Expandable drug delivery system for gastric retention based on shape memory polymers: Development via 4D printing and extrusion
Publication date: Available online 14 September 2019Source: International Journal of PharmaceuticsAuthor(s): Alice Melocchi, Marco Uboldi, Nicoletta Inverardi, Francesco Briatico-Vangosa, Francesco Baldi, Stefano Pandini, Giulia Scalet, Ferdinando Auricchio, Matteo Cerea, Anastasia Foppoli, Alessandra Maroni, Lucia Zema, Andrea GazzanigaAbstractSeveral diseases would benefit from prolonged drug release provided by systems retained in the stomach for extended time periods. Expandable gastroretentive devices are administered in a collapsed configuration enabling swallowing and regain in situ their native shape having larger ...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

One-pot synthesis and characterization of ovalbumin-conjugated gold nanoparticles: A comparative study of adjuvanticity against the physical mixture of ovalbumin and gold nanoparticles
In this study, we report the one-pot synthesis of antigen ovalbumin (OVA)-conjugated gold nanoparticles (OVA@GNPs). A systematical study was performed by comparing OVA@GNPs with the simple mixture of OVA and gold nanoparticles (OVA+GNPs), including their physiochemical properties through spectrometric and electrophoretic analysis, in vitro stability, cytotoxicity and cellular uptake, and in vivo humoral immune responses following subcutaneous and transcutaneous immunization in mice. The results demonstrate a much stronger interaction between protein and GNPs in OVA@GNPs than OVA+GNPs, which makes OVA@GNPs more stable under...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Nanoparticles from Gantrez® AN-poly(ethylene glycol) conjugates as carriers for oral delivery of docetaxel
Publication date: Available online 16 September 2019Source: International Journal of PharmaceuticsAuthor(s): Luisa Ruiz-Gatón, Socorro Espuelas, Judit Huarte, Eneko Larrañeta, Nekane Martin-Arbella, Juan M. IracheAbstractThe oral delivery of docetaxel (DTX) is challenging due to a low bioavailability, related to an important pre-systemic metabolism. With the aim of improving the bioavailability of this cytotoxic agent, nanoparticles from conjugates based on the copolymer of methyl vinyl ether and maleic anhydride (poly(anhydride)) and two different types of PEG, PEG2000 (PEG2) or methoxyPEG2000 (mPEG2), were ...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

aQbD as a platform for IVRT method development–A regulatory oriented approach
Publication date: Available online 16 September 2019Source: International Journal of PharmaceuticsAuthor(s): Margarida Miranda, Alberto A.C.C. Pais, Catarina Cardoso, Carla VitorinoAbstractThe EMA draft guideline on quality and equivalence of topical products and the FDA non-binding product specific guidances release has encouraged the establishment of a regulatory background for in vitro release testing (IVRT). Herein, a novel framework applicable to the development of a discriminatory IVRT method is described, according to analytical quality by design (aQbD) principles. A commercially available diclofenac emulgel formula...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Development, characterization and pharmacokinetics of mupirocin-loaded nanostructured lipid carriers (NLCs) for intravascular administration
The objective of this research is to develop and characterize Mupirocin-Loaded Nanostructured Lipid Carriers (M-NLC) for intravascular administration. The MNLC was produced by a combination of high- shear homogenization and high-pressure homogenization of solid (cetyl palmitate) and liquid (caprylic/caprylic acid) biocompatible lipids in 5 different ratios. The mean particle size, polydispersity index (PDI) and the zeta potential (ZP) of the MNLC formulations were between 99.8 and 235 nm, PDI lower than 0.164, ZP from −25.96 to −19.53 and pH ranging from 6.28–6.49. The MNLC formulation also enhances the...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Long lasting in-situ forming implant loaded with raloxifene HCl: An injectable delivery system for treatment of bone injuries
This study aimed to prepare novel liquid lipid-based PLGA-IFI loaded with raloxifene hydrochloride for prolonged non-surgical treatment of bone injuries by applying solvent-induced phase inversion technique. Labrasol® and Maisine® were added to the selected IFI forming long lasting lipid-based IFI (LLL-IFI). The formulations were characterized by analysing their in-vitro drug release, solidification time, injectability, rheological properties, and DSC in addition to their morphological properties. Results revealed that the LLL-IFI composed of 10%w/v PLGA with a lactide to glycolide ratio of 75:25 with ester termina...
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Phospholipid-based complex of raloxifene with enhanced biopharmaceutical potential: Synthesis, characterization and preclinical assessment
Publication date: Available online 17 September 2019Source: International Journal of PharmaceuticsAuthor(s): Atul Jain, Sumant Saini, Rajendra Kumar, Teenu Sharma, Rajan Swami, Om Prakash Katare, Bhupinder SinghGraphical Abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 20, 2019 Category: Drugs & Pharmacology Source Type: research

