New approach to optimizing risk management of the sticking problem using scale-independent critical material attributes and the quantitative process parameter
In conclusion, we propose that the dispersive SFE and ΔGsp of ethanol are scale-independent CMAs, and that the minimum blending time (BTmin), which can be calculated from the two CMAs, of the quantitative process parameter show the minimum blending time required to achieve higher risk assessment of the sticking problem.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Tetradeca-thiolated cyclodextrins: Highly mucoadhesive and in-situ gelling oligomers with prolonged mucosal adhesion
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Mulazim Hussain Asim, Imran Nazir, Aamir Jalil, Barbara Matuszczak, Andreas Bernkop-SchnürchAbstractThe purpose of this study was to synthesize a highly mucoadhesive tetradeca-thiolated β-cyclodextrin (β-CD) by replacement of all primary –OH groups at C-6 position and all secondary –OH groups at C-2 position of β-CD backbone via –SH groups and to evaluate its rheological and mucoadhesive properties in-vitro. Primary and secondary –OH groups of β-CD were substituted by &...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

A novel flunarizine hydrochloride-loaded organogel for intraocular drug delivery in situ: Design, physicochemical characteristics and inspection
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Manman Dai, Luyu Bai, Huimin Zhang, Qun Ma, Rui Luo, Fang Lei, Qingsong Fei, Ning HeAbstractWe developed a safe and efficacious drug delivery system for treatment of brain diseases. A novel in-situ gel system was prepared using soybean oil, stearic acid and N-methyl-2-pyrrolidinone (NMP) (10:1:3, v/w/v).This system had low viscosity as a sol in vitro and turned into a solid or semi-solid gel in situ after administration. The poorly water-soluble drug flunarizine hydrochloride (FNZ) was incorporated into this “or...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Critical steps during prilling process of molten lipids: main stumbling blocks due to pharmaceutical excipient properties
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): F. Séquier, V. Faivre, J-Y. Lanne, G. Daste, M. Renouard, S. LesieurAbstractPrilling by ultrasonic jet break-up is an efficient process to produce perfectly spherical microparticles homogeneous in size. However, the material properties could affect the manufacturability and the final product properties especially with lipid-based excipients which often exhibit complex structural properties. This work presents the characterisation of six lipid-based excipients differing by their melting point and polymorphic beh...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

A Cellulose-Based Therapeutic Polymer to Deter Intravenous Drug Abuse
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Rand Ahmad, Hamid OmidianAbstractPrescription opioids have widely been abused as an epidemic. In this research, we developed a drug composition based on the crosslinked carboxymethylcellulose (XCMC) and a drug model that can effectively deter abuse by injection via multiple mechanisms. The anionic nature of the XCMC is responsible for complexing the cationic opioids in aqueous solutions, minimizing the free drug amount accessible for extraction. The crosslinked nature of the polymer is responsible for its swelling and...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Excipients in freeze-dried biopharmaceuticals: contributions toward formulation stability and lyophilisation cycle optimisation
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Maja Bjelošević, Alenka Zvonar Pobirk, Odon Planinšek, Pegi Ahlin GrabnarAbstractBiopharmaceuticals are one of the fastest growing areas within the pharmaceutical industry. As protein drugs require parenteral administration, they are commonly formulated as aqueous solutions. However, this is not always feasible due to their general instability. In such cases, lyophilised powders for injection are the dosage form of choice, for the preparation of stable products. Lyophilisation is known to be highly time...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Novel skin permeation enhancers based on amino acid ester ionic liquid: Design and permeation mechanism
In conclusion, this study has generated novel chemical penetration enhancers (CPEs) based on AAE-ILs and may be potentially utilized in drug transdermal delivery systems (TDDSs).Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Transient Swelling Response of pH-Sensitive Hydrogels: A Monophasic Constitutive Model and Numerical Implementation
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Mohammad Reza Bayat, Roshanak Dolatabadi, Mostafa BaghaniAbstractDue to their ability to swell/deswell under alternating pH conditions, pH-sensitive hydrogels present themselves as a potential candidate for controlled drug delivery. In this paper, a coupled electro-chemo-mechanical transient large deformation homogeneous and inhomogeneous swelling theory is developed for pH-sensitive hydrogels. The hydrogel is treated as a single-phase compressible isotropic hyperelastic material. The Nernst-Planck equation is used fo...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Systematic screening of pharmaceutical polymers for hot melt extrusion processing: a comprehensive review
Publication date: 25 February 2020Source: International Journal of Pharmaceutics, Volume 576Author(s): Rishi Thakkar, Ruchi Thakkar, Amit Pillai, Eman A. Ashour, Michael A. RepkaAbstractPharmaceutical research, whether industrial or academic, has attempted to adopt approaches most efficient for the development of innovations. With the abundance of literature and growth of modern techniques available to minimize the number of trials, research is becoming more systematic by the day. Screening and selection of polymers for a pharmaceutical formulation can be challenging, considering the variety of polymers available and under...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Role of Wetting Agents and Disintegrants in Development of Danazol Nanocrystalline Tablets
The objective of this study was to evaluate the effect of wetting agents and disintegrants on the dissolution performance of dried nanocrystals of an active pharmaceutical ingredient (API) with poor wetting property. Danazol, a BCS Class II compound with high LogP and low polar surface area, was chosen as a model compound for this study. Danazol nanocrystalline suspension was prepared by wet-media milling and converted into powder via spray granulation either with mannitol or microcrystalline cellulose as carriers at a drug: carrier ratio of 1:9 w/w. Danazol nanocrystalline suspension showed a superior dissolution performa...
Source: International Journal of Pharmaceutics - January 13, 2020 Category: Drugs & Pharmacology Source Type: research

