Oral administration of colitis tissue-accumulating porous nanoparticles for ulcerative colitis therapy
Publication date: Available online 27 December 2018Source: International Journal of PharmaceuticsAuthor(s): Qiubing Chen, Shuangquan Gou, Panpan Ma, Heliang Song, Xin Zhou, Yamei Huang, Moon Kwon Han, Ying Wan, Yuejun Kang, Bo XiaoAbstractTo improve the penetration and accumulation of anti-inflammatory drugs in colitis tissue, we functionalized the surface of porous poly(lactic-co-glycolic acid) nanoparticles (NPs) using pluronic F127 (PF127) and loaded curcumin (CUR) into the resulting NPs to obtain porous PF127-functionalized CUR-loaded NPs (porous PF127-NPs). These NPs had an average hydrodynamic diameter of about 270 n...
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Impact on intestinal permeability of pediatric hyperosmolar formulations after dilution: studies with rat perfusion method
ConclusionsOsmolality parameter is of particular relevance in oral drug administration in neonate because the risk of damaging the gastrointestinal tract and because of the risk that modifying osmolality also modifies its permeability, resulting in a potential change in bioavailability.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Antimicrobial assessment of phage therapy using a porcine model of biofilm infection
Publication date: Available online 25 December 2018Source: International Journal of PharmaceuticsAuthor(s): C. Milho, M. Andrade, D. Vilas Boas, D. Alves, S. SillankorvaAbstractAntibiotic resistant bacterial communities persist in many types of wounds, chronic wounds in particular, in the form of biofilms. Biofilm formation is a major cause of severe infections and the main reason for a negative treatment outcome and slow healing progression. Chronic wounds are a silent epidemic essentially affecting people with co-morbid conditions such as diabetes and obesity and elderly persons particularly those with movement limitatio...
Source: International Journal of Pharmaceutics - December 25, 2018 Category: Drugs & Pharmacology Source Type: research

Production of dry-state ketoprofen-encapsulated PMMA NPs by coupling micromixer-assisted nanoprecipitation and spray drying
We present a two-step process to produce dry-state Ketoprofen-loaded poly(methyl methacrylate) nanoparticles (NPs) with controllable size and tunable drug release profile. A colloidal suspension of drug-loaded nanoparticles was first obtained from a nanoprecipitation process and then transferred into a commercial spray dryer. Three micromixers of different designs and mixing principles (molecular diffusion and impact mixing) were tested. After the first step, highly monomodal NPs in the size range 100 to 210 nm were obtained as seen by the low polydispersity index value (ca. PDI ∼ 0.2) returned by a dynamic light scatt...
Source: International Journal of Pharmaceutics - December 24, 2018 Category: Drugs & Pharmacology Source Type: research

A New Therapeutic Combination for Osteosarcoma: Gemcitabine and Clofazimine Co-loaded Liposomal Formulation
Publication date: Available online 23 December 2018Source: International Journal of PharmaceuticsAuthor(s): Yagmur Caliskan, Ali Deniz Dalgic, Selin Gerekci, Ezgi A. Gulec, Aysen Tezcaner, Can Ozen, Dilek KeskinAbstractOsteosarcoma is the most common cancer in bone. Drug resistance is a challenge of current treatments that needs to be improved with novel treatment strategies. In this research, a new dual drug delivery system was developed with Gemcitabine (GEM) and Clofazimine (CLF) co-loaded liposome formulations. GEM is a well-known anticancer agent and CLF is a leprostatic and anti-inflammatory drug recently recognized ...
Source: International Journal of Pharmaceutics - December 24, 2018 Category: Drugs & Pharmacology Source Type: research

Towards long-acting adrenaline for cardiopulmonary resuscitation: production and characterization of a liposomal formulation
Publication date: Available online 23 December 2018Source: International Journal of PharmaceuticsAuthor(s): Michele Schlich, Chiara Sinico, Donatella Valenti, Anil Gulati, Medha D. Joshi, Valeria Meli, Sergio Murgia, Theodoros XanthosAbstractThe use of adrenaline in cardiopulmonary resuscitation is a long-standing medical procedure, recommended by several international guidelines. However, its unspecific action on adrenergic receptors and the need for repeated administrations pose serious concerns about its safety, the balance between benefits and risks being still under debate. To address this issue, a sustained release n...
Source: International Journal of Pharmaceutics - December 24, 2018 Category: Drugs & Pharmacology Source Type: research

