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An advanced technique using an electronic taste-sensing system to evaluate the bitterness of orally disintegrating films and the evaluation of model films
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Yoshiko Takeuchi, Rina Usui, Hidekazu Ikezaki, Kohei Tahara, Hirofumi Takeuchi Taste detection systems using electronic sensors are needed in the field of pharmaceutical design. The aim of this study was to propose an advanced technique using a taste-sensing system to evaluate the bitterness of an orally disintegrating film (ODF) samples. In this system, a solid film sample is kept in the test medium with stirring, and the sensor output is recorded. Model films were prepared using a solution-casting method with a...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Peptide modified mesenchymal stem cells as targeting delivery system transfected with miR-133b for the treatment of cerebral ischemia
This study is the first to develop MSCs co-modified with targeting peptide and microRNAs as potential targeting therapeutic agents. This targeting delivery system is expected to be applicable to other cell types and other diseases aside from stroke. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Hesham M. Tawfeek, Ahmed A.H. Abdellatif, Thomas J. Dennison, Afzal R. Mohammed, Younis Sadiq, Imran Y. Saleem The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Turning the screw even further to increase microparticle retention and ocular bioavailability of associated drugs: The bioadhesion goal
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): J. Rodríguez Villanueva, L. Rodríguez Villanueva Ocular drug delivery is one of the most fascinating and challenging tasks facing pharmaceutical researchers. Improving drug ocular residence time and/or penetration is complex. Microparticles (MP) provide interesting opportunities to increase ocular bioavailability of drugs and patient compliance brought about by decreased frequency of dosing. However, sustained-release microsphere formulation would fail to accomplish the task of long-lasting drug rel...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Breaching barriers in glioblastoma. Part II: Targeted drug delivery and lipid nanoparticles
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Ana Miranda, María J Blanco-Prieto, João Sousa, Alberto Pais, Carla Vitorino Tailored nanocarriers have gained huge research focus for brain drug delivery, aimed at combating several neuro-oncological conditions, such as the glioblastoma multiforme (GBM). The progress of knowledge on the pathogenesis of GBM has allowed identifying the major hurdles for efficient treatment, encompassing biological interfaces (blood-brain barrier and blood–brain tumour barrier), specificities of tumour microenvi...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Breaching barriers in glioblastoma. Part I: Molecular pathways and novel treatment approaches
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Ana Miranda, María Blanco-Prieto, João Sousa, Alberto Pais, Carla Vitorino Glioblastoma multiforme (GBM) is the most common primary brain tumour, and the most aggressive in nature. The prognosis for patients with GBM remains poor, with a median survival time of only 1–2 years. The treatment failure relies on the development of resistance by tumour cells and the difficulty of ensuring that drugs effectively cross the dual blood brain barrier/blood brain tumour barrier. The advanced molecular an...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Downstream drug product processing of itraconazole nanosuspension: Factors influencing tablet material properties and dissolution of compacted nanosuspension-layered sugar beads
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): En Hui Tan, Johannes Parmentier, Ariana Low, Jan Peter Möschwitzer There has been limited research done on the downstream processing of nanosuspensions into solid oral dosage forms. This paper demonstrates the bead layering process with a layering level at 150% and 240%, as well as the selection and justification of the outer phase excipients for tabletability and disintegrating properties. In a previous study, an itraconazole nanosuspension stabilised by SDS and HPMC E5 was layered onto sugar beads with co...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Void forming index: A new parameter for detecting microstructural transformation caused by powder agglomeration
In this study, we focused on the application of inverse gas chromatography (iGC) to detect powder agglomeration directly. There was a slight change between the powder state and lactose agglomerates using powder X-ray diffraction, and dynamic vapor sorption. On the other hand, a change in pressure drop was found during measurement of lactose using iGC. After measurement by iGC, powdered lactose agglomerated. This finding suggests that a pressure drop is related to powder agglomeration and can be employed to detect the onset of powder agglomeration. Based on these findings, we propose a novel index—the Void Forming Ind...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

The suitability of common compressibility equations for characterizing plasticity of diverse powders
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Shubhajit Paul, Changquan Calvin Sun The analysis of powder compressibility data yields useful information for characterizing compaction behavior and mechanical properties of powders, especially plasticity. Among the many compressibility equations proposed in powder compaction research, the Heckel equation and the Kawakita equation are the most commonly used, despite their known limitations. Systematic evaluation of the performance in analyzing compressibility data suggested the Kuentz-Leuenberger equation is su...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

