Recent advances in gold and silver nanoparticle based therapies for lung and breast cancers
Publication date: Available online 28 October 2018Source: International Journal of PharmaceuticsAuthor(s): Parth Malik, Tapan K. MukherjeeAbstractIn recent years, gold (Au) and silver (Ag) nanoparticles (NPs) have been the centerstage of improving cancer treatments and therapies, substantially attributed to their size and shape tuneable chemical, optical and photonic properties. Owing to such specialties, diverse shapes of Au and Ag NPs have enabled an efficient cellular uptake along with remarkable improvements in early stage diagnosis of tumors. Robust synthesis methods employing several reducing agents have been the bac...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced oral insulin delivery via surface hydrophilic modification of chitosan copolymer based self-assembly polyelectrolyte nanocomplex
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Chang Liu, Yongqiang Kou, Xin Zhang, Wei Dong, Hongbo Cheng, Shirui MaoAbstractIt is desirable to design nanoparticles for oral insulin delivery that can cross mucus layer and epithelial membrane in the intestine in the meantime. Thus, using chitosan (CS) as the nanocarrier, the objective of this study is to elucidate the contribution of surface hydrophilic and hydrophobic modification on the oral absorption of insulin and the essential for these two strategies combination. First of all, the polyelectronic nanocomplex...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Improving solid-state properties of berberine chloride through forming a salt cocrystal with citric acid
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Qi Lu, Jiangnan Dun, Jia-Mei Chen, Shuyu Liu, Changquan Calvin SunAbstractBerberine chloride (BCl) can exist as an anhydrate, monohydrate, dihydrate, and tetrahydrate. Therefore, it faces the problem of humidity dependent solid phase change when environmental humidity varies during manufacturing and storage of berberine tablets. We have discovered a new 1:1 cocrystal formed between berberine chloride and citric acid (BCl–CA) that exhibits better stability against variations in humidity while maintaining similar ...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of spray nozzle aperture during high shear wet granulation on granule properties and its compression attributes
In this study, nozzles of different aperture sizes were used to introduce the granulating liquid in high shear wet granulation using different process parameters. Design of experiment approach was utilised to assess effect of process parameters on granule properties. Granules produced with different spray nozzles were evaluated for binder distribution inhomogeneity, size, shape, flowability and compression attributes such as tabletability and yield pressure. Coarser granules with better flow properties were produced using the smaller aperture size nozzle. On the other hand, granules had better tabletability and lower yield...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Anti-inflammatory and Anti-cancer Activity of Citral: Optimization of Citral-loaded Solid Lipid Nanoparticles (SLN) using Experimental Factorial Design and LUMiSizer®
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Aleksandra Zielińska, Carlos Martins-Gomes, Nuno R. Ferreira, Amélia M. Silva, Izabela Nowak, Eliana B. SoutoAbstractEssential oils containing monoterpenes are widely used in pharmaceuticals and cosmetic products on account of their wide range of bioactive properties (including anti-cancer activity). Two monoterpenes (citral and geraniol) were firstly tested for their anti-inflammatory activity in a RAW 264.7 cell line, demonstrating citral to have enhanced capacity to inhibit NO production (ca. 84% for citral...
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Facile fabrication of highly photothermal-effective albumin-assisted gold nanoclusters for treating breast cancer
Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Sungin Lee, Changkyu Lee, Sanghyun Park, Kyungseop Lim, Sung Soo Kim, Jong Oh Kim, Eun Seong Lee, Kyung Taek Oh, Han-Gon Choi, Yu Seok YounAbstractGold nanoclusters (AuNCs) have been considered to be a promising candidate for hyperthermia-based anticancer therapy. Herein, we introduce albumin-assisted AuNCs composed of small gold nanoparticles (AuNPs,
Source: International Journal of Pharmaceutics - October 29, 2018 Category: Drugs & Pharmacology Source Type: research

