Long chain fatty acid conjugation remarkably decreases the aggregation induced toxicity of Amphotericin B
Publication date: 10 June 2018 Source:International Journal of Pharmaceutics, Volume 544, Issue 1 Author(s): Kaushik Thanki, Rameshwar Prajapati, Abhay T. Sangamwar, Sanyog Jain Amphotericin B is an antimicrobial membrane-acting drug used in the treatment of systemic fungal infections. However, the clinical utility of AmB is often low as a result of (i) dose-limiting toxicity which is closely associated with its aggregation wherein the selectivity for its target i.e. ergosterol in fungal membranes is diminished and (ii) limited oral bioavailablity. The latter is attributed to the unfavorable physicochemical properties of ...
Source: International Journal of Pharmaceutics - April 13, 2018 Category: Drugs & Pharmacology Source Type: research

Defined drug release from 3D-printed composite tablets consisting of drug-loaded polyvinylalcohol and a water-soluble or water-insoluble polymer filler
In this study, we fabricated composite tablets consisting of two components, a drug and a filler, by using a fused deposition modeling-type 3D printer. Polyvinylalcohol (PVA) polymer containing calcein (a model drug) was used as the drug component and PVA or polylactic acid (PLA) polymer without drug was used as the water-soluble or water-insoluble filler, respectively. Various kinds of drug-PVA/PVA and drug-PVA/PLA composite tablets were designed, and the 3D-printed tablets exhibited good formability. The surface area of the exposed drug component is highly correlated with the initial drug release rate. Composite tablets ...
Source: International Journal of Pharmaceutics - April 11, 2018 Category: Drugs & Pharmacology Source Type: research

Polysorbate 20 alters the oral bioavailability of etoposide in wild type and mdr1a deficient Sprague-Dawley rats
In conclusion, PS20 increases oral bioavailability of etoposide through inhibition of P-glycoprotein. However, the use of the excipient may be challenged by etoposide retention at higher concentrations. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 11, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of sustained release capsules by electrostatic dry powder coating, using traditional dip coating as reference
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Yan Yang, Lian Shen, Feng Yuan, Hui Fu, Weiguang Shan Lately, a great deal of attention is being paid to capsule coating, since the coat protects active pharmaceutical ingredients (APIs) from damage, as is in the case of tablet and pellet. However, moisture and heat sensitivity of gelatin shells make it challenging to coat capsules using the conventional aqueous coating techniques. In an effort to overcome this challenge, the present study aims to coat capsules using two different coating techniques: electr...
Source: International Journal of Pharmaceutics - April 11, 2018 Category: Drugs & Pharmacology Source Type: research

Current regulatory requirements and practical approaches for stability analysis of pharmaceutical products: A comprehensive review
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Pinaki Sengupta, Bappaditya Chatterjee, Rakesh Kumar Tekade Different regulatory guidelines recommend establishing stability profile of pharmaceuticals at the time of drug development. The expiry date, retesting period and storage conditions of active drugs or products are established through stability analysis. Several regulatory guidelines exist for stability testing of pharmaceuticals. Mostly, ICH stability guidelines are followed in practice. This guideline recommends to validate stability indicating me...
Source: International Journal of Pharmaceutics - April 11, 2018 Category: Drugs & Pharmacology Source Type: research

Manipulation of spray-drying conditions to develop dry powder particles with surfaces enriched in hydrophobic material to achieve high aerosolization of a hygroscopic drug
This study aimed to develop dry powder particles with surfaces enriched in hydrophobic material by manipulation of spray-drying conditions and to investigate the effect of hydrophobic surface enrichment on aerosolization of hygroscopic drug. The composite dry powder formulations of kanamycin (hygroscopic drug) and rifampicin (hydrophobic drug) were produced by systematically (23 full factorial design) varying the drug ratio, co-solvent composition and inlet temperature using Buchi B-290 Mini Spray-Dryer. All the composite powder particles were inhalable in size (3.1–3.9 µm), wrinkled, flake-shaped and amorpho...
Source: International Journal of Pharmaceutics - April 10, 2018 Category: Drugs & Pharmacology Source Type: research

