Stability of Lyophilized Albumin Formulation: Role of Excipient Crystallinity and Molecular Mobility
Publication date: Available online 25 July 2019Source: International Journal of PharmaceuticsAuthor(s): Sampreeti Jena, N.S. Krishna Kumar, Alptekin Aksan, Raj SuryanarayananAbstractIn freeze-dried protein formulations, the composition governs the physical forms of the excipients and hence their functionality. It is also necessary to understand the effect of composition on the molecular relaxation behavior, a key factor influencing protein stability. Mannitol (bulking agent) - trehalose (lyoprotectant) – bovine serum albumin (BSA) lyophiles with varying trehalose to BSA mass ratios were investigated. The crystalline ...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

In-situ forming implants loaded with chlorhexidine and ibuprofen for periodontal treatment: Proof of concept study in vivo
In this study, in-situ forming implants (ISFI) loaded with chlorhexidine dihydrochloride (CHX) and ibuprofen (IBU) were developed and tested to optimize periodontal treatment outcomes. Release profiles were promising. Exposure to 1.5% and 5.3% CHX-IBU loaded ISFI’s release media decreased significantly the P.gingivalis growth up to 20-fold and 35-fold, respectively, after 48h (p
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Injectable PLCL/Gelatin Core-shell Nanofibers Support Noninvasive 3D delivery of Stem Cells
Publication date: Available online 25 July 2019Source: International Journal of PharmaceuticsAuthor(s): Jordi Amagat Molas, Menglin ChenAbstractStem cells with their intrinsic ability to differentiate to specific cell types have been clinically used as the most promising cell therapy. However, the injection-based administration in most clinical trials shows cell retention rates as low as 1% within days of transplantation. Herein, core-shell nanofibers of PLCL (Poly(lactide-co-ε-caprolactone)) and Gelatin-Methacrylate (Gel-MA), respectively, were fabricated to support the 3D delivery of human mesenchymal stem cells ...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Development of a novel human stratum corneum model, as a tool in the optimization of drug formulations
Publication date: Available online 26 July 2019Source: International Journal of PharmaceuticsAuthor(s): Zinaida Shakel, Cláudia Nunes, Sofia A. Costa Lima, Salette ReisAbstractTransdermal delivery represents a very attractive administration route that provides various advantages over other methods of administration, including enhanced patient compliance via non-invasive, painless and simple application and reduced side effects. Thereby, the research on suitable drugs for this route continues to increase. However, most of drug candidates face the challenges of low drug permeability across the skin’s biologicall...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Towards a dapivirine and levonorgestrel multipurpose vaginal ring: Investigations into the reaction between levonorgestrel and addition-cure silicone elastomers
Publication date: Available online 26 July 2019Source: International Journal of PharmaceuticsAuthor(s): Yahya H. Dallal Bashi, Clare F. McCoy, Diarmaid Murphy, Peter Boyd, Patrick Spence, Kyle Kleinbeck, Bríd Devlin, R. Karl MalcolmAbstractWith a dapivirine-releasing vaginal ring having successfully completed late-stage clinical testing for HIV prevention and currently undergoing regulatory review, there is now growing interest in next-generation multipurpose prevention technologies that seek to combine antiretroviral and contraceptive drugs within a single product. Here, we focus on ongoing efforts to develop a sil...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Amorphous binary dispersions of chloramphenicol in enantiomeric pure and racemic poly-lactic acid: morphology, molecular relaxations, and controlled drug release
Publication date: Available online 26 July 2019Source: International Journal of PharmaceuticsAuthor(s): Sofia Valenti, Angelica Diaz, Michela Romanini, Luis Javier del Valle, Jordi Puiggalí, Josep Lluis Tamarit, Roberto MacovezAbstractWe characterize amorphous solid dispersions (ASDs) of the Chloramphenicol antibiotic in two biodegradable polylactic acid polymers, namely a commercial sample of enantiomeric pure PLLA and a home-synthesized PDLLA copolymer, investigating in particular the effect of polylactic acid in stabilizing the amorphous form of the drug and controlling its release (e.g. for antitumoral purposes)...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Co-delivery of pretubulysin and siEG5 to EGFR overexpressing carcinoma cells