Novel Biosurfactant and Lipid Core-Shell Type Nanocapsular Sustained Release System for Intravenous Application of Methotrexate
Publication date: Available online 22 December 2018Source: International Journal of PharmaceuticsAuthor(s): Sameer S. Katiyar, Varun Kushwah, Chander Parkash Dora, Sanyog JainAbstractIn an attempt to prepare novel core shell nanocapsules, lipid and Stearic acid-Valine conjugate (Biosurfactant) based nanosystem was prepared to attain high drug loading of hydrophilic drug methotrexate (MTX), with sustained release. Antisolvent nanoprecipitation technique was employed for the formulation of nanoparticles (NPs). Optimized formulation depicted 209.6±31.3nm particle size, 0.209±0.072 PDI and 14.98±1.33 %w/w ...
Source: International Journal of Pharmaceutics - December 22, 2018 Category: Drugs & Pharmacology Source Type: research

Light-responsive nanoparticles based on new polycarbonate polymers as innovative drug delivery systems for photosensitizers in PDT
Publication date: Available online 22 December 2018Source: International Journal of PharmaceuticsAuthor(s): Juliane Anderski, Laura Mahlert, Jingjiang Sun, Wolfgang Birnbaum, Dennis Mulac, Sebastian Schreiber, Fabian Herrmann, Dirk Kuckling, Klaus LangerAbstractNanoparticles based on biodegradable polymers are well-known as approved carrier systems for a diversity of drugs. Despite their advantages, such as the option of an active drug targeting or the physicochemical protection of instable payloads, the controlled drug release often underlies intra- and interindividual influences and is therefore difficult to predict. To ...
Source: International Journal of Pharmaceutics - December 22, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro and ex vivo studies on Diltiazem hydrochloride-loaded microsponges in rectal gels for chronic anal fissures treatment
Publication date: Available online 21 December 2018Source: International Journal of PharmaceuticsAuthor(s): Nadezhda Antonova Ivanova, Adriana Trapani, Cinzia Di Franco, Delia Mandracchia, Giuseppe Trapani, Carlo Franchini, Filomena Corbo, Giuseppe Tripodo, Iliyan Nikolov Kolev, Georgi Stoyanov Stoyanov, Kameliya Zhechkova BratoevaAbstractDiltiazem hydrochloride, topically applied at 2% concentration, is considered effective for the treatment of chronic anal fissures, althought it involves several side effects among which anal pruritus and postural hypotension. To test the hypothesis that a sustained delivery system of dil...
Source: International Journal of Pharmaceutics - December 21, 2018 Category: Drugs & Pharmacology Source Type: research

PEGylated doxorubicin cloaked nano-graphene oxide for dual-responsive photochemical therapy
In this study, DOX-PEG polymers with different PEG molecular weight were synthesized to modify nano graphene oxide (NGO) to simultaneously realize the solubilization of NGO and the high loading capacity of DOX. The result showed that the drug release of NGO@DOX-PEG was pH sensitive. NIR irradiation could augment the drug release, cellular uptake, cytotoxicity and nuclear translocation of nanodrugs. Among the three kinds of nanodrugs, NGO@DOX-PEG5K was superior to others. It suggested that after conjugating with PEG, the bond between DOX-PEG and NGO was weakened, which resulted in a better drug release and treatment effect....
Source: International Journal of Pharmaceutics - December 21, 2018 Category: Drugs & Pharmacology Source Type: research

Quantitative Evaluation of Different Rotary Tablet Presses by Compaction Velocity based on Compaction Simulation Study
Publication date: Available online 21 December 2018Source: International Journal of PharmaceuticsAuthor(s): Takuma Takahashi, Hiroyasu Toyota, Yosuke Kuroiwa, Hiroyuki Yoshino, Hisami Kondou, Kazunari Yamashita, Tadashi Hakomori, Hirofumi TakeuchiGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 21, 2018 Category: Drugs & Pharmacology Source Type: research

Protecting Bactofencin A to enable its Antimicrobial Activity using Mesoporous Matrices
Publication date: Available online 19 December 2018Source: International Journal of PharmaceuticsAuthor(s): Edel Durack, Sarah Mallen, Paula M. O'Connor, Mary C. Rea, R.Paul Ross, Colin Hill, Sarah HudsonAbstractThere is huge global concern surrounding the emergence of antimicrobial resistant bacteria and this is resulting in an inability to treat infectious diseases. This is due to a lack of new antimicrobials coming to the market and irresponsible use of traditional antibiotics. Bactofencin A, a novel antimicrobial peptide which shows potential as an antibiotic, is susceptible to enzyme degradation. To improve its soluti...
Source: International Journal of Pharmaceutics - December 20, 2018 Category: Drugs & Pharmacology Source Type: research