Hybrid nanoparticles as a new technological approach to enhance the delivery of cholesterol into the brain
This article aims to investigate the production of hybrid nanoparticles composed by Chol and PLGA (MIX-NPs) modified with g7 ligand for BBB crossing. We described the impact of ratio between components (Chol and PLGA) and formulation process (nanoprecipitation or single emulsion process) on physico-chemical and structural characteristics, we tested MIX-NPs in vitro using primary hippocampal cell cultures evaluating possible toxicity, uptake, and the ability to influence excitatory synaptic receptors. Our results elucidated that both formulation processes produce MIX-NPs with a Chol content higher that 40%, meaning that Cho...
Source: International Journal of Pharmaceutics - April 7, 2018 Category: Drugs & Pharmacology Source Type: research

Improved properties of fine active pharmaceutical ingredient powder blends and tablets at high drug loading via dry particle coating
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Kuriakose Kunnath, Zhonghui Huang, Liang Chen, Kai Zheng, Rajesh Davé It has been shown that dry coating cohesive active pharmaceutical ingredients (APIs) with nano-silica can improve packing and flow of their blends, facilitating high speed direct compression tableting. This paper examines the broader scope and generality of previous work by examining three fine APIs; micronized Acetaminophen (mAPAP), coarse Acetaminophen (cAPAP) and micronized Ibuprofen (mIBU), and considers dry coating with both h...
Source: International Journal of Pharmaceutics - April 7, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of cationic liposomes with stearylamine against virus infection
In this study, we demonstrated that cationic liposomes with incorporated stearylamine (SA) inhibit viral infectivity without preloaded active pharmaceutical ingredients. Specifically, we correlated physiochemical properties of liposomes, such as zeta potentials and particle sizes, with virus infectivity using the BacMam™ reagent, which is based on recombinant baculovirus (BV). Compared with neutral or negatively-charged liposomes, SA liposomes suppressed BV infectivity in several mammalian cell lines, including A549 cells. SA liposomes inhibited BV infection over 80% by optimizing the liposomal concentration and expo...
Source: International Journal of Pharmaceutics - April 7, 2018 Category: Drugs & Pharmacology Source Type: research

Modeling the effects of material properties on tablet compaction: A building block for controlling both batch and continuous pharmaceutical manufacturing processes
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): M.S. Escotet-Espinoza, S. Vadodaria, F.J. Muzzio, M.G. Ierapetritou As the pharmaceutical industry modernizes its manufacturing practices and incorporates more efficient processing approaches, it is important to reevaluate which process design elements affect product quality and the means to study these systems. The purpose of this work is to provide insight on a methodology to correlate the effect of raw material properties to equipment and process performance using both data-driven and semi-empirical mode...
Source: International Journal of Pharmaceutics - April 6, 2018 Category: Drugs & Pharmacology Source Type: research

On the dilemma of fractal or fractional kinetics in drug release studies: A comparison between Weibull and Mittag-Leffler functions
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Kosmas Kosmidis, Panos Macheras We compare two of the most successful models for the description and analysis of drug release data. The fractal kinetics approach leading to release profiles described by a Weibull function and the fractional kinetics approach leading to release profiles described by a Mittag-Leffler function. We used Monte Carlo simulations to generate artificial release data from euclidean and fractal substrates. We have also used real release data from the literature and found that both mo...
Source: International Journal of Pharmaceutics - April 6, 2018 Category: Drugs & Pharmacology Source Type: research

The application of STEP-technology ® for particle and protein dispersion detection studies in biopharmaceutical research
In conclusion, we could demonstrate some applications as well as limitations of this technique for biopharmaceutical samples. In comparison to orthogonal methods this technique is a great complementary approach if particle data e.g. density or refractive index can be determined. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 5, 2018 Category: Drugs & Pharmacology Source Type: research

