Log in to search using one of your social media accounts:

 

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

Physicochemical characterization and gastrointestinal adhesion of S-layer proteins-coating liposomes
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Wenxi Wang, Anna Shao, Shisen Feng, Min Ding, Gan Luo S-layer proteins (Slps) are crystalline arrays of protein on bacterial cell surface layers. Owning to their capability to reassemble on the surface of lipid layers, Slps have been employed to modify liposomes for various profits. But the interaction information between Slps and positively charged liposomes are destitute, especially the gastrointestinal adhesion of Slps-coating liposomes is rarely reported. In the present work, the Slps extracted from ...
Source: International Journal of Pharmaceutics - July 11, 2017 Category: Drugs & Pharmacology Source Type: research

Thermoplastic polyurethane-based intravaginal rings for prophylaxis and treatment of (recurrent) bacterial vaginosis
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): G. Verstraete, L. Vandenbussche, S. Kasmi, L. Nuhn, D. Brouckaert, J. Van Renterghem, W. Grymonpré, V. Vanhoorne, T. Coenye, B.G. De Geest, T. De Beer, J.P. Remon, C. Vervaet The aim of the present study was to develop thermoplastic polyurethane (TPU)-based intravaginal rings (IVRs) for prophylaxis and treatment of bacterial vaginosis via hot melt extrusion/injection molding. Therefore, different TPU grades were processed in combination with lactic acid or metronidazole, targeting a sustained lact...
Source: International Journal of Pharmaceutics - July 10, 2017 Category: Drugs & Pharmacology Source Type: research

Chitosan centered bionanocomposites for medical specialty and curative applications: A review
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Mudasir Ahmad, Kaiser Manzoor, Sandeep Singh, Saiqa Ikram The polyfunctional nature of chitosan enables its application not only in polymer technology but also shows their importance in the field of nanotechnology for the fabrication of the wide spectrum of functional nanomaterials in biomedical field. Chitosan is a poly aminosaccharide with appealing structure composed of β-(1→4)-linked D-glucosamine (deacetylated unit) and N-acetyl-d-glucosamine (acetylated unit). It has various functional gr...
Source: International Journal of Pharmaceutics - July 10, 2017 Category: Drugs & Pharmacology Source Type: research

Spectroscopic and structural studies of the diosmin monohydrate and anhydrous diosmin
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Łukasz Szeleszczuk, Dariusz Maciej Pisklak, Monika Zielińska-Pisklak, Iwona Wawer Diosmin, a flavone glycoside frequently used in therapy of various veins diseases in monohydrate form, exhibits poor solubility in water and low bioavailability. Due to the fact that the anhydrous forms of drugs generally have better bioavailability than the corresponding hydrates, the aim of this study was to analyze the conversion of diosmin monohydrate (DSNM) to anhydrous diosmin (DSNA) that occurs upon heating. The me...
Source: International Journal of Pharmaceutics - July 9, 2017 Category: Drugs & Pharmacology Source Type: research

Superiority of aromatase inhibitor and cyclooxygenase-2 inhibitor combined delivery: Hyaluronate-targeted versus PEGylated protamine nanocapsules for breast cancer therapy
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Ahmed O. Elzoghby, Shaimaa K. Mostafa, Maged W. Helmy, Maha A. ElDemellawy, Salah A. Sheweita Despite several reports have revealed the beneficial effect of co-administration of COX-2 inhibitors with aromatase inhibitors in managing postmenopausal breast cancer; no nanocarriers for such combined delivery have been developed till now. Therefore, protamine nanocapsules (PMN-NCs) have been developed to co-deliver letrozole (LTZ) that inhibits aromatase-mediated estrogen biosynthesis and celecoxib (CXB) that...
Source: International Journal of Pharmaceutics - July 9, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancement and inhibition effects on the corneal permeability of timolol maleate: Polymers, cyclodextrins and chelating agents
This study investigates how both bioadhesive polymers (chitosan, hyaluronic acid and alginate) and permeability enhancers (ethylene glycol- bis(2-aminoethylether)- N, N, N', N'- tetraacetic acid (EGTA) and hydroxypropyl-ß-cyclodextrin) influence the permeability of the anti-glaucoma drug timolol maleate through ex vivo bovine corneas. Our results showed that only the permeability enhancers alone were able to increase drug permeability, whereas the polymers significantly reduced drug permeation, and however, they increased the pre-corneal residence of timolol. Ternary systems (polymer-enhancer-drug) showed a reduced d...
Source: International Journal of Pharmaceutics - July 9, 2017 Category: Drugs & Pharmacology Source Type: research

Developments of Polysorbate (Tween) based microemulsions: Preclinical drug delivery, toxicity and antimicrobial applications
This article deals with underlying the preclinical factors which affect the solubilization efficacy of Tween formulations, implication of pharmaceutically accepted vectors in terms of absorption, bioavailability, biological fate and potential toxicity. Antimicrobial activity of Tween microemulsion formulations has also been addressed emphasising the role of Tween. The review contains comprehensive knowledge/literature related to physicochemical parameters and biological fate of different Polysorbates and takes into account all the parameters and observations that make Tween a very convenient and safe choice for the use as ...
Source: International Journal of Pharmaceutics - July 7, 2017 Category: Drugs & Pharmacology Source Type: research

An insight into the molecular mechanism of the temporary enhancement effect of isopulegol decanoate on the skin
In conclusion, the lipid bilayer accepted the enhancer as a new component to form a new stable arrangement, resulted the recovery of the skin barrier function. This work processed a novel mechanism of the recovery of skin barrier function after the addition of chemical enhancers. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 6, 2017 Category: Drugs & Pharmacology Source Type: research

