Manufacturing and Characterization of Long-Acting Levonorgestrel Intrauterine Systems
In this study, a twin-syringe method with a customized mold was developed to manufacture hollow cylindrical polydimethylsiloxane (PDMS)-based levonorgestrel intrauterine systems (LNG-IUSs). Different mold materials, curing temperatures and times were screened to fabricate PDMS-drug reservoirs with good quality characteristics (easy demolding, good appearance and appropriate physicochemical characteristics). The prepared PDMS-drug reservoirs were covered with the release rate controlling membrane to fabricate the LNG-IUSs. Physicochemical characterization (drug content and content uniformity, powder X-Ray diffraction (PXRD)...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Vaginal Bifidobacterium breve for preventing urogenital infections: development of delayed release mucoadhesive oral tablets
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): Barbara Giordani, Luz Maria Melgoza, Carola Parolin, Claudio Foschi, Antonella Marangoni, Angela Abruzzo, Francesco Dalena, Teresa Cerchiara, Federica Bigucci, Barbara Luppi, Beatrice VitaliAbstractBifidobacteria are predominant microorganisms in the intestinal flora, but at the same time represent a subdominant group of the vaginal microbiota. For this reason, oral administration of these probiotic bacteria can provide beneficial effect for both intestinal and urogenital ecosystems.The first aim of this study was to...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Downscaling of the tableting process: feasibility of miniaturized forced feeders on a high-speed rotary tablet press
Publication date: Available online 6 September 2018Source: International Journal of PharmaceuticsAuthor(s): W. Grymonpré, B. Blahova Prudilova, V. Vanhoorne, B. Van Snick, F. Detobel, J.P. Remon, T. De Beer, C. VervaetAbstractWith the current transformation of the pharmaceutical industry towards continuous manufacturing, there is an inherent need to embrace this concept already during the early stages of drug formulation. Therefore, this research paper investigated the feasibility of using miniaturized forced feeders on a high-speed rotary tablet press with the intention of downscaling the tableting process. Forced ...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of excipients on encapsulation and release of insulin from spray-dried solid lipid microparticles
In conclusion, spray drying a solution containing both lipids and protein-phospholipid complex is a promising method for encapsulating protein into solid lipid MP, which can be used for sustained delivery of protein drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Loading studies of the anticancer drug Camptothecin into dual stimuli-sensitive nanoparticles. Stability scrutiny
Publication date: Available online 6 September 2018Source: International Journal of PharmaceuticsAuthor(s): Nieves Iglesias, Elsa Galbis, M. Jesús Díaz-Blanco, M.-Violante de-Paz, Juan A. GalbisAbstractIn recent years, the preparation of valuable drug delivery systems (DDS) from self-assembled amphiphilic copolymers has attracted much attention since these nanomaterials provide new opportunities to solve problems such as the lack of solubility in water of lipophilic drugs, improve their bioavailability, prolong their circulation time and decrease the side effects associated with their administration. In the c...
Source: International Journal of Pharmaceutics - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Novel Drug Delivery Systems for Natural Extracts: The Case Study of Vitis Vinifera Extract-SiO2 Nanocomposites
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): A. Scano, F. Ebau, M.L. Manca, V. Cabras, F. Cesare Marincola, M. Manconi, M. Pilloni, A.M. Fadda, G. EnnasAbstractBall Milling technique has been used to prepare for the first time Vitis Vinifera extract-silica nanocomposites (VV- SiO2 NCs), which combine the pharmacological effects of the extract with the effectiveness of silica as drug delivery system and active component in the treatment of wound healing. Different contents (1.0, 9.0 and 33.0 wt%) of Vitis Vinifera ethanolic extract were loaded into the silica ma...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

In Vivo Evaluation of Chitosan Based Local Delivery Systems for Atorvastatin in Treatment of Periodontitis
In this study, the effect of locally delivered atorvastatin (2% w/v) containing chitosan formulations in the treatment of periodontitis was evaluated in rats with ligature induced periodontitis. The levels of interleukin-1beta (IL-1β), IL-6, IL-8, IL-10, transforming growth factor-β1 (TGF-β1), TGF-β2 and TGF-β3 were measured after treatment with formulations. Histomorphometric analysis included the measurements of the area of alveolar bone and the distance between cemento-enamel junction (CEJ) and connective tissue attachment to tooth. Inflammatory and osteoclastic activity scores were given semiqu...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