Pegylated nanoparticles for the oral delivery of nimodipine: Pharmacokinetics and effect on the anxiety and cognition in mice
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Lina Clara Gayoso e Almendra Ibiapina Moreno, Maite Solas, María Cristina Martínez-Ohárriz, Egoitz Muñoz, Nereide Stela Santos-Magalhães, Maria J. Ramirez, Juan M. Irache Nimodipine may be of interest to treat behavioral alterations and memory deficits. However, its oral administration is hampered by a low bioavailability. The aim of this work was to develop pegylated nanoparticles as oral carriers of nimodipine and test their capability to both reverse the anxiety and pro...
Source: International Journal of Pharmaceutics - April 5, 2018 Category: Drugs & Pharmacology Source Type: research

A mechanistic study on tablet ejection force and its sensitivity to lubrication for pharmaceutical powders
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Bekuechukwu Uzondu, Lap Yin Leung, Chen Mao, Chia-Yi Yang Pharmaceutical powders can exhibit markedly different tablet ejection forces. The purpose of this study is to understand the factors leading to the variability of the tablet ejection force and its sensitivity to lubrication. The study showed that the tablet ejection force is mainly governed by 1) tablet diameter and thickness, 2) compact-die wall friction coefficient, and 3) residual die wall stress upon ejection; the latter was further controlled by...
Source: International Journal of Pharmaceutics - April 4, 2018 Category: Drugs & Pharmacology Source Type: research

Star-shaped poly(oligoethylene glycol) copolymer-based gels: Thermo-responsive behaviour and bioapplicability for risedronate intranasal delivery
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Mahmoud E. Soliman, Enas Elmowafy, Luca Casettari, Cameron Alexander The aim of this work was to obtain an intranasal delivery system with improved mechanical and mucoadhesive properties that could provide prolonged retention time for the delivery of risedronate (RS). For this, novel in situ forming gels comprising thermo-responsive star-shaped polymers, utilizing either polyethylene glycol methyl ether (PEGMA-ME 188, Mn 188) or polyethylene glycol ethyl ether (PEGMA-EE 246, Mn 246), with polyethylene glyco...
Source: International Journal of Pharmaceutics - April 4, 2018 Category: Drugs & Pharmacology Source Type: research

Kaempferol-loaded mucoadhesive nanoemulsion for intranasal administration reduces glioma growth in vitro
This study aimed to prepare nanoemulsions containing KPF with and without chitosan to investigate their potential for brain delivery following intranasal administration, and to evaluate their antitumor activity against glioma cells. KPF-loaded nanoemulsion (KPF-NE) and KPF-loaded mucoadhesive nanoemulsion (KPF-MNE) were prepared by high-pressure homogenization technique and were characterized for their globule size, zeta potential, drug content, pH, viscosity, mucoadhesive strength and morphology. KPF from KPF-MNE showed significantly higher permeation across the mucosa in ex vivo diffusion studies. Histopathological exami...
Source: International Journal of Pharmaceutics - April 4, 2018 Category: Drugs & Pharmacology Source Type: research

In situ monitoring of nanoparticle formation: Antisolvent precipitation of azole anti-fungal drugs
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Kate P.M. McComiskey, Naila A. Mugheirbi, Jack Stapleton, Lidia Tajber In this work we report the effect of stabilizer choice and concentration on nanoparticle (NP) stability over time. Three different BCS class II active pharmaceutical ingredient (APIs): itraconazole (ITR), ketoconazole (KETO) and posaconazole (POS) were chosen due to their poor aqueous solubility and closely related chemical structures. Polyethylene glycol, polyethylene glycol methyl ether and polyethylene glycol dimethyl ether (DMPEG) wi...
Source: International Journal of Pharmaceutics - April 4, 2018 Category: Drugs & Pharmacology Source Type: research

RVG29-modified docetaxel-loaded nanoparticles for brain-targeted glioma therapy
In conclusion, these results indicated that the RVG29-modified NPs have potential efficacy for glioma therapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 3, 2018 Category: Drugs & Pharmacology Source Type: research