Co-former selection for co-amorphous drug-amino acid formulations
Publication date: Available online 19 December 2018Source: International Journal of PharmaceuticsAuthor(s): Georgia Kasten, Korbinian Löbmann, Holger Grohganz, Thomas RadesAbstractWe have previously developed a fast screening method on the ability of twenty amino acids (AA) to form co-amorphous formulations with six drugs upon ball milling. In this work, the potential advantages in physical stability and dissolution rate of the 36 successful co-amorphous formulations, compared to the pure amorphous drug, were further investigated. The physical stability of the formulations at dry conditions was assessed by X-ray powde...
Source: International Journal of Pharmaceutics - December 20, 2018 Category: Drugs & Pharmacology Source Type: research

Ion-pair approach coupled with nanoparticle formation to increase bioavailability of a low permeability charged drug
In conclusion, the combination of ion-pair plus polymeric NPs have proved to be a simple and very useful approach to achieve a controlled release and to increase the bioavailability of a low permeability charged drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 20, 2018 Category: Drugs & Pharmacology Source Type: research

Bioresorbable filomicelles for targeted delivery of betulin derivative – in vitro study
Publication date: Available online 18 December 2018Source: International Journal of PharmaceuticsAuthor(s): Katarzyna Jelonek, Janusz Kasperczyk, Suming Li, Thi Hong Nhung Nguyen, Arkadiusz Orchel, Ewa Chodurek, Piotr Paduszyński, Marzena Jaworska-Kik, Elwira Chrobak, Ewa Bębenek, Stanisław Boryczka, Magdalena Jarosz-Biej, Ryszard Smolarczyk, Aleksander ForyśAbstractFilomicelles (worm-like micelles) possess high drug loading capacity and long circulation time in the bloodstream. A novel approach can be filomicelles with folic acid (FA) as a targeting moiety. Folate-drug delivery systems can target FA receptors (FAR) th...
Source: International Journal of Pharmaceutics - December 19, 2018 Category: Drugs & Pharmacology Source Type: research

Design, development and evaluation of PEGylated rhGH with preserving its bioactivity at highest level after modification
In this study, simultaneous optimization of PEGylation efficiency and preserved bioactivity of recombinant human growth hormone (rhGH) was investigated. In this regard, experiments were designed by the response surface methodology (RSM)-central composite design (CCD) utilizing design expert software. Under the obtained optimum conditions of 6.73 molar ratio of PEG to protein and pH 7.71 as the main factors affect the process, 54% PEGylation efficiency and 63% preserved bioactivity can be achieved. Based on the ANOVA table, model F-values equal to 31.16 and 20.8 for PEGylation efficiency and preserved bioactivity, respectiv...
Source: International Journal of Pharmaceutics - December 19, 2018 Category: Drugs & Pharmacology Source Type: research

Novel, Lean and Environment-friendly Granulation Method: Green Fluidized Bed Granulation (GFBG)
Publication date: Available online 17 December 2018Source: International Journal of PharmaceuticsAuthor(s): Hiroshi Takasaki, Atsushi Sakurai, Takuma Katayama, Yuka Matsuura, Naoko Ohyagi, Koichi Wada, Agata Ishikawa, Etsuo YonemochiAbstractThe Green fluidized bed granulation (GFBG) technology is based on the moisture activated dry granulation (MADG) technique and consists only of a mixing and spraying process using a fluidized bed granulator, requiring no heating process. This provides a less energy-consuming and environment-friendly granulation method compared to current fluidized bed granulation (FBG) and high-shear gra...
Source: International Journal of Pharmaceutics - December 18, 2018 Category: Drugs & Pharmacology Source Type: research

Vesicular phospholipid gels as drug delivery systems for small molecular weight drugs, peptides and proteins: state of the art review
Publication date: Available online 18 December 2018Source: International Journal of PharmaceuticsAuthor(s): Michaela Breitsamer, Gerhard WinterAbstractLipid-based drug delivery has been investigated for a long time when it comes to liposomes and solid-lipid implants or solid-lipid nanoparticles. The promising, characteristic properties of these systems have led to the development of newer lipid-based drug delivery systems for the sustained release of drugs like liposomes for sustained delivery of substances, DepoFoamTM technology, phospholipid-based phase separation gels and vesicular phospholipid gels. Vesicular phospholi...
Source: International Journal of Pharmaceutics - December 18, 2018 Category: Drugs & Pharmacology Source Type: research

