Colon-targeting of progesterone using hybrid polymeric microspheres improves its bioavailability and in vivo biological efficacy
This study aims to enhance progesterone (PG) oral bioavailability via its incorporation into hybrid colon-targeted pectin/NaCMC microspheres (MS) cross-linked with Zn2+ and Al3+. The MS were characterized for particle morphology, encapsulation efficiency, swelling behavior, drug release, mucoadhesivity and colon-specific degradability. Response-surface methodology was adopted to optimize the fabrication conditions. Enhancement of in vivo drug performance was evaluated through pharmacokinetic and pharmacodynamic studies. The optimized formulation was typically spherical with a mean diameter of 1031 µm and drug entrapm...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Vitamin E-based Prodrug Self-delivery for Nanoformulated Irinotecan with Synergistic Antitumor Therapeutics
In this study, a novel vitamin E succinate-based formulation of Ir (VES-Ir) combined with nanoscaled characteristics and synergistic combination was constructed through esterification. The conjugation makes amphiphilic VES-Ir prodrug self-assemble into nanoparticles with a fine diameter (VES-Ir NPs, 75.4 nm) of spherical morphology. Furthermore, VES-Ir NPs with a 1:1 drug-to-drug ratio was demonstrated to possess respectable physiological stability within 72 h test, while can react to pH/esterase-sensitive drug release in lysosomes internalized into tumor cells, potentially highlighting their alleviating side effects. Comp...
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Boosting Transdermal delivery of Atorvastatin Calcium via o/w Nanoemulsifying System: Two-step optimization, ex vivo and in vivo evaluation
In conclusion, data revealed no correlation between ex vivo and in vivo studies explained by the collapse of the follicles in ex vivo skin permeation study, leaving only the lipoidal pathway for NE to pass through, thus only NE components, neither nanosizing nor other reported mechanisms, are the main influencing factors. In vivo experiments suggested that o/w NE changed ATOR pathway to follicular delivery leading to accumulation of NE in follicles and consequently a prolonged plasma profile.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Drug-loaded implantable surgical cavity-adaptive hydrogels for prevention of local tumor recurrence
Publication date: Available online 21 January 2020Source: International Journal of PharmaceuticsAuthor(s): Bo Zhuang, Ting Chen, Zhimei Xiao, Yiguang JinAbstractHigh local post-surgical cancer recurrence severely impairs the patients’ prognosis and survival rates. Here, an injectable in situ forming hydrogel was designed to locally controlled release gemcitabine (GEM) and doxorubicin (DOX) to prevent local cancer recurrence. The hydrogel was rapidly formed at the post-surgical cavity after the aldehyde hyaluronic acid (HA-CHO) and the carboxymethyl chitosan (CM-CS) were mixed and immediately injected. Meanwhile, DOX ...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Continuous twin screw granulation: impact of binder addition method and surfactants on granulation of a high-dosed, poorly soluble API
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Christoph Portier, Tamas Vigh, Giustino Di Pretoro, Thomas De Beer, Chris Vervaet, Valérie VanhoorneAbstractDespite the recent commercialization of several drug products manufactured through continuous manufacturing techniques, knowledge on the formulation aspect of these techniques, such as twin screw wet granulation, is still rather limited. Previous research identified lactose/MCC/HPMC as a robust platform formulation for several model formulations, although granulation of the high-dosed, poorly soluble API ...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Synthesis of cationic quaternized pullulan derivatives for miRNA delivery
In conclusion, the formation of polyplexes using cationic derivatives of pullulan with miRNA provided an easy and versatile method for polysaccharide nanoparticle production in aqueous media and could be a new promising platform for gene delivery.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Oral formulation strategies to improve the bioavailability and mitigate the food effect of abiraterone acetate
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Hayley B. Schultz, Tahlia R. Meola, Nicky Thomas, Clive A. PrestidgeAbstractAbiraterone acetate, marketed as Zytiga®, is an antiandrogen medication used in the treatment of prostate cancer. Abiraterone acetate is a BCS Class IV compound associated with several oral delivery challenges. Its low solubility and high lipophilicity lead to poor oral bioavailability (
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Crystallo-co-spray drying as a new approach to manufacturing of drug/excipient agglomerates: impact of processing on the properties of paracetamol and lactose mixtures
Publication date: Available online 22 January 2020Source: International Journal of PharmaceuticsAuthor(s): Alan F. McDonagh, Lidia TajberAbstractThe novel process of crystallo-co-spray drying of paracetamol and α-lactose monohydrate was investigated by varying the spray dryer inlet temperature and inlet feed solvent composition. A crystalline agglomerate was obtained with no change to the physical structure of either component throughout both investigations and with possible interactions between the hydroxyl groups of the α-lactose monohydrate and the amide and hydroxyl groups of the paracetamol detected. The p...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Prediction of drug dissolution from Toremifene 80 mg tablets by NIR spectroscopy
Publication date: 15 March 2020Source: International Journal of Pharmaceutics, Volume 577Author(s): Krista Ojala, Mika Myrskyranta, Anni Liimatainen, Hanna Kortejärvi, Anne JuppoAbstractThe aim of our study was to justify substitution of dissolution analysis for NIR measurement of Toremifene 80 mg tablets. We studied implementation of a NIRS method by integrating the method development to discrimination power of the dissolution method. Hence, we analyzed 20 DoE tablet batches and studied which of the critical formulation factors affecting dissolution were statistically significant. To study if these factors can b...
Source: International Journal of Pharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Source Type: research

Critical steps during the prilling process of molten lipids: Main stumbling blocks due to pharmaceutical excipient properties
Publication date: 25 February 2020Source: International Journal of Pharmaceutics, Volume 576Author(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 behavi...
Source: International Journal of Pharmaceutics - January 21, 2020 Category: Drugs & Pharmacology Source Type: research

