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

Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes: An approach for improved oral pharmacokinetics of Sorafenib
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Muhammad Adeeb Khan, Shaukat Ali, Subbu S. Venkatraman, Muhammad Farhan Sohail, Muhammad Ovais, Abida Raza Sorafenib (SFN), a hydrophobic anticancer drug, has several limitations predominantly poor aqueous solubility and hepatic first-pass effect, limiting its oral delivery that results into several other complications. Present study aims to develop Sorafenib loaded polymersomes using poly butadiene block poly ethylene oxide (PB-b-PEO), an amphiphilic co-block polymer. Prior to drug loading, critical aggrega...
Source: International Journal of Pharmaceutics - March 19, 2018 Category: Drugs & Pharmacology Source Type: research

ε-Poly-l-Lysine/plasmid DNA nanoplexes for efficient gene delivery in vivo
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Haimanti Mandal, Sameer S. Katiyar, Rajan Swami, Varun Kushwah, Parmeshwar B. Katare, Anand Kumar Meka, Sanjay K. Banerjee, Amirali Popat, Sanyog Jain The present work addresses the development and characterization of ε-Poly-l-Lysine/pDNA polyplexes and evaluation for their improved transfection efficacy and safety as compared to polyplexes prepared using Poly-l-Lysine and SuperFect®. Self-assembling polyplexes were prepared by varying the N/P ratio to obtain the optimum size, a net positive zeta...
Source: International Journal of Pharmaceutics - March 16, 2018 Category: Drugs & Pharmacology Source Type: research

Development of itaconic acid-based molecular imprinted polymers using supercritical fluid technology for pH-triggered drug delivery
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Gonçalo Marcelo, Inês C. Ferreira, Raquel Viveiros, Teresa Casimiro A novel pH-responsive molecularly imprinted polymer (MIP) based on Itaconic acid:Ethylene glycol dimethacrylate was developed as a potential body-friendly oral drug delivery system for metronidazole (MZ), a pH-independent drug. MIP performance was evaluated in a simulated oral administration situation, at pHs 2.2 and 7.4. Itaconic acid-based copolymers were synthesized using two different molar ratios of template:monomer:crossli...
Source: International Journal of Pharmaceutics - March 16, 2018 Category: Drugs & Pharmacology Source Type: research

Zaleplon loaded bi-layered chronopatch: A novel buccal chronodelivery approach to overcome circadian rhythm related sleep disorder
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): 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 granule...
Source: International Journal of Pharmaceutics - March 14, 2018 Category: Drugs & Pharmacology Source Type: research

Novel medium-throughput technique for investigating drug-cyclodextrin complexation by pH-metric titration using the partition coefficient method
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): 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 ...
Source: International Journal of Pharmaceutics - March 14, 2018 Category: Drugs & Pharmacology Source Type: research

Size-based anti-tumoral effect of paclitaxel loaded albumin microparticle dry powders for inhalation to treat metastatic lung cancer in a mouse model
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 intravenou...
Source: International Journal of Pharmaceutics - March 14, 2018 Category: Drugs & Pharmacology Source Type: research

Endothelial progenitor cell secretome delivered by novel polymeric nanoparticles in ischemic hindlimb
In this study we use novel nanoparticles (NPs) as carriers for a controlled release of EPC secretome (CM) to improve their angiogenic properties. The in 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. Moreover, hypoxic EPC-CM significantly promoted capillary-like structures on Matrigel. A significant increase of blood perfusion in ischemic limbs at 2 wee...
Source: International Journal of Pharmaceutics - March 14, 2018 Category: Drugs & Pharmacology Source Type: research

The influence of surface active l-leucine and 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) in the improvement of aerosolization of pyrazinamide and moxifloxacin co-spray dried powders
In conclusion, the differences in the aerosolization behaviours of the pyrazinamide and moxifloxacin spray dried powders with and without excipients was a combination of difference in the surface morphology and surface composition. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 14, 2018 Category: Drugs & Pharmacology Source Type: research