Critical Parameters Dictating Efficiency of Membrane-mediated Drug Transfer using Nanoparticles
In this study, we formulated curcumin in two-structurally distinct NPs: a nanoemulsion (Cur-NE) and a Niosome (Cur-NIO), evaluated their in-vitro cytotoxic effects and examined their mechanisms of drug delivery. The use of Cur-NIO resulted in an unexpected increase in the intracellular accumulation of curcumin and induced a potent cytotoxic effect compared to Cur-NE. To our surprise, however, the effects of the endocytosis of NIO as well as that for NE on the cellular delivery of curcumin were negligible. Consequently, we concluded that Cur-NIO delivers curcumin directly to the cytosol via transfer from the NIO to the cell...
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

A detailed analysis of the influence of β-cyclodextrin derivates on the thermal denaturation of lysozyme
This study reveals that CDs are promising systems for inhibiting protein aggregation without protein denaturation, only if designing derivative CDs is carefully controlled.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

Stability and compatibility of Basmisanil granules co-administered with soft food
Publication date: Available online 27 October 2018Source: International Journal of PharmaceuticsAuthor(s): Anikó Szepes, Anni Pabst-Ravot, Kirsten Storch, Carsten TimpeAbstractCo-administration of solid oral dosage forms with soft food or beverages is commonly used to facilitate administration and to improve compliance in the paediatric and geriatric population and in patient groups with swallowing difficulties.The present case study was conducted to investigate the compatibility, stability and dissolution of Basmisanil administered as granules mixed with different soft food matrices. The data were generated to just...
Source: International Journal of Pharmaceutics - October 27, 2018 Category: Drugs & Pharmacology Source Type: research

Dendrimer-like mesoporous silica nanospheres with suitable surface functionality to combat the multidrug resistance
This study indicates that surface functionality design strategy may display the potential of the large pore sized-MSNs as the efficient chemotherapeutic carriers to combat MDR.Graphical abstractThe potential mechanism of surface functionality-modified MSNs carrying DOX to chemotherapeutic-resistant cancer cells to combat the multidrug resistance (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Encapsulation of Poly I:C and the natural phosphodiester CpG ODN enhanced the efficacy of a hyaluronic acid-modified cationic lipid-PLGA hybrid nanoparticle vaccine in TC-1-grafted tumors
In conclusion, the combination of oligonucleotide adjuvants and synthetic particulate systems not only potentiated the immunogenicity of these nanoparticles but also made these adjuvants safer and more economical, which may be helpful for their wide application.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Corneal targeted Sertaconazole nitrate loaded cubosomes: preparation, statistical optimization, in vitro characterization, ex vivo permeation and in vivo studies
Publication date: Available online 26 October 2018Source: International Journal of PharmaceuticsAuthor(s): Nihal Farid Younes, Sally Adel Abdel-Halim, Abdelhalim I. ElassasyAbstractSertaconazole nitrate (STZ) is a poorly soluble antifungal drug commonly used for treating fungal skin infections. Introducing it as a new treatment option for the management of fungal keratitis, requires the development of a delivery system capable of targeting the infected cornea with an adequate STZ concentration. Hence, Sertaconazole nitrate loaded cubosomes (STZ-CUBs) were prepared, characterized and optimized based on a 33 central composit...
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Delimiting the Knowledge Space and the Design Space of Nanostructured Lipid Carriers through Artificial Intelligence Tools
In this study, a two-step experimental design was performed and databases were successfully modelled using Artificial Intelligence techniques as an innovative method to get optimal, reproducible and stable NLC. The initial approach, including a wide range of values for the different variables, was followed by a second set of experiments with variable values in a narrower range, more suited to the characteristics of the system. NLC loaded with rifabutin, a hydrophobic drug model, were produced by hot homogenization and fully characterized in terms of particle size, size distribution, Zeta potential, encapsulation efficiency...
Source: International Journal of Pharmaceutics - October 26, 2018 Category: Drugs & Pharmacology Source Type: research

