phospholipid complex of GEM was successfully prepared and optimized. Physical interaction of GEM with phospholipid was evaluated by DSC, FT-IR, 1H NMR, 31P-NMR and P-XRD. SEM images of GEM-PC showe...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

Improved transdermal delivery of morin efficiently inhibits allergic contact dermatitis
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Jiao Yu, Kawai Wan, Xun Sun The skin is an important site for local or systemic application of drugs. However, most of the drugs have poor permeability through the skin’s outermost layer, stratum corneum. The aim of this study was to develop a method to enable transdermal delivery of morin (3, 5, 7, 2, 4-pentahydroxyflavone), which is a poorly water-soluble drug with anti-inflammatory properties obtained from natural products. Morin phospholipid complex (MPC) was prepared and then loaded in Carb...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

Variable-focus microscopy and UV surface dissolution imaging as complementary techniques in intrinsic dissolution rate determination
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Adam Ward, Karl Walton, Karl Box, Jesper Østergaard, Lisa J. Gillie, Barbara R. Conway, Kofi Asare-Addo This work reports a novel approach to the assessment of the surface properties of compacts used in Surface Dissolution Imaging (SDI). SDI is useful for determining intrinsic dissolution rate (IDR), an important parameter in early stage drug development. Surface topography, post-compaction and post-SDI run, have been measured using a non-contact, optical, three-dimensional microscope based on ...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of polymer type on the surface energy of acetaminophen solid dispersions prepared by melt method
In this study, we used inverse gas chromatography (IGC) to evaluate the surface energies of prepared SDs, and compared them with those obtained for physical mixtures (PMs). SDs containing different weight ratios of crystalline acetaminophen and one of three polymers (Kollidon® 12 PF, Kollidon® VA 64 or Soluplus®) were prepared by the melt-quenching of corresponding PMs. In all cases, as the polymer content increased, the surface energy decreased significantly. For the SDs and PMs containing Soluplus®, this decrease in surface energy showed the same non-linear trend. In the cases of Kollidon® 12 PF and K...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

Nasal nanovaccines
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): B. Bernocchi, R. Carpentier, D. Betbeder Nasal administration of vaccines is convenient for the potential stimulation of mucosal and systemic immune protection. Moreover the easy accessibility of the intranasal route renders it optimal for pandemic vaccination. Nanoparticles have been identified as ideal delivery systems and adjuvants for vaccine application. Heterogeneous protocols have been used for animal studies. This complicates the understanding of the formulation influence on the immune respons...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

Systematic evaluation of the toxicity and biodistribution of virus mimicking mucus-penetrating DLPC-NPs as oral drug delivery system
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Wei Shan, Yi Cui, Min Liu, Lei Wu, Yucheng Xiang, Quan Guo, Zhirong Zhang, Yuan Huang Development of nanoparticle (NP) to simultaneously overcome the diffusion and absorption barrier has drawn much attention. Our group recently demonstrated that the virus mimicking dilauroylphosphatidylcholine functionalized NP (DLPC-NP) could rapidly penetrate across mucus layer and subsequently enter epithelia effectively, and exhibited high potential for oral drug delivery. However, the safety of the NP has provoke...
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

Dual centrifugation – A new technique for nanomilling of poorly soluble drugs and formulation screening by an DoE-approach
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Martin Hagedorn, Ansgar Bögershausen, Matthias Rischer, Rolf Schubert, Ulrich Massing The development of nanosuspensions of poorly soluble APIs takes a lot of time and high amount of active material is needed. In this publication the use of dual centrifugation (DC) for an effective and rapid API-nanomilling is described for the first time. DC differs from normal centrifugation by an additional rotation of the samples during centrifugation, resulting in a very fast and powerful movement of the sam...
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

Shear-responsive injectable supramolecular hydrogel releasing doxorubicin loaded micelles with pH-sensitivity for local tumor chemotherapy
This study demonstrates that injectable DOX/GC-PF127 hydrogel, which can sustainedly release DOX-loaded micelles with tumor-targeting function, is a promising system for local tumor chemotherapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