Lamination of biconvex tablets: Numerical and experimental study
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): 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 p...
Source: International Journal of Pharmaceutics - March 13, 2018 Category: Drugs & Pharmacology Source Type: research

In situ monitoring of cocrystals in formulation development using low-frequency Raman spectroscopy
In this study, in situ monitoring using low-frequency (LF) Raman spectroscopy (10–200 cm−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. This is because LF-Raman spectroscopy obtains information about intermolecular and/or lattice vibrations in the solid state. The monitoring results obtained from Furosemide/Nicotinamide cocrystal indicate that LF-Raman spectroscopy is applicable to in situ monitoring of suspension and fluidized bed granulation...
Source: International Journal of Pharmaceutics - March 13, 2018 Category: Drugs & Pharmacology Source Type: research

Oral insulin delivery, the challenge to increase insulin bioavailability: Influence of surface charge in nanoparticle system
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): 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 effect...
Source: International Journal of Pharmaceutics - March 9, 2018 Category: Drugs & Pharmacology Source Type: research

Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation
In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 9, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced dissolution of solid dispersions containing bicalutamide subjected to mechanical stress
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Joanna Szafraniec, Agata Antosik, Justyna Knapik-Kowalczuk, Krzysztof Chmiel, Mateusz Kurek, Karolina Gawlak, Marian Paluch, Renata Jachowicz The anticancer drug bicalutamide was co-milled with either Macrogol 6000 or Poloxamer 407, and the physicochemical parameters that drive the phase transition of binary systems and influence the dissolution modification of bicalutamide were studied. Milled binary systems with reduced particle size were assessed by scanning electron microscopy and laser diffraction measu...
Source: International Journal of Pharmaceutics - March 8, 2018 Category: Drugs & Pharmacology Source Type: research

Aerosol characterisation of nebulised liposomes co-loaded with erlotinib and genistein using an abbreviated cascade impactor method
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): 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 intensiv...
Source: International Journal of Pharmaceutics - March 6, 2018 Category: Drugs & Pharmacology Source Type: research

Manufacturing and ambient stability of shelf freeze dried bacteriophage powder formulations
Publication date: 5 May 2018 Source:International Journal of Pharmaceutics, Volume 542, Issues 1–2 Author(s): Yajie Zhang, Xiujuan Peng, Hairui Zhang, Alan B. Watts, Debadyuti Ghosh The severity of multidrug resistance to antibiotics has urged development of alternative treatment approaches, including bacteriophage therapy. Given the complexity of the bacteriophage structure, formulation and stability are primary concerns. Our present work optimized process and formulations of phage powder manufacturing and investigated the stability of lyophilized bacteriophage powders under ambient storage. The model phage M13 was...
Source: International Journal of Pharmaceutics - March 6, 2018 Category: Drugs & Pharmacology Source Type: research

Monitoring of multiple solvent induced form changes during high shear wet granulation and drying processes using online Raman spectroscopy
In conclusion, it was possible to simultaneously monitor the three forms in real time during wet granulation and drying using online Raman spectroscopy. The results regarding the effect of process parameters on the degree of transformation are critical for designing a robust process that ensures a consistent form in the final drug product. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 5, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation of a poorly water-soluble drug in sustained-release hollow granules with a high viscosity water-soluble polymer using a fluidized bed rotor granulator
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): 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 th...
Source: International Journal of Pharmaceutics - March 5, 2018 Category: Drugs & Pharmacology Source Type: research

Impact of formulation pH on physicochemical protein characteristics at the liquid-air interface
In this study, the impact of pH on the liquid-air interfacial behavior of three proteins, a polyclonal and two monoclonal antibodies (IgG, mAB1 and mAB2) was investigated using different surface sensitive methods. Equilibrium surface pressure values revealed only a minor impact of pH. Infrared Reflectance Absorbance Spectroscopy (IRRAS) proved not only the presence of the proteins at the interface but also showed that the secondary structure was not considerably affected by the adsorption to the interface independent of pH between pH 3 and 9. Additionally, the physical resistance of the film as determined by the interfacia...
Source: International Journal of Pharmaceutics - March 2, 2018 Category: Drugs & Pharmacology Source Type: research