Thermosensitive glycol chitosan-based hydrogel as a topical ocular drug delivery system for enhanced ocular bioavailability
Publication date: 30 October 2019Source: International Journal of Pharmaceutics, Volume 570Author(s): Hui Shi, Yuan Wang, Zhishu Bao, Deqing Lin, Hui Liu, Ailing Yu, Lei Lei, Xingyi Li, Xu XuAbstractIn the present study, we developed and evaluated an in situ gelling system based on hexanoyl glycol chitosan (H-GCS) for enhanced ocular bioavailability. An aqueous solution of H-GCS exhibited a typical sol-gel transition at 32 °C. The formed H-GCS hydrogel was characterized by rheology and scanning electron microscopy (SEM). H-GCS had minimal in vitro cytotoxicity against L-929 and HCEC cells over a concentration range o...
Source: International Journal of Pharmaceutics - September 19, 2019 Category: Drugs & Pharmacology Source Type: research

Bedaquiline containing triple combination powder for inhalation to treat drug-resistant tuberculosis
Publication date: 30 October 2019Source: International Journal of Pharmaceutics, Volume 570Author(s): Bhamini Rangnekar, Mohammad A.M. Momin, Basanth Babu Eedara, Shubhra Sinha, Shyamal C. DasAbstractDrug-resistant tuberculosis (DR-TB) is an emerging health problem, challenging the effective control of global TB. Current treatment of DR-TB includes administration of multiple anti-TB drugs via oral and parenteral routes for a duration of 20–28 months. High systemic exposure, side effects and lengthy treatment time are problems affecting current treatment. The success rate of current lengthy treatment regimens is gen...
Source: International Journal of Pharmaceutics - September 19, 2019 Category: Drugs & Pharmacology Source Type: research

Vaginal tamoxifen for treatment of vulvar and vaginal atrophy: Pharmacokinetics and local tolerance in a rabbit model over 28 days
Publication date: Available online 10 September 2019Source: International Journal of PharmaceuticsAuthor(s): Janet Chollet, Fred Mermelstein, Stephen C. Rocamboli, David R. FriendAbstractVaginally delivered tamoxifen is being developed as alternative to estrogen-based therapies for the treatment of vulvar and vaginal atrophy (VVA) symptoms in subjects at high risk for breast cancer, undergoing treatment for breast cancer with aromatase inhibitors or are breast cancer survivors. Tamoxifen (1 or 20 mg) was administered intra-vaginally to female rabbits once-daily over a 28-day period to assess its pharmacokinetics, systemic ...
Source: International Journal of Pharmaceutics - September 11, 2019 Category: Drugs & Pharmacology Source Type: research

A Bioavailability Study on Microbeads and NanoLiposomes fabricated by Dense Carbon Dioxide Technologies using human-Primary Monocytes and Flow Cytometry Assay
Publication date: Available online 9 September 2019Source: International Journal of PharmaceuticsAuthor(s): E. Ciaglia, F. Montella, P. Trucillo, M.C. Ciardulli, P. Di Pietro, G. Amodio, P. Remondelli, C. Vecchione, E. Reverchon, N. Maffulli, A.A. Puca, G. Della PortaAbstractSupercritical Emulsion Extraction (SEE) and Supercritical assisted Liposome formation (SuperLip), use dense gases such as carbon dioxide (dCO2) to fabricate advanced micro/nanocarriers.SEE uses dCO2 to extract solvent from the oily phase of an emulsion and obtain biopolymer microbead; For this study, poly-Lactic Acid (PLA) microbeads of 1±0.2 &m...
Source: International Journal of Pharmaceutics - September 9, 2019 Category: Drugs & Pharmacology Source Type: research

Cationic starch derivatives as mucoadhesive and soluble excipients in drug delivery
Publication date: Available online 9 September 2019Source: International Journal of PharmaceuticsAuthor(s): Max Jelkmann, Christina Leichner, Claudia Menzel, Verena Kreb, Andreas Bernkop-SchnürchAbstractThe aim of this study was to develop a novel mucoadhesive cationic polymer by introducing primary amino groups to the polymeric backbone of starch. This newly synthesized polymer should exhibit superior properties over chitosan regarding solubility, mucoadhesiveness and cytotoxicity.Increasing amounts of sodium periodate were used to cleave and oxidize vicinal diols under aldehyde formation obtaining three different de...
Source: International Journal of Pharmaceutics - September 9, 2019 Category: Drugs & Pharmacology Source Type: research