Early Detection of Capping Risk in Pharmaceutical Compacts
Publication date: Available online 24 October 2018Source: International Journal of PharmaceuticsAuthor(s): Xiaochi Xu, Chaitanya Krishna Prasad Vallabh, Stephen W. Hoag, Vivek S. Dave, Cetin CetinkayaAbstractCapping is a common mechanical defect in tablet manufacturing, exhibited during or after the compression process. Predicting tablet capping in terms of process variables (e.g. compaction pressure and speed) and formulation properties is essential in pharmaceutical industry. In current work, a non-destructive contact ultrasonic approach for detecting capping risk in the pharmaceutical compacts prepared under various com...
Source: International Journal of Pharmaceutics - October 25, 2018 Category: Drugs & Pharmacology Source Type: research

The application of temperature-composition phase diagrams for hot melt extrusion processing of amorphous solid dispersions to prevent residual crystallinity
In conclusion, phase diagrams provide a rational basis for designing hot melt extrusion processes of amorphous solid dispersions to minimize residual crystalline content, delineating the minimum processing temperature based on thermodynamic considerations.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 25, 2018 Category: Drugs & Pharmacology Source Type: research

Vibrational spectroscopic and Hirshfeld surface analysis of carvedilol crystal forms
This study deals with the spectroscopic (supported by quantum chemistry calculations) characterization of carvedilol structures. Band assignments were performed considering the isolated molecules and periodic calculations. We discuss the correlation between the vibrational modes and the intermolecular forces in the crystalline structures. Towards a better understanding of the intermolecular interactions, Hirshfeld surface was used. Besides band shifts related to stretching vibrations of N−H and O−H groups, differences between other modes have shown the possibility of using infrared spectroscopy to distinguish t...
Source: International Journal of Pharmaceutics - October 24, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 1 December 2018Source: International Journal of Pharmaceutics, Volume 552, Issues 1–2Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 24, 2018 Category: Drugs & Pharmacology Source Type: research

Design of a new disintegration test system for the evaluation of orally disintegrating films
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): Yoshiko Takeuchi, Misaki Kawamoto, Kohei Tahara, Hirofumi TakeuchiAbstractIn the design of the orally disintegrating films (ODFs), it is important to determine the disintegration time (DT) precisely and properly. These films’ DTs are usually assessed by a disintegration test defined in the pharmacopoeias, but under the conditions of such tests, a much larger volume of water is used and a stronger up-down movement is applied compared to the conditions of the human oral cavity. Here we developed and tested our new...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Phospholipid components of the synthetic pulmonary surfactant CHF5633 probed by fluorescence spectroscopy
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): Serena Faggiano, Luca Ronda, Samanta Raboni, Franco Sartor, Valeria Cavatorta, Elisa Sgarbi, Grazia Caivano, Marisa Pertile, Andrea MozzarelliAbstractCHF5633 (Chiesi Farmaceutici, Italy) is a synthetic pulmonary surfactant currently under clinical development for the treatment of Respiratory Distress Syndrome in premature infants. The product is composed of phospholipids in liposomal organization, together with two peptide analogues of human surfactant proteins B and C. Phospholipids in liposomes can undergo oxidation...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics and pharmacodynamics of glimepiride polymorphs
Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): André Luiz Machado Viana, Antonio Carlos Doriguetto, Olimpia Maria Martins Santos Viana, André Luís Morais Ruela, Jennifer Tavares Jacon Freitas, Bruno Ewerton Meireles Souto, Magali Benjamim de Araújo, Fernanda Borges de Araújo PaulaAbstractGlimepiride (GLIM) is used as an oral antihyperglycemic agent for treatment of type 2 diabetes. The drug presents two polymorphic forms (GLIM form I and GLIM form II) described in the literature, and according to in vitro data, GLIM form II is ab...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Peptide-functionalized and high drug loaded novel nanoparticles as dual-targeting drug delivery system for modulated and controlled release of paclitaxel to brain glioma
Publication date: 20 December 2018Source: International Journal of Pharmaceutics, Volume 553, Issues 1–2Author(s): Primiano Pio Di MauroAbstractA dual-targeting drug delivery system for paclitaxel (PTX) was developed by functionalizing novel polyester-based nanoparticles (NPs) with peptides possessing special affinity for low-density lipoprotein receptor (LDLR), overcoming the limitations of the current chemotherapeutics, to transport drug from blood to brain, and then target glioma cells. Employing novel biodegradable block co-polymers (P and 2P), PTX loaded and peptide-functionalized nanoparticles were prepared by ...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoamorphous Drug Products – Design and Development
Publication date: Available online 22 October 2018Source: International Journal of PharmaceuticsAuthor(s): Rajan Jog, Diane J. BurgessAbstractMost of the recent drug compounds coming out of the drug discovery pipeline are labile (multiple polymorphs), and need to be developed into robust marketed oral drug formulations. There are only 22 oral macroamorphous drug products approved by FDA and till date none approved oral nanoamorphous drug products. However, there are several oral nanoamorphous drug formulations (including both labile and non-labile drugs) being researched and a few of these are in the clinical trials. Due t...
Source: International Journal of Pharmaceutics - October 23, 2018 Category: Drugs & Pharmacology Source Type: research