Application of machine learning in prediction of hydrotrope-enhanced solubilisation of indomethacin
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Safa A. Damiati, Luigi G. Martini, Norman W. Smith, Jayne M. Lawrence, David J. Barlow Systematic in-vitro studies have been conducted to determine the ability of a range of 10 potential hydrotropes to improve the apparent aqueous solubility of the poorly water soluble drug, indomethacin. Solubilisation of the drug in the presence of the hydrotropes was determined experimentally using high-performance liquid chromatography (HPLC) with ultraviolet (UV) detection. These experimental data, together with ...
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

A novel mechanical antrum model for the prediction of the gastroretentive potential of dosage forms
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Marco Neumann, Felix Schneider, Mirko Koziolek, Grzegorz Garbacz, Werner Weitschies The development of gastroretentive dosage forms can be significantly enhanced by the reliable estimation of gastroretentive properties in vitro. In this context, it is mandatory to consider the propulsive contraction waves that occur in the antral region of the stomach, since they are regarded as the major physiological hurdle to overcome. Therefore, the aim of this study was to develop an in vitro model that allowed t...
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

Patient acceptability of 3D printed medicines
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Alvaro Goyanes, Mariagiovanna Scarpa, Michael Kamlow, Simon Gaisford, Abdul W. Basit, Mine Orlu Patient-centric medicine is a derivative term for personalised medicine, whereby the pharmaceutical product provides the best overall benefit by meeting the comprehensive needs of the individual; considering the end-user from the beginning of the formulation design process right through development to an end product is a must. One way in which to obtain personalised medicines, on-site and on-demand is by th...
Source: International Journal of Pharmaceutics - July 29, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of L-leucine in reducing the moisture-induced deterioration of spray-dried salbutamol sulfate power for inhalation
In conclusion, LL is a potential excipient for reducing moisture-induced deterioration in the aerosolization performance of SD amorphous powders, but still has drawbacks in preventing the recrystallization-induced deterioration. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 27, 2017 Category: Drugs & Pharmacology Source Type: research

Innovative pMDI formulations of spray-dried nanoparticles for efficient pulmonary drug delivery
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Hao-Ying Li, En-Yu Xu For drug delivery to the lungs, the aerodynamic size of drug particles plays a predominant role in determining the sites of deposition in the airway, and the particles with the size less than 2μm are highly expected as they will be preferably delivered to the ideal site of alveolar regions. In this paper, a novel platform technology has been developed, where the water (containing pharmaceutically active agents)-in-oil (w/o) microemulsions were spray-dried to generate nanosized...
Source: International Journal of Pharmaceutics - July 26, 2017 Category: Drugs & Pharmacology Source Type: research

In-line Raman spectroscopic monitoring and feedback control of a continuous twin-screw pharmaceutical powder blending and tableting process
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Brigitta Nagy, Attila Farkas, Martin Gyürkés, Szofia Komaromy-Hiller, Balázs Démuth, Bence Szabó, Dávid Nusser, Enikő Borbás, György Marosi, Zsombor Kristóf Nagy The integration of Process Analytical Technology (PAT) initiative into the continuous production of pharmaceuticals is indispensable for reliable production. The present paper reports the implementation of in-line Raman spectroscopy in a continuous blending and tableting process of a...
Source: International Journal of Pharmaceutics - July 26, 2017 Category: Drugs & Pharmacology Source Type: research

Response surface optimization, Ex vivo and In vivo investigation of nasal spanlastics for bioavailability enhancement and brain targeting of risperidone
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Fatma Elzahraa Abdelrahman, Ibrahim Elsayed, Mary Kamal Gad, Ahmed Hassen Elshafeey, Magdi Ibrahim Mohamed Transnasal brain drug targeting could ensure better drug delivery to the brain through the olfactory pathway. Risperidone bioavailability is 66% in extensive metabolizers and 82% in slow metabolizers. The aim of this study is to investigate the ability of the nanovesicular spanlastics to effectively deliver risperidone through the nasal route to the brain and increase its bioavailability. Spanlas...
Source: International Journal of Pharmaceutics - July 25, 2017 Category: Drugs & Pharmacology Source Type: research

