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Improvement in insulin absorption into gastrointestinal epithelial cells by using molecularly imprinted polymer nanoparticles: Microscopic evaluation and ultrastructure
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Pijush Kumar Paul, Jongdee Nopparat, Mitree Nuanplub, Alongkot Treetong, Roongnapa Suedee A molecularly imprinted polymer nanoparticle (MIP) was prepared by integrating a mixed functional monomer into a highly cross-linked polymer. The nanosized insulin as a template transferred into the binding cavities, anchored functional monomer(s) that the insulin structure formed within free space of the molecular size region by MIP nanoparticles. The oral administration with the insulin-loaded MIP resulted in h...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Mesoporous silica nanoparticles as a promising skin delivery system for methotrexate
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Simona Sapino, Simonetta Oliaro-Bosso, Daniele Zonari, Andrea Zattoni, Elena Ugazio The systemic administration of methotrexate (MTX), a commonly used, antineoplastic drug which is also used in cutaneous disorders, is primarily associated with prolonged retention in the body and consequently with side effects. Innovative drug delivery techniques and alternative administration routes would therefore contribute to its safe and effective use. The general objective of this study is thus the development of...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Analysis of the dehydration process of caffeine using backscattering and transmission Raman spectroscopy
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Rina Takeshima, Yusuke Hattori, Satoshi Managaki, Makoto Otsuka In the present study, the dehydration process of caffeine hydrate (CAH) was investigated by calibrating the moisture content in the caffeine tablet using backscattering Raman spectroscopy (BRS) and transmission Raman spectroscopy (TRS). The detectable depth of BRS is limited by its shallow laser penetration, while TRS is a powerful tool to determine the content of active pharmaceutical ingredients in a tablet. Our results suggest that the...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Development of an analytical method for crystalline content determination in amorphous solid dispersions produced by hot-melt extrusion using transmission Raman spectroscopy: A feasibility study
This study reported the development and the comparison of the analytical performances of two techniques, based on backscattering and transmission Raman spectroscopy, determining the crystalline remaining content in amorphous solid dispersions produced by HME. Principal Component Analysis (PCA) and Partial Least Squares (PLS) regression were performed on preprocessed data and tended towards the same conclusions: for the backscattering Raman results, the use of the DuoScan™ mode improved the PCA and PLS results, due to a larger analyzed sampling volume. For the transmission Raman results, the determination of low cryst...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained-release mitochondrial protonophore reverses nonalcoholic fatty liver disease in rats
In this study, we developed an injectable liquid crystal gel (DNP-LC-gel) to reduce the toxicity of DNP. DNP-LC-gel achieved sustained release and maintained DNP plasma concentration at an effective drug level. In a rat model of NAFLD, DNP-LC-gel treated rats reduced hepatic steatosis, liver triglyceride content, plasma triacylglycerol (TG) and total cholesterol (TC) content. Compared with DNP solution (DNP-soln), rats after DNP-LC-gel treatment showed no body temperature toxicity and local irritation. All results above indicated that DNP-LC-gel has a great potential for NAFLD therapy. Graphical abstract (Source: Internati...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of probiotics to enhance gastrointestinal stability and intestinal colonisation
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Cornelius C. Dodoo, Jie Wang, Abdul W. Basit, Paul Stapleton, Simon Gaisford The aim of this work was to assess the viability of some commercial probiotics after exposure to gastric acid and the possibility of modifying these formulations for delivery into the distal parts of the intestines. Gastrointestinal tolerance testing was conducted for three commercial probiotics and an in-house freeze-dried Lactobacillus acidophilus strain. The contents of the commercial products and the in-house freeze-dried...
Source: International Journal of Pharmaceutics - August 5, 2017 Category: Drugs & Pharmacology Source Type: research

Early pediatric formulation development with new chemical entities: Opportunities of e-tongue besides human taste assessment
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Laura Isabell Immohr, Angela Dischinger, Peter Kühl, Heidemarie Kletzl, Stefan Sturm, Andreas Günther, Miriam Pein-Hackelbusch The palatability of a pediatric drug formulation is one of the key prerequisites for therapeutic success. Liquid formulations are often chosen for pediatric drug products, and they require special attention regarding their taste, as they have direct contact to the taste buds and a relatively long residence time in the oral cavity. For ethical reasons, the role of ele...
Source: International Journal of Pharmaceutics - August 2, 2017 Category: Drugs & Pharmacology Source Type: research

Genotoxic evaluation of poly(anhydride) nanoparticles in the gastrointestinal tract of mice
In conclusion, GN-MA-NP are promising nanocarriers as oral drug delivery systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 1, 2017 Category: Drugs & Pharmacology Source Type: research

Towards understanding polyol additive effects on the pH shift-induced aggregation of a monoclonal antibody using high throughput screening and quantitative structure-activity modeling
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Olubukayo-Opeyemi Oyetayo, Oscar Méndez-Lucio, Andreas Bender, Hans Kiefer pH shift-induced aggregation is frequently observed in downstream processing of monoclonal antibodies and has been shown to depend on solvent composition. To quantify the stabilizing effect of polyol additives against aggregation, we determined aggregation rate constants in the presence of a set of 14 compounds. Rate constants were then correlated with molecular descriptors in a quantitative structure activity relationsh...
Source: International Journal of Pharmaceutics - August 1, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancement of nose-to-brain delivery of hydrophilic macromolecules with stearate- or polyethylene glycol-modified arginine-rich peptide
In conclusion, the results of this study support the possibility that drug delivery pathways can be controlled depending on the properties of different carrier complexes. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 1, 2017 Category: Drugs & Pharmacology Source Type: research

Optimization of high-concentration endostatin formulation: Harmonization of excipients ’ contributions on colloidal and conformational stabilities
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Shujing Wang, Xinyi Zhang, Guoliang Wu, Zhou Tian, Feng Qian Recently, increasing research efforts have been devoted into developing high-concentration protein drugs for subcutaneous injection, especially for those with short half-lives and high-dose requirement. Proteins at high concentrations normally present increased colloidal and structural instability, such as aggregation, fibrillation and gelation, which significantly challenges the high-concentration formulation development of protein drugs. H...
Source: International Journal of Pharmaceutics - August 1, 2017 Category: Drugs & Pharmacology Source Type: research

Development of biomedical 5-fluorouracil nanoplatforms for colon cancer chemotherapy: Influence of process and formulation parameters
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Elena Pretel, José L. Arias, Laura Cabeza, Consolación Melguizo, José Prados, Mireia Mallandrich, Joaquim Suñer, Beatriz Clares In the present investigation solvent displacement or nanoprecipitation, and emulsion/solvent evaporation methods were utilized to optimize poly(D,L-lactide-co-glycolide) nanoparticles for the vehiculization of the 5-fluorouracil. Formulation components from both the aqueous and organic phases, as well as, operating conditions were varied. Particles...
Source: International Journal of Pharmaceutics - July 30, 2017 Category: Drugs & Pharmacology Source Type: research

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