A novel multi-tiered experimental approach unfolding the mechanisms behind cyclodextrin-vitamin inclusion complexes for enhanced vitamin solubility and stability
This study was conducted to provide a mechanistic account for understanding the synthesis, characterization and solubility phenomena of vitamin complexes with cyclodextrins (CD) for enhanced solubility and stability employing experimental and in silico molecular modeling strategies. New geometric, molecular and energetic analyses were pursued to explicate experimentally derived cholecalciferol complexes. Various CD molecules (α-, β-, γ-, and hydroxypropyl β-) were complexed with three vitamins: cholecalciferol, ascorbic acid and α-tocopherol. The Inclusion Efficiency (IE%) was computed for each ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Broadening the spectrum of small-molecule antibacterials by metallic nanoparticles to overcome microbial resistance
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Mahendra Rai, Avinash P. Ingle, Raksha Pandit, Priti Paralikar, Indarchand Gupta, Marco V. Chaud, Carolina Alves dos Santos Now-a-days development of microbial resistancce have become one of the most important global public health concerns. It is estimated that about 2 million people are infected in USA with multidrug resistant bacteria and out of these, about 23,000 die per year. In Europe, the number of deaths associated with infection caused by MDR bacteria is about 25,000 per year, However, the situation in ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Advances in intravesical drug delivery systems to treat bladder cancer
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Oluwadamilola M. Kolawole, Wing Man Lau, Hugh Mostafid, Vitaliy V. Khutoryanskiy Chemotherapeutic agents administered intravesically to treat bladder cancer have limited efficacy due to periodic dilution and wash-out during urine formation and elimination. This review describes the pathophysiology, prevalence and staging of bladder cancer, and discusses several formulation strategies used to improve drug residence within the bladder. These include the use of amphiphilic copolymers, mucoadhesive formulations, hyd...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Supersaturating drug delivery systems: The potential of co-amorphous drug formulations
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Riikka Laitinen, Korbinian Löbmann, Holger Grohganz, Petra Priemel, Clare J. Strachan, Thomas Rades Amorphous solid dispersions (ASDs) are probably the most common and important supersaturating drug delivery systems for the formulation of poorly water-soluble compounds. These delivery systems are able to achieve and maintain a sustained drug supersaturation which enables improvement of the bioavailability of poorly water-soluble drugs by increasing the driving force for drug absorption. However, ASDs often ...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Engineering PLGA nano-based systems through understanding the influence of nanoparticle properties and cell-penetrating peptides for cochlear drug delivery
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Hui Cai, Zhongping Liang, Wenli Huang, Lu Wen, Gang Chen The properties of poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) and penetration enhancers play a deciding role in the inner ear drug delivery of NPs across the round window membrane (RWM). Thus, PLGA nano-based systems with a variety of particle sizes and surface chemistries and those combined with cell-penetrating peptides (CPPs) as penetration enhancers were devised to explore their impact on the cochlear drug delivery in vivo. First, we demon...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Relationships between response surfaces for tablet characteristics of placebo and API-containing tablets manufactured by direct compression method
In this study, we evaluated the correlation between the response surfaces for the tablet characteristics of placebo and active pharmaceutical ingredient (API)-containing tablets. The quantities of lactose, cornstarch, and microcrystalline cellulose were chosen as the formulation factors. Ten tablet formulations were prepared. The tensile strength (TS) and disintegration time (DT) of tablets were measured as tablet characteristics. The response surfaces for TS and DT were estimated using a nonlinear response surface method incorporating multivariate spline interpolation, and were then compared with those of placebo tablets....
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Amphiphilic lipopeptide significantly enhances uptake of charge-neutral splice switching morpholino oligonucleotide in spinal muscular atrophy patient-derived fibroblasts
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Behnoosh Tajik-Ahmadabad, Anastasios Polyzos, Frances Separovic, Fazel Shabanpoor Splice-switching antisense oligonucleotides (SSOs) are emerging therapeutics with two SSOs recently approved by the FDA for Duchenne muscular dystrophy and spinal muscular atrophy. SSOs are administered without any delivery vector and require large doses to achieve the therapeutic benefit, primarily due to their poor cellular uptake. Although cell-penetrating peptides (CPP) have shown great potential in delivering SSOs into cells, ...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Mechanistic modeling of a capsule filling process
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Peter Loidolt, Stefan Madlmeir, J.G. Khinast Filling a dosator nozzle moving into a powder bed was investigated using the Discrete Element Method (DEM). Various particle diameters and contact properties were modeled. The simulations qualitatively showed the influence of powder properties on the amount of dosed powder. Two factors that influence the dosed mass were observed. First, the ratio between the particle and dosator diameters affects the packing of particles inside the dosator chamber. Second, the flow be...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Combining R-DOTAP and a particulate antigen delivery platform to trigger dendritic cell activation: Formulation development and in-vitro interaction studies
This study aimed therefore to explore the potential of R-DOTAP stabilized microparticles (MP) to act as a carrier platform for antigens e.g. for cancer vaccination. It was investigated whether or not a combination of R-DOTAP and PLGA leads to a boosted adjuvant effect in dendritic cell maturation. For proper comparison, neutral and negatively charged MPs of comparable sizes were developed. Toxicity, uptake, routing and maturation of the MP platform was assessed in-vitro on human immature dendritic cells (iDCs). Interestingly, none of the tested placebo formulations (without antigen) was capable to induce DC maturation when...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Mechanism study on ion-pair complexes controlling skin permeability: Effect of ion-pair dissociation in the viable epidermis on transdermal permeation of bisoprolol
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Hanqing Zhao, Chao Liu, Peng Quan, Xiaocao Wan, Meiyue Shen, Liang Fang Though ion-pair strategy has been widely used in transdermal drug delivery system, knowledge about the molecular mechanisms involved in the skin permeation processes of ion-pair complexes is still limited. In the present study, a homologous series of fatty acids were chosen to form model ion-pair complexes with bisoprolol (BSP) to rule out the influence of functional groups on polar surface area, stability and other physicochemical propertie...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Scale-up of water-based spider silk film casting using a film applicator
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Elisa Agostini, Gerhard Winter, Julia Engert Spider silk proteins for applications in drug delivery have attracted an increased interest during the past years. Some possible future medical applications for this biocompatible and biodegradable material are scaffolds for tissue engineering, implantable drug delivery systems and coatings for implants. Recently, we reported on the preparation of water-based spider silk films for drug delivery applications. In the current study, we describe the development of a manuf...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Nanoprecipitation process: From encapsulation to drug delivery
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Claudia Janeth Martínez Rivas, Mohamad Tarhini, Waisudin Badri, Karim Miladi, Hélène Greige-Gerges, Qand Agha Nazari, Sergio Arturo Galindo Rodríguez, Rocío Álvarez Román, Hatem Fessi, Abdelhamid Elaissari Drugs encapsulation is a suitable strategy in order to cope with the limitations of conventional dosage forms such as unsuitable bioavailability, stability, taste, and odor. Nanoprecipitation technique has been used in the pharmaceutical and agricultural researc...
Source: International Journal of Pharmaceutics - September 8, 2017 Category: Drugs & Pharmacology Source Type: research