In-depth experimental analysis of pharmaceutical twin-screw wet granulation in view of detailed process understanding
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Maxim Verstraeten, Daan Van Hauwermeiren, Kai Lee, Neil Turnbull, David Wilsdon, Mary am Ende, Pankaj Doshi, Chris Vervaet, Davinia Brouckaert, Séverine T.F.C. Mortier, Ingmar Nopens, Thomas De Beer Twin-screw wet granulation is gaining increasing interest within the pharmaceutical industry for the continuous manufacturing of solid oral dosage forms. However, limited prior fundamental physical understanding has been generated relating to the granule formation mechanisms and kinetics along the inte...
Source: International Journal of Pharmaceutics - July 23, 2017 Category: Drugs & Pharmacology Source Type: research

Water-induced phase separation of miconazole-poly (vinylpyrrolidone-co-vinyl acetate) amorphous solid dispersions: Insights with confocal fluorescence microscopy
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Sugandha Saboo, Lynne S. Taylor The aim of this study was to evaluate the utility of confocal fluorescence microscopy (CFM) to study the water-induced phase separation of miconazole-poly (vinylpyrrolidone-co-vinyl acetate) (mico-PVPVA) amorphous solid dispersions (ASDs), induced during preparation, upon storage at high relative humidity (RH) and during dissolution. Different fluorescent dyes were added to drug-polymer films and the location of the dyes was evaluated using CFM. Orthogonal techniques, in p...
Source: International Journal of Pharmaceutics - July 23, 2017 Category: Drugs & Pharmacology Source Type: research

Intracorneal melatonin delivery using 2-hydroxypropyl- β-cyclodextrin ophthalmic solution for granular corneal dystrophy type 2
In conclusion, MT/HPβCD formulations can lower irritation, enhance MT stability, and improve therapeutic efficacy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 23, 2017 Category: Drugs & Pharmacology Source Type: research

Discrete particle modeling and micromechanical characterization of bilayer tablet compaction
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): B. Yohannes, M. Gonzalez, A. Abebe, O. Sprockel, F. Nikfar, S. Kiang, A.M. Cuitiño A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particles is crucial for the mechanical strength of the bilayer tablet. The bonding and the contact forces ...
Source: International Journal of Pharmaceutics - July 23, 2017 Category: Drugs & Pharmacology Source Type: research

Nano lipid-drug conjugate: An integrated review
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Piya Adhikari, Paulami Pal, Anup Kr. Das, Subhabrata Ray, Arpita Bhattacharjee, Bhaskar Mazumder Lipid-drug conjugates (LDC), which may also be addressed as lipoidal prodrug, have the therapeutic actives chemically bound to a lipid moiety like fatty acids or phospholipids. Fabricated in nano-size, lipid-drug conjugate forms another breed of lipid nanoparticles. LDCs are prepared in order to increase the drug loading and hence prevent leakage of a highly polar drug from a lipophilic matrix. In turn, it as...
Source: International Journal of Pharmaceutics - July 23, 2017 Category: Drugs & Pharmacology Source Type: research