Fundamental evaluation and optimization of porous spherical silica for developing functional fine particles via fluidized bed coating
This study evaluated the physical properties and drug release capability of microbead silicate with different pore sizes. Although microbead silicate with small pores displayed a rapid drug release profile, drug release was incomplete. Contrastingly, microbead silicate with large pores achieved complete drug release even with high drug loading. Furthermore, in the case of 100% layering, the porosity of microbead silicate was maintained, thus sufficiently preventing aggregation due to the prevention of formation of liquid bridging of the coating solution. These results suggest that using microbead silicate with large pores ...
Source: International Journal of Pharmaceutics - September 9, 2019 Category: Drugs & Pharmacology Source Type: research

Binary and ternary solid dispersions of an anticancer preclinical lead, IIIM-290: In vitro and in vivo studies
The objective of this study was to formulate an anticancer preclinical lead, IIIM-290, loaded in solid dispersions to enhance its solubility, dissolution, and oral pharmacokinetics. IIIM-290 is an in-house preclinical anticancer lead prepared by semisynthetic modification of the natural product rohitukine. It is an orally bioavailable Cdk inhibitor showing efficacy in xenograft models of pancreatic, colon and leukemia cancer. It demonstrated in vivo efficacy at a relatively higher dose owing to its poor aqueous solubility (∼8.6 µg/mL). Binary and ternary solid dispersions containing PVP K-30, xanthan gum, and PEG...
Source: International Journal of Pharmaceutics - September 9, 2019 Category: Drugs & Pharmacology Source Type: research

Concentration of a Microemulsion Influences the Mechanical Properties of Ibuprofen In Situ Microgels
Publication date: Available online 7 September 2019Source: International Journal of PharmaceuticsAuthor(s): Rania Hamed, Yasmeen Al-Adhami, Rana Abu-HuwaijAbstractThe aim of this study was to develop an ibuprofen microemulsion (IBU–ME) incorporated into in situ gels (microgels) for local delivery into periodontal pockets. The IBU–ME was prepared at a concentration of 1% w/v IBU. Various concentrations of the thermosensitive Pluronic® F127 (P127) solution and a series of combinations of the P127 solution and IBU–ME at a 1:1 ratio were initially developed and tested to determine their sol–gel tran...
Source: International Journal of Pharmaceutics - September 8, 2019 Category: Drugs & Pharmacology Source Type: research

Optimization, thermodynamic characteristics and solubility predictions of natural deep eutectic solvents used for sulfonamide dissolution
Publication date: Available online 7 September 2019Source: International Journal of PharmaceuticsAuthor(s): Piotr Cysewski, Tomasz JelińskiAbstractThe limited water solubility of sulfonamides provokes a search for new solvents offering not only increased solubility but also environmental and health safety. Therefore, six sulfonamides were studied in a series of natural deep eutectic solvents (NADES) comprising choline chloride with multi-hydroxyl compounds. Experimental screening aimed at finding the optimized NADES composition revealed that unimolar proportion of choline chloride and glycerol offers the highest solubilit...
Source: International Journal of Pharmaceutics - September 8, 2019 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 8, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of conventionally and naturally coloured coatings marked by laser technology for unique 2D coding of pharmaceuticals
Publication date: Available online 6 September 2019Source: International Journal of PharmaceuticsAuthor(s): Krisztina Ludasi, Orsolya Jójárt-Laczkovich, Tamás Sovány, Béla Hopp, Tomi Smausz, Géza RegdonAbstractSubstandard and/or falsified medicines are a growing global threat for health and they cause serious social and economic damage. In low- and middle-income countries the failure rate of these medical products is approximately 10.5%. 50% of medicines purchased over the Internet may be fake.According to Directive 2011/62/EU as regards the prevention of falsified medicines from e...
Source: International Journal of Pharmaceutics - September 8, 2019 Category: Drugs & Pharmacology Source Type: research

Anti-counterfeiting DNA molecular tagging of pharmaceutical excipients: An evaluation of lactose containing tablets
Publication date: Available online 6 September 2019Source: International Journal of PharmaceuticsAuthor(s): Mohamad Jamal Altamimi, Joanna C. Greenwood, Kim Wolff, Michael E. Hogan, Ahuti Lakhani, Gary P. Martin, Paul G. RoyallAbstractThe licensed pharmaceutical industry and regulators use many approaches to control counterfeiting, but it remains a very difficult task to differentiate between counterfeit and real products. Moreover, there is a lack of techniques available for providing a batch specific molecular bar code for tablets that has the required traceability, specificity and sensitivity to be fit for purpose. The ...
Source: International Journal of Pharmaceutics - September 8, 2019 Category: Drugs & Pharmacology Source Type: research

