Composite particle formulations of colistin and meropenem with improved in-vitro bacterial killing and aerosolization for inhalation
In conclusion, our results show that co-spray drying with colistin improves the antibacterial activity and aerosol performance of meropenem and produces a formulation with synergistic bacterial killing.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 13, 2018 Category: Drugs & Pharmacology Source Type: research

Challenges for pulmonary delivery of high powder doses
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Imco Sibum, Paul Hagedoorn, Anne Haaije de Boer, Henderik Willem Frijlink, Floris GrasmeijerAbstractIn recent years there is an increasing interest in the pulmonary delivery of large cohesive powder doses, i.e. drugs with a low potency such as antibiotics or drugs with a high potency that need a substantial fraction of excipient(s) such as vaccines stabilized in sugar glasses. The pulmonary delivery of high powder doses comes with unique challenges. For low potency drugs, the use of excipients should be minimized...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

A practical framework for implementing Quality by Design to the development of topical drug products: Nanosystem-based dosage forms
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ana Simões, Francisco Veiga, Ana Figueiras, Carla VitorinoAbstractSkin has been increasingly recognized as an important drug administration route with topical formulations, offering a targeted approach for the treatment of several dermatological disorders. The effectiveness of this route is hampered by its natural barrier, the stratum corneum (SC), and hence, different strategies have been investigated to improve percutaneous drug transport. The design of nanodelivery systems, aiming at solving skin delive...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

All disease begins in the gut: Influence of gastrointestinal disorders and surgery on oral drug performance
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Grace B. Hatton, Christine M. Madla, Sarit C. Rabbie, Abdul W. BasitAbstractThe term “disease” conjures a plethora of graphic imagery for many, and the use of drugs to combat symptoms and treat underlying pathology is at the core of modern medicine. However, the effects of the various gastrointestinal diseases, infections, co-morbidities and the impact of gastrointestinal surgery on the pharmacokinetic and pharmacodynamic behaviour of drugs have been largely overlooked. The better elucidation of disea...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Surface-dependent endocytosis of poly(isobutylcyanoacrylate) nanoparticles by Trichomonas vaginalis
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Sophia Malli, Christian Bories, Mickaël Bourge, Philippe.M. Loiseau, Kawthar BouchemalAbstractPrevious data from our research group showed that chitosan-coated poly(isobutylcyanoacrylate) nanoparticles (NPs) (denoted PIBCA/Chito20) exhibited intrinsic anti-Trichomonas vaginalis activity, while PIBCA/pluronic® F68 without chitosan (PIBCA/F68) were inactive. However, the mechanism of anti-T. vaginalis activity of chitosan-coated PIBCA NPs is still unknown. Our hypothesis is that chitosan-coated NPs are int...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of a smart pH-cleavable PEG polymer towards the development of dual pH-sensitive liposomes
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Manju Kanamala, Brian D. Palmer, William R. Wilson, Zimei WuAbstractTo facilitate the development of PEG-cleavable pH-sensitive liposomes (CL-pPSL), this study aimed to fully characterize a new pH-sensitive polymer, PEGB-Hz-CHEMS. Polyethylene glycol (PEG) functionalised with 4-carboxybenzaldehyde (PEGB) was linked to cholesteryl hemisuccinate (CHEMS) via an acid labile hydrazide–hydrazone hybrid bond (CONHNCH) to form PEGB-Hz-CHEMS. The polymer was post-inserted into DOPE/CHEMS liposomes to form CL-pPSL. A...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-coated superparamagnetic nanoparticles for thermoresponsive cancer treatment
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ayat A. Allam, Sarah J. Potter, Sergey L. Bud'ko, Donglu Shi, Dina F. Mohamed, Fawzia S. Habib, Giovanni M. PaulettiAbstractPoor aqueous solubility, chemical instability, and indiscriminate cytotoxicity have limited clinical development of camptothecin (CPT) as potent anticancer therapeutic. This research aimed at fabricating thermoresponsive nanocomposites that enhance solubility and stability of CPT in aqueous milieu and enable stimulus-induced drug release using magnetic hyperthermia. 1,2-Dipalmitoyl-sn-glycer...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

A modified USP induction port to characterize nasal spray plume geometry and predict turbinate deposition under flow
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Daniel Moraga-Espinoza, Zachary Warnken, Amanda Moore, Robert O. Williams, Hugh D.C. SmythAbstractThere is currently no in vitro technique for assessing plume geometry of nasal sprays under airflow conditions. However, a majority of FDA approved nasal products recommend that patients inhale during actuation. Therefore, a reproducible in vitro test that measures plume angles under physiologically relevant inhalation flow rates would be useful. The purpose of this study was to adapt the recently described Plume Ind...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Deciphering magnesium stearate thermotropic behavior