Evaluating supersaturation in vitro and predicting its performance in vivo with Biphasic Gastrointestinal Simulator: A case study of a BCS IIB drug
In conclusion, CoPVP and HPMC increased and prolonged the supersaturation of apatinib, and then improved its bioavailability. Moreover, BGIS was demonstrated to be a significant approach for simulating in vivo conditions for in vitro-in vivo correlation in a supersaturation study. This study presents a promising approach for evaluating supersaturation, screening precipitation inhibitors in vitro, and predicting their performances in vivo.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 19, 2020 Category: Drugs & Pharmacology Source Type: research

Sincere thanks to Véronique Préat and Thorsteinn Loftsson and a Warm Welcome to Carmen Alvarez-Lorenzo and Juan Manuel Irache
Publication date: Available online 17 January 2020Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 18, 2020 Category: Drugs & Pharmacology Source Type: research

Poorly soluble drugs
Publication date: Available online 17 January 2020Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann, Thomas Rades, Anette Muellertz, Thorsteinn Loftsson (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 18, 2020 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers-mediated brain delivery of carbamazepine for improved in vivo anticonvulsant and anxiolytic activity
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Namrah Khan, Fawad Ali Shah, Isra Rana, Muhammad Mohsin Ansari, Fakhar ud Din, Syed Zaki Husain Rizvi, Waqar Aman, Gwan-Yeong Lee, Eun-Sun Lee, Jin-Ki Kim, Alam ZebAbstractThe limited brain delivery of carbamezapine (CBZ) presents a major hurdle in the successful epilepsy treatment. The potential of carbamezapine-loaded nanostructured lipid carriers (CBZ-NLCs) for improved brain delivery is investigated in the current study. CBZ-NLCs were prepared by using binary mixture of trilaurin and oleic acid as a lipid core sta...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Efficacy of SPM-NONOate following intrapulmonary delivery in promoting absorptions of poorly absorbed macromolecules in rats and the underling mechanism
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Yang Gao, Guangli Liao, Shucong Wang, Ya Sun, Xin Long, Yan Ma, Hailong ZhangAbstractThis research aims to investigate the potential of N-[4-[1-(3-Aminopropyl)-2-hydroxy-2-nitrosohydrazino]butyl]-1,3-propanediamine (SPM-NONOate) for promoting the absorption of poorly absorbed macromolecules delivered by intrapulmonary route. Influence of SPM-NONOate on the drug absorption was characterized by using a series of fluorescein isothiocyanate-labeled dextrans (FDs) as affordable models of hydrophilic macromolecules with est...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Prediction of drug dissolution from Toremifene 80 mg tablets using NIR spectroscopy
Publication date: Available online 16 January 2020Source: International Journal of PharmaceuticsAuthor(s): Krista Ojala, Mika Myrskyranta, Anni Liimatainen, Hanna Kortejärvi, Anne JuppoAbstractThe aim of our study was to justify substitution of dissolution analysis for NIR measurement of Toremifene 80 mg tablets. We studied implementation of a NIRS method by integrating the method development to discrimination power of the dissolution method. Hence, we analyzed 20 DoE tablet batches and studied which of the critical formulation factors affecting dissolution were statistically significant. To study if these factors can...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Application of machine learning to predict monomer retention of therapeutic proteins after long term storage
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Lorenzo Gentiluomo, Dierk Roessner, Wolfgang FrießAbstractAn important aspect of initial developability assessments as well formulation development and selection of therapeutic proteins is the evaluation of data obtained under accelerated stress condition, i.e. at elevated temperatures. We propose the application of artificial neural networks (ANNs) to predict long term stability in real storage condition from accelerated stability studies and other high-throughput biophysical properties e.g. the first apparent ...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Formulation of simvastatin chitosan nanoparticles for controlled delivery in bone regeneration: optimization using Box-Behnken design, stability and in vivo study
This study aims to formulate and optimize simvastatin loaded chitosan-tripolyphosphate nanoparticle (SIM CS-TPP NPs) using ionic gelation method to provide a local delivery system that control and sustain the release of simvastatin in the desired dose to promote bone regeneration. Box-Behnken design was adopted for optimization of the formulation variables of the prepared nanoparticles namely, CS percentage, TPP percentage and homogenization time. The optimized formula was selected and characterized by transmission electronic microscopy, in-vitro release, swelling index and storage stability. The ability of the optimum for...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

Novel ultrasmall nanomicelles based on rebaudioside A: A potential nanoplatform for the ocular delivery of pterostilbene
Publication date: Available online 15 January 2020Source: International Journal of PharmaceuticsAuthor(s): Kaichao Song, Meng Xin, Fan Zhang, Wenjing Xie, Mingyue Sun, Xianggen WuAbstractRebaudioside A (RA) self-assembled into ultrasmall nanomicelles can be utilized as ocular drug delivery system; nevertheless, the therapeutic efficacy of RA micelles has not evaluated thus far. In this manuscript, the RA micelles are thought to strengthen the therapeutic effects of pterostilbene (Pt). Results showed that Pt can be highly encapsulated into RA micelles with ultrasmall particle sizes (3.99 ± 0.03 nm) with a uniform dis...
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

ChABC-Loaded PLGA Nanoparticles: A Comprehensive Study on Biocompatibility, Functional Recovery, and Axonal Regeneration in Animal Model of Spinal Cord Injury
According to this study, the loaded particles can potentially serve as a suitable candidate for spinal cord repair, functional recovery and axonal regeneration.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 16, 2020 Category: Drugs & Pharmacology Source Type: research

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

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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