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Polymeric micelles: Basic research to clinical practice
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Anand S. Deshmukh, Pratik N. Chauhan, Malleshappa N. Noolvi, Kiran Chaturvedi, Kuntal Ganguly, Shyam S. Shukla, Mallikarjuna N. Nadagouda, Tejraj M. Aminabhavi Rapidly developing polymeric micelles as potential targeting carriers has intensified the need for better understanding of the underlying principles related to the selection of suitable delivery materials for designing, characterizing, drug loading, improving stability, targetability, biosafety and efficacy. The emergence of advanced analytical tools such...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Designing lipid nanoparticles for topical ocular drug delivery
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Jesus Alvarez-Trabado, Yolanda Diebold, Alejandro Sanchez Topically-applied dosage forms, such eye drops, are the most used formulations in the treatment of ocular diseases. Nonetheless, because of the special protection of the eye associated with the ocular surface, drug bioavailability and subsequent therapeutic efficiency obtained with these conventional dosage forms are very low. Recently, novel drug delivery systems have been proposed to solve the main drawbacks of conventional formulations. Nanotechnology,...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Protease-functionalized mucus penetrating microparticles: In-vivo evidence for their potential
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Arshad Mahmood, Flavia Laffleur, Gintare Leonaviciute, Andreas Bernkop-Schnürch The focus of the current study was to explore whether immobilization of proteases to microparticles could result in their enhanced penetration into mucus. The proteases papain (PAP) and bromelain (BROM) were covalently attached to a polyacrylate (PAA; Carbopol 971P) via amide bond formation based on carbodiimide reaction. Microparticles containing these conjugates were generated via ionic gelation with calcium chloride and were ...
Source: International Journal of Pharmaceutics - September 12, 2017 Category: Drugs & Pharmacology Source Type: research