A novel test system for the evaluation of oral mucoadhesion of fast disintegrating tablets
Publication date: Available online 5 September 2018Source: International Journal of PharmaceuticsAuthor(s): Anja Hoffmann, Rolf DanielsAbstractOromucosal drug delivery is necessary when a local effect in the oral cavity is required. Bioadhesive formulations should be advantageous because a larger fraction of the active principal is retained at the site of action allowing for an enhanced and prolonged effect. Despite a variety of mucoadhesion test systems being described in literature, none of these in-vitro tests does relate to physiological conditions in the oral cavity and suites for the testing of complete dosage forms,...
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development of a skin-friendly microemulsion for dermal allergen-specific immunotherapy
We examined epidermal penetration of Alexa Fluor-647 labelled bee-venom phospholipase A2 (Api m 1) using the Franz diffusion cell set up and confocal laser-scanning microscopy. First results of an in-vivo Api m 1-allergic mouse model indicated the protective efficacy of dermal AIT with our newly developed microemulsion.Summarily, the developed microemulsion is a suitable, stable drug delivery system for the topical administration of proteogenic allergens into the epidermis and is able to reach dendritic cells in the skin.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

High dose dry powder inhalers to overcome the challenges of tuberculosis treatment
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Mohammad A.M. Momin, Ian G. Tucker, Shyamal C. DasAbstractTuberculosis (TB) is a major global health burden. The emergence of the human immunodeficiency virus (HIV) epidemic and drug resistance has complicated global TB control. Pulmonary delivery of drugs using dry powder inhalers (DPI) is an emerging approach to treat TB. In comparison with the conventional pulmonary delivery for asthma and chronic obstructive pulmonary disease (COPD), TB requires high dose delivery to the lung. However, high dose delivery depends ...
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Multifunctional carbamazepine loaded nanostructured lipid carrier (NLC) formulation
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Mohammed Elmowafy, Khaled Shalaby, Mohamed M. Badran, Hazim M. Ali, Mohamed S. Abdel-Bakky, Hussein M. IbrahimAbstractCarbamazepine is a valuable pharmacological agent prescribed in treatment of epilepsy and trigeminal neuralgia. Poor bioavailability, successive dose adjustments and reported long term toxic effects are the main hurdles associated with carbamazepine oral administration. Bees wax containing NLC formulations were developed using high shear homogenization/sonication technique to overcome drug limitations...
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Curcumin-loaded low-energy nanoemulsions as a prototype of multifunctional vehicles for different administration routes: physicochemical and in vitro peculiarities important for dermal application
Publication date: Available online 1 September 2018Source: International Journal of PharmaceuticsAuthor(s): Ines Nikolic, Dominique Jasmin Lunter, Danijela Randjelovic, Ana Zugic, Vanja Tadic, Bojan Markovic, Nebojsa Cekic, Lada Zivkovic, Dijana Topalovic, Biljana Spremo-Potparevic, Rolf Daniels, Snezana SavicGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 2, 2018 Category: Drugs & Pharmacology Source Type: research