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Rahul V. Haware, Bhavani Prasad Vinjamuri, Amrita Sarkar, Morgan Stefik, William C. StagnerAbstractMagnesium stearate (MgSt) is the most commonly used excipient for oral solid dosage forms, yet there is significant commercial physicochemical variability that can lead to variable performance of critical product attributes. Differential scanning calorimetry (DSC) is often used as a quality control tool to characterize MgSt, but little data is available regarding the physicochemical relevance for the DSC thermograms...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

In-situ forming PLGA implants for intraocular dexamethasone delivery
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): C. Bode, H. Kranz, F. Siepmann, J. SiepmannAbstractDifferent types of in-situ forming implants based on poly(lactic-co-glycolic acid) (PLGA) and N-methyl-pyrrolidone (NMP) were prepared for controlled ocular delivery of dexamethasone. The impact of the volume of the release medium, initial drug content, polymer molecular weight and PLGA concentration on the resulting drug release kinetics were studied and explained based on a thorough physico-chemical characterization of the systems. This included for instance th...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Development of customised 3D printed biodegradable projectile for administrating extended-release contraceptive to wildlife
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Jingjunjiao Long, Ashveen V. Nand, Sudip Ray, Sam Mayhew, David White, Craig R. Bunt, Ali SeyfoddinAbstractCustomisation of sustained and controlled release of contraceptives plays a key role in veterinary applications. A biodegradable projectile containing different doses of contraceptive progesterone was prepared using fused deposition modelling 3D printing. Three concentrations of progesterone (2, 5 and 10% w/w) with polylactic acid was prepared as a 1.75 mm filament by hot melt extrusion. Solvent dissolutio...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of novel phospholipid-based sonocomplexes for improved intestinal permeability of rosuvastatin: In vitro characterization, dynamic simulation, Caco-2 cell line permeation and in vivo assessment studies
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Wessam Hamdy Abd-Elsalam, Sara Nageeb El-Helaly, Mohammed Abdallah Ahmed, Abdulaziz Mohsen Al-mahallawiAbstractThe study aimed to fabricate innovative drug-phospholipid complexes termed “sonocomplexes” adopting ultrasound irradiation to increase the liposolubility and to enhance the intestinal absorption of rosuvastatin as a model drug for BCS class III active pharmaceutical ingredients (APIs). A 22 full factorial design was fashioned to investigate the influence of phosphatidylcholine content in the ...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Assessment of hot-processability and performance of ethylcellulose-based materials for injection-molded prolonged-release systems: An investigational approach
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): F. Casati, F. Briatico-Vangosa, F. Baldi, A. Melocchi, A. Maroni, A. Gazzaniga, L. ZemaAbstractThe present work focuses on application of an investigational approach to assess the hot-processability of pharmaceutical-grade polymers with a potential for use in the manufacturing of reservoir drug delivery systems via micromolding, and the performance of resulting molded barriers. An inert thermoplastic polymer, ethylcellulose (EC), widely exploited for preparation of prolonged-release systems, was employed as a mod...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Self-microemulsifying tablets prepared by direct compression for improved resveratrol delivery
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Katarina Bolko Seljak, Ilija German Ilić, Mirjana Gašperlin, Alenka Zvonar PobirkAbstractThe purpose of this study was to develop self-microemulsifying (SME-) tablets to improve resveratrol solubility whilst delivering resveratrol in a preferred tablet dosage form. Resveratrol was dissolved in liquid self-microemulsifying drug delivery system (SMEDDS) (10% w/w) and solidified through adsorption on several different solid carriers. Two ranges of synthetic amorphous silica (Sylysia® 290, 350, 470, 580; ...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of spray dried submicron particles: Part A – Particle generation by aerosol conditioning
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ramona Strob, Adrian Dobrowolski, Gerhard Schaldach, Peter Walzel, Markus ThommesAbstractThe preparation of submicron-sized particles is relevant in chemical, food and pharmaceutical applications. In pharmaceutics, spray dried submicron-sized particles (0.1–1 µm) can increase the dissolution rate as well as the solubility of poorly water-soluble drugs. Since the particle size during spray drying is mainly influenced by the droplet size, the preparation of uniform droplets smaller than 3 µm i...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Varun Kushwah, Sameer S. Katiyar, Ashish Kumar Agrawal, Isha Saraf, Inder Pal Singh, Dimitrios A. Lamprou, Ramesh C. Gupta, Sanyog JainAbstractThe present study investigates effect of linkers [zero length (without linker), short length linker (glycine and lysine) and long length linker (PEG1000, PEG2000 and PEG3500)] on pharmacokinetics and toxicity of docetaxel (DTX) and gemcitabine (GEM) bio-conjugates. Conjugates were synthesized via carbodiimide chemistry and characterized by 1H NMR and FTIR. Conjugation of D...