In this study, siRNA against the kinesin related mRNA EG5 gene (siEG5) and the microtubule inhibitor pretubulysin (PT) were co-formulated into polyplexes using azide-containing lipo-oligomer 1198. Nanoparticles were further modified by click reaction using shielding agent DBCO-PEG or EGFR targeting peptide GE11 (DBCO-PEG-GE11). Polyplexes displayed efficient payload incorporation and homogenous particle sizes of 200 nm. The biological effects of the unmodified and surface-functionalized polyplexes were investigated. The successful GE11-mediated intracellular delivery of siRNA into the EGFR overexpressing KB and Huh7 cell l...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Magnetic nanocarriers for the specific delivery of siRNA: contribution of breast cancer cells active targeting for down-regulation efficiency
In conclusion, TS-MSN are promising nanocarriers for the specific and efficient delivery of siRNA to HER2-overexpressing breast cancer cells.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Molecular modelling of TLR agonist Pam3CSK4 entrapment in PLA nanoparticles as a tool to explain loading efficiency and functionality
Publication date: Available online 26 July 2019Source: International Journal of PharmaceuticsAuthor(s): Myriam Lamrayah, Fanny Charriaud, Shangnong Hu, Simon Megy, Raphael Terreux, Bernard VerrierAbstractDesigning potent and safe-of-use therapies against cancers and infections remains challenging despite the emergence of novel molecule classes like checkpoint inhibitors or Toll-Like-Receptor ligands. The latest therapeutic perspectives under development for immune modulator administration exploits vectorization, and biodegradable delivery systems are one of the most promising vehicles. Nanoparticles based on Poly (D,L) Lac...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Influence of stabilizer type and concentration on the lung deposition and retention of resveratrol nanosuspension-in-microparticles
In conclusion, the deposition and lung retention behavior of NS-in-MPs could be well tuned by selecting different type or concentration of stabilizers, which could facilitate local lung diseases therapy.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Coloring of PLGA implants to better understand the underlying drug release mechanisms
Publication date: Available online 24 July 2019Source: International Journal of PharmaceuticsAuthor(s): C. Bode, H. Kranz, F. Siepmann, J. SiepmannAbstractDifferent dyes and a colored vitamin (riboflavin) were used to better understand the underlying drug release mechanisms in poly(lactic-co-glycolic acid) (PLGA)-based implants. The latter were prepared by hot melt extrusion (HME) or formed in-situ, upon solvent exchange when injecting a PLGA solution in N-methyl-pyrrolidone (NMP) into phosphate buffer pH 7.4. Methylene blue was used as water-soluble dye to stain the release medium, riboflavin as a yellow, water-solub...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Could spray-dried microbeads with chitosan glutamate be considered as promising vaginal microbicide carriers? The effect of process variables on the in vitro functional and physicochemical characteristics
Publication date: Available online 25 July 2019Source: International Journal of PharmaceuticsAuthor(s): Szymanska Emilia, Czarnomysy Robert, Jacyna Julia, Basa Anna, Wilczewska Agnieszka Zofia, Markuszewski Michal, Winnicka KatarzynaAbstractIn order to improve efficacy and accessibility of vaginal microbicides, development of smart polymer-based delivery carriers appears essential. In scope of this study, the potential of chitosan glutamate in technology of microbicide multiunit formulations containing zidovudine-loaded microbeads was investigated. Spray-drying optimization was supported by statistical design of experiment...
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Novel antipsoriatic fluidized spanlastic nanovesicles: in vitro physicochemical characterization, ex vivo cutaneous retention and exploratory clinical therapeutic efficacy
Publication date: Available online 23 July 2019Source: International Journal of PharmaceuticsAuthor(s): Enas Elmowafy, Riham I. El-Gogary, Maha H. Ragai, Maha NasrAbstractTazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SN...
Source: International Journal of Pharmaceutics - July 24, 2019 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of PLA-coated co-micellar nanosystem of Resveratrol for the intra-articular treatment of arthritis
Publication date: Available online 24 July 2019Source: International Journal of PharmaceuticsAuthor(s): Rabab Kamel, Haidy Abbas, Nermine M. ShaffieAbstractArthritis is a chronic degenerative joint disease decreasing the patient's quality of life. Mixed micellar system (MM) was exploited as a nanotechnology platform suitable for the encapsulation of the water-insoluble drug, Resveratrol (RES). MM were prepared using different ratios of poloxamer 188 (P188) and poloxamer 407 (P407), and then subjected to in-vitro evaluation. The selected MM (MM3) composed of P188: P407 in a ratio of 2:1 attained the most compromised propert...
Source: International Journal of Pharmaceutics - July 24, 2019 Category: Drugs & Pharmacology Source Type: research