Controlled dual drug release by coaxial electrospun fibers – Impact of the core fluid on drug encapsulation and release
Publication date: Available online 18 December 2018Source: International Journal of PharmaceuticsAuthor(s): Jing Wang, Maike WindbergsAbstractControlled release of hydrophilic drugs from carriers is still faced with problems due to the poor compatibility of such substances with slowly degradable polymers leading to challenges regarding fabrication as well as undesired burst release of the encapsulated drugs. In this context, coaxial electrospinning being capable of simultaneously using two different solvent systems provides a promising strategy. However, the coaxial electrospinning process is extremely complex and numerous...
Source: International Journal of Pharmaceutics - December 18, 2018 Category: Drugs & Pharmacology Source Type: research

Emodin-nicotinamide (1:2) cocrystal identified by thermal screening to improve emodin solubility
Publication date: Available online 18 December 2018Source: International Journal of PharmaceuticsAuthor(s): Boosung Park, Woojin Yoon, Jungmin Yun, Eunmi Ban, Hoseop Yun, Aeri KimAbstractEmodin (EM), an anthraquinone obtained from natural products, is known for many pharmacological activities. However, further evaluation and interpretation of toxicity or pharmacological activity of emodin are limited due to its poor aqueous solubility. We aimed to identify an emodin cocrystal with improved pharmaceutical properties. Among various compounds screened by thermal analysis, nicotinamide (NCT) was identified as a potential cocry...
Source: International Journal of Pharmaceutics - December 18, 2018 Category: Drugs & Pharmacology Source Type: research

Macrophage functionality and homeostasis in response to oligoethyleneglycol-coated IONPs: impact of a dendritic architecture
Publication date: Available online 14 December 2018Source: International Journal of PharmaceuticsAuthor(s): Anne Casset, Julien Jouhannaud, Antonio Garofalo, Coralie Spiegelhalter, Dinh-Vu Nguyen, Delphine Felder-Flesch, Geneviève Pourroy, Françoise PonsAbstractThe engineering of iron oxide nanoparticles (IONPs) for biomedical use has received great interest over the past decade. In the present study we investigated the biocompatibility of IONPs grafted with linear (2P) or generation 1 (2PG1) or 2 (2PG2) dendronized oligoethyleneglycol units in THP-1-derived macrophages. To evaluate IONP effects on cell funct...
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

Dissolvable microneedle patch containing doxorubicin and docetaxel is effective in 4T1 xenografted breast cancer mouse model
Publication date: Available online 14 December 2018Source: International Journal of PharmaceuticsAuthor(s): Shubhmita Bhatnagar, Neha Gajanan Bankar, Mrunal Vijay Kulkarni, Venkata Vamsi Krishna VenugantiAbstractMicroneedle-devices provide a promising alternative to syringe-injection-based administration of chemotherapeutics. Dissolvable polymeric microneedles provide possibility of carrying greater payload and dual drugs. Here, we report development of polyvinyl pyrrolidone and polyvinyl alcohol composite dissolvable polymeric microneedle system for co-delivery of doxorubicin HCl and docetaxel. Microneedle patches were ch...
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

RGD-modified PEGylated paclitaxel nanocrystals with enhanced stability and tumor-targeting capability
This study was to modify paclitaxel nanocrystals with polyethylene glycol (PEG) for stabilization and RGD peptide for tumor targeting. Inspired by the structure of mussel's foot protein, polydopamine (PDA) was introduced to the drug delivery system for the modification of nanocrystals. Briefly, PDA was coated on the surface of nanocrystals to form a reaction platform for further PEGylation and RGD peptide conjugation. PEGylated nanocrystals with RGD peptide modification (NC@PDA-PEG-RGD) were prepared with near-spheroid shape, drug loading 45.12 ± 1.81% and a hydrodynamic diameter 419.9±80.9nm. The size of NC@...
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

Methotrexate-loaded biodegradable polymeric micelles for lymphoma therapy
In conclusion, MPEG-PCL-MTX micelle is an excellent intravenously injectable formulation of MTX with both good solubility and enhanced anti-tumor activity, which perfectly meets clinical demands, especially for administration of HD MTX.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro Drug Release from Acetylated High Amylose Starch-Zein Films for Oral Colon-Specific Drug Delivery
This study describes the preparation of free films of zein with and without acetylated high amylose maize starch (HAS) and their corresponding coated tablets as a novel approach to colonic drug delivery. We hypothesise that the embedding of a digestible starch component within the inert zein would allow the film to remain intact until the large intestine is reached. Free films of zein alone and starch/zein were prepared and characterised. SEM and AFM images of film surface showed that films were morphologically inhomogeneous, particularly at lower HAS/Zein ratios; however, nanothermal analysis data suggested that these dif...
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