D-Optimal mixture design: Formulation development, mechanical characterization, and optimization of curcumin chewing gums using Oppanol® B 12 elastomer as a gum-base
This study highlighted the impact of each gum ingredient on the quality of the MCGs and demonstrated the feasibility of preparing chewing gums with up to 50% drug loading.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 21, 2018 Category: Drugs & Pharmacology Source Type: research

Coated microneedles mediated intradermal delivery of octaarginine/BRAF siRNA nanocomplexes for anti-melanoma treatment
In this study, we for the first time developed a siBraf delivery system based on cell penetrating peptide octaarginine (R8) nanocomplexes combined with coated microneedles (MNs), i.e. R8/siBraf coated MNs, for targeted anti–melanoma treatment. The R8/siBraf nanocomplexes were optimized based on the internalization of siBraf by A375 cells. In vitro A375 cell experiments presented that R8/siBraf can enhance siBraf transfection, silence BRAF gene, and inhibit tumor cells growth, comparable to polyethylenimine (PEI)/siBraf. R8/siBraf coated MNs can effectively deliver R8/siBraf into the disease site. In vivo anti-melanom...
Source: International Journal of Pharmaceutics - October 21, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation, characterization, and evaluation of celecoxib eutectic mixtures with adipic acid/saccharin for improvement of wettability and dissolution rate
In this study, eutectic mixtures, as binary pharmaceutical compositions of CEL with adipic acid (ADI) and saccharin (SAC), were identified through a phase diagram and Tammann’s triangle intended to improve the wettability and dissolution rate of poorly water-soluble CEL. The contact angles at 0s in the liquid-solid interface were approximately θs (theta) 79.7° ± 0.50° and 86.65° ± 0.45° for CEL-ADI and CEL-SAC, respectively, which were much lower than the value obtained for CEL (92.05° ± 0.75° θ). Moreover, a comparison of the disk intrinsic dissolution rate an...
Source: International Journal of Pharmaceutics - October 21, 2018 Category: Drugs & Pharmacology Source Type: research

Antibacterial layer-by-layer coatings to control drug release from soft contact lenses material
In this study we investigated the possibility of using polyelectrolytes with antibacterial properties to form layer-by-layer (LbL) coatings on contact lens materials with the objective of controlling the release of ophthalmic drugs, while minimizing bacterial growth. A silicone-based hydrogel recently proposed by our group was chosen as a drug releasing soft contact lens (SCL) material and three drugs were tested: moxifloxacin hydrochloride (MXF), chlorhexidine diacetate monohydrate (CHX), and diclofenac sodium salt (DIC). Employed coatings involved combinations of sodium alginate (ALG), chitosan (CHI), sodium hyaluronate ...
Source: International Journal of Pharmaceutics - October 18, 2018 Category: Drugs & Pharmacology Source Type: research