Source: International Journal of Pharmaceutics - July 12, 2018 Category: Drugs & Pharmacology Source Type: research

Predicting Physical Stability of Ternary Amorphous Solid Dispersion Using Specific Mechanical Energy in a Hot Melt Extrusion Process
This study focuses on the relationship between drug dissolution properties, physical stability against recrystallization, and specific mechanical energy (SME) from a hot melt extrusion (HME) process of ternary amorphous solid dispersions (ASDs) containing indomethacin (IND), HPMC and mesoporous silica (XDP) prepared using different HME screw condition (the number of kneading zones /rotation speed). The screw condition greatly influenced the amorphous characteristics of the processed material and SME values. The higher SME samples demonstrated a larger parachute effect in dissolution test and reduced the rate of recrystalli...
Source: International Journal of Pharmaceutics - July 11, 2018 Category: Drugs & Pharmacology Source Type: research

Amorphous Magnesium Carbonate Nanoparticles with Strong Stabilizing Capability for Amorphous Ibuprofen
This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved. Biocompatibility of the nanoparticles was demonstrated in vitro using Human dermal fibroblasts and stability of the nanocomposite formulation was verified with a storage time of six months. The succ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

A stimuli-responsive insulin delivery system based on reversible phenylboronate modified cyclodextrin with glucose triggered host-guest interaction
In this study, a smart drug carrier that can release insulin depending on the changes in blood glucose levels was designed. Combining two popular molecules through facile synthetic processes, a drug carrier of reversible phenylboronate group modified cyclodextrin (β-CD-EPDME) was fabricated. The drug carrier is composed of cyclodextrin, which can encapsulate insulin, and phenylboronate, which is sensitive to the cis-diols in some saccharides. Moreover, β-CD-EPDME can successfully encapsulate insulin and almost completely release insulin in the presence of glucose. The detached phenylboronic acid moiety triggered ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Competing for Water: A New Approach to Understand Disintegrant Performance
In this study, water uptake and force development as well as water sorption experiments were performed of tablets containing either a soluble or an insoluble filler, one of four different binders, and one of four different disintegrants. For both fillers, one disintegrant performed distinctly worse than the others. For the insoluble filler, dibasic calcium phosphate (DCP), sodium starch glycolate resulted in the longest disintegration, for the soluble filler, lactose, croscarmellose sodium performed worst. Based on the experimental results, the authors introduce the competition-for-water hypotheses, which takes into consid...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of drug incorporation technique and polymer combination on the performance of biopolymeric antifungal buccal films
Publication date: Available online 6 July 2018Source: International Journal of PharmaceuticsAuthor(s): G. Tejada, M.C. Lamas, L. Svetaz, C.J. Salomón, V.A. Alvarez, D. LeonardiAbstractNumerous films with a dissolved or dispersed active principle within a polymeric matrix have been described in literature. However, the incorporation of solid crystals into the films may influence several relevant properties. Additionally, it has been reported that different polymeric matrices lead to films presenting a different performance. The aim of this work was to evaluate the effect of the combination of chitosan with carrageena...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

A novel nasal almotriptan loaded solid lipid nanoparticles in mucoadhesive in situ gel formulation for brain targeting: Preparation, characterization and in vivo evaluation
Publication date: Available online 6 July 2018Source: International Journal of PharmaceuticsAuthor(s): Nancy Abdel Hamid Abou Youssef, Abeer Ahmed Kassem, Ragwa Mohamed Farid, Fatma Ismail, Magda Abd Elsamea EL-Massik, Nabila Ahmed BoraieAbstractThis work aimed at designing efficient safe delivery system for intranasal (IN) brain targeting of the water soluble anti- migraine drug Almotriptan malate (ALM). Solid lipid nanoparticles (SLNs) were prepared by w/o/w double emulsion-solvent evaporation method. Selection of the optimized SLNs formula was based on evaluating particle size (PS), poly dispersity index (PDI) and entra...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