Inhaled powder formulation of naked siRNA using spray drying technology with l-leucine as dispersion enhancer
In this study, siRNA was co-spray dried with mannitol and l-leucine, the latter being a dispersion enhancer. To the best of our knowledge, this is the first time that siRNA in its naked form was formulated into an inhalable dry powder using spray drying technology. The aerosol performance of the powder was evaluated by Next Generation Impactor (NGI). The presence of l-leucine in the formulation could improve the aerosolization of siRNA-containing powders. Results from the X-ray photoelectron spectroscopy (XPS) suggested that l-leucine was enriched on the particle surface and promote powder dispersion. Among the different s...
Source: International Journal of Pharmaceutics - September 6, 2017 Category: Drugs & Pharmacology Source Type: research

Prediction and characterization of the stability enhancing effect of the Cherry-Tag ™ in highly concentrated protein solutions by complex rheological measurements and MD simulations
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Pascal Baumann, Marie-Therese Schermeyer, Hannah Burghardt, Cathrin Dürr, Jonas Gärtner, Jürgen Hubbuch Solution stability attributes are one of the key parameters within the production and launching phase of new biopharmaceuticals. Instabilities of active biological compounds can reduce the yield of biopharmaceutical productions, and may induce undesired reactions in patients, such as immunogenic rejections. Protein solution stability thus needs to be engineered and monitored throughout production...
Source: International Journal of Pharmaceutics - September 4, 2017 Category: Drugs & Pharmacology Source Type: research