A rapid In-Process Control (IPC) test to monitor the functionality of taste masking polymer coatings using Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS)
In this study, the functional polymer loading of the coating process is investigated by testing pellets via BARDS technology (Broadband Acoustic Resonance Dissolution Spectroscopy). The technique offers a rapid approach (
Source: International Journal of Pharmaceutics - July 24, 2019 Category: Drugs & Pharmacology Source Type: research

Determinants of preferential renal accumulation of synthetic polymers in acute kidney injury
This study demonstrates for the first time that polymers with specific physicochemical characteristics exhibit promising ability to accumulate in the injured AKI kidney, providing initial insights on their use as polymeric drug delivery systems in AKI.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 23, 2019 Category: Drugs & Pharmacology Source Type: research

Chitosan-Polycaprolactone Blend Sponges for Management of Chronic Osteomyelitis: A Preliminary Characterization and In vitro Evaluation
Publication date: Available online 22 July 2019Source: International Journal of PharmaceuticsAuthor(s): Vaishali Pawar, Rohit SrivastavaAbstractBlending two polymers is an effective technique to obtain a novel material with desirable properties. Chitosan (CH) has limited applications in tissue engineering owing to its poor mechanical strength in a wet state. Polycaprolactone (PCL) has low toxicity with good mechanical strength and controlled release properties, but the slower degradation rate restricts its applications in drug delivery. Thus, the blending of CH and PCL (CH/PCL) polymers would provide a better biomaterial r...
Source: International Journal of Pharmaceutics - July 23, 2019 Category: Drugs & Pharmacology Source Type: research

How broadly can poly(urethane)-based implants be applied to drugs of varied properties?
Publication date: Available online 20 July 2019Source: International Journal of PharmaceuticsAuthor(s): Michael B. Lowinger, James Ormes, Yongchao Su, James H. Small, Robert O. Williams, Feng ZhangAbstractImplants offer the opportunity to improve patient adherence and real-world outcomes. However, most polymers used today are hydrophobic and limit drug properties suitable for development. Thermoplastic poly(urethanes) (TPUs) form pores upon hydration and may facilitate the development of implants containing drugs exhibiting broadly different properties. We sought to investigate the effect of drug physicochemical properties...
Source: International Journal of Pharmaceutics - July 21, 2019 Category: Drugs & Pharmacology Source Type: research

The subdivision behavior of polymeric tablets
Publication date: Available online 20 July 2019Source: International Journal of PharmaceuticsAuthor(s): Marcilio Cunha-Filho, Maíra T. Teixeira, Víctor Santos-Rosales, Livia L. Sa-Barreto, Ricardo N. Marreto, Manuel Martin-Pastor, Carlos A. García-González, Mariana LandinAbstractThe subdivision behavior of polymeric tablets produced with the well-known polymers Soluplus® (SOL), polyvinyl pyrrolidone co-vinyl acetate (PVPVA) and hydroxypropyl methylcellulose (HPMC) was evaluated in this study. The polymeric tablets were submitted to different post-treatments (aging, thermal and exposure to co...
Source: International Journal of Pharmaceutics - July 21, 2019 Category: Drugs & Pharmacology Source Type: research