3D printed medicines: A new branch of digital healthcare
This article reviews the current state-of-the-art in FDM technology for medical and pharmaceutical research, including its use for personalised treatments and interconnection within digital health networks. The outstanding challenges are also discussed, with a focus on the future developments that are required to facilitate its integration within pharmacies and hospitals.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Stabilization of unilamellar catanionic vesicles induced by β-cyclodextrins: a strategy for a tunable drug delivery depot
This study focuses on the impact of β-cyclodextrins for the stabilization of SDS/CTAB catanionic vesicles. Molar ratio and sample preparation procedures have been investigated to evaluate the temperature stability of catanionic vesicles. Diffusion and spectroscopic techniques evidenced that when β-cyclodextrins are added, unilamellar structures are stabilized above the multilamellar-unilamellar vesicles critical temperature. The results evidence encouraging perspectives for the use of vesicular nanoresevoirs for drug depot applications.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalized carbon nanotubes as emerging delivery system for the treatment of cancer
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Shubhangi Mahajan, Abhimanyu Patharkar, Kaushik Kuche, Rahul Maheshwari, Pran Kishore Deb, Kiran Kalia, Rakesh K. TekadeAbstractIn recent time, carbon nanotubes (CNTs) have gained vital importance for pharmaceutical formulation scientist for delivering drugs and genes, owing to their excellent surface properties. For example, their aspect ratio is thought to be responsible for their excellent cell penetration aptitude; anisotropic conductivity/semi-conductivity along their axis is ideal for integration with nervous and mu...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Treatment merits of Latanoprost/Thymoquinone – encapsulated liposome for glaucomatus rabbits
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Heba Mohamed Fahmy, Engy Abd El-Malek Saeed Saad, Neveen Moustafa Sabra, Amal Ahmed El-Gohary, Faten Fathy Mohamed, Mohamed Hassaneen GaberAbstractElevation of the intraocular pressure (IOP) is recognized as a risk factor for glaucoma development. Latanoprost (LAT) is a prostaglandin analog used to reduce the (IOP). Thymoquinone (TQ) is a major bioactive ingredient of Nigella sativa. The aim of this study was to develop novel liposomal drug carriers for ocular delivery of LAT, TQ and a mixture of them to investigate their...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Audible Acoustic Emission Data Analysis for Drug Content Prediction during Tableting Processes
Publication date: Available online 9 July 2018Source: International Journal of PharmaceuticsAuthor(s): Ryoma Tanaka, Kenta Kojima, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Surface-induced crystallization of pharmaceuticals and biopharmaceuticals: A review
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Fiora Artusio, Roberto PisanoAbstractDespite the wide occurrence of crystallization in the pharmaceutical industry, deep understanding and fine control of the process remain a tricky issue. Nevertheless, the successful manufacturing of finished pharmaceutical products, as well as the structural determination of biopharmaceuticals, depend on the size, form, shape and purity of the crystals. The ability of substrates with precise chemistry and topological features to induce nucleation has been thoroughly ass...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers-based drug delivery for treating various lung diseases: A State‐of‐the‐Art Review
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Tulshidas S. Patil, Ashwini S. DeshpandeAbstractAccording to the list published by the WHO for global top ten causes of death, lung diseases contribute nearly one-third of the total mortality. The current treatment on lung diseases provide only symptomatic relief rather than restoring the complete lung functions. Nanostructured lipid carriers-based drug delivery system (NLCs-based DDS) provide a breakthrough in treating various lung diseases.This review provides the readers with background information for ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical cocrystallization techniques. Advances and challenges