Dermal miconazole nitrate nanocrystals – formulation development, increased antifungal efficacy & amp; skin penetration
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Sung Min Pyo, David Hespeler, Cornelia M. Keck, Rainer H. Müller Miconazole nitrate nanosuspension was developed to increase its antifungal activity and dermal penetration. In addition, the nanosuspension was combined with the synergistic additive chlorhexidine digluconate. The production was performed by wet bead milling and both production and formulation parameters were optimized. A stabilizer screening revealed poloxamer 407 and Tween 80 both at 0.15% as the most effective stabilizers for miconazole nano...
Source: International Journal of Pharmaceutics - September 2, 2017 Category: Drugs & Pharmacology Source Type: research

Pickering emulsions stabilized by biodegradable block copolymer micelles for controlled topical drug delivery
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Faiza Laredj-Bourezg, Marie-Alexandrine Bolzinger, Jocelyne Pelletier, Yves Chevalier Surfactant-free biocompatible and biodegradable Pickering emulsions were investigated as vehicles for skin delivery of hydrophobic drugs. O/w emulsions of medium-chain triglyceride (MCT) oil droplets loaded with all-trans retinol as a model hydrophobic drug were stabilized by block copolymer nanoparticles: either poly(lactide)-block-poly(ethylene glycol) (PLA-b-PEG) or poly(caprolactone)-block-poly(ethylene glycol) (PCL-b-PEG). ...
Source: International Journal of Pharmaceutics - August 24, 2017 Category: Drugs & Pharmacology Source Type: research

Multipurpose tenofovir disoproxil fumarate electrospun fibers for the prevention of HIV-1 and HSV-2 infections in vitro
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Kevin M. Tyo, Hung R. Vuong, Danial A. Malik, Lee B. Sims, Houda Alatassi, Jinghua Duan, Walter H. Watson, Jill M. Steinbach-Rankins Sexually transmitted infections affect hundreds of millions of people worldwide. Both human immunodeficiency virus (HIV-1 and −2) and herpes simplex virus-2 (HSV-2) remain incurable, urging the development of new prevention strategies. While current prophylactic technologies are dependent on strict user adherence to achieve efficacy, there is a dearth of delivery vehicles that...
Source: International Journal of Pharmaceutics - August 24, 2017 Category: Drugs & Pharmacology Source Type: research

Formulation and characterization of biocompatible and stable I.V. itraconazole nanosuspensions stabilized by a new stabilizer polyethylene glycol-poly( β-Benzyl-l-aspartate) (PEG-PBLA)
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Lanlan Zong, Xiaohua Li, Haiyan Wang, Yanping Cao, Li Yin, Mengmeng Li, Zhihao Wei, Dongxiao Chen, Xiaohui Pu, Jihong Han Amphiphilic block copolymers, PEG-PBLA with different molecular weights, were synthesized and used as new stabilizers for Itraconazole nannosuspensions (ITZ-PBLA-Nanos). ITZ-PBLA-Nanos were prepared by the microprecipitation-high pressure homogenization method, and the particle size and zeta potential were measured using a ZetaSizer Nano-ZS90. Morphology and crystallinity were studied using TE...
Source: International Journal of Pharmaceutics - August 24, 2017 Category: Drugs & Pharmacology Source Type: research

Electrospun tri-layered zein/PVP-GO/zein nanofiber mats for providing biphasic drug release profiles
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Hoik Lee, Gang Xu, Davood Kharaghani, Masayoshi Nishino, Kyung Hun Song, Jung Soon Lee, Ick Soo Kim Simple sequential electrospinning was utilized to create a functional tri-layered nanofiber mesh that achieves time-regulated biphasic drug release behavior. A tri-layered nanofiber mesh −composed of zein and poly(vinylpyrrolidone) (PVP) as the top/bottom and middle layers, respectively − was constructed through sequential electrospinning with ketoprofen (KET) as the model drug. PVP was blended with gra...
Source: International Journal of Pharmaceutics - August 24, 2017 Category: Drugs & Pharmacology Source Type: research

Organoids as preclinical models to improve intraperitoneal chemotherapy effectiveness for colorectal cancer patients with peritoneal metastases: Preclinical models to improve HIPEC
Conclusion & discussion Organoids are relevant models to study the chemosensitivity of peritoneal metastases from CRCs. These models could be used for large scale drug screening strategies or personalized medicine, for colorectal carcinoma but also for PM from other origins. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 24, 2017 Category: Drugs & Pharmacology Source Type: research