Enhanced intracellular and intranuclear drug delivery mediated by biomimetic peptide SVS-1 for anticancer therapy
Publication date: Available online 5 September 2019Source: International Journal of PharmaceuticsAuthor(s): Yucheng Xiang, Liqiang Chen, Rui Zhou, Yuan HuangAbstractTumor cell nucleus is the ultimate target of many first-line chemotherapeutics and therapeutic genes. However, nuclear drug delivery is always hampered by multiple intracellular obstacles especially low efficiency of cellular uptake and insufficient nuclear trafficking. It is urgent to establish novel nuclear drug delivery systems to simultaneously overcome barriers including cell membranes and nuclear envelope. Herein, an N-(2-hydroxypropyl) methacrylamide (HP...
Source: International Journal of Pharmaceutics - September 6, 2019 Category: Drugs & Pharmacology Source Type: research

Hypericin inclusion complexes encapsulated in liposomes for antimicrobial photodynamic therapy
Publication date: Available online 5 September 2019Source: International Journal of PharmaceuticsAuthor(s): Nikola Plenagl, Benjamin Sebastian Seitz, Lili Duse, Shashank Reddy Pinapireddy, Jarmila Jedelska, Jana Brüßler, Udo BakowskyAbstractThe naturally occurring anthraquinone derivative hypericin is a highly potent photosensitiser. Several in vitro studies show high phototoxicity of the pigment towards gram-positive bacteria. Nevertheless, the highly lipophilic nature and poor bioavailability prevent its application in daily clinical practice thus leading to a limited therapeutic value of hypericin. Liposomal ...
Source: International Journal of Pharmaceutics - September 6, 2019 Category: Drugs & Pharmacology Source Type: research

Pioglitazone-loaded three-dimensional composite polymeric scaffolds: a proof of concept study in wounded diabetic rats
In this study, the anti-diabetic drug, Pioglitazone hydrochloride (PG), was loaded in three-dimensional (3D) composite scaffolds (SC) designed to be applied topically for the management of diabetic wounds. Hydroxypropyl methyl cellulose (HPMC) of different molecular weight (E5, K4M or K15M) were used, in different ratios, with chitosan (CS) for the preparation of the 3D-SC. Investigations to examine the prepared SCs revealed that SC-F3 composed of CS /HPMC E5 (2:1) attained the highest porosity (99.12±5.01), highest water absorption capacity % (300.09± 20.20), and attained the fastest drug release profile (p
Source: International Journal of Pharmaceutics - September 6, 2019 Category: Drugs & Pharmacology Source Type: research

Carrier-free nanodrug: a novel strategy of cancer diagnosis and synergistic therapy
Publication date: Available online 4 September 2019Source: International Journal of PharmaceuticsAuthor(s): Ming-Yue Yang, Rui-Rui Zhao, Yi-Fan Fang, Jia-Li Jiang, Xiao-Tian Yuan, Jing-Wei ShaoAbstractNanoformulations with advantages in drug delivery, safety and pharmacodynamics have been booming as a promising strategy for cancer therapy. However, the traditional nanocarrier still suffers from the low drug loading capacity, potential systematic toxicity, unclear metabolism, and other uncertainties. To overcome these issues, carrier-free nanodrugs with desirable bioactivity were developed rapidly and drawn considerable att...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Understanding the effects of formulation and process variables on the printlets quality manufactured by selective laser sintering 3D printing
Publication date: Available online 4 September 2019Source: International Journal of PharmaceuticsAuthor(s): Sogra F. Barakh Ali, Eman M. Mohamed, Tanil Ozkan, Mathew A. Kuttolamadom, Mansoor A. Khan, Amir Asadi, Ziyaur RahmanAbstractThe focus of the study was to understand the effects of formulation and process variables on the printlets quality manufactured by selective laser sintering (SLS) 3D printing. The Box-Behnken response surface methodology was used to evaluate effects of individual variables and combinations thereof. The formulation and process variables studied were printing chamber temperature (°C, X1), las...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Preclinical safety of topically administered nanostructured lipid carriers (NLC) for wound healing application: biodistribution and toxicity studies
Publication date: 5 October 2019Source: International Journal of Pharmaceutics, Volume 569Author(s): C. Vairo, M. Collantes, G. Quincoces, S. Villullas, I. Peñuelas, M. Pastor, A.G. Gil, E. Gainza, R.M. Hernandez, M. Igartua, G. GainzaAbstractRe-activation of the healing process is a major challenge in the field of chronic wound treatment. For that purpose, lipid-nanoparticles, especially nanostructured lipid carriers (NLC), possess extremely useful characteristics such as biodegradability, biocompatibility and long-term stability, besides being suitable for drug delivery. Moreover, they maintain wound moisture due ...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Ex vivo intestinal perfusion model for investigating mucoadhesion of microcontainers
Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Mette D. Mosgaard, Sophie Strindberg, Zarmeena Abid, Ritika Singh Petersen, Lasse H.E. Thamdrup, Alina J. Andersen, Stephan Sylvest Keller, Anette Müllertz, Line Hagner Nielsen, Anja BoisenAbstractMicro fabricated delivery systems have shown promise in increasing oral bioavailability of drugs. Micrometer-sized polymeric devices (microcontainers) have the potential to facilitate unidirectional drug release directly into the intestinal mucosa whereby, drug absorption can be enhanced. The aim of this study was to d...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