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Marisa Rodrigues, Bárbara Baptista, João Almeida Lopes, Mafalda Cruz SarraguçaAbstractCocrystals are homogenous (single-phase) crystalline structures composed by two or more components in a definite stoichiometric ratio bonded together by noncovalent bonds. Pharmaceutical industry has been showing interest in cocrystals due to their ability to improve active pharmaceutical ingredients (API’s) properties, such as solubility, dissolution, bioavailability, stability and processabili...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Promising nanotherapy in treating leishmaniasis
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Aline de Souza, Débora Soares Souza Marins, Samir Leite Mathias, Lis Marie Monteiro, Megumi Nishitani Yukuyama, Cauê Benito Scarim, Raimar Löbenberg, Nádia Araci Bou-ChacraAbstractLeishmaniases are infectious diseases caused by an intracellular protozoan in humans by 20 different species of Leishmania among more than 53 species. There are at least twelve million cases of infections worldwide and three hundred and fifty million people are at risk in at least 98 developing countries ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Chemical modifications of insulin: Finding a compromise between stability and pharmaceutical performance
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Mohsen Akbarian, Younes Ghasemi, Vladimir N. Uversky, Reza YousefiAbstractInsulin, a key peptide hormone that conjointly with its receptor regulates blood glucose levels, is used as the major means to treat diabetes. This therapeutic hormone may undergo different chemical modifications during industrial processes, pharmaceutical formulation, and through its endogenous storage in the pancreatic β-cells. Insulin is highly sensitive to the environmental stresses and easily undergoes structural changes, b...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoemulsion containing 8-methoxypsoralen for topical treatment of dermatoses: Development, characterization and ex vivo permeation in porcine skin
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Catarina Amorim Oliveira, Marcos Martins Gouvêa, Gabriel Ramos Antunes, Zaida Maria Faria de Freitas, Flávia Ferreira de Carvalho Marques, Eduardo Ricci-JuniorAbstractOral therapy with 8-methoxypsoralen (8-MOP) may cause major side effects, whereas the topical treatment might not be much effective due to the low penetration induced by typical formulations. Therefore, the objectives of this work are the development and characterization of a nanoemulsion (NE) containing 8-MOP together with an ex...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced cellular uptake and osteogenic differentiation efficiency of melatonin by inclusion complexation with 2-hydroxypropyl β-cyclodextrin
In this study, an inclusion complex of MLT with 2-hydroxypropyl β-cyclodextrin (HP-β-CD) was prepared to improve the water solubility, and the osteogenic differentiation ability of the inclusion complex was investigated in MC3T3-E1 cells. The formation of HP-β-CD/MLT inclusion complex was confirmed by 1H and 13C nuclear magnetic resonance spectroscopy and wide-angle X-ray diffraction. The water solubility of MLT increased linearly upon addition of HP-β-CD because of the formation of the inclusion complex. Additionally, treatment of the cells with HP-β-CD/MLT inclusion complex showed higher uptake a...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of high pressure homogenization and stirred bead milling for the production of nano-crystalline suspensions
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Mostafa Nakach, Jean-René Authelin, Marc-Antoine Perrin, Harivardhan Reddy LakkireddyAbstractCurrently, the two technologies primarily used for the manufacturing of nano-crystalline suspensions using top down process (i.e. wet milling) are high pressure homogenization (HPH) and stirred bead milling (SBM). These two technologies are based upon different mechanisms, i.e., cavitation forces for HPH and shear forces for stirred bead milling. In this article, the HPH and SBM technologies are compared in ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

A novel fusion protein attenuates collagen–induced arthritis by targeting interleukin 17A and tumor necrosis factor α
This study was undertaken to generate a novel dual targeting fusion protein (DTF), targeting tumor necrosis factor α (TNF-α) and interleukin 17A (IL-17A), and determine its anti-arthritis properties in vitro and in vivo. DTF consisted of an anti-IL-17A single chain variable fragment, a soluble TNF receptor 1, and an Fc fragment. Both clinical and histopathological evaluations suggest that DTF and etanercept can ameliorate collagen induced arthritis. However, the arthritis severity score of DTF-treated mice was lower than that of etanercept-treated mice. In addition, DTF was more potent than etanercept in decrea...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin-grafted poly(anhydride) nanoparticles for oral glibenclamide administration. In vivo evaluation using C. elegans