Development and Applications of a Material Library for Pharmaceutical Continuous Manufacturing of Solid Dosage Forms
This study included 20 pharmaceutical materials, and each material was characterized by 44 properties, capturing 880 data points. The stress conditions of a commonly used feeder hopper were calculated using the Janssen model for six selected materials. Multivariate analysis, such as principal component analysis and clustering analysis, was used to explore the knowledge space of the material library. Statistically similar and dissimilar material properties were evaluated for material feeding performance from a loss-in-weight feeder to test utility of the material library. 20 materials included in this study show a wide rang...
Source: International Journal of Pharmaceutics - July 21, 2019 Category: Drugs & Pharmacology Source Type: research

A Predictive Integrated Framework Based on the Radial Basis Function for the Modelling of the Flow of Pharmaceutical Powders
This study presents a modelling framework to predict the flowability of various commonly used pharmaceutical powders and their blends. The flowability models were trained and validated on 86 samples including single components and binary mixtures. Two modelling paradigms based on artificial intelligence (AI) namely, a radial basis function (RBF) and an integrated network were employed to model the flowability represented by the flow function coefficient (FFC) and the bulk density (RHOB). Both approaches were utilized to map the input parameters (i.e. particle size, shape descriptors and material type) to the flow propertie...
Source: International Journal of Pharmaceutics - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Assessing particle segregation using near-infrared chemical imaging in twin screw granulation
Publication date: Available online 19 July 2019Source: International Journal of PharmaceuticsAuthor(s): Aquino L. Mundozah, Jiankai Yang, Claire C. Tridon, James J. Cartwright, Chalak Omar, Agba D. SalmanAbstractIn the present study the application of near-infrared chemical imaging (NIR-CI) for assessing particle segregation in granules from continuous twin screw granulation (TSG) granules, were the complex attributes of the machinery configuration in relation to particle segregation is not well understood was investigated. Experiments were performed along the compartmental length of the TSG barrel channel by varying the s...
Source: International Journal of Pharmaceutics - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “PLGA nanoformulation of sparfloxacin enhanced antibacterial activity with photoprotective potential under ambient UV-R exposure” [Int. J. Pharm. 541 (2018) 173–187]
Publication date: Available online 19 July 2019Source: International Journal of PharmaceuticsAuthor(s): Jyoti Singh, Ashish Dwivedi, Lipika Ray, Deepti Chopra, Divya Dubey, Ajeet K. Srivastva, Smita Kumari, Randhir Kumar Yadav, Saroj Kumar Amar, Chandana Haldar, Ratan Singh Ray (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 15 August 2019Source: International Journal of Pharmaceutics, Volume 567Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Rheological temperature sweeping in a quality by design approach for formulation development and optimization
In conclusion, RTS enables a rapid screening of liquid and semi-solid products in a quantitative manner for pharmaceutical development and formulation optimization.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 19, 2019 Category: Drugs & Pharmacology Source Type: research