Improvement of the skin penetration of hydrophobic drugs by polymeric micelles
Publication date: Available online 16 October 2018Source: International Journal of PharmaceuticsAuthor(s): Kensuke Yotsumoto, Kenta Ishii, Miho Kokubo, Sakiko YasuokaAbstractPolymeric micelles, which form through the self-assembly of poly(ethylene glycol)–poly(amino acid) block copolymers, are systemic nanocarriers in targeted cancer therapy. These micelles can encapsulate therapeutic compounds, such as lipophilic substances, charged compounds, and metal complexes, that have characteristics of increased solubility, sustained release, and improved tissue distribution. However, few studies have been conducted on the lo...
Source: International Journal of Pharmaceutics - October 18, 2018 Category: Drugs & Pharmacology Source Type: research

A study of the impact of excipient shielding on initial drug release using UV imaging
The objective of this study was to explore the potential of using an ultraviolet (UV) imaging technique to examine the effect of drug-excipient ratio on the initial dissolution of the drug, when formulated with a hydrophilic, water insoluble excipient. A series of drug-excipient binary blends with different ratios were prepared and compacted into 2 mm compacts, and their dissolution profiles captured with a UV imager. Chemical imaging via Raman spectroscopy was also performed on the compacts to quantify the fraction of drug presented on the compact surface. At low drug concentrations, a suppression in drug dissolution was ...
Source: International Journal of Pharmaceutics - October 18, 2018 Category: Drugs & Pharmacology Source Type: research

Spiral mouthpiece design in a dry powder inhaler to improve aerosolization
This study presents the effect of a spiral mouthpiece design in a carrier-based dry powder inhalation on particle aerosol characteristics. Two kinds of mouthpieces, with spiral and non-spiral shaped flow channels, were fabricated by 3D-printing; particle image velocimetry and Anderson cascade impactor were performed to evaluate the drug aerosol characteristics. The obtained experimental results were in agreement with the simulation results of the computational fluid dynamics analysis. The spiral channel created a strong swirl motion of the air flow emitted from the mouthpiece exit, which produced angular momentum rather th...
Source: International Journal of Pharmaceutics - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Biocompatible antimicrobial electrospun nanofibers functionalized with ε-poly-L-lysine
Publication date: Available online 16 October 2018Source: International Journal of PharmaceuticsAuthor(s): Georgiana Amariei, Vanja Kokol, Vera Vivod, Karina Boltes, Pedro Letón, Roberto RosalAbstractThe antimicrobial polypeptide ε-poly(L-lysine) (ε-PL) was electrostatically incorporated to poly(acrylic acid) (PAA)/poly(vinyl alcohol) (PVA) electrospun nanofibers. ε-PL loading and distribution was assessed by infrared spectra, ζ-potential measurements and the primary amino reactive dye fluorescamine. Functionalized fibers with 485 ± 140 nm diameter, could be loaded with 0.57-0.74 ...
Source: International Journal of Pharmaceutics - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Apoferritin nanocages loading mertansine enable effective eradiation of cancer stem-like cells in vitro
Publication date: Available online 16 October 2018Source: International Journal of PharmaceuticsAuthor(s): Tao Tan, Yuqi Wang, Hong Wang, Haiqiang Cao, Zhiwan Wang, Jing Wang, Jie Li, Yaping Li, Zhiwen Zhang, Siling WangAbstractCancer stem-like cells (CSCs) are proposed to be responsible for tumor metastasis, resistance and relapse after therapy, but are unable to be eliminated by many current therapies. Herein, we report that the apoferritin nanocages loading cytotoxic mertansine (M-AFN) can significantly improve their uptake in CSCs-enriched tumorspheres and effectively eradicate CSCs in tumorspheres for anticancer thera...
Source: International Journal of Pharmaceutics - October 16, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation Performance and Processability Window for Manufacturing a Dual-Polymer Amorphous Solid Dispersion via Hot-Melt Extrusion and Strand Pelletization
Publication date: Available online 14 October 2018Source: International Journal of PharmaceuticsAuthor(s): T.R. Hörmann, N. Jäger, A. Funke, R.-K. Mürb, J.G. Khinast, A. PaudelAbstractThis work evaluates several compositions of an amorphous solid dispersion (ASD) comprising nimodipine (NMD) as poorly soluble model API in a dual-polymer carrier system. HPMC E5 and Eudragit E were used for the two polymeric carriers. The formulation was designed for hot-melt extrusion (HME) and subsequent strand pelletization. The aim was to identify a formulation window with desired functional ASD performance, i.e. physical s...
Source: International Journal of Pharmaceutics - October 15, 2018 Category: Drugs & Pharmacology Source Type: research