Smart copolymer coated SPIONs for colon cancer chemotherapy
Publication date: 10 February 2019Source: International Journal of Pharmaceutics, Volume 556Author(s): Mariano Licciardi, Cinzia Scialabba, Roberto Puleio, Giovanni Cassata, Luca Cicero, Gennara Cavallaro, Gaetano GiammonaAbstractHuman colon cancer is one of the higher aggressive solid tumors, whose high mortality, much like many other solid tumors, results from metastasis formation. To reduce this high mortality, more effective chemotherapy, allowing a specific tumor accumulation and an efficient early-stage medical imaging as well, are still needed. At this regard, stimuli-responsive nanocarriers for anticancer drug deli...
Source: International Journal of Pharmaceutics - December 15, 2018 Category: Drugs & Pharmacology Source Type: research

Gelatin-based Hydrogels as Potential Biomaterials for Colonic Delivery of Oxaliplatin
Publication date: Available online 13 December 2018Source: International Journal of PharmaceuticsAuthor(s): Kaleem Ullah, Shujaat Ali Khan, Ghulam Murtaza, Muhammad Sohail, Azizullah, Abdul Manan, Attia AfzalAbstractIn present investigation, gelatin-based (AA-co-AMPS) hydrogels were prepared using N, N’-Methylenebisacrylamide (MBA) as a cross-linker and ammonium per sulfate (APS) as an initiator. The successful crosslinking and network formation was confirmed by Fourier transform infrared spectroscopy (FT IR). Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) investigations proved the highe...
Source: International Journal of Pharmaceutics - December 14, 2018 Category: Drugs & Pharmacology Source Type: research

How changes in molecular weight and PDI of a polymer in amorphous solid dispersions impact dissolution performance
This study evaluated the impact of HME process conditions on physical characteristics of poly(vinylpyrrolidone-co-vinyl-acetate) 60:40 (PVP-VA64) which is a widely used polymer for HME. Focus was set on molecular weight (Mw) and polydispersity index (PDI), by means of absolute molar mass detection via multi-angle light scattering. The generation of a high Mw fraction together with a decrease of the average Mw was detected. In a next step, the influence of these changes on the dissolution behavior of ASD was evaluated. Different stress conditions were applied onto PVP-VA64 in placebo extrusions. The obtained stressed polyme...
Source: International Journal of Pharmaceutics - December 14, 2018 Category: Drugs & Pharmacology Source Type: research

Self-implanted tiny needles as alternative to traditional parenteral administrations for controlled transdermal drug delivery
Publication date: Available online 13 December 2018Source: International Journal of PharmaceuticsAuthor(s): Bo Zhi Chen, Yuan Yang, Bei Bei Wang, Mohammad Ashfaq, Xin Dong GuoAbstractControlled drug-delivery systems have potential as substitutes for traditional medication systems due to the advantages in safety, efficacy, and patient compliance that these long-acting dosage forms provide. In this context, the present study focus on the development of self-implanted hyaluronic acid (HA) tiny needles that encapsulate ivermectin (IVM)-poly (lactic-co-glycolic acid) (PLGA) microparticles for controlled transdermal IVM rel...
Source: International Journal of Pharmaceutics - December 14, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro evaluation of drug release and antibacterial activity of a silver-loaded wound dressing coated with a multilayer system
Publication date: Available online 13 December 2018Source: International Journal of PharmaceuticsAuthor(s): Alejandra Mogrovejo-Valdivia, Oumaira Rahmouni, Nicolas Tabary, Mickael Maton, Christel Neut, Bernard Martel, Nicolas BlanchemainAbstractThe goal of the study was to elaborate an antibacterial silver wound dressing covered by a protective coating that would prevent silver diffusion toward skin without losing its biocide properties. Therefore, non woven polyethyleneterephtalate (PET) textiles were pre-treated by two types of polysaccharides – chitosan and cyclodextrin – both crosslinked with citric acid by...
Source: International Journal of Pharmaceutics - December 14, 2018 Category: Drugs & Pharmacology Source Type: research