3D Characterisation of Dry Powder Inhaler Formulations: Developing X-ray Micro Computed Tomography Approaches
This study has demonstrated for the first time that XCT provides an invaluable, non-destructive and analytical approach to obtain number- and volume-based particle size distributions of DPI formulations in 3D space, and for unique 3D characterisation of powder micro-structure.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 13, 2020 Category: Drugs & Pharmacology Source Type: research

Transcutaneous Anaesthetic Nano-enabled Hydrogels for Eyelid Surgery
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Aikaterini Lalatsa, Priyanka V. Patel, Yujiao Sun, Chong C. Kiun, Ferishtah Karimi, Jurgita Zekonyte, Krisztina Emeriewen, George M. SalehAbstractLocal anaesthetics are administered as a diffuse superficial slow injection in blepharoplasty. Current transcutaneous local anaesthetic formulations are not licensed for use on the face due to safety concerns. Here we report for the first time the permeation of local anaesthetics (lidocaine, bupivacaine loaded SNEDDS and their hydrogels) across human eyelid and mouse skin as...
Source: International Journal of Pharmaceutics - January 13, 2020 Category: Drugs & Pharmacology Source Type: research

Continuous twin screw granulation: influence of process and formulation variables on granule quality attributes of model formulations
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Christoph Portier, Kenny Pandelaere, Urbain Delaet, Tamas Vigh, Ashish Kumar, Giustino Di Pretoro, Thomas De Beer, Chris Vervaet, Valérie VanhoorneAbstractIn recent years, continuous manufacturing techniques, such as twin screw wet granulation, have gained significant momentum. Due to the large diversity of the (model) formulations and equipment, it is often difficult to generalize conclusions about the importance of process settings. As only limited knowledge is available on the importance of formulation varia...
Source: International Journal of Pharmaceutics - January 13, 2020 Category: Drugs & Pharmacology Source Type: research

In vivo preclinical evaluation of the new 68Ga-labeled beta-cyclodextrin in prostaglandin E2 (PGE2) positive tumor model using positron emission tomography
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): György Trencsényi, Adrienn Kis, Judit P. Szabó, Ágnes Ráti, Katalin Csige, Éva Fenyvesi, Lajos Szente, Milo Malanga, Gábor Méhes, Miklós Emri, István Kertész, Miklós Vecsernyés, Ferenc Fenyvesi, István HajduAbstractThe cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) pathway plays an important role in tumor development and formation of metastases. It was earlier reported that cyclodextrin derivatives have a high affinity to...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