Osmolality predictive models of different polymers as tools in parenteral and ophthalmic formulation development
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Diana Arbelaez-Camargo, Manel Roig-Carreras, Encarna García-Montoya, Pilar Pérez-Lozano, Montserrat Miñarro-Carmona, Josep Ramon Ticó-Grau, Josep Maria Suñé-Negre During the development of parenteral dosage forms, different physicochemical studies are required to ensure stable, effective and safe formulations. The osmolality of this kind of dosage forms should bear a close similarity to the body fluids to prevent local irritation, pain or even more significant side ...
Source: International Journal of Pharmaceutics - April 3, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid bilayer-coated mesoporous silica nanoparticles carrying bovine hemoglobin towards an erythrocyte mimic
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Jing Tu, Jeroen Bussmann, Guangsheng Du, Yue Gao, Joke A. Bouwstra, Alexander Kros Hemoglobin (Hb)-loaded mesoporous silica nanoparticles (MSNs) coated with a lipid bilayer (LB-MSNs) were investigated as an erythrocyte mimic. MSNs with a large average pore size (10 nm) act as a rigid core and provide a protective environment for Hb encapsulated inside the pores. The colloidal stability of Hb-loaded MSNs was enhanced upon the application of a lipid bilayer, through fusion of PEGylated liposomes onto the ex...
Source: International Journal of Pharmaceutics - April 1, 2018 Category: Drugs & Pharmacology Source Type: research

Bone regeneration in osteoporosis by delivery BMP-2 and PRGF from tetronic –alginate composite thermogel
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Elisabet Segredo-Morales, Patricia García-García, Ricardo Reyes, Edgar Pérez-Herrero, Araceli Delgado, Carmen Évora As the life expectancy of the world population increases, osteoporotic (OP) fracture risk increase. Therefore in the present study a novel injectable thermo-responsive hydrogel loaded with microspheres of 17β-estradiol, microspheres of bone morphogenetic protein-2 (BMP-2) and plasma rich in growth factors (PRGF) was applied locally to regenerate a calvaria crit...
Source: International Journal of Pharmaceutics - April 1, 2018 Category: Drugs & Pharmacology Source Type: research

Continuous synthesis of nano-drug particles by antisolvent crystallization using a porous hollow-fiber membrane module
This study reports an experimental and numerical approach to obtain a further understanding of the fundamental principles of antisolvent crystallization using a porous hollow fiber membrane. This includes producing a particle size-controlled drug nanosuspension experimentally using a commercial microfiltration (MF) pencil scale module, and a numerical analysis of mixing behavior using a computational fluid dynamics (CFD) simulation. From the results obtained, a nanosuspension of a model drug, Indomethacin, with particles of average diameter 0.320 µm was prepared. Furthermore, this nanosuspension has higher stabilit...
Source: International Journal of Pharmaceutics - March 31, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of a new dispersion technique for assessing triboelectric charging of powders
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): U. Zafar, F. Alfano, M. Ghadiri In a number of applications, especially in pharmaceutical drug development, there is often a very small powder quantity available for evaluating the manufacturability of new drugs. However, it is highly desirable to be able to quickly evaluate processing issues, and where possible using the smallest powder quantity. In the present work, a proprietary commercial powder dispersion device (the disperser of Malvern© Morphologi G3) is adapted to evaluate the triboelectric cha...
Source: International Journal of Pharmaceutics - March 31, 2018 Category: Drugs & Pharmacology Source Type: research