A novel and organic solvent-free preparation of solid lipid nanoparticles using natural biopolymers as emulsifier and stabilizer
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Jingyi Xue, Taoran Wang, Qiaobin Hu, Mingyong Zhou, Yangchao Luo In this work, a new and novel organic solvent-free and synthetic surfactant-free method was reported to fabricate stable solid lipid nanoparticles (SLNs) from stearic acid, sodium caseinate (NaCas) and pectin, as well as water. Melted stearic acid was directly emulsified into an aqueous phase containing NaCas and pectin, followed by pH adjustment and thermal treatment to induce the formation of a compact and dense polymeric coating which stabilized ...
Source: International Journal of Pharmaceutics - August 19, 2017 Category: Drugs & Pharmacology Source Type: research

Atomic layer deposition —A novel method for the ultrathin coating of minitablets
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Jaana Hautala, Tommi Kääriäinen, Pekka Hoppu, Marianna Kemell, Jyrki Heinämäki, David Cameron, Steven George, Anne Mari Juppo We introduce atomic layer deposition (ALD) as a novel method for the ultrathin coating (nanolayering) of minitablets. The effects of ALD coating on the tablet characteristics and taste masking were investigated and compared with the established coating method. Minitablets containing bitter tasting denatonium benzoate were coated by ALD using three different TiO2 na...
Source: International Journal of Pharmaceutics - August 19, 2017 Category: Drugs & Pharmacology Source Type: research

Bioactive mesoporous silica nanostructures with anti-microbial and anti-biofilm properties
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Paul Cătălin Balaure, Bianca Boarca, Roxana Cristina Popescu, Diana Savu, Roxana Trusca, Bogdan Ștefan Vasile, Alexandru Mihai Grumezescu, Alina Maria Holban, Alexandra Bolocan, Ecaterina Andronescu The increasing rate of antibiotic resistant bacteria associated with nosocomial infections in severely ill patients has urged the need for new antibacterial therapies. Nanostructured materials represent emerging innovative approaches to controlled delivery of different antimicrobial drugs. Delivery systems encapsul...
Source: International Journal of Pharmaceutics - August 18, 2017 Category: Drugs & Pharmacology Source Type: research

A polychromatic turbidity microplate assay to distinguish discovery stage drug molecules with beneficial precipitation properties
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): John Morrison, Michelle Nophsker, Paul Elzinga, Maria Donoso, Hyunsoo Park, Roy Haskell A material sparing microplate screening assay was developed to evaluate and compare the precipitation of discovery stage drug molecules as a function of time, concentration and media composition. Polychromatic turbidity time course profiles were collected for cinnarizine, probucol, dipyridamole as well as BMS-932481, and compared with turbidity profiles of monodisperse particle size standards. Precipitation for select sample c...
Source: International Journal of Pharmaceutics - August 18, 2017 Category: Drugs & Pharmacology Source Type: research

Ultra thin hydro-films based on lactose-crosslinked fish gelatin for wound healing applications
This study focuses on the development and characterization of an ultra thin hydro-film based on lactose-mediated crosslinking of fish gelatin by Maillard reaction. Lactose results in the only efficient crosslinker able to produce resistant to handling hydro-films when compared to conventional crosslinkers such as glutaraldehyde or genipin (tested at 25 and 37°C in phosphate buffer saline solution (PBS)).The disappearance of the peak related to the N-containing groups (XPS) and the images obtained by SEM and AFM demonstrate the highly ordered nano-scaled structure of lactose-crosslinked gelatin, confirming the crosslink...
Source: International Journal of Pharmaceutics - August 17, 2017 Category: Drugs & Pharmacology Source Type: research

A novel technique for the visualization of tablet punch surfaces: Characterization of surface modification, wear and sticking
In conclusion, this novel technique may serve as a valuable tool for systematic punch surface characterization, wear status check‐up and optimization of the punch surface quality e.g. for improvement of the anti‐sticking behavior. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 12, 2017 Category: Drugs & Pharmacology Source Type: research