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): David Lucio, María Cristina Martínez-Ohárriz, Zhongwei Gu, Yiyan He, Paula Aranaz, José Luis Vizmanos, Juan M. IracheAbstractThe aim of this work was to prepare and evaluate cyclodextrins-modified poly(anhydride) nanoparticles to enhance the oral administration of glibenclamide. A conjugate polymer was synthesized by incorporating hydroxypropyl-β-cyclodextrin to the backbone of poly(methylvinyl ether-co-maleic anhydride) via Steglich reaction. The degree of substitution of ...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of mannitol granules and powder: A comparative study using two flowability testers
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Yoshiko Takeuchi, Tomoka Tomita, Junko Kuroda, Akihiro Kageyu, Chihiro Yonekura, Yukiyoshi Hiramura, Kohei Tahara, Hirofumi TakeuchiAbstractIn the manufacture of tablets, especially in direct tableting processes, the flowability of excipient powders and formulated powders is one of the most important characteristics. In the past two decades, orally disintegrating tablets (ODTs) have been prepared as popular solid dosage forms for elderly patients. Many types of mannitol granules have been developed and mar...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery
This study aims to develop and characterize inhalable ciprofloxacin (CPx)-loaded poly(vinyl alcohol) (PVA) microparticles by a single-step spray-drying procedure. The optimization of the processing parameters was achieved by an orthogonal design of the most relevant processing parameters (polymer concentration, feed rate and inlet temperature). The obtained spray-dried particles showed a drug encapsulation efficiency higher than 90%. Furthermore, PVA-CPx formulations, with drug contents up to 10 wt%, showed a morphology and size suitable for inhalation, with a sustained release profile over 24 h. Data from Fourier tran...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Improved design and characterization of PLGA/PLA-coated Chitosan based micro-implants for controlled release of hydrophilic drugs
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Soumyarwit Manna, Anna M. Donnell, Necati Kaval, Marwan F. Al-Rjoub, James J. Augsburger, Rupak K. BanerjeeAbstractRepetitive intravitreal injections of Methotrexate (MTX), a hydrophilic chemotherapeutic drug, are currently used to treat selected vitreoretinal (VR) diseases, such as intraocular lymphoma. To avoid complications associated with the rapid release of MTX from the injections, a Polylactic acid (PLA) and Chitosan (CS)-based MTX micro-implant prototype was fabricated in an earlier study, which sh...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Comparative evaluation of powder flow parameters with reference to particle size and shape
This study showed that while the various flow characterisation techniques were different in terms of their applications, there were common physical attributes that governed the measurements.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Deformation behavior of crystallized mannitol during compression using a rotary tablet press simulator
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Nicolas Tarlier, Ian Soulairol, Noelia Sanchez-Ballester, Gilles Baylac, Adrien Aubert, Philippe Lefevre, Bernard Bataille, Tahmer SharkawiAbstractMannitol is commonly used as a pharmaceutical excipient for tablets; the most widely used oral dosage form for drug delivery. For tableting, mannitol is provided in two different forms: native crystals and textured particles. In order to optimize its formulation, a good understanding of the mechanical behavior mechanism of mannitol is necessary. Thus, the aim of...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

The effects of three absorption-modifying critical excipients on the in vivo intestinal absorption of six model compounds in rats and dogs
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): D. Dahlgren, C. Roos, P. Johansson, C. Tannergren, A. Lundqvist, P. Langguth, M. Sjöblom, E. Sjögren, H. LennernäsAbstractPharmaceutical excipients that may affect gastrointestinal (GI) drug absorption are called critical pharmaceutical excipients, or absorption-modifying excipients (AMEs) if they act by altering the integrity of the intestinal epithelial cell membrane. Some of these excipients increase intestinal permeability, and subsequently the absorption and bioavailability of the drug....