Coexistence of Oil Droplets and Lipid Vesicles in Propofol Drug Products
In this study, we investigate the use of high-resolution cryogenic transmission electron microscopy (cryo-TEM) in morphological characterization of four commercially available propofol drug products. The TEM result, for the first time, reveals that all propofol drug products contain lipid vesicles and oil droplet-lipid vesicle aggregated structures, in addition to oil droplets. Statistical analysis shows the size and ratio of the lipid vesicles varies across four different products. To evaluate the impact of such morphological differences on active pharmaceutical ingredient (API)’s distribution, we separate the lipid...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

A model to simultaneously evaluate the compressibility and compactibility of a powder based on the compression ratio
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Yating Yu, Lijie Zhao, Xiao Lin, Youjie Wang, Yi FengAbstractThe present study aimed to establish a new model to evaluate the compressibility and compactibility of materials simultaneously. Eighteen types of pharmaceutical excipients were studied via direct compaction. The model was established as CR = y0 + Ae- bP, r2 ≥ 0.9649 (where CR is the compression ratio and P is the compaction force and y0, A, b is constant). The physical meaning of y0 and b were studied in the model. The results show that y0 has a strong c...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

Systematic screening of pharmaceutical polymers for hot melt extrusion processing
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Rishi Thakkar, Ruchi Thakkar, Amit Pillai, Eman Ashour, Michael RepkaAbstractPharmaceutical research, whether industrial or academic, has attempted to adopt approaches most efficient for the development of innovations. With the abundance of literature and growth of modern techniques available to minimize the number of trials, research is becoming more systematic by the day. Screening and selection of polymers for a pharmaceutical formulation can be challenging, considering the variety of polymers available and under d...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

Continuous twin screw granulation: a complex interplay between formulation properties, process settings and screw design
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Christoph Portier, Kenny Pandelaere, Urbain Delaet, Tamas Vigh, Giustino Di Pretoro, Thomas De Beer, Chris Vervaet, Valérie VanhoorneAbstractDue to the numerous advantages over batch manufacturing, continuous manufacturing techniques such as twin screw wet granulation are rapidly gaining importance in pharmaceutical production. Since a large knowledge gap on the importance of formulation variables exists, this study systematically assessed the impact of different screw configurations and process settings on eig...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

Development of Inhalable Quinacrine Loaded Bovine Serum Albumin Modified Cationic Nanoparticles: Repurposing Quinacrine for Lung Cancer Therapeutics
Publication date: Available online 11 January 2020Source: International Journal of PharmaceuticsAuthor(s): Bhuvaneshwar Vaidya, Nishant S Kulkarni, Snehal K Shukla, Vineela Parvathaneni, Gautam Chauhan, Jenna K Damon, Apoorva Sarode, Jerome V Garcia, Nitesh Kunda, Samir Mitragotri, Vivek GuptaAbstractDrug repurposing is on the rise as an atypical strategy for discovery of new molecules, involving use of pre-existing molecules for a different therapeutic application than the approved indication. Using this strategy, the current study aims to leverage effects of quinacrine (QA), a well-known anti-malarial drug, for treatment...
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

New nanoparticles for topical ocular delivery of erythropoietin
In conclusion, CS/HA6-EPO NPs could be a promising formulation for increasing EPO ocular bioavailability by enhancing its retention time and permeation through the different ocular membranes.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 12, 2020 Category: Drugs & Pharmacology Source Type: research

Antimicrobial Activity and Biocompatibility of Slow-release Hyaluronic Acid-antibiotic Conjugated Particles
Publication date: Available online 9 January 2020Source: International Journal of PharmaceuticsAuthor(s): Ze Zhang, Selin S. Suner, Diane A. Blake, Ramesh S. Ayyala, Nurettin SahinerAbstractHere, the aim was to design and use a long-lasting antibiotic release system for prevention of postoperative infections in ophthalmic surgery. Ciprofloxacin and vancomycin-conjugated hyaluronic acid (HA) particles were prepared as drug carriers for sustained release of antibiotics. The antimicrobial effects of the released drugs were determined by disc-diffusion and macro-dilution tests at different times up to 2 weeks. Slow degradable ...
Source: International Journal of Pharmaceutics - January 10, 2020 Category: Drugs & Pharmacology Source Type: research