Proposed algorithm for healthcare professionals based on product characteristics and in vitro performances in different use conditions using formoterol-based marketed products for inhalation
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Nathalie Wauthoz, Ismaël Hennia, Bieke Dejaeger, Susana Ecenarro, Karim Amighi Healthcare professionals require an easy algorithm for selecting the most appropriate inhalation product for each patient at the beginning of a treatment. As a case study, we selected five marketed formoterol products: Foradil® and Formagal®, capsule-based dry powder inhalers (DPIs), Novolizer® Formoterol and Oxis®, reservoir-based DPIs and Formoair®, a pressurized metered dose inhaler. We generated...
Source: International Journal of Pharmaceutics - August 12, 2017 Category: Drugs & Pharmacology Source Type: research

pH and NIR-light-responsive magnetic iron oxide nanoparticles for mitochondria-mediated apoptotic cell death induced by chemo-photothermal therapy
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Yunok Oh, Jae-Young Je, Madhappan Santha Moorthy, Hansoo Seo, Won Ho Cho Recently, various therapeutic strategies in anticancer drug development are focused to reduce adverse side effects and to enhance the therapeutic efficacy. Mostly, the iron oxide (Fe3O4) nanoparticles have widely been utilized as an efficient drug delivery system towing to their unique properties such as excellent magnetic behavior, considerably low toxicity, easy surface modification and high drug-loading efficacy. In the present study, we ...
Source: International Journal of Pharmaceutics - August 12, 2017 Category: Drugs & Pharmacology Source Type: research

Dry powder aerosols to co-deliver antibiotics and nutrient dispersion compounds for enhanced bacterial biofilm eradication
This study demonstrates that dry powder aerosols containing high concentrations of a combination treatment effective against P. aeruginosa biofilms could be developed with high yield, aerodynamic properties appropriate for inhalation, and no loss of potency. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 12, 2017 Category: Drugs & Pharmacology Source Type: research

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Francesca Maestrelli, Paola Mura, María Luisa González-Rodríguez, María José Cózar-Bernal, Antonio María Rabasco, Lorenzo Di Cesare Mannelli, Carla Ghelardini Metformin is an oral hypoglycemic agent used in the type 2 diabetes, whose poor bioavailability and short half-life make the development of effective extended-release formulations highly desirable. Different metformin-loaded chitosomal and niosomal formulations were developed and suitably characte...
Source: International Journal of Pharmaceutics - August 11, 2017 Category: Drugs & Pharmacology Source Type: research

Redox sensitive cationic pullulan for efficient gene transfection and drug retention in C6 glioma cells
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Priya S.S., Rekha M.R. Thiolated cationic pullulan was synthesized by conjugating pullulan with polyethyleneimine (PEI) and mercaptosuccinic acid (MSA). The formed conjugate was oxidized to obtain disulfide linked cationic pullulan (PPMSS). PPMSS exhibited good buffering capacity and nanoplexes formulated were of size less than 150nm. Nanoplexes formed with PPMSS are redox sensitive and susceptible to reductive cleavage by dithiothreitol (DTT) ensuring the intracellular release of DNA. In vitro, cytot...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced efficacy of anti-miR-191 delivery through stearylamine liposome formulation for the treatment of breast cancer cells
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Shivani Sharma, Vinoth Rajendran, Ritu Kulshreshtha, Prahlad C. Ghosh MicroRNAs are gaining rapid attention as promising targets for cancer treatment; however, efficient delivery of therapeutic miRNA or anti-miRNA into cancer cells remains a major challenge. Our previous work identified miR-191 as an oncogenic miRNA overexpressed in breast cancer that assists in progression of malignant transformation. Thus, inhibition of miR-191 using antisense miR-191 (anti-miR-191) has immense therapeutic potential...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Gas adsorption on commercial magnesium stearate: Effects of degassing conditions on nitrogen BET surface area and isotherm characteristics
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Darren P. Lapham, Julie L. Lapham Commercial grades of magnesium stearate have been analysed by nitrogen adsorption having been pre-treated at temperatures between 30°C and 110°C and in the as-received state. Characteristics of nitrogen adsorption/desorption isotherms are assessed through the linearity of low relative pressure isotherm data and the BET transform plot together with the extent of isotherm hysteresis. Comparison is made between thermal gravimetric analysis and mass loss on drying...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Solubilization of α-galactosylceramide in aqueous medium: Impact on Natural Killer T cell activation and antitumor responses
In conclusion, it is possible to increase α-GalCer solubility in aqueous solution without limiting its antitumor properties. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Development and in vitro characterization of a papain loaded mucolytic self-emulsifying drug delivery system (SEDDS)
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Christina Leichner, Claudia Menzel, Flavia Laffleur, Andreas Bernkop-Schnürch The aim of the study was to create a self-emulsifying drug delivery system (SEDDS) with mucolytic properties based on incorporated papain for improved mucus permeation. In order to increase the lipophilicity of the enzyme and to dissolve it in SEDDS, hydrophobic ion pairing with sodium deoxycholate in a molar ratio of 20:1 (surfactant: enzyme) was performed. The yield of precipitated papain was 86.8±2.7% and the ...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Comparing the acidities of aqueous, frozen, and freeze-dried phosphate buffers: Is there a “pH memory” effect?
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Ľubica Vetráková, Vít Vykoukal, Dominik Heger The concept of “pH memory” has been established in the literature for the correlation between the pH of a pre-lyophilization solution and the ionization state of freeze-dried powder (lyophile). In this paper, the concept of “pH memory” is explored for the system of an aqueous solution, a frozen solution, and a lyophile. Sodium and potassium phosphate buffers in the pH range of 5–9 were frozen and lyophili...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Supramolecular structure of glibenclamide and β-cyclodextrins complexes
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): David Lucio, Juan Manuel Irache, María Font, María Cristina Martínez-Ohárriz Glibenclamide is an antidiabetic drug showing low bioavailability as consequence of its low solubility. To solve this drawback, the interaction with cyclodextrins has been proposed. The formation of GB-βCDs inclusion complexes was carried out using different methods, βCD derivatives and drug-to-cyclodextrin ratios. The structures of the corresponding complexes have been studied by molecul...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Non-invasive strategies for targeting the posterior segment of eye
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Asadullah Madni, Muhammad Abdur Rahem, Nayab Tahir, Muhammad Sarfraz, Abdul Jabar, Mubashar Rehman, Prince Muhammad Kashif, Syed Faisal Badshah, Kifayat Ullah Khan, Hélder A. Santos The safe and effective treatment of eye diseases has been remained a global myth. Several advancements have been done and various drug delivery and treatment techniques have been suggested. The Posterior segment disorders are the leading cause of visual impairments and blindness. Targeting the therapeutic agents to ...
Source: International Journal of Pharmaceutics - August 10, 2017 Category: Drugs & Pharmacology Source Type: research