Human serum albumin nanoparticles for ocular delivery of bevacizumab
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Inés Luis de Redín, Carolina Boiero, María Cristina Martínez-Ohárriz, Maite Agüeros, Rocío Ramos, Iván Peñuelas, Daniel Allemandi, Juan M. Llabot, Juan M. Irache Bevacizumab-loaded nanoparticles (B-NP) were prepared by a desolvation process followed by freeze-drying, without any chemical, physical or enzymatic cross-linkage. Compared with typical HSA nanoparticles cross-linked with glutaraldehyde (B-NP-GLU), B-NP displayed a significantly higher...
Source: International Journal of Pharmaceutics - February 28, 2018 Category: Drugs & Pharmacology Source Type: research

Dual-effect liposomes with increased antitumor effects against 67-kDa laminin receptor-overexpressing tumor cells
In conclusion, EPL appear to have superior antitumor activity against high 67LR-expressing tumor cells, as the liposomes had dual effects, namely antitumor effects due to the loaded DOX and apoptosis induced by the bound EGCG. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 28, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of a semi-batch tablet coating process for a continuous manufacturing line by design of experiments
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Shirin Barimani, Rok Šibanc, Peter Kleinebudde The aim of the study was to optimize a tablet coating process for a continuous manufacturing line. High throughputs should be achieved while inter-tablet coating variability should be as small as possible. Drug-free cores were coated with a colored suspension. All processes were monitored in-line with Raman spectroscopy. A statistical design of experiment was performed to find optimum process parameters. Tablet loading, spray rate and drum rotation spe...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro stabilization and in vivo improvement of ocular pharmacokinetics of the multi-therapeutic agent baicalin: Delineating the most suitable vesicular systems
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Orchid Ashraf, Maha Nasr, Marianne Nebsen, Azza Mohamed Ahmed Said, Omaima Sammour Baicalin is a multi-purpose flavonoid used in the treatment of different ocular diseases. Owing to its poor stability in basic pH and its poor solubility, a suitable carrier system is needed to enhance its ocular therapeutic potential. Therefore, the objective of this work was to prepare and contrast different baicalin vesicular systems; namely liposomes, penetration enhancer vesicles PEVs and transfersomes. Results reveale...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Quantitative estimation of phenytoin sodium disproportionation in the formulations using vibration spectroscopies and multivariate methodologies
In conclusion, chemometric models based on NIR and Raman spectroscopies provides a fast and easy way to monitor the disproportionation of PS in the drug products. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Membrane properties for permeability testing: Skin versus synthetic membranes
In this study, the permeability of human skin was compared using two synthetic membranes: cellulose acetate and Strat-M® membrane and lipophilic and hydrophilic compounds either as saturated or formulated solutions as well as marketed dosage forms. Our data suggests that hydrophilic compounds have higher permeation in Strat-M membranes compared with lipophilic ones. High variation in permeability values, a typical property of biological membranes, was not observed with Strat-M. In addition, the permeability of Strat-M was closer to that of human skin than that of cellulose acetate (CA > Strat-M > ...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Statistical Design of Experiment (DoE) based development and optimization of DB213 in situ thermosensitive gel for intranasal delivery
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Qianwen Wang, Chun-Ho Wong, H.Y. Edwin Chan, Wai-Yip Lee, Zhong Zuo DB213 is an HIV-1 replication inhibitor targeting the Central Nervous System for the treatment of HIV-associated neurocognitive disorders. Current study aims to develop an in situ thermosensitive gelling system for intranasal delivery of DB213 facilitated by Statistical Design of Experiment (DoE) to conduct a more efficient experimentation by extracting the maximum amount of information from limited experiments. In our current study, info...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