PLGA nanoparticles embedding molybdenum cluster salts: influence of chemical composition on physico-chemical properties, encapsulation efficiencies, colloidal stabilities and in vitro release
We present a screening of poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles embedding a series of inorganic molybdenum octahedral clusters intended for photodynamic therapy (PDT) of cancer. Three cluster compounds from 2 cluster units, [{Mo6Br8}Br6]2- and [{Mo6I8}(OOC2F5)6]2- were studied. [{Mo6Br8}Br6]2-cluster units are found in the soluble ternary salt Cs2[{Mo6Br8}Br6] (CMB) prepared by solid state chemistry at high temperature. In solution Cs+ cations are replaced by tetrabutyl ammonium cations (C4H9)4N+) to form the salt ((C4H9)4N)2[{Mo6Br8}Br6] (TBA2). [{Mo6I8}(OOC2F5)6]2- was prepared combining solid state and so...
Source: International Journal of Pharmaceutics - January 10, 2020 Category: Drugs & Pharmacology Source Type: research

Prilling of API/fatty acid suspensions: screening of additives for drug release modification
Publication date: Available online 8 January 2020Source: International Journal of PharmaceuticsAuthor(s): E. De Coninck, V. Vanhoorne, M. Boone, G. Van Assche, B.G. De Geest, T. De Beer, C. VervaetAbstractCurrent study screened additives which could modify the drug release from prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension, without negatively influencing the processability and/or stability of the formulation. Therefore, 11 additives (i.e. emulsifiers, pore-formers and FA-based lubricants) were added in a 20% concentration to a paracetamol/behenic acid formulation. Two additives, Kollipho...
Source: International Journal of Pharmaceutics - January 10, 2020 Category: Drugs & Pharmacology Source Type: research

Sink conditions do not guarantee the absence of saturation effects
This articles aims at: (i) giving a brief overview on the underlying physico-chemical phenomena involved in drug dissolution and drug release, (ii) clarifying some key terms, and (iii) presenting several examples of dosage forms in which drug saturation effects within the system are of importance, even when providing sink conditions in the surrounding bulk fluid. Interestingly, this can also include highly hydrated delivery systems containing freely water-soluble drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 7, 2020 Category: Drugs & Pharmacology Source Type: research

Carboxyl-, sulfonyl-, and phosphate-terminal dendrimers as a nanoplatform with lymph node targeting
In this study, three anionic dendrimers with carboxyl-, sulfonyl-, and phosphate-terminal groups were prepared to examine the lymph node targeting and the association with immune cells in the lymph nodes. These anionic dendrimers were accumulated in the lymph node by intradermal injection. Although the carboxyl- and sulfonyl-terminal dendrimers were diffused from the injection site, the phosphate-terminal dendrimers were mostly retained. The phosphate-terminal dendrimer was recognized by the macrophages, dendritic cells, and B cells in the lymph node, whereas the carboxyl- and sulfonyl-terminal dendrimers were not. Our res...
Source: International Journal of Pharmaceutics - January 7, 2020 Category: Drugs & Pharmacology Source Type: research

Developing an injectable co-formulation of two antidiabetic drugs: excipient impact on peptide aggregation and pharmacokinetic properties
This study describes the development and characterisation of a stable parenteral co-formulation of a sodium glucose co-transporter 2 inhibitor (dapagliflozin) and a therapeutic lipidated peptide, using hydroxypropyl-β-cyclodextrin as an enabling excipient. Using NMR, calorimetry, computational modelling and spectroscopic methods, we show that besides increasing the solubility of dapagliflozin, cyclodextrin prevents self-association of the peptide through interaction with the lipid chain and amino acids prone to aggregation including aromatic groups and ionisable residues. While those interactions cause a dramatic seco...
Source: International Journal of Pharmaceutics - January 4, 2020 Category: Drugs & Pharmacology Source Type: research