A novel tumor-targeted thermosensitive liposomal cerasome used for thermally controlled drug release
Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Sixie Li, Guangfu Yin, Ximing Pu, Zhongbin Huang, Xiaoming Liao, Xianchun ChenAbstractDrug carriers with tumor targeting and controlled release have strong prospects for application in safe and efficient chemotherapy. Among various carriers, liposomes have good biocompatibility and can enhance the uptake of drugs by cancer cells. However, traditional liposomes have no specific targeting to cancer cells and are prone to insufficient stability, causing early leakage of the drug. Accordingly, organic-inorganic hybrid ph...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Chitosan/Hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: in vitro and in vivo evaluation
Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Juçara R. Franca, Giselle Foureaux, Leonardo L. Fuscaldi, Tatiana G. Ribeiro, Rachel O. Castilho, Maria I. Yoshida, Valbert N. Cardoso, Simone O.A. Fernandes, Sebastião Cronemberger, José Carlos Nogueira, Anderson J. Ferreira, André A.G. FaracoAbstractEye drops containing hydrophilic drugs are commonly used to reduce intraocular pressure (IOP) in glaucoma patients, but compliance to the treatement is commonly reduced by frequent dosing and eventual systemic side effects. Sustained-release ...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Development of an optimized avanafil-loaded invasomal transdermal film: ex vivo skin permeation and in vivo evaluation
Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Osama A.A. Ahmed, Shaimaa M. Badr-EldinAbstractAvanafil (AVA) is a recent FDA approved selective phosphodiesterase type 5 inhibitor used for oral treatment of erectile dysfunction. The oral bioavailability of the drug is challenged by its reduced water solubility, considerable presystemic metabolism, and altered absorption in the presence of food. Accordingly, this work aimed to surmount the aforementioned challenges through the development of optimized nanosized AVA invasomes with enhanced transdermal delivery. AVA ...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

Immediate-released pelletized solid dispersion containing fenofibrate: formulation, in vitro characterization, and bioequivalence studies in experimental beagle dogs
Publication date: Available online 3 September 2019Source: International Journal of PharmaceuticsAuthor(s): Chien Ngoc Nguyen, Cuong Viet Pham, Giap Le Thien, Bao Tran Ngoc, Ha Le Thi, Chang Pham Thi Huyen, Thuan Nguyen ThiAbstractThere have been many strategies to increase solubility, dissolution rates, and oral bioavailability of fenofibrate such as micronization, nanonization, solid dispersion, and emulsion so far. To our knowledge, only first three technologies have been applied in producing marketed products, and no combination of solid dispersion and pellet has been found even in laboratory-based reports. Therefore, ...
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

A dual-action chitosan-based nanogel system of triclosan and flurbiprofen for localised treatment of periodontitis
In conclusion, a dual action NG was successfully developed and proved to have superior therapeutic effects in comparison to physical mixtures of the individual drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 5, 2019 Category: Drugs & Pharmacology Source Type: research

ROS-responsive “smart” polymeric conjugate: synthesis, characterization and proof-of-concept study
Publication date: Available online 31 August 2019Source: International Journal of PharmaceuticsAuthor(s): Natalia Oddone, Francesca Pederzoli, Jason T. Duskey, Chiara A. De Benedictis, Andreas M. Grabrucker, Flavio Forni, Maria Angela Vandelli, Barbara Ruozi, Giovanni TosiAbstractNew approaches integrating stimuli-responsive linkers into prodrugs are currently emerging. These “smart” prodrugs can enhance the effectivity of conventional prodrugs with promising clinical applicability. Oxidative stress is central to several diseases, including cancer. Therefore, the design of prodrugs that respond to ROS stimulus,...
Source: International Journal of Pharmaceutics - September 2, 2019 Category: Drugs & Pharmacology Source Type: research

