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International Journal of Pharmaceutics

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 contact ultrasonic approach and an associated testing procedure are presented and employed to quantify and relate the acoustically extracted mechanical properties of pharmaceutical compacts to direct porosity and tensile strength measurements...
March 10, 2018: International Journal of Pharmaceutics
Bin Li, Xiao-Xue Zhang, Hao-Yan Huang, Li-Qing Chen, Jing-Hao Cui, Yanli Liu, Hehua Jin, Beom-Jin Lee, Qing-Ri Cao
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 pH5.0 (68%) than pH7.4 (49%). The RGD-CS-SWCNT-DTX could significantly inhibit the growth of A549 tumor cells in vitro, and the uptake amount of A549 cells was obviously higher than that of MCF-7 cells...
March 10, 2018: International Journal of Pharmaceutics
Yang Mai, Sudaxshina Murdan, Marwa Awadi, Abdul W Basit
No abstract text is available yet for this article.
March 9, 2018: International Journal of Pharmaceutics
Gergő Dargó, Krisztina Boros, László Péter, Milo Malanga, Tamás Sohajda, Lajos Szente, György T Balogh
The present study was aimed to develop a medium-throughput screening technique for investigation of cyclodextrin (CD) - active pharmaceutical ingredient (API) complexes. Dual-phase potentiometric lipophilicity measurement, as gold standard technique, was combined with the partition coefficient method (plotting the reciprocal of partition coefficients of APIs as a function of CD concentration). A general equation was derived for determination of stability constants of 1:1 CD-API complexes (K1:1,CD ) based on solely the changes of partition coefficients (logPo/w N - logPapp N ), without measurement of the actual API concentrations...
March 9, 2018: International Journal of Pharmaceutics
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® L 100-55 (EL100-55) and processed into fibers using electrospinning. Ketoprofen (KET), a model drug, was also incorporated into the composite fibers, and fibers based on a single polymer additionally prepared. The fibers had smooth cylindrical morphologies, and no obvious phase separation could be seen...
March 8, 2018: International Journal of Pharmaceutics
Michael M Farag, Nevine S Abd El Malak, Soad A Yehia
The aim of this study was to develop a novel buccal bi-layered chronopatch capable of eliciting pulsatile release pattern of drugs treating diseases with circadian rhythm related manifestation. Zaleplon (ZLP) was used as a model drug intended to induce sleep and to treat middle of night insomnia. The chronopatch was prepared adopting double casting technique. The first layer was composed of a controlled release patch containing ZLP-Precirol melt granules intended to release ZLP in a sustained manner to maintain sleep and to prevent early morning awakening...
March 8, 2018: International Journal of Pharmaceutics
Gonçalo Marcelo, Inês C Ferreira, Raquel Viveiros, Teresa Casimiro
A novel class of molecularly imprinted polymer (MIP) based on Itaconic acid:Ethylene glycol dimethacrylate were developed as a potential body-friendly oral drug delivery system for metronidazole (MZ), a pH-independent drug, simulating a real environment. Itaconic acid-based copolymers were synthesized with two different molar ratios of template:monomer:crosslinker (T:M:C), 1:5:25 and 1:5:50, in supercritical carbon dioxide (scCO2 ) in high yields. Further, impregnation of MZ was performed in scCO2 environment...
March 8, 2018: International Journal of Pharmaceutics
Francesca Felice, Anna Maria Piras, Silvia Rocchiccioli, Maria Chiara Barsotti, Tatiana Santoni, Angela Pucci, Silvia Burchielli, Federica Chiellini, Nadia Ucciferri, Roberto Solaro, Angelina Altomare, Antonella Cecchettini, Rossella Di Stefano
Endothelial progenitor cells (EPCs) contribute to ischemic tissue repair by paracrine secretion up-regulated by hypoxia. In this study we use novel nanoparticles (NPs) as carriers for a controlled release of EPC secretome (CM) to improve their angiogenic properties. Thein vivo effect in ischemic hindlimb rat model was evaluated, comparing hypoxic EPC-CM-NPs with hypoxic EPC-CM alone. A proteomic characterization of hypoxic CM and the in vitro effect on endothelial cells (HUVECs) were also performed. Up to 647 protein, 17 of which with angiogenic properties, were upregulated by hypoxia...
March 8, 2018: International Journal of Pharmaceutics
Maria Aponte, Francesca Ungaro, Ivana d'Angelo, Carmen De Caro, Roberto Russo, Giuseppe Blaiotta, Fabrizio Dal Piaz, Antonio Calignano, Agnese Miro
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...
March 8, 2018: International Journal of Pharmaceutics
Vincent Mazel, Harona Diarra, Jérôme Malvestio, Pierre Tchoreloff
Capping and lamination are common industrial problems during the manufacturing of pharmaceutical tablets. Even if they are commonly treated together, these phenomena correspond to different failure patterns of the tablet and, as a consequence, to different mechanisms of cracking. In this work, a specific case of lamination of biconvex tablets was studied. It corresponds to a breakage into two parts of the tablets along a failure plan normal to the compression direction and located approximately at the center of the tablet band...