Physicochemical characteristics that affect carbon dot safety: lessons from a comprehensive study on a nanoparticle library
In conclusion, the size, aggregation in culture medium, charge, nitrogen content, nature of the passivation agent and synthesis procedure were found to influence CD toxicity, making it difficult to predict CD safety from a single characteristic.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Rationally designed hyaluronic acid-based nano-complexes for pentamidine delivery
Publication date: Available online 16 July 2019Source: International Journal of PharmaceuticsAuthor(s): Flavia Carton, Yves Chevalier, Letizia Nicoletti, Małgorzata Tarnowska, Barbara Stella, Silvia Arpicco, Manuela Malatesta, Lars Petter Jordheim, Stéphanie Briançon, Giovanna LolloAbstractNanoparticles of polymeric complexes made of hyaluronic acid and polyarginine were investigated for the encapsulation of the cationic hydrophilic drug pentamidine isethionate. The interaction between the anionic hyaluronic acid and the cationic pentamidine and the formation of polyelectrolyte complexes of them were firstly...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Ethosomes and Lipid-Coated Chitosan Nanocarriers for Skin Delivery of a Chlorophyll Derivative: A Potential Treatment of Squamous Cell Carcinoma by Photodynamic Therapy
In conclusion, both types of nanocarriers can be used for their potential treatment of SCC using PDT depending on the tumour localization in the skin.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Curcumin encapsulation in yeast glucan particles promotes its anti-inflammatory potential in vitro
Publication date: Available online 16 July 2019Source: International Journal of PharmaceuticsAuthor(s): Zuzana Plavcová, Petra Šalamúnová, Ivan Saloň, František Štěpánek, Jaroslav Hanuš, Jan HošekAbstractGlucan particles (GPs) from Saccharomyces cerevisiae are hollow shells that are composed mainly of β-1,3-d-glucan, which has demonstrated immunomodulatory and anti-inflammatory potential both in vitro and in vivo. Curcumin is a natural hydrophobic phenolic compound, which possesses a significant anti-inflammatory effect and is used as supportive therapy ...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Rapamycin loaded TPGS-Lecithins-Zein nanoparticles based on Core-Shell structure for Oral Drug Administration
Publication date: Available online 16 July 2019Source: International Journal of PharmaceuticsAuthor(s): Zhonghui Xie, Zhenhai Zhang, Huixia LvAbstractRapamycin as a novel macrolide immunosuppressive agent has been commonly used in organ transplantation owing to its stronger immunosuppressive effect, non-nephrotoxicity and lower side effect. However its drawbacks of low bioavailability and big individual difference remain to be improved in clinical application. Here rapamycin loaded TPGS-Lecithins-Zein nanoparticles (RTLZ-NPs) with core-shell structure were prepared by the phase separation method. The RTLZ-NPs were approxim...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Cubic Liquid Crystalline Structures in Diluted, Concentrated and Highly Concentrated Emulsions for Topical Application: Influence on Drug Release and Human Skin Permeation
In this study, oil-in-water (O/W) emulsions with two surfactant/water (S/W) weight ratios of 40:60 and 35:65, and oil concentrations of 10wt% (diluted emulsion), 40wt% (concentrated emulsion) and 85wt% (highly concentrated emulsion) have been investigated to identify the presence of liquid crystalline structures and their influence on drug release and skin permeation. The emulsions have been characterized in terms of visual appearance, rheology and drug release. The presence of cubic liquid crystalline structures in emulsions with S/W 40:60 was confirmed by small angle X-ray scattering (SAXS). Rheology results showed a mar...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Nanotechnology-based siRNA Delivery Strategies for Metastatic Colorectal Cancer Therapy
Publication date: Available online 16 July 2019Source: International Journal of PharmaceuticsAuthor(s): Ana Rita Sousa, Ana Vanessa Oliveira, Maria José Oliveira, Bruno SarmentoAbstractColorectal cancer (CRC) is the second most common cause of cancer-related death in the world, mainly due to distant metastases events. The metastatic CRC (mCRC) stages are resistant to the therapeutic recommended. Therefore, it urges the development of more efficient strategies to impair the disease. Small interfering RNA (siRNA) is a well-known silencing tool with impact on targeted cancer therapy, even though in vivo challenges diff...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Managing API raw material variability in a continuous manufacturing line – Prediction of process robustness
In this study, the possibility to manage the batch-to-batch variability of an active pharmaceutical ingredient (API) in a high drug loaded formulation on a continuous line was investigated to obtain consistent tablet CQAs. As the ultimate goal of continuous manufacturing is to produce 24/7, current study also aimed at guaranteeing long term stability of the process. To do so, previously identified API critical material attributes (CMAs) were varied together with granulation, drying and milling critical process parameters (CPPs) in a screening design of experiments to understand the influence of these factors upon product C...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Correlation between the Stability Constant and pH for β-Cyclodextrin Complexes
Publication date: Available online 15 July 2019Source: International Journal of PharmaceuticsAuthor(s): Lisa Samuelsen, René Holm, Audrey Lathuile, Christian SchönbeckAbstractIn drug formulations, cyclodextrins are used to increase aqueous solubility and chemical stability of drugs via formation of inclusion complexes. For ionizable drug molecules, the complexation strength depends on pH. Increased ionization leads to a more soluble drug, but also results in destabilization of cyclodextrin complexes. Therefore, formulation scientists aim to find a balance between increased drug solubility and high complexation ...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Screening of different polysaccharides in a composite film based on Eudragit RS for subsequent use as a coating for delivery of 5-ASA to colon
This study aims at identifying the more suitable polysaccharide in a composite film based on Eudragit RS for 5-ASA delivery to the colon. Different polysaccharides (pectin, chitosan, guar, inulin, and dextran) were examined. The mechanical properties, swelling index, loss of film mass and permeability of films to 5-ASA were recorded at simulating gastric (SGF), intestinal (SIF) and colonic fluids (SCF). Films containing inulin or dextran were more flexible and showed better mechanical properties. Films containing chitosan, pectin or guar exhibited extensive swelling in SGF and SIF. Loss of film mass and drug permeation was...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