The alteration of temoporfin distribution in multicellular tumor spheroids by β-cyclodextrins
This study aimed to investigate the ability of methyl-β-cyclodextrin (Me-β-CD) and 2-hydroxypropyl-β-cyclodextrin (Hp-β-CD) to alter the penetration and diffusion of temoporfin (mTHPC) in HT29 multicellular tumor spheroids. mTHPC had а nonhomogenous distribution only on the periphery of spheroids. The presence of β-CDs significantly altered the distribution of mTHPC consisting in the increase of both the depth of photosensitizer penetration and accumulation in HT29 spheroids. We suggest that this improvement is related to the nanoshuttle mechanism of β-CD action, when β-CDs facilitate mT...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Tacrolimus loaded biocompatible lecithin-based microemulsions with improved skin penetration: Structure characterization and in vitro/in vivo performances
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Vedrana Savić, Marija Todosijević, Tanja Ilić, Milica Lukić, Evgenia Mitsou, Vassiliki Papadimitriou, Spyridon Avramiotis, Bojan Marković, Nebojša Cekić, Snežana Savić In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the siz...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Formulations and toxicologic in vivo studies of aqueous cyclosporin A eye drops with cyclodextrin nanoparticles
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Sunna Jóhannsdóttir, Johannes K. Kristinsson, Zoltán Fülöp, Gudrún Ásgrímsdóttir, Einar Stefánsson, Thorsteinn Loftsson Cyclosporin A (CyA) is an immunosuppressive drug used topically to treat ocular inflammatory disorder such as dry eye disease (DES). It is a lipophilic cyclic peptide with molecular weight of 1202.6Da. The aim of this study was to develop surfactant free aqueous 0.2% (w/v) CyA eye drops where the drug is present in an aqu...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Layering of different materials to achieve optimal conditions for treatment of painful wounds
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): T. Maver, L. Gradišnik, M. Kurečič, S. Hribernik, D.M. Smrke, U. Maver, K. Stana Kleinschek Despite a range of advanced wound dressings that can facilitate wound healing, there are still no clinically used dressings for effective local pain management. The latter was the main motivation of the present study. We designed a novel wound dressing with three layers. A macro-porous polyethylene terephthalate (PET) mesh with incorporated lidocaine, a fast-acting local anesthetic, was chosen as the laye...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Dual antibiotherapy of tuberculosis mediated by inhalable locust bean gum microparticles
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Susana Rodrigues, Ana D. Alves, Joana S. Cavaco, Jorge F. Pontes, Filipa Guerreiro, Ana M. Rosa da Costa, Francesca Buttini, Ana Grenha Despite the existence of effective oral therapy, tuberculosis remains a deadly pathology, namely because of bacterial resistance and incompliance with treatments. Establishing alternative therapeutic approaches is urgently needed and inhalable therapy has a great potential in this regard. As pathogenic bacteria are hosted by alveolar macrophages, the co-localisation of a...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Direct compaction: An update of materials, trouble-shooting, and application
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Zhe Li, LiJie Zhao, Xiao Lin, Lan Shen, Yi Feng Direct compaction (DC) is the preferred choice for tablet manufacturing; however, only less than 20% of active pharmaceutical ingredients could be compacted via DC as its high requirement for functional properties of materials. Materials with improper functionalities could lead to serious troubles during DC manufacturing, such as content non-uniformity, sticking, and capping, all of which profoundly affect the properties of final products and, thus, severel...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Recent advances in TPGS-based nanoparticles of docetaxel for improved chemotherapy
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Hira Choudhury, Bapi Gorain, Manisha Pandey, Santosh Ashok Kumbhar, Rakesh Kumar Tekade, Arun K. Iyer, Prashant Kesharwani Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to resist sudden systemic exposure of DTX with more specific delivery to ...
Source: International Journal of Pharmaceutics - July 22, 2017 Category: Drugs & Pharmacology Source Type: research