Characterizing Drug Product Continuous Manufacturing Residence Time Distributions of Major/Minor Excipient Step Changes using Near Infrared Spectroscopy and Process Parameters
Publication date: Available online 31 August 2018Source: International Journal of PharmaceuticsAuthor(s): Leo Manley, Zhenqi ShiAbstractThe material residence time distribution in a continuous manufacturing process can be utilized to develop, design and justify the process control strategy. This paper successfully demonstrates using both major and minor formulation component step changes to determine the system response using either Near Infrared Spectroscopy or process parameters. These options provide development flexibility to determine the system’s material residence time earlier in the development process and mo...
Source: International Journal of Pharmaceutics - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Material tracking in a continuous direct capsule-filling process via residence time distribution measurements
Publication date: Available online 30 August 2018Source: International Journal of PharmaceuticsAuthor(s): Julia Kruisz, Jakob Rehrl, Eva Faulhammer, Andreas Witschnigg, Johannes G. KhinastAbstractContinuous production of pharmaceuticals requires traceability from the raw material to the final dosage form. With that regard, understanding the residence time distribution (RTD) of the whole process and its unit operations is crucial. This work describes a structured approach to characterizing and modelling of RTDs in a continuous blender and a tamping pin capsule filling machine, including insights into data processing. The pa...
Source: International Journal of Pharmaceutics - August 31, 2018 Category: Drugs & Pharmacology Source Type: research

3D Printed Capsules for Quantitative Regional Absorption Studies in the GI Tract
Publication date: Available online 30 August 2018Source: International Journal of PharmaceuticsAuthor(s): Derrick Smith, Yash Kapoor, Andre Hermans, Rebecca Nofsinger, Filippos Kesisoglou, Tiffany Gustafson, Adam ProcopioAbstractDrug development is a long process which requires careful evaluation of the drug substance (active pharmaceutical ingredient, API), drug product (tablet, capsule etc.) and the bioperformance (both pre-clinical and clinical) before testing the efficacy of the final dosage form. The earliest assessment of a new drug substance requires an understanding of the safety and clinical performance (Phase 1) ...
Source: International Journal of Pharmaceutics - August 31, 2018 Category: Drugs & Pharmacology Source Type: research

Residence time and uptake of porous and cationic maltodextrin-based nanoparticles in the nasal mucosa: comparison with anionic and cationic nanoparticles
Publication date: Available online 29 August 2018Source: International Journal of PharmaceuticsAuthor(s): Minh Quan Le, Rodolphe Carpentier, Isabelle Lantier, Céline Ducournau, Isabelle Dimier-Poisson, Didier BetbederAbstractDifferent types of biodegradable nanoparticles (NP) have been studied as nasal mucosa cell delivery systems. These nanoparticles need to strongly interact with mucosa cells to deliver their payload. However, only a few simultaneous comparisons have been made and it is therefore difficult to determine the best candidate. Here we compared 5 types of nanoparticles with different surface charge (ani...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

Protein aggregation – Mechanisms, detection, and control
Publication date: 25 October 2018Source: International Journal of Pharmaceutics, Volume 550, Issues 1–2Author(s): Wei Wang, Christopher J. RobertsAbstractProtein aggregation has been recognized as one of the major challenges in the development and commercialization of successful protein-based drug products because of the inherent and high aggregation tendency during various manufacturing processes, storage, and administration. Protein aggregates may impact significantly the product quality, safety and/or efficacy. This review is intended to summarize four major aspects of protein aggregation – (1) aggregation m...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

The effect of administration media on palatability and ease of swallowing of multiparticulate formulations
Publication date: Available online 28 August 2018Source: International Journal of PharmaceuticsAuthor(s): Felipe L. Lopez, Terry B. Ernest, Mine Orlu, Catherine TuleuAbstractMultiparticulate formulations based on pellets, granules or beads, could be advantageous for paediatrics, geriatrics and patients with swallowing difficulties. However, these formulations may require suitable administration media to facilitate administration. The aim of this work was to investigate the effect of administration media properties on palatability and ease of swallowing of multiparticulates. A range of vehicles were developed using xanthan ...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

The combination of Nanomicelles with Terpenes for Enhancement of Skin Drug Delivery
Publication date: Available online 29 August 2018Source: International Journal of PharmaceuticsAuthor(s): Emine Kahraman, Neşet Neşetoğlu, Sevgi Güngör, Duri Şehvar Ünal, Yıldız ÖzsoyAbstractThe nanomicelles have recently drawn a great deal of attention for drug delivery into the skin. However, these carriers have only deposited in hair follicles and furrows, and drug in the micelles may not therapeutically reach into viable skin layers. The aim of this study was to formulate a combination of nanomicelles with terpenes to overcome this challenge and evaluate their potential for topical drug delive...
Source: International Journal of Pharmaceutics - August 30, 2018 Category: Drugs & Pharmacology Source Type: research