P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) limit brain accumulation of the FLT3 inhibitor quizartinib in mice
Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Jing Wang, Changpei Gan, Irene A. Retmana, Rolf W. Sparidans, Wenlong Li, Maria C. Lebre, Jos H. Beijnen, Alfred H. SchinkelAbstractQuizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acute myeloid leukemia. We studied its pharmacokinetic interactions with the multidrug efflux transporters ABCB1 and ABCG2 and the multidrug metabolizing enzyme CYP3A, using in vitro transport assays and knockout and transgenic mouse models. Quizartinib was transported by human ABCB1 in vitro...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Composite nanofibrous membranes of PLGA/Aloe vera containing lipid nanoparticles for wound dressing applications
In this study, a wound dressing based on PLGA and Aloe vera containing lipid nanoparticles (NLCs) was developed. NLCs were added in order to add a lipid component that could avoid the adhesion of the dressing to the wound and improve its handling. Membranes with and without NLCs were composed of uniform fibers of about 1 µm in diameter. Their porosity was above 80 % and their thickness was about 160 µm. Both dressings showed similar water vapour transmission rate 1100 g/m2day. The formulation containing NLCs presented a higher ultimate tensile strength (2.61 ± 0.46 MPa) and a higher water uptake. Both fo...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

A comprehensive analysis and optimization of continuous twin-screw granulation processes via sequential experimentation strategy
This study was geared towards better process design and understanding with emphasis on bridging the knowledge gap between input and output variables by employing sequential experimentation strategy. A low-dose formulation for granulation experiments contained anhydrous caffeine as the model drug. In the first phase of parameter screening, D-optimal design and stepwise regression were leveraged to develop interaction models following the examination of various quantitative and qualitative factors of potential importance. To maximize the design space dictated by predefined quality target values, several variables were fixed ...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Dual 0.02% chlorhexidine digluconate – 0.1% disodium EDTA loaded thermosensitive ocular gel for Acanthamoeba keratitis treatment
Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Annamaria Cucina, Samira Filali, Arnaud Risler, Camille Febvay, Damien Salmon, Christine Pivot, Michel Pelandakis, Fabrice PirotAbstractPoor bioavailability and low residence time limit the efficiency of conventional biguanide-based eye drops against Acanthamoeba keratitis. The aim of this work was to formulate an original anti-amoebic thermoreversible ocular gel combining biguanide and metalloproteases inhibitor - chelating agent. Chlorhexidine digluconate (CHX)-ethylenediaminetetraacetic acid disodium salt (Na2EDTA...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Automated small-scale in vitro transfer model as screening tool for the prediction of in vivo-dissolution and precipitation of poorly solubles
Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Christian Jede, Christian Wagner, Holger Kubas, Christian Weber, Markus Weigandt, Mirko Koziolek, Werner WeitschiesAbstractPrecipitation testing, especially for weakly basic APIs, represents a key parameter in drug substance characterization during early development stages, where the amount of API available is limited. Therefore, it was the aim of this study to develop an automated small-scale in vitro transfer model to characterize the supersaturation and precipitation behavior of two poorly water-soluble drugs. Fol...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Chitosan-hydroxypropyl methylcellulose tioconazole films: A promising alternative dosage form for the treatment of vaginal candidiasis
Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Natalia L. Calvo, Laura A. Svetaz, Vera A. Alvarez, Ariel D. Quiroga, María C. Lamas, Darío LeonardiAbstractVaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on chitosan, hydroxypropyl methylcellulose and blends of these polymers containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. M...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Gelatinized core liposomes: A new Trojan horse for the development of a novel timolol maleate glaucoma medication
Publication date: Available online 12 December 2018Source: International Journal of PharmaceuticsAuthor(s): Rania M. Hathout, Heba A. Gad, Salma M. Abdel-Hafez, Naira Nasser, Noha Khalil, Toka Ateyya, Alaa Amr, Nesreen Yasser, Sandy Nasr, Abdelkader A. MetwallyAbstractGlaucoma treatment with ocular medications requires overcoming the corneal barrier to drug penetration. Liposomes have a great corneal penetration ability and affinity while suffering from poor stability and low entrapment of hydrophilic drugs accompanied by rapid drug release. This work aims to develop a new, effective and stable glaucoma medication with sus...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Revival of a Potent Therapeutic Maytansinoid Agent using a Strategy that Combines Covalent Drug Conjugation with Sequential Nanoparticle Assembly
Publication date: Available online 13 December 2018Source: International Journal of PharmaceuticsAuthor(s): Ke Xie, Shanshan Song, Liqian Zhou, Jianqin Wan, Yiting Qiao, Min Wang, Haiyang Xie, Lin Zhou, Shusen Zheng, Hangxiang WangAbstractMaytansine and its related analogues are a class of highly potent anti-proliferation agents that have failed to be exploited as clinical drugs for human therapy due to unacceptable systemic toxicity. Here, we delineate a novel strategy that combines rational drug conjugation with subsequent nanoparticle assembly to systemically deliver this highly potent and toxic drug. To demonstrate thi...
Source: International Journal of Pharmaceutics - December 13, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of material properties and process variables on the residence time distribution in twin screw feeding equipment
Publication date: Available online 11 December 2018Source: International Journal of PharmaceuticsAuthor(s): B. Van Snick, A. Kumar, M. Verstraeten, K. Pandelaere, J. Dhondt, G. Di Pretoro, T. De Beer, C. Vervaet, V. VanhoorneAbstractScrew feeders are integrated as dispensing units in most continuous manufacturing platforms. Hence, characterizing and modelling the residence time distribution (RTD) of materials in feeders is indispensable to understand the traceability of raw materials from the drum till tablet, enabling the separation of non-confirming material. The proposed methodology addressed this leap in knowledge by c...
Source: International Journal of Pharmaceutics - December 12, 2018 Category: Drugs & Pharmacology Source Type: research