Industrial approaches and consideration of clinical relevance in setting impurity level specification for drug substances and drug products
Publication date: Available online 3 January 2020Source: International Journal of PharmaceuticsAuthor(s): Dhruvisha Pokar, Niraj Rajput, Pinaki SenguptaAbstractThe safety and efficacy of drug substances or products do not solely depend on its active(s). The quantity of impurities present in the product has a significant role in its safety profile. Pharmaceutical impurities are one of the primary reasons for the withdrawal of many approved products from the market. Therefore, the level of impurities in the pharmaceuticals needs to be controlled within a specified safe limit. Nowadays, setting impurity level specification re...
Source: International Journal of Pharmaceutics - January 4, 2020 Category: Drugs & Pharmacology Source Type: research

Self-assembled Angelica sinensis polysaccharide nanoparticles with an instinctive liver-targeting ability as a drug carrier for acute alcoholic liver damage protection
Publication date: Available online 3 January 2020Source: International Journal of PharmaceuticsAuthor(s): Kaiping Wang, Jingya Xu, Yan Liu, Zheng Cui, Zihao He, Ziming Zheng, Xiao Huang, Yu ZhangAbstractThe present work aimed to study the feasibility of Angelica sinensis polysaccharide (ASP) as an instinctive liver-targeting drug delivery carrier with applications in acute alcoholic liver damage (ALD). Amphipathic cholesteryl hemisuccinate-ASP (ASP-CHEMS) conjugate was synthesized by an esterification reaction and characterized by conventional methods. ASP-CHEMS self-assembled nanoparticles (ACNPs) and Curcumin-loaded ACNP...
Source: International Journal of Pharmaceutics - January 4, 2020 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 25 January 2020Source: International Journal of Pharmaceutics, Volume 574Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 4, 2020 Category: Drugs & Pharmacology Source Type: research

Influence of Cell-Penetrating Peptides on the Activity and Stability of Virus-Based Nanoparticles
In this study, four cell-penetrating peptides (CPPs), cationic octaarginine (R8), histidine-rich peptides (LAH4 and KH27K) and fusogenic peptide (FUSO), are investigated for their effect on infection by mouse polyomavirus (MPyV) or on transduction of reporter genes delivered by MPyV or related viral vectors. Peptides noncovalently associated with viral particles enhance gene transfer (with the exception of FUSO). Removal of cellular heparan sulfates by the heparinase does not significantly change the enhancing potential of CPPs. Instead, CPPs influences the physical state of viral particles: R8 slightly destabilizes the in...
Source: International Journal of Pharmaceutics - January 1, 2020 Category: Drugs & Pharmacology Source Type: research

Characteristics of unique endocytosis induced by weak current for cytoplasmic drug delivery
Publication date: Available online 31 December 2019Source: International Journal of PharmaceuticsAuthor(s): Tasuku Torao, Miyuki Mimura, Yasufumi Oshima, Koki Fujikawa, Mahadi Hasan, Tatsuharu Shimokawa, Naoshi Yamazaki, Hidenori Ando, Tatsuhiro Ishida, Tatsuya Fukuta, Tamotsu Tanaka, Kentaro KogureAbstractWe previously reported that a weak current (WC, 0.3-0.5mA/cm2) applied to cells can induce endocytosis to promote cytoplasmic delivery of hydrophilic macromolecules (MW:
Source: International Journal of Pharmaceutics - January 1, 2020 Category: Drugs & Pharmacology Source Type: research

GSH responsive nanomedicines self-assembled from small molecule prodrug alleviate the toxicity of cardiac glycosides as potent cancer drugs
Publication date: Available online 30 December 2019Source: International Journal of PharmaceuticsAuthor(s): Huiyun Zhang, Yuan Zhu, Congyong Sun, Yujiao Xie, Michael Adu-Frimpong, Wenwen Deng, Jiangnan Yu, Ximing Xu, Zhongfei Han, Gang QiAbstractCardiac glycosides (CGs) have been used to treat cancer for hundreds of years. However, the narrow therapeutic window and system toxicity have hindered their wide clinical applications. Herein, the small molecule prodrug strategy and nanotechnology were integrated into one drug delivery system with enhanced therapeutic effect. Using periplocymarin (PPM) as a target agent, we design...
Source: International Journal of Pharmaceutics - December 31, 2019 Category: Drugs & Pharmacology Source Type: research