Complexation of Chol-DsiRNA in place of Chol-siRNA greatly increases the duration of mRNA suppression by polyplexes of PLL(30)-PEG(5K) in primary murine syngeneic breast tumors after i.v. administration
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Vishakha V. Ambardekar, Rajesh R. Wakaskar, Zhen Ye, Stephen M. Curran, Timothy R. McGuire, Don W. Coulter, Rakesh K. Singh, Joseph A. Vetro RNA interference has tremendous potential for cancer therapy but is limited by the insufficient potency of RNAi molecules after i.v. administration. We previously found that complexation with PLL(30)-PEG(5K) greatly increases the potency of 3′-cholesterol-modified siRNA [Chol-siRNA] in primary murine syngeneic 4T1 breast tumors after i.v. administration but mRNA ...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Nevirapine-polycaprolactone crystalline inclusion complex as a potential long-acting injectable solid form
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Xiaotong Yang, Beihang Yu, Zhi Zhong, Bao-hua Guo, Yanbin Huang Nevirapine (NVP) is recommended by WHO as the antiretroviral treatment to prevent HIV passing from mother to child. However, the once-daily oral administration results in poor patient compliance, and a long-acting injectable form of NVP is desirable. Using single-crystal X-ray diffraction and other characterization methods, we demonstrated NVP can form crystalline inclusion complex (IC) with the biodegradable hydrophobic poly(ε-caprolac...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Effective cellular internalization, cell cycle arrest and improved pharmacokinetics of Tamoxifen by cholesterol based lipopolymeric nanoparticles
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Samrat Mazumdar, Kishan S. Italiya, Saurabh Sharma, Deepak Chitkara, Anupama Mittal The present study aims at the development of cholesterol based lipopolymeric nanoparticles for improved entrapment, better cell penetration and improved pharmacokinetics of Tamoxifen (TMX). Self-assembling cholesterol grafted lipopolymer, mPEG-b-(CB-{g-chol}-co-LA) was synthesized from poly(ethyleneglycol)-block-2-methyl-2-carboxyl-propylenecarboxylic acid-co-poly (l-lactide) [mPEG-b-(CB-{g-COOH}-co-LA)] copolymer followed b...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Partitioning of dispersed nanoparticles in a realistic nasal passage for targeted drug delivery
This study numerically detailed the naturally inhaled nanoparticle transport process from the initial releasing locations to the final deposited sites using a realistic human nasal passage. Dispersed nanoparticles at different coronal cross-sections were partitioned into multiple groups according to their final deposited locations. Results showed inhaled nanoparticles are more likely to move along the septum. Olfactory deposited particles entered the nose through the inner superior corner of the nostril; the middle meatus deposited particles entered the nose through the top third of the nostril; the inferior deposited part...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Improving in vivo conversion of oleuropein into hydroxytyrosol by oral granules containing probiotic Lactobacillus plantarum 299v and an Olea europaea standardized extract
This study reports novel food-grade granules for co-delivery of L. plantarum 299v and a standardized extract of Olea europaea leaves (Phenolea®) as oral carrier of probiotics and hydroxytyrosol. Different granule formulations containing either L. plantarum 299v (Lac), or the olive leave extract (Phe) or their combination (Lac-Phe) have been successfully produced through wet granulation employing excipients generally regarded as safe as granulating/binding agents. L. plantarum cells withstood the manufacturing process and were stable upon storage at 4 °C for more than 6 months. In vitro dissolution studies in si...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Effective deactivation of A549 tumor cells in vitro and in vivo by RGD-decorated chitosan-functionalized single-walled carbon nanotube loading docetaxel
This study aims to construct and evaluate RGD-decorated chitosan (CS)-functionalized pH-responsive single-walled carbon nanotube (SWCNT) carriers using docetaxel (DTX) as a model anticancer drug. DTX was loaded onto SWCNT via π–π stacking interaction (SWCNT-DTX), followed by the non-covalent conjugation of RGD-decorated CS to SWCNT-DTX to prepare RGD-CS-SWCNT-DTX. The RGD-CS-SWCNT-DTX showed significantly higher drug release than the pure drug, giving higher release rate at pH 5.0 (68%) than pH 7.4 (49%). The RGD-CS-SWCNT-DTX could significantly inhibit the growth of A549 tumor cells in vitro, and the uptake am...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Control of three different continuous pharmaceutical manufacturing processes: Use of soft sensors
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Jakob Rehrl, Anssi-Pekka Karttunen, Niels Nicolaï, Theresa Hörmann, Martin Horn, Ossi Korhonen, Ingmar Nopens, Thomas De Beer, Johannes G. Khinast One major advantage of continuous pharmaceutical manufacturing over traditional batch manufacturing is the possibility of enhanced in-process control, reducing out-of-specification and waste material by appropriate discharge strategies. The decision on material discharge can be based on the measurement of active pharmaceutical ingredient (API) concentra...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Microsuspension of fatty acid esters of entecavir for parenteral sustained delivery
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Myoung Jin Ho, Dae Ro Lee, Sung Hyun Im, Jeong A. Yoon, Chang Yong Shin, Hyun Jung Kim, Sun Woo Jang, Young Wook Choi, Young Taek Han, Myung Joo Kang Entecavir (EV), an anti-viral agent for hepatitis B infection, should be administered under fasted state, as intestinal absorption of this hydrophilic compound is markedly decreased under post-prandial conditions. Herein, in order to improve therapeutic adherence, a parenteral sustained delivery system was constructed, by synthesizing water-insoluble ester pro...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Relating the tableting behavior of piroxicam polytypes to their crystal structures using energy-vector models
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Pratik P. Upadhyay, Changquan C. Sun, Andrew D. Bond Piroxicam crystallises into two polytypes, α1 and α2, with crystal structures that contain identical molecular layers but differ in the way that these layers are stacked. In spite of having close structural similarity, the polytypes have significantly different powder tabletting behaviour: α2 forms only weak tablets at low pressures accompanied by extensive capping and lamination, which make it impossible to form intact tablets above 100...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Micelle directed chemical polymerization of polypyrrole particles for the electrically triggered release of dexamethasone base and dexamethasone phosphate
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Dedeepya Uppalapati, Manisha Sharma, Zaid Aqrawe, Frazer Coutinho, Ilva D. Rupenthal, Ben J. Boyd, Jadranka Travas-Sejdic, Darren Svirskis Conducting polymers such as polypyrrole (PPy) can be used as electrically responsive drug delivery systems typically prepared by electrochemical polymerisation, however, the amount of drug that can be delivered is typically low. To increase drug delivery capacity and prepare larger amounts of polymer, PPy nanoparticles were produced by chemical polymerisation over drug-l...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Current advanced therapy cell-based medicinal products for type-1-diabetes treatment
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Alberto Cañibano-Hernández, Laura Sáenz del Burgo, Albert Espona-Noguera, Jesús Ciriza, Jose Luis Pedraz In the XXI century diabetes mellitus has become one of the main threats to human health with higher incidence in regions such as Europe and North America. Type 1 diabetes mellitus (T1DM) occurs as a consequence of the immune-mediated destruction of insulin producing β-cells located in the endocrine part of the pancreas, the islets of Langerhans. The administration of exog...
Source: International Journal of Pharmaceutics - March 30, 2018 Category: Drugs & Pharmacology Source Type: research