Polyarginine nanocapsules: A versatile nanocarrier with potential in transmucosal drug delivery
The objective of this work was to investigate the potential utility of nanocapsules composed of an oily core decorated with a single polyarginine (PARG), or double PARG/polyacrylic acid (PAA) layer as oral peptide delivery carrier. A step-by-step formulation optimization process was designed, which involved the study of the influence of the surfactants, oils and polymer shells (PARG of different molecular weight and PAA) on the nanocapsules physicochemical properties, peptide loading efficiency, stability in simulated intestinal fluids (SIF) and capacity to enhance the permeability of the intestinal epithelium. Despite the...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Glycyrrhetinic acid-modified TPGS polymeric micelles for hepatocellular carcinoma-targeted therapy
In this study, glycyrrhetinic acid (GA)-modified D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) polymeric micelles (TGA PMs) were developed for the delivery of etoposide (ETO) to hepatoma cells. GA was incorporated as a ligand because of its high affinity to the hepatocytes, while TPGS functioned as a P-gp inhibitor to reverse multidrug resistance. ETO-loaded TGA PMs (ETO-TGA PMs) displayed a mean particle size of 133.6±1.2nm with a low poly-dispersity index (0.224±0.013) and negative zeta potential (−16.30mV). The drug loading and entrapment efficiency of ETO-TGA PMs were 10.4% and 79.8...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Transcutaneous immunotherapy of pollinosis using solid-in-oil nanodispersions loaded with T cell epitope peptides
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Qingliang Kong, Momoko Kitaoka, Rie Wakabayashi, Noriho Kamiya, Masahiro Goto Pollinosis, a typical seasonal allergy, is a serious public health problem. Limited numbers of patients receive curative immunotherapy instead of symptomatic therapy; however, there are still some concerns about the inconvenience and side effects of subcutaneous injections and sublingual administration caused by immunotherapy. Here, we propose a simple and safe transcutaneous immunotherapy using solid-in-oil (S/O) nanodispersio...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Transdermal delivery of dimethyl fumarate for Alzheimer ’s disease: Effect of penetration enhancers
The objective of this study was to investigate the feasibility of transdermal delivery of DMF by studying the effect of different penetration enhancers on the skin permeation of DMF. The permeation of saturated DMF solutions was investigated in propylene glycol (PG) with varying concentrations of each of the following enhancers: Polysorbate 80 (T80), N-methyl pyrrolidone (NMP), laurocapram (Azone®) (Az), Transcutol P (Tc), Terpineol (Terp), and cineole (Cin) using vertical Franz diffusion cells and human cadaver skin. The results showed that all penetration enhancers improved the rate of permeation of DMF. The rank ord...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

The impact of guest compounds on cyclodextrin aggregation behavior: A series of structurally related parabens
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Jef Stappaerts, Thao Do Thi, Elena Dominguez-Vega, Govert W. Somsen, Guy Van den Mooter, Patrick Augustijns Several studies have demonstrated the presence of aggregates in aqueous cyclodextrin containing solutions. The presence of guest compounds has been shown to influence this cyclodextrin aggregation process. In an attempt to gain insight into the effect of the physicochemical properties of the guest compound on 2-hydroxypropyl-β-cyclodextrin aggregation formation, a series of structurally relate...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Skin permeability enhancement by Bacillus subtilis alkaline protease: Application to transdermal drug delivery
In this study, the effect of alkaline protease produced by recombinant Bacillus subtilis cells on the ex-vivo permeability of rabbit ear skin was investigated under different conditions of enzyme activity (5–60 units) and exposure time (15–60min). Data for transepidermal water loss (TEWL) and permeation of a hydrophilic dye, rhodamine B (Rb), indicated biphasic activity-dependent and exposure time-dependent skin permeability. Maximum effects were obtained at 20 proteolytic units and 30min exposure. Findings proved consistent with histopathological changes indicating progressive stratum corneum (SC) loss and dis...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Application of continuous twin screw granulation for the metformin hydrochloride extended release formulation
This study focuses on evaluating the potential of transferring from a batch process to continuous process for manufacturing of the extended release formulation. Metformin hydrochloride (HCl) was used in the model formulation which was intended to contain the high amount of hydrophilic drug. The effects of barrel temperature, binder type, powder feed rate, and screw speed on granule properties (size and strength) and torque value in twin screw granulation were investigated. Due to the high content of hydrophilic model drug, the granules prepared at a higher temperature with HPMC binding solution had the narrower size distri...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Investigate the control release effect of ion-pair in the development of escitalopram transdermal patch using FT-IR spectroscopy, molecular modeling and thermal analysis
In conclusion, a controlled release ESP transdermal patch was developed and a novel insight of ion-pair controlled release was proposed at molecular level. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

Improvement of the surface hydrophilic properties of naproxen particles with addition of hydroxypropylmethyl cellulose and sodium dodecyl sulphate: In vitro and in vivo studies
In this study, a new surface-modified naproxen was developed to enhance brain concentration in acute migraine treatment. Fast-dissolving naproxen granules were made by mixing hydroxypropylmethylcellulose (HPMC) sodium dodecyl sulphate (SDS) and sodium croscarmellose with micronized naproxen particles. The aim of this study was to evaluate the effect of adding proportions of SDS to the HPMC film caused changes in the polymer chains of the HPMC, producing a new hydrophilic HPMC-SDS structure. These formulations with different HPMC/SDS ratios were characterised using electron microscopy (SEM), powder X-ray diffraction (PXRD),...
Source: International Journal of Pharmaceutics - July 20, 2017 Category: Drugs & Pharmacology Source Type: research