Erlotinib-loaded albumin nanoparticles: A novel injectable form of erlotinib and its in vivo efficacy against pancreatic adenocarcinoma ASPC-1 and PANC-1 cell lines
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): M. Noorani, N. Azarpira, K. Karimian, H. Heli Erlotinib was loaded on albumin nanoparticles for the first time and the cytotoxic effect of the resulting nanoparticles against ASPC-1 and PANC-1 pancreatic adenocarcinoma cell lines was evaluated. The carrier (albumin nanoparticles, ANPs) was synthesized by desolvation method using a mixed solvent followed by thermal crosslinking for stabilization. ANPs and the drug-loaded ANPs were characterized by field emission scanning and transmission electron microscopies, par...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Voriconazole-loaded nanostructured lipid carriers (NLC) for drug delivery in deeper regions of the nail plate
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Kamilla Amaral David Rocha, Anna Paula Krawczyk-Santos, Lígia Marquez Andrade, Luana Clara de Souza, Ricardo Neves Marreto, Tais Gratieri, Stephânia Fleury Taveira Voriconazole-loaded nanostructured lipid carriers (VOR-NLC) were developed and drug penetration evaluated in porcine hooves in vitro. Synergistic effect of urea (Ur), selected among other known chemical enhancers according to hoof hydration potential, was also evaluated. VOR-NLC presented a high encapsulation efficiency (74.52±2.13%...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Increasing the affinity of cationized polyacrylamide-paclitaxel nanoparticles towards colon cancer cells by a surface recognition peptide
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Sanjay Tiwari, Boaz Tirosh, Abraham Rubinstein Nanoparticles of cationized polyacrylamide (CPAA NP), decorated with the recognition peptide VRPMPLQ (to produce CPAA-Pep NP), were prepared, characterized and tested biologically. They were designed to target dysplasia regions in the colon, characterized by overexpressed sialic acid. This targetability was augmented by the addition of VRPMPLQ. Their mean hydrodynamic size was 137nm with narrow size distribution and positive zeta potential. When incubated with three ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Nanosuspensions of a new compound, ER- β005, for enhanced oral bioavailability and improved analgesic efficacy
In conclusion, by using β-CN as a stabilizer, nanosuspensions of ER-β005 were developed and oral absorption was enhanced. Moreover, ER-β005 is a powerful drug that inhibits pain reactions, and its therapeutic efficacy was markedly increased in the Nano-ER-β005. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Antibacterial and anti-encrustation biodegradable polymer coating for urinary catheter
In this study, the strategy used to resist bacterial adhesion and encrustation represents a combination of the antibacterial effects of norfloxacin and silver nanoparticles and the PLGA-based neutralisation of alkali products of urea hydrolysis gained through the degradation of the polymer in an aqueous milieu. Silver nanoparticles were coated with tetraether lipids (TEL) to avoid aggregation when dispersed in acetone and during the film formation. The polymer films loaded with the two antibacterial agents were applied on Polyurethane (PUR) and Silicon sheets. We demonstrated the antibacterial and anti-adhesion effectivene...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of long-circulating nanoparticles loaded with betulinic acid for improved anti-tumor efficacy
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Ankit Saneja, Robin Kumar, Amarinder Singh, Ravindra Dhar Dubey, Mubashir J. Mintoo, Gurdarshan Singh, Dilip M. Mondhe, Amulya K. Panda, Prem N. Gupta The clinical application of betulinic acid (BA), a natural pentacyclic triterpenoid with promising antitumor activity, is hampered due to its extremely poor water solubility and relatively short half-life in the systemic circulation. In order to address these issues, herein, we developed betulinic acid loaded polylactide-co-glycolide- monomethoxy polyethylene glyco...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Electrospun collagen-based nanofibres: A sustainable material for improved antibiotic utilisation in tissue engineering applications
In this study, the effects of collagen type I in polylactic acid-drug electrospun scaffolds for tissue engineering applications are examined. The samples produced were subsequently characterised using a range of techniques. Scanning electron microscopy analysis shows that the fibre morphologies varied across PLA-drug and PLA-collagen-drug samples − the addition of collagen caused a decrease in average fibre diameter by nearly half, and produced nanofibres. Atomic force microscopy imaging revealed collagen-banding patterns which show the successful integration of collagen with PLA. Solid-state characterisation suggest...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Integrated hot-melt extrusion – injection molding continuous tablet manufacturing platform: Effects of critical process parameters and formulation attributes on product robustness and dimensional stability
This study provides a framework for robust tablet development using an integrated hot-melt extrusion-injection molding (IM) continuous manufacturing platform. Griseofulvin, maltodextrin, xylitol and lactose were employed as drug, carrier, plasticizer and reinforcing agent respectively. A pre-blended drug-excipient mixture was fed from a loss-in-weight feeder to a twin-screw extruder. The extrudate was subsequently injected directly into the integrated IM unit and molded into tablets. Tablets were stored in different storage conditions up to 20 weeks to monitor physical stability and were evaluated by polarized light micros...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Impact of Eudragit EPO and hydroxypropyl methylcellulose on drug release rate, supersaturation, precipitation outcome and redissolution rate of indomethacin amorphous solid dispersions
In conclusion, the concentration-time profiles achieved from indomethacin ASD dissolution are a complex interplay of drug release rate, precipitation kinetics and outcome, and precipitate redissolution rate, whereby each of these processes is highly dependent on the polymer(s) employed in the formulation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release
In this study, we found that the in vitro release profile of DNS could be affected by adjusting the weight ratio of benzyl benzoate to sesame oil (the solvent/oil ratio). A longer release period could be attained by increasing the solvent/oil ratio in the formulation. A pharmacokinetic study was conducted in beagle dogs to verify the relationship between the in vitro release and the drug release from the formulations in vivo. The pharmacokinetic study confirmed that the formulation with a higher benzyl benzoate to oil ratio exhibits a longer drug release profile with a lower maximum concentration (Cmax) and a longer time t...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of crystal habit on the sticking propensity of ibuprofen —A case study
This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regularity. The surface energy of the extreme habits were shown to be different where particles that were more regular in shape exhibited surface energies of 9mJ/m2 higher than those that were needle-like in habit. Computational and experimental data reveals that the increase in surface energy of the regular shaped particles can be attributed to the in...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Bilayered buccal films as child-appropriate dosage form for systemic administration of propranolol
The objective of the present study was to develop bilayered buccal films for the release of propranolol hydrochloride. A primary polymeric layer was prepared by casting and drying of solutions of film-forming polymers, such as polyvinylpyrrolidone (PVP) or polyvinylalcohol (PVA), added with different weight ratios of gelatin (GEL) or chitosan (CH). In order to achieve unidirectional drug delivery towards buccal mucosa, a secondary ethylcellulose layer was applied onto the primary layer. Bilayered films were characterized for their physico-chemical (morphology, thickness, drug content and solid state) and functional (water ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Downstream processing from hot-melt extrusion towards tablets: A quality by design approach
This study was designed to screen the influence of process parameters and drug load during HME on both extrudate properties and tableting behaviour of an amorphous solid dispersion formulation using a quality-by-design (QbD) approach. A full factorial experimental design with 19 experiments was used to evaluate the effect of several process variables (barrel temperature: 160–200°C, screw speed: 50–200rpm, throughput: 0.2-0.5kg/h) and drug load (0–20%) as formulation parameter on the hot-melt extrusion (HME) process, extrudate and tablet quality of Soluplus®-Celecoxib amorphous solid dispersions. A...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Poly(glycerol adipate) – indomethacin drug conjugates – synthesis and in vitro characterization
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): T. Wersig, M.C. Hacker, J. Kressler, K. Mäder The linear biodegradable polyester poly(glycerol adipate) (PGA) was synthesized via enzymatic polycondensation using lipase B from Candida antarctica (CAL-B). Every monomer unit of PGA possesses a pendant hydroxyl group which is responsible for the hydrophilic character and moisture swelling. These OH groups were esterified to different degrees with the anti-inflammatory drug indomethacin in order to create a prodrug with a pH-sensitive linker for modified drug r...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

A compressibility based model for predicting the tensile strength of directly compressed pharmaceutical powder mixtures
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Gavin K. Reynolds, Jacqueline I. Campbell, Ron J. Roberts A new model to predict the compressibility and compactability of mixtures of pharmaceutical powders has been developed. The key aspect of the model is consideration of the volumetric occupancy of each powder under an applied compaction pressure and the respective contribution it then makes to the mixture properties. The compressibility and compactability of three pharmaceutical powders: microcrystalline cellulose, mannitol and anhydrous dicalcium phosphate...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Modelling and understanding powder flow properties and compactability of selected active pharmaceutical ingredients, excipients and physical mixtures from critical material properties
In this study, predictive multilinear regression models were effectively developed from critical material properties to estimate static powder flow parameters from particle size distribution data for a single component and for binary systems. A multilinear regression model, which was successfully developed for ibuprofen, also efficiently predicted the powder flow properties for a range of batches of two other active pharmaceutical ingredients processed by the same manufacturing route. The particle size distribution also affected the compactability of ibuprofen, and the scope of this work will be extended to the development...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

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