Mechanistic understanding of the phase behavior of supersaturated solutions of poorly water-soluble drugs
In this study, the phase behavior of supersaturated solutions generated by antisolvent addition and upon the dissolution of ASDs was evaluated using fluorescence lifetime measurements and several other orthogonal techniques, including steady-state fluorescence spectroscopy, ultraviolet (UV) extinction and concentration profiles, ultracentrifuge measurements and nanoparticle tracking analysis. Ritonavir and lopinavir were chosen as poorly water-soluble model drugs, and the polymer, Kollidon VA64, was selected to form the dispersions. The fluorescence lifetime of the environment-sensitive fluoroprobe, PRODAN, was monitored t...
Source: International Journal of Pharmaceutics - March 27, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of melibiose and trehalose as stabilising excipients for spray-dried β-galactosidase formulations
In conclusion, protein formulations with melibiose could be spray dried into amorphous powders that were physically stable, contained lower moisture contents and protected protein activity at least as well as trehalose formulations. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 26, 2018 Category: Drugs & Pharmacology Source Type: research

Co-delivery of doxorubicin and imatinib by pH sensitive cleavable PEGylated nanoliposomes with folate-mediated targeting to overcome multidrug resistance
In this study, doxorubicin (DOX) and imatinib (IM) were co-loaded into folate receptor targeted (FR-targeted) pH-sensitive liposomes (denoted as FPL-DOX/IM) to fulfill intracellular acid-sensitive release and reverse drug resistance. FPL-DOX/IM could maintain stability in blood circulation with approximate diameters of 100 nm and rapidly release encapsulated drugs in tumor acidic microenvironment. Moreover, the IM in combination therapy could overcome chemoresistance associated with DOX effectively by inhibiting ABC transporter function and improving chemotherapy sensitivity. The designed liposomes co-loaded with DOX and...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