Glycine microparticles loaded with functionalized nanoparticles for pulmonary delivery
Publication date: Available online 30 August 2019Source: International Journal of PharmaceuticsAuthor(s): Amlan Chakraborty, Simon G. Royce, Magdalena Plebanski, Cordelia SelomulyaAbstractThe use of nanoparticles for pulmonary delivery poses challenges such as the presence of anatomical barriers, and the loss of bioactive components. Excipients are often used to facilitate delivery. Excipients suitable for nanoparticle delivery are still being explored. Herein we introduce for the first time, spray-dried glycine microparticle-based excipients loaded with nanoparticles of the size range known to be taken up by alveolar macr...
Source: International Journal of Pharmaceutics - August 31, 2019 Category: Drugs & Pharmacology Source Type: research

The effect of co-amorphization of glibenclamide on its dissolution properties and permeability through an MDCKII-MDR1 cell layer
Publication date: Available online 28 August 2019Source: International Journal of PharmaceuticsAuthor(s): Henri Sormunen, Marika Ruponen, Riikka LaitinenAbstractCo-amorphous mixtures have been demonstrated to represent a promising approach for enhancing the dissolution of poorly water-soluble drugs. However, little is known of their permeability properties, especially through biological membranes, or about the relationship between their dissolution and permeability. In the present study, co-amorphous glibenclamide (GBC) mixtures with two amino acids, arginine (ARG) and serine (SER), in molar ratios of 1:1 were prepared by ...
Source: International Journal of Pharmaceutics - August 30, 2019 Category: Drugs & Pharmacology Source Type: research

Improvement of tabletability via twin-screw melt granulation: focus on binder distribution
In this study, the impact of binder distribution on the tabletability and compactibility of granules produced by twin-screw melt granulation was investigated. To this end, two grades of dicalcium phosphate anhydrous (fine and coarse) were used as model substances (filler) in combination with two grades of poloxamer (fine and coarse) as melt binder at three concentrations. For the fine filler, granule forming followed the immersion mechanism, whereas a distribution mechanism was observed in case of the coarse filler. Compared to the granules prepared with the coarse filler, the tabletability of granules prepared with the fi...
Source: International Journal of Pharmaceutics - August 30, 2019 Category: Drugs & Pharmacology Source Type: research

Casein nanoparticles in combination with 2-hydroxypropyl-β-cyclodextrin improves the oral bioavailability of quercetin
Publication date: Available online 28 August 2019Source: International Journal of PharmaceuticsAuthor(s): Rebeca Peñalva, Irene Esparza, Jorge Morales, Carlos J. González-Navarro, Eneko Larrañeta, Juan M. IracheAbstractThe aim of this work was to optimize the preparative process of quercetin loaded casein nanoparticles as well as to evaluate the pharmacokinetics of this flavonoid when administered orally in Wistar rats. Nanoparticles were obtained by coacervation after the incubation of casein, 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and quercetin in an aqueous environment. Then, nanoparticl...
Source: International Journal of Pharmaceutics - August 30, 2019 Category: Drugs & Pharmacology Source Type: research

Combining cryo-TEM and energy-filtered TEM for imaging organic core-shell nanoparticles and defining the polymer distribution
Publication date: Available online 27 August 2019Source: International Journal of PharmaceuticsAuthor(s): Agnes-Valencia Weiss, Marcus Koch, Marc SchneiderAbstractNanoparticulate systems intended for the use in drug delivery are getting more and more complex. Composite nanoparticles, such as core-shell particles are designed in order to be used for co-delivery of drugs or a modified release profile. Often the structure can only be postulated by the preparation process, such as surface polymerization, but cannot be experimentally determined due to a lack of appropriate analytical methods. Here a core-shell particle system c...
Source: International Journal of Pharmaceutics - August 28, 2019 Category: Drugs & Pharmacology Source Type: research

Construction of a biomimetic chemokine reservoir stimulates rapid in situ wound repair and regeneration
In this study, we successfully developed a chemokine loaded biomimetic hydrogel as a functional reservoir to stimulate the rapid in situ recruitment of BMSCs for fast wound repair and regeneration. The biomimetic hydrogel was fabricated by using the Polyvinyl alcohol (PVA) combined with chitosan (CS) as the hybrid materials. The fabricated hydrogel possesses many features such as the porous structure, high swelling rate and moisture retention property. More importantly, the incorporated chemokine could be released with a sustained manner from the hydrogel and recruited the bone marrow mesenchymal stem cells (BMSCs) signifi...
Source: International Journal of Pharmaceutics - August 27, 2019 Category: Drugs & Pharmacology Source Type: research