Dendrimer as a new potential carrier for topical delivery of siRNA: a comparative study of dendriplex vs. lipoplex for delivery of TNF-α siRNA
Publication date: Available online 27 August 2018Source: International Journal of PharmaceuticsAuthor(s): Palpandi Pandi, Anjali Jain, Nagavendra Kommineni, Maksim Ionov, Maria Bryszewska, Wahid KhanAbstractTopical delivery of siRNA is challenging task due to complex barrier property of stratum corneum and cationic lipid based carriers have been widely explored for this purpose due to improved permeation through skin. For gene delivery application, dendrimers are considered as efficient carrier due to their cationic nature and well-defined surface groups. However, they are not well explored for topical delivery. This work ...
Source: International Journal of Pharmaceutics - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Diffusion through the ex vivo vitreal body – Bovine, porcine, and ovine models are poor surrogates for the human vitreous
In this study, the mechanical, physical and rheological properties of ovine, porcine, and bovine surrogates were investigated and compared to human vitreous. In addition, a bespoke Franz cell construct was used to compare the diffusion of a model drug (fluorescein) through vitreous samples. Despite the similarity in rheological properties between bovine, porcine and human vitreous samples, diffusion of fluorescein through the different vitreous samples revealed great differences in values of steady-state flux and diffusion coefficient. In addition, a first-generation vitreous mimic, composed of 4.5 mg/mL hyaluronic acid ...
Source: International Journal of Pharmaceutics - August 28, 2018 Category: Drugs & Pharmacology Source Type: research

Application of Box-Behnken experimental design for the formulation and optimisation of selenomethionine-loaded chitosan nanoparticles coated with zein for oral delivery
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Giuliana Vozza, Minna Danish, Hugh J. Byrne, Jesús M. Frías, Sinéad M. RyanAbstractSelenomethionine is an essential amino acid with a narrow therapeutic index and susceptibility to oxidation. Here it was encapsulated into a nanoparticle composed of chitosan cross-linked with tripolyphosphate for oral delivery. The formulation was optimised using a three-factor Box-Behnken experimental design. The chitosan:tripolyphosphate ratio, chitosan solvent pH, and drug load concentration were independently va...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Micro/nanostructured inhalable formulation based on polysaccharides: Effect of a thermoprotectant on powder properties and protein integrity
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Sonia Al-Qadi, Pablo Taboada, Carmen Remuñán-LópezAbstractCombined micro- and nanosystems are appealing for pulmonary protein delivery, fulfilling the specific physiological requirements for efficient outcomes in-vivo. However, fabrication of protein formulations may impose stresses perturbing protein conformational stability and, hence, biological activity. Herein, a protein, insulin (INS), was nanoencapsulated inside chitosan nanoparticles (CS NPs) by ionic gelation. By spray drying, the resultan...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of ring size and drug loading on the pharmacokinetics of a combination dapivirine-darunavir vaginal ring in cynomolgus macaques
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Diarmaid J. Murphy, Delphine Desjardins, Peter Boyd, Nathalie Dereuddre- Bosquet, Lev Stimmer, Anna Caldwell, Roger Le Grand, Charles Kelly, Jens van Roey, R. Karl MalcolmAbstractThis work investigates the impact of vaginal ring size and drug loading on the in vitro release, safety, ease of fit, and pharmacokinetics in cynomolgus macaques of matrix-type silicone elastomer vaginal rings containing a combination of the non-nucleoside reverse transcriptase inhibitor dapivirine and the protease inhibitor darunavir. Drug-fr...
Source: International Journal of Pharmaceutics - August 26, 2018 Category: Drugs & Pharmacology Source Type: research