The synergistic fungicidal effect of low-frequency and low-intensity ultrasound with amphotericin B-loaded nanoparticles on C. albicans in vitro
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Min Yang, Shuang Xie, Vishnu Prasad Adhikari, Yu Dong, Yonghong Du, Dairong Li It is difficult to effectively eradicate C. albicans using traditional antifungal agents, mainly because the low permeability of the C. albicans cell wall creates strong drug resistance. The aim of this study was to investigate the synergistic fungicidal effect and the underlying mechanisms of low-frequency and low-intensity ultrasound combined with a treatment of amphotericin B-loaded nanoparticles (AmB-NPs) against C. albicans. ...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of molecular rearrangement of amphiphilic stabilizers on physical stability of itraconazole nanoparticles prepared by flash nanoprecipitation
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Ka Yee Wan, Ka Wai Wong, Albert Hee Lum Chow, Shing Fung Chow Flash nanoprecipitation (FNP) is a controlled antisolvent precipitation process that has proven effective for consistent production of drug nanoparticles with a defined mean particle size and narrow particle size distribution. However, physical instability of the generated nanoparticles remains a major challenge in the application of this technology in pharmaceutical formulation. Aimed at resolving this problem, the present study has investigated ...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Liposomes, lipid nanocapsules and smartCrystals ®: A comparative study for an effective quercetin delivery to the skin
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): T. Hatahet, M. Morille, A. Hommoss, J.M. Devoisselle, R.H. Müller, S. Bégu Quercetin is a flavonoid with strong antioxidant and antiinflammatory activities considered as a potential drug candidate for skin exogenous supplementation. Nevertheless, crude quercetin suffers from poor water solubility and consequently topical inactivity. Therefore, quercetin formulation within a suitable system that overcomes its solubility limitation is a matter of investigation. Three approaches were tested to impro...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Establishing an in vitro permeation model to predict the in vivo sex-related influence of PEG 400 on oral drug absorption
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Yang Mai, Sudaxshina Murdan, Marwa Awadi, Abdul W. Basit The notion that certain formerly regarded “inert” pharmaceutical excipients are capable of modifying the bioavailability of oral drugs has gained increasing attention in recent years. For instance, the commonly-used solubilizing agent polyethylene glycol 400 (PEG 400) exhibits a sex-specific effect on the bioavailability of ranitidine in both humans and rats, mediated by the efflux transporter P-glycoprotein (P-gp). To determine whether suc...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

One-pot synthesis of dopamine-conjugated hyaluronic acid/polydopamine nanocomplexes to control protein drug release
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Dae Gon Lim, Racelly Ena Prim, Eunah Kang, Seong Hoon Jeong The self-organizing complexes with hyaluronic acid (HA) and polydopamine (PDA), an adhesion mediator via hydrogen bonding, were investigated for use as protein drug carriers. The complexes were prepared with HA of different molecular weights (20 kDa and 200 kDa) and various molar ratios of dopamine and lysozyme, a model protein. Dopamine-conjugated HA (HADA)/PDA complexes were prepared by one-pot synthesis by relying on the self-polymerization o...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Transdermal anti-nuclear kappaB siRNA therapy for atopic dermatitis using a combination of two kinds of functional oligopeptide
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Hisako Ibaraki, Takanori Kanazawa, Yuuki Takashima, Hiroaki Okada, Yasuo Seta Nucleic acid-based targeting of nuclear factor kappaB (NF-κB) is gaining attention as a treatment option for skin diseases like atopic dermatitis (AD). Transdermal administration improves patient quality of life because of non-invasive; however, siRNA delivery into the skin can be challenging owing to the barrier of tight junctions in the granular layer. Therefore, we aimed to develop a delivery system of siRNA for topical sk...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Development of pectin microparticles by using ionotropic gelation with chlorhexidine as cross-linking agent
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): M. Lascol, S. Bourgeois, C. Barratier, P. Marote, P. Lantéri, C. Bordes Having previously highlighted the gelation of pectin with chlorhexidine (CX), pectinate microparticles were prepared here by vibrational prilling using CX, not only as an active ingredient encapsulated but also as a cross-linking agent. CX amount required for pectin gelation was smaller than usual dications (Ca2+, Zn2+) used as cross-linking agent for pectin ionotropic gelation: CX seemed to bind more easily to pectin chains that ...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Correlation of solid dosage porosity and tensile strength with acoustically extracted mechanical properties
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Xiaochi Xu, Connor Mack, Zachary J. Cleland, Chaitanya Krishna Prasad Vallabh, Vivek S. Dave, Cetin Cetinkaya Currently, the compressed tablet and its oral administration is the most popular drug delivery modality in medicine. The accurate porosity and tensile strength characterization of a tablet design is vital for predicting its performance such as disintegration, dissolution, and drug-release efficiency upon administration as well as ensuring its mechanical integrity. In current work, a non-destructive c...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