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-tumor and anti-metastasis efficacy against breast cancer with an intratumoral injectable phospholipids-based phase separation gel co-loaded with 5-fluotouracil and magnesium oxide by neutralizing acidic microenvironment
In conclusion, the novel 5FU + MgO-PPSG system might have a great potential to improve treatment method against breast metastasis.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of glycerol on the physical and mechanical properties of thin gellan gum films for oral drug delivery
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Patrizia Paolicelli, Stefania Petralito, Gabriele Varani, Martina Nardoni, Settimio Pacelli, Laura Di Muzio, Jacopo Tirillò, Cecilia Bartuli, Stefania Cesa, Maria Antonietta Casadei, Alessandra AdroverAbstractIn this work, deacylated gellan gum and the plasticizer glycerol were used as primary components for the preparation of thin films intended for the oral delivery of therapeutic molecules. The samples were prepared by a solvent casting method and characterized for their thickness, tensile proper...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Rapid paper based colorimetric detection of glucose using a hollow microneedle device
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Dean Nicholas, Keiran A. Logan, Yingjie Sheng, Jinhui Gao, Sian Farrell, Dorian Dixon, Bridgeen Callan, Anthony P. McHale, John F. CallanAbstractThe monitoring of blood glucose is a key aspect of diabetes care in limiting the negative effects of hyperglycaemia to both the microvasculature and macrovasculature. Self-monitoring of blood glucose (SMBG) gives an indication of blood glucose at a specific point in time and is recommended to be carried out four times daily. However, due to the inconvenience and a...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Immunogenicity of diphtheria toxoid and poly(I:C) loaded cationic liposomes after hollow microneedle-mediated intradermal injection in mice
In this study, we aimed to investigate the immunogenicity of cationic liposomes loaded with diphtheria toxoid (DT) and poly(I:C) after hollow microneedle-mediated intradermal vaccination in mice. The following liposomal formulations were studied: DT loaded liposomes, a mixture of free DT and poly(I:C)-loaded liposomes, a mixture of DT-loaded liposomes and free poly(I:C), and liposomal formulations with DT and poly(I:C) either individually or co-encapsulated in the liposomes. Reference groups were DT solution adjuvanted with or without poly(I:C) (DT/poly(I:C)). The liposomal formulations were characterized in terms of parti...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Phase transitions of antibiotic clarithromycin forms I, IV and new form VII crystals
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Masataka Ito, Rika Shiba, Miteki Watanabe, Yasunori Iwao, Shigeru Itai, Shuji NoguchiAbstractMetastable crystal form I of the antibiotic clarithromycin has a pharmaceutically valuable characteristic that its crystalline phase transition can be applied for its sustained release from tablets. The phase transition of form I was investigated in detail by single crystal and powder X-ray analyses, dynamic vapor sorption analysis and thermal analysis. The single crystal structure of form I revealed that form I wa...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Calcium enhances gene expression when using low molecular weight poly-l-lysine delivery vehicles
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Sheng-Xue Xie, Abdulgader A. Baoum, Nabil A. Alhakamy, Cory J. BerklandAbstractFour molecular weights of poly-l-lysine (PLL) [1000–5000 Da, 1500–8000 Da, 4000–15,000 Da and 15,000–30,000 Da] and three molecular weights of polyethyleneimine (PEI) [800 Da, 2,000 Da, and 25,000 Da] were used to systematically study the effect of calcium (Ca2+) to improve transfection efficiency of polyelectrolyte complexes. Complexes made using different molecular weights of PLL or PEI po...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of lidocaine forms (salt vs. freebase) on properties of drug–eudragit® L100-55 extrudates prepared by reactive melt extrusion
This study examines the preparation of sustained-release lidocaine polyelectrolyte complex using reactive melt extrusion. Eudragit L100-55 was selected as the ionic polymer. The influence of drug forms (freebase vs. hydrochloride salt) on lidocaine–Eudragit L100-55 interactions, physical stability, and dissolution properties of extrudates was investigated. It was confirmed by DSC, FT-IR and Raman spectroscopy that polyelectrolyte could only form via the acid–base reaction between Eudragit L100-55 and lidocaine freebase. Due to this ionic interaction, the lidocaine extrudate was physically more stable than the l...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research