Use of a Water-Based Probiotic to Treat Common Gut Pathogens
Publication date: Available online 11 December 2018Source: International Journal of PharmaceuticsAuthor(s): Cornelius C. Dodoo, Paul Stapleton, Abdul W. Basit, Simon GaisfordAbstractThis work reports the anti-pathogenic effect of a commercially available water-based probiotic suspension, Symprove™, against three commonly encountered infectious organisms; Escherichia coli, methicillin-resistant Staphylococcus aureus (MRSA) and Shigella sonnei. An isothermal calorimetric assay was used to the monitor growth of the species individually and in binary combinations, while colony plate counting was used to enumerate viable ...
Source: International Journal of Pharmaceutics - December 11, 2018 Category: Drugs & Pharmacology Source Type: research

Novel Extended In Vitro-In Vivo Correlation Model for the Development of Extended-Release Formulations for Baclofen: from Formulation Composition to in vivo Pharmacokinetics
Publication date: Available online 11 December 2018Source: International Journal of PharmaceuticsAuthor(s): Tae Hwan Kim, Jürgen B. Bulitta, Do-Hyung Kim, Soyoung Shin, Beom Soo ShinAbstractIn vitro-in vivo correlation (IVIVC), a predictive mathematical model between the in vitro dissolution and the in vivo pharmacokinetics has been utilized for the development of new extended release (ER) formulations. The aim of the present study was to extend the IVIVC approach, which correlates among the formulation composition, the in vitro dissolution, and the plasma drug concentration, to predict plasma drug concentrations from...
Source: International Journal of Pharmaceutics - December 11, 2018 Category: Drugs & Pharmacology Source Type: research

Composite scaffold obtained by electro-hydrodynamic technique for infection prevention and treatment in bone repair
Publication date: Available online 11 December 2018Source: International Journal of PharmaceuticsAuthor(s): Javier Aragón, Sergio Feoli, Silvia Irusta, Gracia MendozaAbstractBone infection is a devastating condition resulting from implant or orthopaedic surgery. Therapeutic strategies are extremely complicated and may result in serious side effects or disabilities. The development of enhanced 3D scaffolds, able to promote efficient bone regeneration, combined with targeted antibiotic release to prevent bacterial colonization, is a promising tool for the successful repair of bone defects. Herein, polymeric electrospu...
Source: International Journal of Pharmaceutics - December 11, 2018 Category: Drugs & Pharmacology Source Type: research

Challenging identification of polymorphic mixture: polymorphs I, II and III in olanzapine raw materials
Publication date: Available online 11 December 2018Source: International Journal of PharmaceuticsAuthor(s): Carla G. Testa, Livia D. Prado, Rogéria N. Costa, Michelle L. Costa, Yamila G. Linck, Gustavo A. Monti, Silvia L. Cuffini, Helvécio V.A. RochaAbstractOlanzapine (OLZ), a drug for the treatment of schizophrenia, presents in more than 60 crystal forms. Polymorphs I, II and III were reported, however, the preparation conditions for pure II and III have not been reported. Polymorph IV was reported but this form is actually polymorph II described at different temperature. The diversity of solid forms of OLZ,...
Source: International Journal of Pharmaceutics - December 11, 2018 Category: Drugs & Pharmacology Source Type: research