Preservation of exosomes at room temperature using lyophilization
In conclusion, lyophilization with trehalose is an effective method for the storage of exosomes for various applications.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 15, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of capsule type on aerodynamic performance of inhalation products: a case study using a formoterol-lactose binary or ternary blend
This study evaluated the impact of gelatine capsules (Quali-GTM and Hard Gelatine Capsules for DPIs), cold-gelled hypromellose (HPMC) capsules (Quali-V®-I and Vcaps®) and thermal-gelled HPMC capsules (Vcaps®Plus) from Qualicaps® and Capsugel® respectively, on the delivered dose (DD), fine particle dose (FPD), and capsule retention for formoterol-lactose binary and ternary blends. This study used a low resistance Axahaler® DPI based on the RS01 design (Plastiape, Italy). Similar trends were observed with the different capsule types that packaged both dry powder formulations. The highest DD and FPD an...
Source: International Journal of Pharmaceutics - October 14, 2018 Category: Drugs & Pharmacology Source Type: research

An experimental study of die filling of pharmaceutical powders using a rotary die filling system
Publication date: Available online 12 October 2018Source: International Journal of PharmaceuticsAuthor(s): A. Zakhvatayeva, W. Zhong, H.A. Makroo, C. Hare, C.Y. WuAbstractDie filling is a critical process step in pharmaceutical tablet manufacturing. Mass and content uniformity of the tablets as well as production throughput depend upon the die filling performance of the formulations. The efficiency of the die filling process is influenced by powder properties, such as flowability, cohesion, particle size and morphology, as well as the process conditions. It is hence important to understand the influence of powder propertie...
Source: International Journal of Pharmaceutics - October 14, 2018 Category: Drugs & Pharmacology Source Type: research

Peptide-functionalized and high drug loaded novel nanoparticles as dual–targeting drug delivery system for modulated and controlled release of paclitaxel to brain glioma
Publication date: Available online 12 October 2018Source: International Journal of PharmaceuticsAuthor(s): Primiano Pio Di MauroAbstractA dual-targeting drug delivery system for paclitaxel (PTX) was developed by functionalizing novel polyester–based nanoparticles (NPs) with peptides possessing special affinity for low-density lipoprotein receptor (LDLR), overcoming the limitations of the current chemotherapeutics, to transport drug from blood to brain, and then target glioma cells. Employing novel biodegradable block co-polymers (P and 2P), PTX loaded and peptide-functionalized nanoparticles were prepared by a modifi...
Source: International Journal of Pharmaceutics - October 14, 2018 Category: Drugs & Pharmacology Source Type: research