CD123/CD33 dual-antibody modified liposomes effectively target acute myeloid leukemia cells and reduce antigen-negative escape
In this study, antibody mixture of CD123 and CD33 (1:1, molar ratio) were thiolated and coupled to Mal-PEG2000-DSPE, then the antibody-Mal-PEG2000-DSPE conjugations were inserted on the DNR-loaded PEGylated liposomes (PEG-LP-DNR) via a post insertion method to prepare CD123/CD33-LP-DNR (antibody/S100PC, molar ratio, 0.06%). The cellular uptake and cytotoxicity were evaluated in THP-1 (CD123brightCD33bright) and HL-60 (CD123dimCD33bright) cells. Compared to the unmodified liposome, CD123/CD33-LP-DNR showed higher cellular uptake which was 1.8-times and 1.6-times in both THP-1 and HL-60 cells, respectively, while the cellula...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Pulmonary Delivery of Nanocomposite Microparticles (NCMPs) incorporating miR-146a for Treatment of COPD
In this study, Nanocomposite Microparticles (NCMPs) of microRNA (miR-146a) containing PGA-co-PDL nanoparticles (NPs) for dry powder inhalation were formulated using L-leucine and mannitol. The spray-drying (Buchi B290) process was optimised and used to incorporate NPs into NCMPs using mix of L-leucine and mannitol excipients in different ratios (F1; 100:0 % w/w, F2; 75:25 % w/w, F3; 50:50 % w/w, F4; 25:75 % w/w, F5; 0:100 % w/w) to investigate yield %, moisture content, aerosolisation performance and miR-146a biological activity. The optimum condition was performed at feed rate 0.5 mL/min, aspirator rate 28 m3/h, atomizing...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

BET surface area measurement of commercial magnesium stearate by krypton adsorption in preference to nitrogen adsorption
Publication date: Available online 15 July 2019Source: International Journal of PharmaceuticsAuthor(s): Darren P Lapham, Julie L LaphamAbstractMagnesium stearate is an extremely common pharmaceutical excipient and the measurement of BET surface area via nitrogen adsorption is undertaken during pharmaceutical formulation and manufacture. In this paper, four commercial magnesium stearate materials in mono- and di-hydrated forms are analysed by nitrogen and krypton adsorption for the calculation of BET surface area. BET surface area via nitrogen adsorption is shown to be erroneously high due to a structural swelling and adsor...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

Polyoxazolines based mixed micelles as PEG free formulations for an effective quercetin antioxidant topical delivery
This study aims to prove the value of the polyoxazolines polymer family as surfactant in formulations for topical application and as an alternative to PEG overuse. The amphiphilic polyoxazolines (POx) were demonstrated to have less impact on cell viability of mice fibroblasts (NIH3T3) than their PEG counterparts. Mixed micelles, made of POx and phosphatidylcholine, were manufactured using thin film and high pressure homogenizer process. The mixed micelles were optimized to produce nanosized of vesicles about 20 nm with a spherical shape and stable over 28 days. The natural lipophilic antioxidant, quercetin, was successfull...
Source: International Journal of Pharmaceutics - July 17, 2019 Category: Drugs & Pharmacology Source Type: research