Encapsulation of poorly soluble drugs in yeast glucan particles by spray drying improves dispersion and dissolution properties
Publication date: Available online 30 December 2019Source: International Journal of PharmaceuticsAuthor(s): Gabriela Ruphuy, Ivan Saloň, Jan Tomas, Petra Šalamúnová, Jaroslav Hanuš, František ŠtěpánekAbstractIn this work, novel amorphous solid dispersions based on yeast glucan particles were produced. Yeast glucan particles are hollow and porous, and they are mainly composed of amorphous polysaccharides. We hypothesized that these particles are suitable candidates for the amorphization of drugs with low water solubility. Model drugs ibuprofen and curcumin were successfully...
Source: International Journal of Pharmaceutics - December 31, 2019 Category: Drugs & Pharmacology Source Type: research

Design of a Zero-order Sustained Release PLGA Microspheres for Palonosetron Hydrochloride with High Encapsulation Efficiency
Publication date: Available online 30 December 2019Source: International Journal of PharmaceuticsAuthor(s): Ziyi Yang, Lu Liu, Lili Su, Xueqing Wu, Yicheng Wang, Lei Liu, Xia LinAbstractEfficient encapsulation of hydrophilic drugs was substantially challenging when using emulsion solvent evaporation approach. The aim of present study was to design palonosetron hydrochloride-loaded PLGA microspheres (Pal-MS) with high encapsulation efficiency (EE) to sustain drug release for over several days. Pal-MS were prepared using emulsion-solvent evaporation method. Results showed that the pH of external phase could significantly aff...
Source: International Journal of Pharmaceutics - December 31, 2019 Category: Drugs & Pharmacology Source Type: research

Antimicrobial properties of benzalkonium chloride derived polymerizable deep eutectic solvent
Publication date: Available online 30 December 2019Source: International Journal of PharmaceuticsAuthor(s): Jing Wang, Jing Xue, Xiaoqing Dong, Qingsong Yu, Sheila N. Baker, Ming Wang, Haofei HuangAbstractBenzalkonium chloride (BC) is a quaternary ammonium antimicrobial agent used in a variety of applications. In this work, BC was prepared into deep eutectic solvent (DES) with acrylic acid (AA) or methacrylic acid (MA). Within the newly prepared DES, BC is responsible for antimicrobial properties, while AA and MA are responsible for polymerization. Three types of microorganisms, E. coli (gram-negative bacilli), S. aureus (...
Source: International Journal of Pharmaceutics - December 31, 2019 Category: Drugs & Pharmacology Source Type: research

Enhancing the Stability of Amorphous Drug-Polyelectrolyte Nanoparticle Complex Using a Secondary Small-Molecule Drug as the Stabilizer: A Case Study of Ibuprofen-Stabilized Curcumin-Chitosan Nanoplex
Publication date: Available online 29 December 2019Source: International Journal of PharmaceuticsAuthor(s): Li Ming Lim, Kunn HadinotoAbstractWhile the solubility enhancement capability of amorphous drug-polyelectrolyte nanoparticle complex (nanoplex) has been widely established, its amorphous form stability during long-term storage is often lacking for poorly-soluble drugs with high crystallization propensity, such as curcumin (CUR). Herein we presented a new stabilization strategy of amorphous CUR nanoplex using a secondary small-molecule drug - ibuprofen (IBU) - as the auxiliary stabilizer to the polyelectrolytes (i.e. ...
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

Borneol and poly (ethylene glycol) dual modified BSA nanoparticles as an itraconazole vehicle for brain targeting
In this study, a novel brain targeting drug delivery system based on bovine serum albumin (BSA) was constructed for enhancing ITZ distribution in brain. Firstly, ITZ was loaded into BSA nanoparticles (ITZ-NPs) with 11.6 % of drug loading. Subsequently, the nanoparticles were modified with borneol (BO) and polyethylene glycol (PEG) (PEG/BO-ITZ-NPs). The resulting nanoparticles retained their nanosize (186.3 nm), uniform and spherical morphology, and negative surface charge (-21.03 mV). Cell uptake studies showed that compared with ITZ-NPs, PEG/BO-ITZ-NPs had significantly increased uptake in bEnd.3 cells, and the increase i...
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