Interactions between UV filters and active substances in emulsion: effect on microstructure, physicochemical and in-vivo properties
The objective of the present study was to develop, characterize and evaluate the clinical efficacy of topical formulations containing or not active substances and UV-filters, separate and in combination. To this end a stable formulation was developed to which four aqueous active substances and four lipophilic UV-filters were added. The formulations were then submitted to microscopic characterization by light microscopy, to particle size measurement, and to macroscopic characterization by rheology and texture analysis. Finally, a clinical efficacy study was conducted to determine the effect of the formulations on the skin a...
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of Curcuma comosa tablets using liquisolid techniques: In vitro and in vivo evaluation
This study aimed to investigate the use of liquisolid technique to prepare tablets containing oleoresin-like crude extract of C. comosa, and to improve the dissolution profiles of its major compounds, diarylheptanoids (DAs). Free flowing powders of C comosa extract were obtained by adsorption onto solid carriers, microcrystalline cellulose, with colloidal silica as coating material. FTIR results ruled out possible interactions between C. comosa extract and excipients. The results indicated that all of liquisolid tablets met the USP requirements. The release of DAs were significantly increased through liquisolid formulation...
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Preservation of exosomes at room temperature using lyophilizationγAuthor Names
In conclusion, lyophilization with trehalose is an effective method for the storage of exosomes for various applications.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 13, 2018 Category: Drugs & Pharmacology Source Type: research

Computational Modelling and Experimental Validation of Drug Entrainment in a Dry Powder Inhaler
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Thomas Kopsch, Darragh Murnane, Digby SymonsAbstractIn a passive dry powder inhaler (DPI) a patient inhales to entrain drug powder. The goal of this study is to demonstrate experimentally that an Eulerian-Eulerian (EE CFD) computational fluid dynamics (CFD) method can accurately predict the entrainment of the dry powder formulation in DPIs. A CFD method that makes accurate predictions of the entrainment process can be applied in DPI design and optimization processes. Three different DPI entrainment geometries were tes...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Advanced formulations for Intranasal Delivery of Biologics
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Julia Rohrer, Noemi Lupo, Andreas Bernkop-SchnürchAbstractIntroductionThe global biologics market has been ever increasing over the last decades and is predicted to top Euro 350 by 2020. Facing this scenario, the parenteral route of biologics administration as hitherto standard route is inconvenient for the future. Among the alternatives, the intranasal delivery of therapeutic biologicals seems to be most promising but researchers are still facing challenges as indicated by the scarce number of successfully marke...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Analytical aspects of printed oral dosage forms
We describe the different printing techniques and give an overview of film-based oral dosage forms produced using them. The main part of the review focuses on the non-destructive analytical methods used for evaluation of qualitative aspects of printed dosage forms, e.g., solid-state properties, as well as for quantification of the active pharmaceutical ingredient (API) in the printed dosage forms, with an emphasis on spectroscopic methods. Finally, the authors share their view on the future of printed dosage forms.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

TPGS modified nanoliposomes as an effective ocular delivery system to treat glaucoma
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Quansheng Jin, Huili Li, Zhaohui Jin, Lingjing Huang, Fazhan Wang, Yang Zhou, Yongmei Liu, Chunling Jiang, James Oswald, Jinhui Wu, Xiangrong SongAbstractThe aim of this study is to investigate the potential of D-alpha-tocopheryl poly (ethylene glycol 1000) succinate (TPGS) modified nanoliposomes as an ophthalmic delivery system of brinzolamide (Brz) for glaucoma treatment. The Brz loaded nanoliposomes containing TPGS (T-LPs/Brz) were firstly developed by a thin-film dispersion method. The average particle size was 96...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of Surface Chemistry of Polymeric Nanoparticles on Cutaneous Penetration of Cholecalciferol
Publication date: Available online 11 October 2018Source: International Journal of PharmaceuticsAuthor(s): Augustine Lalloz, Marie-Alexandrine Bolzinger, Jimmy Faivre, Pierre-Luc Latreille, Araceli Garcia Ac, Cyrielle Rakotovao, Jean-Michel Rabanel, Patrice Hildgen, Xavier Banquy, Stéphanie BriançonAbstractWe investigated the influence of nanoparticle (NP) surface composition on different aspects of skin delivery of a lipophilic drug: chemical stability, release and skin penetration. Cholecalciferol was chosen as a labile model drug. Poly(lactic acid) (PLA)-based NPs without surface coating, with a non-ionic ...
Source: International Journal of Pharmaceutics - October 12, 2018 Category: Drugs & Pharmacology Source Type: research