In-vitro Studies of Jet Injections
In this study, needle-free jet injection dynamics were studied using homogeneous gelatin as model substrates. Whilst keeping nozzle properties such as orifice diameter (do) and ampoule volume (V) constant, we demonstrate the effect of standoff (s), confinement around the gel, storage modulus (G’) of model gel and liquid viscosity (μ) on the penetration depth of the jet injection. High-speed imaging was used to observe the liquid jet propagation and dispersion dynamics, whilst a load cell was implemented to measure the impact force for different standoff distance and viscosity of the liquid. The different parameter...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

3D printed mold-based capsaicin candy for the treatment of oral ulcer
Publication date: Available online 12 July 2019Source: International Journal of PharmaceuticsAuthor(s): Heliu Jiang, Xiang Yu, Rongzhen Fang, Zhimei Xiao, Yiguang JinAbstractOral ulcer is one common mucosal disease with high prevalence. Here, capsaicin candies were prepared based on stereolithographically (SLA) 3D printed molds. The molds can be freely designed depending on the needs of patients, involving symmetric shapes (e.g., round, four-lead clover and cube), asymmetric shapes (e.g., car) and various color (e.g., blue, red and yellow). A two-part-combined mold was poured with the xylitol-based material and separated t...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Science and Art of Protein Formulation Development
Publication date: Available online 12 July 2019Source: International Journal of PharmaceuticsAuthor(s): Wei Wang, Satoshi OhtakeAbstract:Protein pharmaceuticals have become a significant class of marketed drug products and are expected to grow steadily over the next decade. Development of a commercial protein product is, however, a rather complex process. A critical step in this process is formulation development, enabling the final product configuration. A number of challenges still exist in the formulation development process. This review is intended to discuss these challenges, to illustrate the basic formulation develo...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Hydrocortisone loaded poly-(3-hydroxybutyrate-co-3-hydroxyvalerate) nanoparticles for topical ophthalmic administration: preparation, characterization and evaluation of ophthalmic toxicity
Publication date: Available online 13 July 2019Source: International Journal of PharmaceuticsAuthor(s): Lucía Álvarez-Álvarez, Luis Barral, Rebeca Bouza, Yousof Farrag, Francisco Otero-Espinar, Sandra Feijóo-Bandín, Francisca LagoAbstractPoly-(3-hydroxybutyrate-co-3-hydroxyvalerate) nanoparticles (PHBV-NPs) to encapsulate hydrocortisone (HC) for topical ophthalmic administration were prepared and characterized. The technique used to prepare the nanoparticles (NPs) was emulsification/solvent evaporation. The obtained size was 237.3 ± 2.7 nm, suitable for topical ocular administratio...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Enhance the efficiency of 5-fluorouracil targeted delivery by using a prodrug approach as a novel strategy for prolonged circulation time and improved permeation
Publication date: Available online 2 July 2019Source: International Journal of PharmaceuticsAuthor(s): Samaneh Pasban, Heidar Raissi, Majid Pakdel, Farzaneh FarzadAbstractDue to the toxicity and resistance to treatment with anticancer drugs, various methods are used to improve their efficacy in cancer treatment. In this present study, in order to overcome the limitation of 5-Fluorouracil (5-FU), prodrug strategy has been pursued with using density functional theory (DFT) and molecular dynamics simulation (MDs). The main objective of this study is to examine the mechanisms of drug release from its prodrug form by using the ...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics and biodistribution study of self-assembled Gd-micelles demonstrating blood-pool contrast enhancement for MRI