Targeted Efflux Transporter Inhibitors – A Solution to Improve Poor Cellular Accumulation of Anti-Cancer Agents
In this study, we prepared 5 LAT1-utilizing prodrugs of an efflux pump inhibitor, probenecid (PRB). All novel compounds were transported into human breast cancer cells (MCF-7) mainly via LAT1. The compounds also interacted with either multiresistant proteins (MRPs), P-glycoprotein (P-gp) or breast cancer resistant protein (BCRP) and increased significantly (3-4 -fold) the cellular accumulation of anti-cancer agent vinblastine (VBL). Consequently, this improved the anti-proliferative efficacy of VBL by decreasing the cell growth after 72 h from 100% (VBL treatment alone) to 48-75% (combination treatment). However, the same ...
Source: International Journal of Pharmaceutics - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Acrylic microparticles increase daptomycin intracellular and in vivo anti-biofilm activity against Staphylococcus aureus
Publication date: Available online 25 August 2018Source: International Journal of PharmaceuticsAuthor(s): Anne-Kathrin Woischnig, Lidia M. Gonçalves, Maxime Ferreira, Richard Kuehl, Judith Kikhney, Annette Moter, Isabel A.C. Ribeiro, António J. Almeida, Nina Khanna, Ana Francisca BettencourtGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Freeze-drying of Monoclonal Antibody-Conjugated Gold Nanorods: Colloidal Stability and Biological Activity
Publication date: Available online 23 August 2018Source: International Journal of PharmaceuticsAuthor(s): Majd A. Hamaly, Samer R. Abulateefeh, Khaled M. Al-Qaoud, Alaaldin M. AlkilanyAbstractMaintaining colloidal stability of nanoparticles in suspensions is a major challenge. Therefore, freeze-drying (lyophilization) is recently proposed to preserve colloidal stability of nanoparticles through maintaining them in a solid state. However, freeze-drying would itself induce nanoparticle aggregation unless proper formulation with a careful selection of cryoprotectants is considered. Herein, we evaluate the colloidal stability ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

Protein Aggregation - Mechanisms, Detection, and Control
Publication date: Available online 23 August 2018Source: International Journal of PharmaceuticsAuthor(s): Wei Wang, Christopher J. RobertsAbstractProtein aggregation has been recognized as one of the major challenges in the development and commercialization of successful protein-based drug products because of the inherent and high aggregation tendency during various manufacturing processes, storage, and administration. Protein aggregates may impact significantly the product quality, safety and/or efficacy. This review is intended to summarize four major aspects of protein aggregation – (1) aggregation mechanisms,(2) ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

Self-emulsifying drug delivery systems changing their zeta potential via a flip-flop mechanism
Publication date: Available online 24 August 2018Source: International Journal of PharmaceuticsAuthor(s): Esmaeil Salimi, Bao Le-Vinh, Forouhe Zahir-Jouzdani, Barbara Matuszczak, Azadeh Ghaee, Andreas Bernkop-SchnürchAbstractTo overcome the mucus layer and cell membrane barrier, self-emulsifying drug delivery systems (SEDDS) exhibiting negative zeta potential, switching to positive values when having reached the cell membrane is a promising approach. Accordingly, a novel conjugate was synthesized by covalent attachment of phosphotyrosine to octadecylamine, which was incorporated into SEDDS. Generated system presented ...
Source: International Journal of Pharmaceutics - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

A comparative assessment of continuous production techniques to generate sub-micron size PLGA particles
Publication date: Available online 23 August 2018Source: International Journal of PharmaceuticsAuthor(s): Maria Camilla Operti, David Fecher, Eric A.W. van Dinther, Silko Grimm, Rima Jaber, Carl G. Figdor, Oya TagitAbstractThe clinical and commercial development of polymeric sub-micron size formulations based on poly(lactic-co-glycolic acid) (PLGA) particles is hampered by the challenges related to their good manufacturing practice (GMP)-compliant, scale-up production without affecting the formulation specifications. Continuous process technologies enable large-scale production without changing the process or formulation p...
Source: International Journal of Pharmaceutics - August 23, 2018 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 22 August 2018Source: 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 - August 23, 2018 Category: Drugs & Pharmacology Source Type: research