IR780 based nanomaterials for cancer imaging and photothermal, photodynamic and combinatorial therapies
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Cátia G. Alves, Rita Lima-Sousa, Duarte de Melo-Diogo, Ricardo O. Louro, Ilídio J. Correia IR780, a molecule with a strong optical absorption and emission in the near infrared (NIR) region, is receiving an increasing attention from researchers working in the area of cancer treatment and imaging. Upon irradiation with NIR light, IR780 can produce reactive oxygen species as well as increase the body temperature, thus being a promising agent for application in cancer photodynamic and photothermal ...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoparticles for dendritic cell-based immunotherapy
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Tuan Hiep Tran, Thi Thu Phuong Tran, Hanh Thuy Nguyen, Cao Dai Phung, Jee-Heon Jeong, Martina H. Stenzel, Sung Giu Jin, Chul Soon Yong, Duy Hieu Truong, Jong Oh Kim Crosstalk among immune cells has attracted considerable attention with the advent of immunotherapy as a novel therapeutic approach for challenging diseases, especially cancer, which is the leading cause of mortality worldwide. Dendritic cells—the key antigen-presenting cells—play a pivotal role in immunological response by presenting ...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Current development in the formulations of non-injection administration of paclitaxel
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Xiyou Du, Abdur Rauf Khan, Manfei Fu, Jianbo Ji, Aihua Yu, Guangxi Zhai Paclitaxel (PTX) belongs to a class of taxane anti-tumor drug used for the clinic treatment of breast cancer, ovarian cancer, non-small-cell lung cancer, and so on. PTX has poor water solubility and oral bioavailability. It is generally administered via intravenous (i.v.) infusion. Traditional PTX injectable preparations contain Cremophor-EL and ethanol to improve its solubility, which would result in adverse reactions like severe hypers...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Dual-responsive drug delivery systems prepared by blend electrospinning
Publication date: 30 May 2018 Source:International Journal of Pharmaceutics, Volume 543, Issues 1–2 Author(s): Heyu Li, Qingqing Sang, Junzi Wu, Gareth R. Williams, Haijun Wang, Shiwei Niu, Jianrong Wu, Li-Min Zhu To prepare temperature and pH dual-responsive drug delivery systems, the thermosensitive polymer poly(N-isopropylacrylamide) (PNIPAAm) was first synthesized by free-radical polymerization. It was then co-dissolved with the pH-sensitive polymer Eudragit® L100-55 (EL100-55) and processed into fibers using electrospinning. Ketoprofen (KET), a model drug, was also incorporated into the composite fibers, an...
Source: International Journal of Pharmaceutics - March 23, 2018 Category: Drugs & Pharmacology Source Type: research

Scaling laws and size effects for amorphous crystallization kinetics: Constraints imposed by nucleation and growth specificities
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Marc Descamps, Jean-François Willart In the present paper we review different aspects of the crystallization of amorphous compounds in relation to specificities of the nucleation and growth rates. Its main purpose is: i) to underline the interest of a scaling analysis of recrystallization kinetics to identify similarities or disparities of experimental kinetic regimes. ii) to highlight the intrinsic link between the nucleation rate and growth rate with a temperature dependent characteristic transforma...
Source: International Journal of Pharmaceutics - March 19, 2018 Category: Drugs & Pharmacology Source Type: research