Development and in vitro characterization of polymeric nanoparticles containing recombinant adrenomedullin-2 intended for therapeutic angiogenesis
In this study, we aimed to develop PLGA nanoparticles containing ADM-2 intended for therapeutic angiogenesis. PLGA nanoparticles containing ADM-2 were prepared by a double emulsion modified method, resulting in 300 nm-sized stable particles with zeta potential around – 30 mV. Electron microscopy analysis by SEM and TEM revealed spherical particles with a smooth surface. High encapsulation efficiency was reached (ca.70%), as quantified by ELISA. ADM-2 associated to polymer nanoparticles was also determined by EDS elemental composition analysis, SDS-PAGE and LC-MS/MS for peptide identification. In vitro release assays ...
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

Sinomenine hydrochloride loaded thermosensitive liposomes combined with microwave hyperthermia for the treatment of rheumatoid arthritis
In this study, a novel thermosensitive liposome loaded with sinomenine hydrochloride (SIN-TSL) was developed by a pH gradient method. The SIN-TSL had a mean particle size of around 100 nm, and an high entrapment efficiency and drug loading capacity. The results also suggested that SIN-TSL had a thermosensitive drug release behaviour, with the drug release rate at 43 °C was much faster than the one at 37 °C. The SIN-TSL could be effectively taken up by lipopolysaccharide-activated HUVECs, without any cytotoxicity was observed. In addition, both in vitro and in vivo studies indicated that the SIN-TSL combined with mi...
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

Exploring the influence of drug content on DPI powder properties and potential prediction of pulmonary drug deposition
In conclusion, drug content has a significant influence on powder properties. DPI formulations with a stronger interaction and meanwhile a better flowability are desirable for enhanced pulmonary drug delivery.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

Cancer-Targeted PEDF-DNA Therapy for Metastatic Colorectal Cancer
In this study, we prepared a PEDF-DNA-loaded liposome for cancer-targeted gene therapy for metastatic CRC using an iRGD peptide. Our results showed that cancer-targeted PEDF-DNA liposomes (R-LP/PEDF) exhibited enhanced inhibitory effects on invasion, migration, and pro-apoptosis of CRC cells in vitro. In addition, it reduced metastasis tumor nodules in lung and prolonged the survival time in a mouse model of metastatic CRC.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 30, 2019 Category: Drugs & Pharmacology Source Type: research

A systematic evaluation of poloxamers as tablet lubricants
In this study, we have systematically evaluated two poloxamers, P188 and P407, for their suitability as alternative tablet lubricants. For two excipients with different mechanical properties, i.e., microcrystalline cellulose and lactose, both poloxamers exhibit acceptable lubrication efficiency without negatively impacting tabletability. Compared to 1% MgSt, the performance of both poloxamers at 2% in an experimental tablet formulation of ritonavir led to better lubrication, higher tabletability, and enhanced in vitro drug release. Thus, the use of P188 and P407 as alternative tablet lubricants deserves further evaluations...
Source: International Journal of Pharmaceutics - December 29, 2019 Category: Drugs & Pharmacology Source Type: research

Iontophoresis enhances voriconazole antifungal potency and corneal penetration
In conclusion, iontophoresis increases drug potency and enhances drug penetration into the cornea, showing potential to be used as “an emergency burst delivery approach”.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 27, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of Compaction Pressure, Speed and Punch Head Profile on the Ultrasonically-Extracted Physical Properties of Pharmaceutical Compacts
In this study, we detail a non-destructive, easy-to-use approach for characterizing the porosity and tensile strength of pharmaceutical tablets.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 27, 2019 Category: Drugs & Pharmacology Source Type: research