Hybrid Silica-coated Gd-Zn-Cu-In-S/ZnS Bimodal Quantum Dots as an Epithelial Cell Adhesion Molecule Targeted Drug Delivery and Imaging system
In this study, we developed a potent nanocarrier with an effective photoluminescent emission and MR imaging capacity to deliver the doxorubicin to breast cancer 4T1 cells. The nanocarrier was fabricated by coating of quantum dots (QDs) with mesoporous silica followed by amine functionalization of the silica surface. Then, the doxorubicin was loaded into the silica pores and biheterofunctional PEG was covalently bound to the surface of core-shell quantum dot mesoporous silica nanoparticles. In order to target the DOX-loaded nanoparticles, the EpCAM DNA aptamer was attached on the surface of the DOX-loaded PEGylated nanopart...
Source: International Journal of Pharmaceutics - August 27, 2019 Category: Drugs & Pharmacology Source Type: research

Colon-specific microspheres loaded with puerarin reduce tumorigenesis and metastasis in colitis-associated colorectal cancer
Publication date: Available online 26 August 2019Source: International Journal of PharmaceuticsAuthor(s): Xiao-Qing Deng, Hong-Bo Zhang, Gui-Fang Wang, Dong Xu, Wen-Yan Zhang, Qiang-Song Wang, Yuan-Lu CuiAbstractColitis-associated colorectal cancer (CAC) is a common malignancy that develops in chronically inflamed mucosa and is usually accompanied by metastases at other sites. Puerarin, a natural isoflavone isolated from the root of the Pueraria lobata (Willd.) Ohwi, has potential anti-colon cancer activity. However, the poor solubility and low bioavailability of puerarin has restricted its application in the pharmaceutica...
Source: International Journal of Pharmaceutics - August 27, 2019 Category: Drugs & Pharmacology Source Type: research

Glycoengineered nanoparticles enhance the delivery of 5-fluoroucil and paclitaxel to gastric cancer cells of high metastatic potential
Publication date: Available online 26 August 2019Source: International Journal of PharmaceuticsAuthor(s): Elisabete Fernandes, Dylan Ferreira, Andreia Peixoto, Rui Freitas, Marta Relvas-Santos, Carlos Palmeira, Gabriela Martins, Anabela Barros, Lúcio Lara Santos, Bruno Sarmento, José Alexandre FerreiraAbstractGastric cancer is the third leading cause of cancer-related death worldwide, with half of patients developing metastasis within 5 years after curative treatment. Moreover, many patients cannot tolerate or complete systemic treatment due severe side-effects, reducing their effectiveness. Thus, targeted th...
Source: International Journal of Pharmaceutics - August 26, 2019 Category: Drugs & Pharmacology Source Type: research

Importance of Free Water in Controlling Granule and Tablet Properties in a Novel Granulation Method, Green Fluidized Bed Granulation (GFBG)
Publication date: Available online 26 August 2019Source: International Journal of PharmaceuticsAuthor(s): Hiroshi Takasaki, Atsushi Sakurai, Takuma Katayama, Yuka Matsuura, Naoko Ohyagi, Masashi Mizoguchi, Jyunichi Takano, Koichi Wada, Koh Matsui, Takuya Nagato, Agata Ishikawa, Etsuo YonemochiAbstractIn the pharmaceutical field, green fluidized bed granulation (GFBG) is a novel and eco-friendly manufacturing technology used to produce desired granules via simple blending and spraying steps at ambient temperature using a standard fluidized bed granulator. However, the relations between water content and granule and tablet q...
Source: International Journal of Pharmaceutics - August 26, 2019 Category: Drugs & Pharmacology Source Type: research

Complex methodology for rational design of Apremilast-Benzoic acid co-crystallization process
Publication date: Available online 26 August 2019Source: International Journal of PharmaceuticsAuthor(s): Jan Jirát, Daniel Ondo, Martin Babor, Luděk Ridvan, Miroslav ŠoóšAbstractA new co-crystal of pharmaceutical active ingredient Apremilast was successfully designed in this work. The discovered co-crystal with benzoic acid significantly improves key properties like the dissolution and stability of an otherwise poorly soluble Apremilast. A crystallization process was developed, which includes efficient solvent selection and ternary phase diagram construction to minimize risks during scale up. ...
Source: International Journal of Pharmaceutics - August 26, 2019 Category: Drugs & Pharmacology Source Type: research