pH-sensitive pullulan-doxorubicin nanoparticles loaded with 1,1,2-trichlorotrifluoroethane as a novel synergist for high intensity focused ultrasound mediated tumor ablation
In conclusion, Pu-DOX/CFC nanoemulsions might serve as a novel synergist for HIFU therapy, and possess great potential in clinical implication.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 11, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoformulation of curcumin-loaded eudragit-nutriosomes to counteract malaria infection by a dual strategy: improving antioxidant intestinal activity and systemic efficacy
Publication date: Available online 7 December 2018Source: International Journal of PharmaceuticsAuthor(s): Maria Manconi, Maria Letizia Manca, Elvira Escribano-Ferrer, Elisabet Martí Coma-Cros, Arnau Biosca, Elena Lantero, Xavier Fernàndez-Busquets, Anna Maria Fadda, Carla CaddeoAbstractIn this paper, nutriosomes (phospholipid vesicles associated with Nutriose® FM06) were modified to obtain new systems aimed at enhancing the efficacy of curcumin in counteracting malaria infection upon oral administration. Eudragit® L100, a pH-sensitive co-polymer, was added to these vesicles, thus obtaining eudragit-n...
Source: International Journal of Pharmaceutics - December 8, 2018 Category: Drugs & Pharmacology Source Type: research

Development of levofloxacin-loaded PLGA microspheres of suitable properties for sustained pulmonary release
In this study, the aim was the development of LVX-loaded PLGA microspheres (MS) for pulmonary administration as a dry powder. MS were prepared, for the first time, by a modified double emulsion solvent evaporation method with premix membrane homogenization. Aqueous phases were saturated with LVX and a fatty acid (lauric acid) was added to avoid the drug escaping from the organic phase. MS were characterized in terms of size, drug content, morphology and in vitro release properties. X-ray diffraction, Fourier-transform infrared spectroscopy, differential and gravimetric thermal analysis, and cytotoxicity analyses were perfo...
Source: International Journal of Pharmaceutics - December 8, 2018 Category: Drugs & Pharmacology Source Type: research

A “Ship-in-a-Bottle” strategy to create folic acid nanoclusters inside the nanocages of γ-cyclodextrin metal-organic frameworks
Publication date: Available online 8 December 2018Source: International Journal of PharmaceuticsAuthor(s): Jian Xu, Li Wu, Tao Guo, Guoqing Zhang, Caifen Wang, Haiyan Li, Xue Li, Vikramjeet Singh, Weidong Chen, Ruxandra Gref, Jiwen ZhangAbstractAssembled between γ-cyclodextrins (CD) and potassium ions, γ-cyclodextrin metal-organic frameworks (CD-MOF) create spatially extended and ordered cage-like structures. Herein, it was demonstrated that folic acid (FA), a model molecule, could be densely packed inside CD-MOF reaching 2:1 FA:CD molar ratio. This “Ship-in-Bottle” strategy leads to a 1450 fold inc...
Source: International Journal of Pharmaceutics - December 8, 2018 Category: Drugs & Pharmacology Source Type: research

Development of Co-solvent Freeze-Drying Method for the Encapsulation of Water-insoluble Thiostrepton in Sterically Stabilized Micelles
In conclusion, we found optimum conditions to prepare TST-SSM using the co-solvent freeze-drying method. This scalable production method can facilitate the further clinical development and industrial production of TST-SSM nanomedicine.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 7, 2018 Category: Drugs & Pharmacology Source Type: research

High-dose coenzyme Q10-loaded oleogels for oral therapeutic supplementation
Publication date: Available online 6 December 2018Source: International Journal of PharmaceuticsAuthor(s): Natalia Ehrenhaus Masotta, Manuela R. Martinefski, Silvia Lucangioli, Ana M. Rojas, Valeria P. TripodiAbstractCoenzyme Q10 (CoQ10) is a mitochondrial respiratory cofactor and potent endogenous antioxidant. In CoQ10-deficient patients, early treatment with high-oral doses (5-50 mg/kg/day) can limit the progression of renal disease and the onset of neurological manifestations. Crystalline CoQ10 is lipophilic, water-insoluble, and poorly absorbed in the gut. Here, CoQ10 showed low bulk density, another important disadvan...
Source: International Journal of Pharmaceutics - December 7, 2018 Category: Drugs & Pharmacology Source Type: research

On the mechanism of colloidal silica action to improve flow properties of pharmaceutical excipients
Publication date: Available online 6 December 2018Source: International Journal of PharmaceuticsAuthor(s): Diem Trang Tran, Diana Majerová, Martin Veselý, Lukáš Kulaviak, Marek C. Ruzicka, Petr ZámostnýAbstractThe mechanism of colloidal silica action to improve flow properties of pharmaceutical powders is known to be based on inter-particle force disruption by silica particles adhered to the particle surface. In the present article, the kinetic aspects of this action are investigated, focusing on non-spherical particles of different size. Blends comprising microcrystalline cellulos...
Source: International Journal of Pharmaceutics - December 7, 2018 Category: Drugs & Pharmacology Source Type: research