Development and functional characterization of composite freeze dried wafers for potential delivery of low dose aspirin for elderly people with dysphagia
This study involves the development, characterization and optimization of composite wafers for potential oral and buccal delivery of low dose aspirin to prevent thrombosis in elderly patients with dysphagia. Blank (BLK) wafers (no loaded drug) were initially formulated by dissolving combinations of metolose (MET) with carrageenan (CAR) and MET with low molecular weight chitosan (CS) in different weight ratios in water, to identify optimum polymer combinations. However, drug loaded (DL) wafers were prepared using 45% v/v ethanol to help complete solubilization of the aspirin. The formulations were characterized using textur...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Azithromycin-loaded liposomes for enhanced topical treatment of methicillin-resistant Staphyloccocus aureus (MRSA) infections
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Zora Rukavina, Maja Šegvić Klarić, Jelena Filipović-Grčić, Jasmina Lovrić, Željka VanićAbstractAntibiotic delivery via liposomal encapsulation represents a promising approach for the efficient topical treatment of skin infections. The present study aimed to investigate the potential of using different types of azithromycin (AZT)-loaded liposomes to locally treat skin infections caused by methicillin-resistant Staphylococcus aureus (MRSA) strains. Conventional liposomes (CLs), deformable liposomes (DLs), ...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Chemoresponsive Smart Mesoporous Silica Systems – an Emerging Paradigm for Cancer Therapy
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Baranya Murugan, Uma Maheswari KrishnanAbstractNanotechnology-based interventions have gained popularity in the past decade for cancer therapy owing to their ability to overcome several shortcomings encountered in conventional therapy. Among the various nanoparticles that have been explored as drug carriers, mesoporous silica possesses certain desirable properties such as regulated pore size, high surface area, chemical and thermal stability, amenability for surface modification and biocompatibility. These systems hav...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

Post-insertion parameters of PEG-derivatives in phosphocholine-liposomes
Publication date: Available online 10 October 2018Source: International Journal of PharmaceuticsAuthor(s): Rosario Mare, Donatella Paolino, Christian Celia, Roberto Molinaro, Massimo Fresta, Donato CoscoAbstractThe insertion of specific derivatives into pre-formed colloidal systems has been shown to be a useful method for modifying their pharmacokinetic characteristics and biodistribution profiles.In this experimental work the effect of the post-insertion of different PEG-derivatives into pre-formed 100-nm liposomes made up of various lipid mixtures (DMPC, DPPC, DOPC, DSPC and cholesterol at different molar ratios) was inv...
Source: International Journal of Pharmaceutics - October 11, 2018 Category: Drugs & Pharmacology Source Type: research

The physiochemical, mechanical, and adhesive properties of solvent-cast Vitamin E/Soluplus® films
Publication date: Available online 9 October 2018Source: International Journal of PharmaceuticsAuthor(s): Ahmad Salawi, Sami NazzalAbstractSoluplus® is an amphiphilic graft copolymer used in hot melt extrusion applications and electrospinning. Very little information is available on the use of Soluplus® as a film former and in the development of film-based formulations. The overall aim of this work was to study the mechanical and adhesive properties of Soluplus® films prepared by the solvent casting technique. More specifically, we discovered that vitamin E can serve as a plasticizer for the Soluplus® polym...
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research

Pollen grains as a novel microcarrier for oral delivery of proteins
In conclusion, upon use of a protein-friendly solvent for Eudragit L100-55, proteins could be encapsulated in ragweed pollen without denaturing them, and the resulting formulation exhibited selective release of the proteins at intestinal pH suggesting that the ragweed pollen grain-based formulation could be promising for oral delivery of proteins.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 9, 2018 Category: Drugs & Pharmacology Source Type: research