Publication date: Available online 3 July 2019Source: International Journal of PharmaceuticsAuthor(s): V. Vorobiev, A. Babič, L.A. Crowe, Y. Van De Looij, S. Lenglet, A. Thomas, L. Helm, J.-P. Vallée, E. AllémannAbstractMagnetic resonance angiography (MRA) requires the use of contrast agents (CAs) to enable accurate diagnosis. There are currently no CAs on the market with appropriate pharmacokinetic (PK) parameters, namely long persistence in the blood, that can be easily used for MRA. We have recently synthesized amphiphilic building blocks loaded with gadolinium (Gd), which self-assemble into Gd-micelles i...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Advances in Delivery of Irinotecan (CPT-11) Active Metabolite 7-Ethyl-10-Hydroxycamptothecin
Publication date: Available online 9 July 2019Source: International Journal of PharmaceuticsAuthor(s): Jingxing Si, Xiaobao Zhao, Shan Gao, Dongsheng Huang, Meihua SuiAbstractCPT-11 is a first-line chemotherapy for advanced or metastatic colorectal cancers (mCRC). SN38 (7-ethyl-10-hydroxycamptothecin), the active metabolite of CPT-11, has an anticancer efficacy 100-1000 folds more than CPT-11 in vitro. However, the drawbacks such as ultralow solubility and poor stability, greatly limit the clinical applications of SN38. Recently, SN38-based nanomedicines have greatly improved the pharmaceutical and therapeutic characterist...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Correlations between surface composition and aerosolization of jet-milled dry powder inhaler formulations with pharmaceutical lubricants
This study aims to establish the relationship between surface lubricant coverage and aerosolization behavior of a model drug (ciprofloxacin HCl) co-jet-milled with lubricants [magnesium stearate (MgSt) or L-leucine]. The co-jet-milled formulations were characterized for their particle size, morphology, cohesion, Carr’s index, and aerosolization performance. The surface lubricant coating was assessed by probing surface chemical composition using X-ray photoelectron spectroscopy (XPS) and time-of-flight secondary-ion mass spectrometry (ToF-SIMS). The effects of co-jet-milling on the surface energy and in vitro dissolut...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Multi-walled carbon nanotube-incorporating electrospun composite fibrous mats for controlled drug release profile
Publication date: Available online 10 July 2019Source: International Journal of PharmaceuticsAuthor(s): Y. Emre Bulbul, Ş. Melda Eskitoros-Togay, Funda Demirtas Korkmaz, Nursel DilsizAbstractThe fabrication of electrospun composite nanofiber mats used as drug delivery systems with controlled release property is of general interest in biomaterial sciences. The aim of this study was to investigate the effect of MWCNTs on the release profile of the hydrophilic drug. For this aim, tetracycline hydrochloride (TCH) loaded poly (lactic acid) (PLA)/polyvinylpyrrolidone (PVP)/TCH-multiwall carbon nanotubes (MWCNTs) composite fibro...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Downstream Processing of Irbesartan Nanocrystalline Suspension and Mini-Tablet Development – Part II
The objectives of this study were to evaluate the impact of formulation variables on the drying of nanocrystalline suspensions either via bead layering or spray granulation and develop mini-tablets from the dried nanocrystalline powders. Irbesartan (crystalline Form B), a poorly soluble drug substance was chosen as a model compound. An optimized irbesartan nanocrystalline suspension with a mean particle size of 300 nm was utilized for the downstream processing. Irbesartan nanocrystalline suspension was dried either by layering onto the microcrystalline cellulose beads (i.e. 200 or 500 micron) or by granulation (mannitol or...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research

Is prodrug design an approach to increase water solubility?
Publication date: Available online 10 July 2019Source: International Journal of PharmaceuticsAuthor(s): Bruna M.A. Sanches, Elizabeth I. FerreiraAbstractWater solubility has been identified as a critical parameter and the main responsible by affecting poor performance of oral drug delivery. Poorly soluble drugs can originate unsatisfactory ADME properties leading to low oral bioavailability, insufficient chemical stability, low half-life, fast pre-systemic metabolism and difficulties in formulation. In this context, the prodrug design is an alternative in order to improve physicochemical, biopharmaceutical and pharmacokine...
Source: International Journal of Pharmaceutics - July 13, 2019 Category: Drugs & Pharmacology Source Type: research