Sequential delivery of erlotinib and doxorubicin for enhanced triple negative Breast cancer treatment using polymeric nanoparticle
In this study, a development of a polymeric nanoparticle system for sequential delivery is reported. The nanoparticle system can co-encapsulate and co-deliver a combination of therapeutic agents with different physicochemical properties [i.e. epidermal growth factor receptor (EGFR) inhibitor, erlotinib (Ei), and doxorubicin (Dox)]. Dox is hydrophilic and was complexed with anionic lipid, 1,2-dioleoyl-sn-glycero-3-phosphate (DOPA), via ion pairing to form a hydrophobic entity. Then it was co-encapsulated with hydrophobic Ei in a poly(L-lactide)-b-polyethylene glycol (PLA-b-PEG) nanoparticle by nanoprecipitation. The complex...
Source: International Journal of Pharmaceutics - August 9, 2017 Category: Drugs & Pharmacology Source Type: research

Near-infrared spectroscopy monitoring and control of the fluidized bed granulation and coating processes —A review
This article reviewed the application of NIR spectroscopy in CQA (moisture content, particle size and tablet/pellet thickness) monitoring during fluidized bed granulation and coating processes. Through this review, we would like to provide references for realizing automated control and intelligent production in fluidized bed granulation and pellets coating of pharmaceutical industry. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 9, 2017 Category: Drugs & Pharmacology Source Type: research

Anti-Alzheimer's potential of berberine using surface decorated multi-walled carbon nanotubes: A preclinical evidence
Publication date: 15 September 2017 Source:International Journal of Pharmaceutics, Volume 530, Issues 1–2 Author(s): Shikha Lohan, Kaisar Raza, S.K. Mehta, Gurjit Kaur Bhatti, Sumant Saini, Bhupinder Singh Carbon nanotubes (CNTs), a sub-family of fullerenes, are nanosized seamless cylinders of graphene sheets with enormous drug loading potential. The current studies entail the systematic development of berberine (BRB)-loaded multiwalled carbon nanotubes (MWCNTs) with polysorbate and phospholipid coating for effective management of Alzheimer’s Disease (AD). For systematic optimization using design of experiment...
Source: International Journal of Pharmaceutics - August 6, 2017 Category: Drugs & Pharmacology Source Type: research