The effect of poly (lactic-co-glycolic) acid composition on the mechanical properties of electrospun fibrous mats
In conclusion, this study shows that the mechanical properties of EFMs, which depend on the polymer molecule-solvent affinity, can be predicted by the inter-molecular interactions in the starting polymer solutions and over the drying process of electrospinning. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 18, 2017 Category: Drugs & Pharmacology Source Type: research

A novel penetratin-modified complex for noninvasive intraocular delivery of antisense oligonucleotides
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Lingyu Tai, Chang Liu, Kuan Jiang, Xishan Chen, Linglin Feng, Weisan Pan, Gang Wei, Weiyue Lu Inhibition of gene expression by nucleic acids is a promising strategy in the treatment of ocular diseases. However, intraocular delivery of nucleic acids to the posterior ocular tissues remains a great challenge due to the presence of various biological barriers. To circumvent this problem, we established a novel penetratin (P) modified poly(amidoamine) dendrimer (D)/hyaluronic acid (H) complex to deliver antis...
Source: International Journal of Pharmaceutics - July 16, 2017 Category: Drugs & Pharmacology Source Type: research

Functionalized PLA-PEG nanoparticles targeting intestinal transporter PepT1 for oral delivery of acyclovir
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Betty Gourdon, Caroline Chemin, Amélie Moreau, Thomas Arnauld, Philippe Baumy, Salvatore Cisternino, Jean-Manuel Péan, Xavier Declèves Targeting intestinal di- and tri-peptide transporter PepT1 with prodrugs is a successful strategy to improve oral drug bioavailability, as demonstrated with valacyclovir, a prodrug of acyclovir. The aim of this new drug delivery strategy is to over-concentrate a poorly absorbed drug on the intestinal membrane surface by targeting PepT1 with functional...
Source: International Journal of Pharmaceutics - July 15, 2017 Category: Drugs & Pharmacology Source Type: research

Development of a continuous direct compression platform for low-dose drug products
This study provided abundant evidence that an optimized continuous direct compression process allows direct compression of challenging low-dose drug products. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 14, 2017 Category: Drugs & Pharmacology Source Type: research

Mechanistic understanding of the link between Sodium Starch Glycolate properties and the performance of tablets made by wet granulation
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): S.A.C. Wren, F. Alhusban, A.R. Barry, L.P. Hughes The impact of varying Sodium Starch Glycolate (SSG) grade and wet granulation intensity on the mechanism of disintegration and dissolution of mannitol-based Immediate Release (IR) placebo tablets was investigated. MRI and 1H NMR provided mechanistic insight, and revealed a four-fold range in both tablet disintegration and dissolution rates. MRI was used to quantify the rates of change in tablet volumes and the data fitted to a hydration/erosion model. Red...
Source: International Journal of Pharmaceutics - July 14, 2017 Category: Drugs & Pharmacology Source Type: research

Comparative in vitro and in vivo taste assessment of liquid praziquantel formulations
In conclusion, the BATA model was identified as a more efficient taste assessment tool for the pure PZQ and liquid formulations in contrast to the electronic tongue and the phase solubility study. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 14, 2017 Category: Drugs & Pharmacology Source Type: research

Reducing agent-free synthesis of curcumin-loaded albumin nanoparticles by self-assembly at room temperature
This study suggests that ionic strength can be a key parameter affecting the preparation of albumin-based NPs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 13, 2017 Category: Drugs & Pharmacology Source Type: research