Dual Mechanism of Microenvironmental pH Modulation and Foam Melt Extrusion to Enhance Performance of HPMCAS Based Amorphous Solid Dispersion
Publication date: Available online 21 August 2018Source: International Journal of PharmaceuticsAuthor(s): Anh Q. Vo, Xin Feng, Jiaxiang Zhang, Feng Zhang, Michael A. RepkaAbstractHydroxypropyl methylcellulose acetate succinate (HPMCAS) is an excellent polymeric carrier for melt extrusion amorphous solid dispersion. However, its pH-dependent solubility limits its application, especially for narrow absorption window drugs. The current study proposed a novel dual approach of foam extrusion and microenvironmental pH modulation to overcome this limitation. Sodium bicarbonate was used as a blowing agent and the remaining sodium ...
Source: International Journal of Pharmaceutics - August 21, 2018 Category: Drugs & Pharmacology Source Type: research

Diffusion through the ex vivo vitreal body - bovine, porcine, and ovine models are poor surrogates for the human vitreous
In this study, the mechanical, physical and rheological properties of ovine, porcine, and bovine surrogates were investigated and compared to human vitreous. In addition, a bespoke Franz cell construct was used to compare the diffusion of a model drug (i.e. fluorescein) through vitreous samples. Despite the similarity in rheological properties between bovine, porcine and human vitreous samples (p> 0.05), diffusion of fluorescein through the different vitreous samples revealed great differences in values of steady-state flux and diffusion coefficient. In addition, a first-generation vitreous mimic, composed of 4.5 mg/mL ...
Source: International Journal of Pharmaceutics - August 21, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of exosome-mimicking liposomes with conventional liposomes for intracellular delivery of siRNA
This study may encourage further pursuit of more exosome-mimicking delivery vehicles with higher efficiency and biocompatibility.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 21, 2018 Category: Drugs & Pharmacology Source Type: research

Carrier-free Janus Nano-prodrug Based on Camptothecin and Gemcitabine: Reduction-triggered Drug Release and Synergistic in Vitro Antiproliferative Effect in Multiple Cancer Cells
Publication date: Available online 20 August 2018Source: International Journal of PharmaceuticsAuthor(s): Yanyun Xu, Yushu Huang, Xiongwen Zhang, Wei Lu, Jiahui Yu, Shiyuan LiuAbstractA carrier-free and reduction-degradable Janus prodrug, termed as CPT-SS-GEM, was fabricated by redox-sensitive disulfide bond linked gemcitabine and camptothecin. This amphiphilic prodrug showed high drug loading capacity, 42.6% of CPT and 32.2% of GEM, respectively. Benefiting from its amphiphilic property, CPT-SS-GEM prodrug could self-assemble into Janus nano-prodrug in water without aid of any excipient. The morphology of the nano-prodrug...
Source: International Journal of Pharmaceutics - August 21, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics
In conclusion, the developed non-effervescent floating tablets are promising candidates for once-daily delivery of pregabalin.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 21, 2018 Category: Drugs & Pharmacology Source Type: research

Valproate sensitizes human glioblastoma cells to 3-bromopyruvate-induced cytotoxicity
In conclusion, we suggested that valproate enhanced 3-BrPA-induced cell death. This might be attributable to the increase in cellular ATP consumption owing to valproate-induced MRP2 or BCRP expression.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 20, 2018 Category: Drugs & Pharmacology Source Type: research

Poly (L-glutamic acid)-g-methoxy poly (ethylene glycol)-gemcitabine conjugate improves the anticancer efficacy of gemcitabine
Publication date: Available online 20 August 2018Source: International Journal of PharmaceuticsAuthor(s): Chenguang Yang, Wantong Song, Dawei Zhang, Haiyang Yu, Lei Yin, Na Shen, Mingxiao Deng, Zhaohui Tang, Jingkai Gu, Xuesi ChenAbstractGemcitabine is widely used for anticancer therapy. However, its short blood circulation time and poor stability greatly impair its application. To solve this problem, we prepared a poly (L-glutamic acid)-g-methoxy poly (ethylene glycol)-gemcitabine conjugate (L-Gem) with a 14.3 wt% drug-loading content. L-Gem showed concentration- and time-dependent cytotoxicity towards 4T1, LLC, MIA PaCa-...
Source: International Journal of Pharmaceutics - August 20, 2018 Category: Drugs & Pharmacology Source Type: research