A thermoresponsive hydrophobically modified hydroxypropylmethylcellulose/cyclodextrin injectable hydrogel for the sustained release of drugs
The objective of this study was to develop a thermoresponsive injectable hydrogel for the sustained release of drugs by taking advantage of host-guest interactions between a hydrophobically modified hydroxypropylmethyl cellulose (HM-HPMC) and cyclodextrin (CD). A thermoresponsive injectable hydrogel was prepared by simply adding CDs to HM-HPMC hydrogel. The HM-HPMC hydrogel was converted into a sol with a low viscosity through host-guest interactions with CDs. The HM-HPMC/β-CD hydrogel became a gel near body temperature where the host dissociated from the hydrophobic moieties of the polymer in response to the temperat...
Source: International Journal of Pharmaceutics - December 27, 2019 Category: Drugs & Pharmacology Source Type: research

Rapid Microneedle Fabrication by Heating and Photolithography
This study aims to fabricate a dissolving MN patch in a simple and efficient manner under mild conditions, using a combination of thermal and photo polymerisation. The MN patch was fabricated by pre-polymerisation of vinylpyrrolidone solution with heating followed by photolithography. The heating temperature and time of pre-polymer solution curing were optimized based on viscosity measurement. The MN properties including shape, size, skin penetration, dissolution, moisture absorption were determined. The fabricated MNs were sharp and consistent. The heated N-vinylpyrrolidone solution required less UV exposure time, thus re...
Source: International Journal of Pharmaceutics - December 27, 2019 Category: Drugs & Pharmacology Source Type: research

Melt electrohydrodynamic 3D printed Poly (ε-caprolactone)/Polyethylene glycol/Roxithromycin scaffold as a potential anti-infective implant in bone repair
In this study, a poly (ε-caprolactone) (PCL)/polyethylene glycol (PEG)/roxithromycin (ROX) composite scaffold was prepared via melt electrohydrodynamic (EHD) 3D printing. Fourier transform infrared spectroscopy (FTIR) spectroscopy was performed to verify the existence of PEG and ROX in the scaffolds. By water contact angle measurement, the addition of both PEG and ROX was found to improve the hydrophilicity of the scaffolds. By in vitro drug release assay, the PCL/PEG/ROX scaffolds showed an initial burst drug release and subsequent long-term sustained release behaviour, which is favourable for the prevention and t...
Source: International Journal of Pharmaceutics - December 25, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of quercetin nanorod/microcrystalline cellulose formulation via fluid bed coating crystallization for dissolution enhancement
This study reports a novel quercetin nanorod/microcrystalline cellulose (MCC) formulation prepared by fluid bed coating crystallization technique. The process comprises fluidized bed spray coating of quercetin acetone solution onto MCC particles, solvent evaporation and crystallization of quercetin nanorods on MCC surface. Depending on the quercetin solution concentration, quercetin nanorods with 100-300 nm in diameter and 1-3 µm in length were obtained. Owing to the small particle size and large surface area, a higher dissolution rate was achieved for quercetin nanorods in contrast to the raw quercetin, which theref...
Source: International Journal of Pharmaceutics - December 24, 2019 Category: Drugs & Pharmacology Source Type: research

Potential application of novel liquid crystal nanoparticles of isostearyl glyceryl ether for transdermal delivery of 4-biphenyl acetic acid
Publication date: 15 February 2020Source: International Journal of Pharmaceutics, Volume 575Author(s): Mika Yoshimura Fujii, Yoko Asakawa, Toshiro FukamiAbstractNovel liquid crystal nanoparticles (LCNs) composed of isostearyl glyceryl ether (GE-IS) and ethoxylated hydrogenated castor oil (HCO-60) were developed for the enhanced transdermal delivery of 4-biphenyl acetic acid (BAA).The physical properties and pharmaceutical properties of the LCNs were measured. The interaction between the intercellular lipid model of the stratum corneum and the LCNs was observed to elucidate the skin permeation mechanism.In the formulation, ...
Source: International Journal of Pharmaceutics - December 24, 2019 Category: Drugs & Pharmacology Source Type: research

Formulation development of lipid nanoparticles: improved lipid screening and development of tacrolimus loaded nanostructured lipid carriers (NLC)
In conclusion, an optimized method for the selection of lipids that results in a limited number of experiments could be established and tacrolimus loaded lipid nanoparticles with similar drug load as a marketed formulation was successfully developed in this study.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 22, 2019 Category: Drugs & Pharmacology Source Type: research