Comparative study on radiolabeling and biodistribution of core-shell silver/polymeric nanoparticles-based theranostics for tumor targeting
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Nourihan S. Farrag, Hanan A. El-Sabagh, Abdulaziz M. Al-mahallawi, Abeer M. Amin, Ahmed AbdEl-Bary, Wael Mamdouh A simple and rapid method for radiolabeling of three types of Ag NPs has been performed using 125I isotope, with high labeling yields, >90% without disturbing the optical properties. All the factors affecting labeling yield were studied. In order to monitor the in-vivo tissue uptake of radiolabeled Ag NPs using γ-rays, Ag-based radioiodo-NPs with a maximum labeling yield were intr...
Source: International Journal of Pharmaceutics - July 4, 2017 Category: Drugs & Pharmacology Source Type: research

Co-delivery of paclitaxel and anti-survivin siRNA via redox-sensitive oligopeptide liposomes for the synergistic treatment of breast cancer and metastasis
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Xinyan Chen, Yidi Zhang, Chunming Tang, Chunli Tian, Qiong Sun, Zhigui Su, Lingjing Xue, Yifan Yin, Caoyun Ju, Can Zhang The overexpression of survivin in breast cancer cells is an important factor of paclitaxel (PTX) resistance in breast cancer. To overcome PTX resistance and improve the antitumor effect of PTX, we developed a novel liposome-based nanosystem (PTX/siRNA/SS-L), composed of a redox-sensitive cationic oligopeptide lipid (LHSSG2C14) with a proton sponge effect, natural soybean phosphatidylch...
Source: International Journal of Pharmaceutics - June 29, 2017 Category: Drugs & Pharmacology Source Type: research

Production and characterization of aluminium oxide nanoshells on spray dried lactose
In conclusion, the aluminium oxide nanoshells prevented moisture sorption and dramatically improved the long term physical stability of amorphous lactose. This shows the potential of the ALD-technique to protect drug microparticles. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 29, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of the surface layer on drug release from delefilcon-A (Dailies Total1 ®) contact lenses
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Phillip Dixon, Anuj Chauhan Contact lenses are receiving significant attention for delivering ophthalmic drugs with higher bioavailability compared to eye drops. Here we explore drug transport from delefilcon-A Dailies Total1® lenses which are designed to have a thin, high-water content layer on the surface. Our goal is to determine the impact of this high water content layer on drug transport for both hydrophobic (dexamethasone and cyclosporine) and hydrophilic (timolol and levofloxacin) drugs. Drug...
Source: International Journal of Pharmaceutics - June 29, 2017 Category: Drugs & Pharmacology Source Type: research

Controlled release from aspirin based linear biodegradable poly(anhydride esters) for anti-inflammatory activity
Publication date: 7 August 2017 Source:International Journal of Pharmaceutics, Volume 528, Issues 1–2 Author(s): Queeny Dasgupta, Sahitya Movva, Kaushik Chatterjee, Giridhar Madras This work reports the synthesis of a novel, aspirin-loaded, linear poly (anhydride ester) and provides mechanistic insights into the release of aspirin from this polymer for anti-inflammatory activity. As compared to conventional drug delivery systems that rely on diffusion based release, incorporation of bioactives in the polymer backbone is challenging and high loading is difficult to achieve. In the present study, we exploit the pentaf...
Source: International Journal of Pharmaceutics - June 28, 2017 Category: Drugs & Pharmacology Source Type: research

Ribbon thickness influences fine generation during dry granulation
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Wei-Jhe Sun, Changquan Calvin Sun Uncontrolled fine generation during the milling process is a challenge for dry granulation by roller compaction. Here, we report the observation that ribbon thickness can significantly influence percentage of fines. Thus, among other parameters, ribbon thickness needs to be controlled for the development of a robust roller compaction process and ensure successful scale up. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 27, 2017 Category: Drugs & Pharmacology Source Type: research

Synthesis, physiochemical characterization, and in vitro antitumor activity of the amide and pH cleavable hydrazone conjugates of γ-tocotrienol isomer of vitamin E with methoxy-poly(ethylene) glycol
Publication date: 30 August 2017 Source:International Journal of Pharmaceutics, Volume 529, Issues 1–2 Author(s): Ahmed Abu-Fayyad, Sami Nazzal The anticancer activity of water soluble methoxy polyethylene glycol (mPEG) derivatives of tocotrienol (T3) isomers of vitamin E was previously found to be reduced when compared to the parent free isomers. This could be due to the ester bond formation between the mPEG and the 6-OH group on the chroman moiety of the T3 isomer. To further investigate, the objectives of the current study were to (1) synthesize and characterize stable amide and cleavable hydrazone conjugates bet...
Source: International Journal of Pharmaceutics - June 27, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted release of transcription factors for human cell reprogramming by ZEBRA cell-penetrating peptide
This study provides powerful tools for cell fate reprogramming without genetic interferences. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 27, 2017 Category: Drugs & Pharmacology Source Type: research

Topical bioavailability of diclofenac from locally-acting, dermatological formulations
The objective of this work was to evaluate in vitro skin penetration and stratum corneum tape-stripping in vivo as tools with which to measure topical diclofenac bioavailability from three approved and commercialized products (two gels and one solution). Drug uptake into, and its subsequent clearance from, the stratum corneum of human volunteers was used to estimate the input rate of diclofenac into the viable skin layers. This flux was compared to that measured across excised porcine skin in conventional diffusion cells. Both techniques clearly demonstrated (a) the superiority in terms of drug delivery from the solution, ...
Source: International Journal of Pharmaceutics - June 27, 2017 Category: Drugs & Pharmacology Source Type: research