Spray dried cubosomes with ovalbumin and Quil-A as a nanoparticulate dry powder vaccine formulation
Publication date: Available online 19 August 2018Source: International Journal of PharmaceuticsAuthor(s): Christoffer von Halling Laier, Blake Gibson, Marco van de Weert, Ben J. Boyd, Thomas Rades, Anja Boisen, Sarah Hook, Line Hagner NielsenAbstractSubunit vaccine formulations are often produced as liquid dispersions through complicated processes. It is desirable, however, to have simple, cheap and up-scalable methods to produce nanoparticulate subunit vaccines in powder form. Here, a simple single-step spray drying process for production of powder cubosome precursors with the model antigen ovalbumin (OVA) and the adjuvan...
Source: International Journal of Pharmaceutics - August 19, 2018 Category: Drugs & Pharmacology Source Type: research

Preclinical evaluation of thermosensitive poly(N-(2-hydroxypropyl) methacrylamide mono/dilactate)-grafted liposomes for cancer thermochemotherapy
In conclusion, thermosensitive chol-pHPMAlac-grafted liposomes rapidly release DOX during mild hyperthermia. The liposomes are stable in a physiological milieu, are not taken up by cells that are encountered in an in vivo setting, and are non-antagonistic towards platelets. Chol-pHPMAlac-grafted liposomes are therefore good candidates for DOX delivery to tumors and temperature-triggered release in tumor stroma.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 19, 2018 Category: Drugs & Pharmacology Source Type: research

Development of a new formulation of roflumilast for pulmonary drug delivery to treat inflammatory lung conditions
Publication date: Available online 18 August 2018Source: International Journal of PharmaceuticsAuthor(s): Érika Yoko Suzuki, Maria Inês Amaro, Gabriella Silva de Almeida, Lucio Mendes Cabral, Anne Marie Healy, Valeria Pereira de SousaAbstractThe aim of this study was to develop roflumilast dry powder inhaler (DPI) formulations by spray drying using hydroxypropyl-β-cyclodextrin (HPβCD) and to determine their suitability for pulmonary delivery. Different feed solution concentrations, solvent systems and spray drying parameters were used to obtain the formulations which were characterized using X-ray po...
Source: International Journal of Pharmaceutics - August 19, 2018 Category: Drugs & Pharmacology Source Type: research

Methacrylated chitosan as a polymer with enhanced mucoadhesive properties for transmucosal drug delivery
Publication date: Available online 18 August 2018Source: International Journal of PharmaceuticsAuthor(s): Oluwadamilola M. Kolawole, Wing Man Lau, Vitaliy V. KhutoryanskiyAbstractChitosan is a cationic polysaccharide that exhibits mucoadhesive properties which allow it to adhere to mucosal tissues. In this work, we explored chemical modification of chitosan through its reaction with methacrylic anhydride to synthesise methacrylated derivative with the aim to improve its mucoadhesive properties. The reaction products were characterised using 1H NMR, FTIR and UV-Vis spectroscopy. 1H NMR and ninhydrin test were used to quanti...
Source: International Journal of Pharmaceutics - August 19, 2018 Category: Drugs & Pharmacology Source Type: research