March 8, 2018: International Journal of Pharmaceutics
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 could be explained by its large molecular size. Three batches of CX microparticles with different mean size were prepared...
March 8, 2018: International Journal of Pharmaceutics
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 of dopamine under oxidative, weakly basic conditions. Lysozyme was bound via coacervation and hydrogen bonding into HADA/PDA complexes...
March 7, 2018: International Journal of Pharmaceutics
Takashi Otaki, Yuta Tanabe, Takashi Kojima, Masaru Miura, Yukihiro Ikeda, Tatsuo Koide, Toshiro Fukami
In recent years, to guarantee a quality-by-design approach to the development of pharmaceutical products, it is important to identify properties of raw materials and excipients in order to determine critical process parameters and critical quality attributes. Feedback obtained from real-time analyses using various process analytical technology (PAT) tools has been actively investigated. In this study, in situ monitoring using low-frequency (LF) Raman spectroscopy (10-200cm-1 ), which may have higher discriminative ability among polymorphs than near-infrared spectroscopy and conventional Raman spectroscopy (200-1800 cm-1 ), was investigated as a possible application to PAT...
March 7, 2018: International Journal of Pharmaceutics
Basanth Babu Eedara, Bhamini Rangnekar, Colin Doyle, Alex Cavallaro, Shyamal C Das
Pharmacotherapy of tuberculosis is potentially more efficient when delivered by the inhaled route than by the current oral and/or parenteral routes due to the higher concentration of drug reaching the primary region of infection in the lungs. This study investigated the influence of the amino acid L-leucine alone and in combination with the phospholipid, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), on the aerosolization behaviour of the anti-TB drugs, pyrazinamide and moxifloxacin HCl. Spray dried powders of pyrazinamide (P), moxifloxacin (M) alone and in combination with 10% L-leucine (PL and ML) and 10% DPPC (PLD and MLD) were produced...
March 7, 2018: International Journal of Pharmaceutics
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 transformation time τ(T), and a characteristic size ξ(T)...
March 3, 2018: International Journal of Pharmaceutics
Elodie Czuba, Mouhamadou Diop, Carole Mura, Anais Schaschkow, Allan Langlois, William Bietiger, Romain Neidl, Aurélien Virciglio, Nathalie Auberval, Diane Julien-David, Elisa Maillard, Yves Frere, Eric Marchioni, Michel Pinget, Séverine Sigrist
Oral administration of insulin increases patient comfort and could improve glycemic control thanks to the hepatic first passage. However, challenges remain. The current approach uses poly (D, lactic-co-glycolic) acid (PLGA) nanoparticles (NPs), an effective drug carrier system with a long acting profile. However, this system presents a bioavailability of less than 20% for insulin encapsulation. In this context, physico-chemical parameters like surface charge could play a critical role in NP uptake by the intestinal barrier...
February 28, 2018: International Journal of Pharmaceutics
Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
Nattika Nimmano, Satynarayana Somavarapu, Kevin M G Taylor
Erlotinib and genistein co-loaded liposomes were prepared by the thin-film hydration method. The effect of probe sonication as a size reduction method on drug incorporation and the properties of aerosols generated using air-jet and vibrating-mesh nebulisers was studied. The use of the Next Generation Impactor (NGI) to characterise inhaler formulations is limited by the need accurately to quantify drug deposited across 8 stages and is labour intensive to use. The Fast Screening Impactor (FSI) comprising two impaction stages was compared with the NGI to evaluate its applicability as a simple screening and labour-saving tool to characterise nebulised systems...
February 26, 2018: International Journal of Pharmaceutics
Birendra Chaurasiya, Liping Huang, Yunai Du, Baoqiang Tang, Zijie Qiu, Li Zhou, Jiasheng Tu, Chunmeng Sun
In this study, we prepared paclitaxel (PTX) loaded bovine serum albumin (BSA) microparticles (MPs) of different sizes (0.5, 1.0, and 3.0 µm) and converted them into dry powders (DPs) of a uniform size (∼5.0 µm) through spray-drying techniques. The aim of preparing different sized PTX-MPs is to investigate the size-based in vivo biodistribution and retention of PTX in the lungs after intratracheal administration. Following the in vitro characterizations, the anti-tumor efficacy of the DPs containing differently sized PTX-BSA-MPs administered through intratracheal insufflation was compared with intravenously administered PTX solution (Taxol)...
February 26, 2018: International Journal of Pharmaceutics
Takumi Asada, Naoki Yoshihara, Yasushi Ochiai, Shin-Ichiro Kimura, Yasunori Iwao, Shigeru Itai
Water-soluble polymers with high viscosity are frequently used in the design of sustained-release formulations of poorly water-soluble drugs to enable complete release of the drug in the gastrointestinal tract. Tablets containing matrix granules with a water-soluble polymer are preferred because tablets are easier to handle and the multiple drug-release units of the matrix granules decreases the influences of the physiological environment on the drug. However, matrix granules with a particle size of over 800 μm sometimes cause a content uniformity problem in the tableting process because of the large particle size...
February 26, 2018: International Journal of Pharmaceutics
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