Design and evaluation of mesenchymal stem cells seeded chitosan/glycosaminoglycans quaternary hydrogel scaffolds for wound healing applications
Publication date: Available online 19 August 2019Source: International Journal of PharmaceuticsAuthor(s): José L. Soriano-Ruiz, Patricia Gálvez-Martín, Elena López-Ruiz, Joaquim Suñer-Carbó, Ana C. Calpena-Campmany, Juan A. Marchal, Beatriz Clares-NaverosAbstractThe main goal of this study was the design, development and characterization of a chitosan based scaffolding substrate including three glycosaminoglycans and collagen to provide an optimal microenvironment for human mesemchymal stem cells isolated from adipose tissue (hMSCs). Chitosan scaffolds provide a moist wound environ...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Dual chamber cartridges in a continuous pharmaceutical freeze-drying concept: determination of the optimal dynamic infrared heater temperature during primary drying
Publication date: Available online 20 August 2019Source: International Journal of PharmaceuticsAuthor(s): Laurens De Meyer, Joris Lammens, Brecht Vanbillemont, Pieter Jan Van Bockstal, Jos Corver, Chris Vervaet, Wolfgang Friess, Thomas De BeerAbstractThe applicability of DCCs in a continuous freeze-drying concept based on spin freezing and infrared heating was evaluated. Maximum applicable filling volume was evaluated. Secondly the mechanistic model for the determination of the optimal dynamic infrared heater temperature during primary drying of regular vials during continuous freeze-drying was adapted and validated for DC...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Strategies to facilitate or block nose-to-brain drug delivery
Publication date: Available online 21 August 2019Source: International Journal of PharmaceuticsAuthor(s): Patricia P. Martins, Hugh D.C. Smyth, Zhengrong CuiAbstractNose-to-brain delivery has gained significant interest over the past several decades. This has resulted in numerous strategies described to improve the delivery of drugs to the brain directly through the olfactory epithelium of the nasal cavity. In some cases, intranasal administration may be more effective than other routes of administration in treating central nervous system and related disorders. Here, we briefly review the strategies that have been used to ...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Potential applications of nanoparticles for tumor microenvironment remodeling to ameliorate cancer immunotherapy
Publication date: Available online 22 August 2019Source: International Journal of PharmaceuticsAuthor(s): Yuzhuo Bai, Yun Wang, Xudong Zhang, Jianhua Fu, Xiuli Xing, Chunlan Wang, Longlan Gao, Yu Liu, Li ShiAbstractIn recent years, researchers have made significant innovations in the field of tumor immunotherapy based on the knowledge of biology, oncology, and immunology. Tumor immunotherapy involves the use of immune checkpoint inhibitors and CAR (chimeric antigen receptor)-T cell therapy. As compared with conventional chemotherapy, immunotherapy is a potential approach to induce a more powerful immune response against tu...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Development of mucoadhesive vaginal films based on HPMC and zein as novel formulations to prevent sexual transmission of HIV
Publication date: Available online 22 August 2019Source: International Journal of PharmaceuticsAuthor(s): Fernando Notario-Pérez, Araceli Martín-Illana, Raúl Cazorla-Luna, Roberto Ruiz-Caro, Luis-Miguel Bedoya, Juan Peña, María-Dolores VeigaAbstractAlthough vaginal films were initially developed for a fast release of the drug, with the adequate formulation they can also be useful for sustained release. The latest strategies for the prevention of the sexual transmission of HIV have moved towards sustained-release dosage forms, so films may be an effective strategy that could also improve t...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Development of a Poly(vinyl alcohol)/Lysine electrospun membrane-based drug delivery system for improved skin regeneration
Publication date: Available online 22 August 2019Source: International Journal of PharmaceuticsAuthor(s): Rosa S. Sequeira, Sónia P. Miguel, Cátia S.D. Cabral, André F. Moreira, Paula Ferreira, Ilídio J. CorreiaAbstractNanofiber-based wound dressings are currently being explored as delivery systems of different biomolecules for avoiding skin infections as well as improve/accelerate the healing process. In the present work, a nanofibrous membrane composed of poly(vinyl alcohol) (PVA) and lysine (Lys) was produced by using the electrospinning technique. Further, anti-inflammatory (ibuprofen (IBP))...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research

Confocal Raman spectroscopy: evaluation of a non-invasive technique for the detection of topically applied ketorolac tromethamine in vitro and in vivo
Publication date: Available online 22 August 2019Source: International Journal of PharmaceuticsAuthor(s): Christian J.F. Bertens, Shuo Zhang, Roel J. Erckens, Frank J.H.M. van den Biggelaar, Tos T.J.M. Berendschot, Carroll A.B. Webers, Rudy M.M.A. Nuijts, Marlies GijsAbstractCurrent information about the pharmacokinetics of an ocular drug can only be achieved by invasive sampling. However, confocal Raman spectroscopy bears the potential to quantify drug concentrations non-invasively. In this project, we evaluated the detection and quantification of ocular ketorolac tromethamine levels with confocal Raman spectroscopy after...
Source: International Journal of Pharmaceutics - August 24, 2019 Category: Drugs & Pharmacology Source Type: research