Towards a better understanding of solid dispersions in aqueous environment by a fluorescence quenching approach
Publication date: Available online 18 August 2018Source: International Journal of PharmaceuticsAuthor(s): Simone Aleandri, Sandra Jankovic, Martin KuentzAbstractSolid dispersions (SDs) represent an important formulation technique to achieve supersaturation in gastro-intestinal fluids and to enhance absorption of poorly water-soluble drugs. Extensive research was leading to a rather good understanding of SDs in the dry state, whereas the complex interactions in aqueous medium are still challenging to analyze. This paper introduces a fluorescence quenching approach together with size-exclusion chromatography to study drug an...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation and evaluation of 4-benzylpiperidine drug-in-adhesive matrix type transdermal patch
The objective of our study was to develop a transdermal patch of 4-benzylpiperidine and to evaluate its in vitro transdermal permeation profile. Appropriate pressure sensitive adhesives and additives were selected based on solubility and slide crystallization studies. Release liners and backing membranes were selected based on their ability to peel without leaving a residue and their affinity to formulation respectively. Drug-in-adhesive patches developed were investigate for their in vitro drug permeation over 48 hours across dermatomed human skin using Franz diffusion cells. Silicone based pressure sensitive adhesive alo...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Buccal adhesive films with moisturizer- the next level for dry mouth syndrome?
This study was undertaken to prepare films by solvent evaporation method comprising well-known polymers in order to investigate their potential for buccal suitability. Mucoadhesive films were manufactured using different polymers such as ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose as well as carboxymethyl cellulose. Buccal films were evaluated in regards of mucoadhesiveness, swelling and physico-chemical properties. Furthermore rheological measurement and adhesion study were carried out on the buccal porcine mucosa. Moreover, allantoin as humectant was incorporated and trans-mucosal water loss wa...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Bile salt enhancers for inhalation: correlation between in vitro and in vivo lung effects
Publication date: Available online 17 August 2018Source: International Journal of PharmaceuticsAuthor(s): Jorid B. Sørli, Kinga Balogh Sivars, Emilie Da Silva, Karin S. Hougaard, Ismo K. Koponen, Yi Y. Zuo, Ingrid E.K. Weydahl, Per M. Åberg, Rebecca FranssonAbstractThe lungs have potential as a means of systemic drug delivery of macromolecules. Systemic delivery requires crossing of the air-blood barrier, however with molecular size-dependent limitations in lung absorption of large molecules. Systemic availability after inhalation can be improved by absorption enhancers, such as bile salts. Enhancers may poten...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Analytical Considerations for Measuring the Globule Size Distribution of Cyclosporine Ophthalmic Emulsions
Publication date: Available online 17 August 2018Source: International Journal of PharmaceuticsAuthor(s): Peter Petrochenko, Naresh Pavurala, Yong Wu, Sook Yee Wong, Hamideh Parhiz, Kang Chen, Sharadrao M. Patil, Haiou Qu, Patrick Buoniconti, Absar Muhammad, Stephanie Choi, Darby Kozak, Muhammad Ashraf, Celia N. Cruz, Jiwen Zheng, Xiaoming XuAbstractMeasurement of particle size and size distribution of complex drug products exhibiting complex rheological behaviors can be challenging as these properties may be beyond the theoretical assumptions of the measurement technique. Herein cyclosporine (CsA) ophthalmic emulsion was ...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced oral bioavailability and anti-gout activity of [6]-shogaol-loaded solid lipid nanoparticles
In this study, a significant quantity of high-purity [6]-shogaol (yield: 3.6%; purity: 98.65%) was extracted and encapsulated in solid lipid nanoparticles (SLNs) via high-pressure homogenization (encapsulation efficiency: 87.67%) to improve its solubility and oral bioavailability. The resulting [6]-shogaol-loaded solid lipid nanoparticles (SSLNs) were stable, homogeneous and well-dispersed. Its mean particle size and zeta potential were 73.56 ± 5.62 nm and −15.2 ± 1.3 mV, respectively. Importantly, the in vitro release profile and in vivo oral bioavailability of SSLNs were significantly improved compare...
Source: International Journal of Pharmaceutics - August 18, 2018 Category: Drugs & Pharmacology Source Type: research

Nanotechnologies for site specific drug delivery: changing the narrative
The objective is to discuss some trends which have led to over-confident extrapolations of experimental work in animals to treatment. It is argued that a greater appreciation of the physics, biology and pharmaceutics involved could clarify the sense of any work done and the manner in which this is conveyed in publications. The essential content to be addressed in submitted papers is outlined. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 17, 2018 Category: Drugs & Pharmacology Source Type: research