Development of long-acting ciliary neurotrophic factor by site-specific conjugation with different-sized polyethylene glycols and transferrin
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Chun Zhang, Rong Yu, Zenglan Li, Cui Feng, Qi Wang, Yongdong Liu, Zhiguo Su To overcome the deficiency of rapid elimination from blood, the truncated human recombinant ciliary neurotrophic factor was formulated by site-specific attachment of different-sized PEG-maleimide or by cross-linking with human transferrin through a hetero-bi-functional PEG linker (NHS-PEG5k-MAL). The PEGylated CNTF was purified by a two-step chromatography procedure and the transferrin coupling CNTF conjugate was separated throug...
Source: International Journal of Pharmaceutics - July 13, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the solubility of nilotinib through novel spray-dried solid dispersions
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Maikel Herbrink, Jan H.M. Schellens, Jos H. Beijnen, Bastiaan Nuijen The tyrosine kinase inhibitor nilotinib has a very low aqueous solubility and a low and variable oral bioavailability. A pharmaceutical formulation with an improved solubility may enhance the bioavailability and reduce the variability thereof and of the pharmacokinetics. The aim of this study was to enhance the solubility of nilotinib by developing a spray dried solid dispersion. A broad selection of polymer excipients were tested for s...
Source: International Journal of Pharmaceutics - July 13, 2017 Category: Drugs & Pharmacology Source Type: research

Selective laser sintering (SLS) 3D printing of medicines
In conclusion, this work has demonstrated that SLS is a versatile and practical 3D printing technology which can be applied to the pharmaceutical field, thus widening the armamentarium of 3D printing technologies available for the manufacture of modern medicines. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 13, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of multiphase multicomponent aerosol flow dictating pMDI-spacer interactions
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Saurabh Sarkar, S. Prasad Peri, Bodhisattwa Chaudhuri The use of Pressurized metered dose inhalers (pMDIs) for the treatment of asthma and other chronic obstructive pulmonary diseases is frequently associated with breath–actuation synchronization problems and poor pulmonary delivery, particularly amongst the pediatric and geriatric population groups. Spacers, or Valved Holding Chambers (VHCs), are frequently used to address these problems. However, the performance of spacers with different pMDIs is...
Source: International Journal of Pharmaceutics - July 12, 2017 Category: Drugs & Pharmacology Source Type: research

Optimised NLC: a nanotechnological approach to improve the anaesthetic effect of bupivacaine
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Gustavo H. Rodrigues da Silva, Lígia N.M. Ribeiro, Hery Mitsutake, Viviane A. Guilherme, Simone R. Castro, Ronei J. Poppi, Márcia C. Breitkreitz, Eneida de Paula The short time of action and systemic toxicity of local anaesthetics limit their clinical application. Bupivacaine is the most frequently used local anaesthetic in surgical procedures worldwide. The discovery that its S(−) enantiomeric form is less toxic than the R(+) form led to the introduction of products with enantiomeric...
Source: International Journal of Pharmaceutics - July 12, 2017 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical versatility of cationic niosomes derived from amino acid-based surfactants: Skin penetration behavior and controlled drug release
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Rita Muzzalupo, Lourdes Pérez, Aurora Pinazo, Lorena Tavano The natural capability shown by cationic vesicles in interacting with negatively charged surfaces or biomolecules has recently attracted increased interest. Important pharmacological advantages include the selective targeting of the tumour vasculature, the promotion of permeation across cell membranes, as well as the influence of cationic vesicles on drug delivery. Accordingly, cationic amphiphiles derived from amino acids may represent a...
Source: International Journal of Pharmaceutics - July 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development of expanded polytetrafluoroethylene cardiovascular graft platform based on immobilization of poly lactic-co-glycolic acid nanoparticles using a wet chemical modification technique
In this study, poly lactic-co-glycolic acid (PLGA) nanoparticles were covalently immobilized on ePTFE surface for local therapeutic purposes. First, the ePTFE surface was primarily oxidized by H2O2/H2SO4 solution to create hydroxyl groups. Consequently, free amino groups were introduced onto ePTFE surface by an aminolyzation reaction of the activated hydroxyl groups using 3-aminopropyl triethoxysilane. The produced amino groups were further used as anchor sites for covalent immobilization of previously prepared PLGA nanoparticles. The functional groups originated on ePTFE surface were confirmed by FTIR analysis. Furthermor...
Source: International Journal of Pharmaceutics - July 11, 2017 Category: Drugs & Pharmacology Source Type: research