When drugs plasticize film coatings: Unusual formulation effects observed with metoprolol and Eudragit RS
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Youness Karrout, Florence Siepmann, Youcef Benzine, Laurent Paccou, Yannick Guinet, Alain Hedoux, Juergen Siepmann Metoprolol tartrate and metoprolol free base loaded pellet starter cores were coated with Eudragit RS, plasticized with 25% triethyl citrate (TEC). The initial drug loading and coating level were varied from 10 to 40 and 0 to 20%, respectively. Drug release was measured in 0.1 N HCl and phosphate buffer pH 7.4. The water uptake and swelling kinetics, mechanical properties and TEC leaching o...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Mechanochemical effect on swelling and drug release of natural polymer matrix tablets by X-ray computed tomography
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Yusuke Hattori, Tomomi Takaku, Makoto Otsuka The relationships between the physicochemical properties of milled starch and drug release from tablets were investigated quantitatively using a drug release kinetic method and X-ray computed tomography (XCT). The samples were prepared from raw β-starch by milling in a planetary ball mill. The tablets, containing 5% theophylline (TH), 94% milled starch, and 1% magnesium stearate, were compressed at 6 kN. The drug-release and gel-forming processes were me...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of surfactant-based permeation enhancers on mannitol permeability, histology, and electrogenic ion transport responses in excised rat colonic mucosae
This study examined the interaction of a test panel of surfactant-based PEs with isolated rat colonic mucosae mounted in Ussing chambers in an attempt to determine if increases in transepithelial permeability can be separated from induction of mucosal perturbation. The aim was to assess the effects of PEs on (i) apparent permeability coefficient (Papp) of [14C]-mannitol (ii) histology score and (iii) short-circuit current (ΔIsc) responses to a cholinomimetic (carbachol, CCh). Enhancement ratio increases for Papp values followed the order: C10 > C9 = C11:1 > a bile salt blend > sod...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

The relevance of shear, sedimentation and diffusion during spin freezing, as potential first step of a continuous freeze-drying process for unit doses
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Joris Lammens, Séverine Thérèse F.C. Mortier, Laurens De Meyer, Brecht Vanbillemont, Pieter-Jan Van Bockstal, Simon Van Herck, Jos Corver, Ingmar Nopens, Valérie Vanhoorne, Bruno G. De Geest, Thomas De Beer, Chris Vervaet Recently, a continuous freeze-drying process for the production of unit doses was presented and evaluated. In this concept, the freezing step is modified compared to traditional batch freeze-drying, as glass vials filled with a liquid formulation, are rotated ...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Inorganic nanoparticles: A potential cancer therapy for human welfare
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Arivalagan Pugazhendhi, Thomas Nesakumar Jebakumar Immanuel Edison, Indira Karuppusamy, Brindhadevi Kathirvel Cancer is an abnormal condition leading to uncontrolled cell division which causes damage to the body tissues. Around 100 types of cancer are studied so far namely breast cancer, lung cancer, skin cancer, prostate cancer, colon cancer and lymphoma. Major cancer therapies include chemotherapy, surgery and radiations but their major drawbacks are non-specifically distributed antitumor agents, uneven...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Interdependence of particle properties and bulk powder behavior of indomethacin in quench-cooled molten two-phase solid dispersions
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Kristian Semjonov, Maia Salm, Tiina Lipiäinen, Karin Kogermann, Andres Lust, Ivo Laidmäe, Osmo Antikainen, Clare J. Strachan, Henrik Ehlers, Jouko Yliruusi, Jyrki Heinämäki Solid dispersions (SDs) hold a proven potential in formulating poorly water-soluble drugs. The present paper investigates the interfacial phenomena associated with the bulk powder flow, water sorption, wetting and dissolution of the SDs prepared by a modified melt and quench-cooling (QC) method. Poorly water-soluble...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

Buccal drug delivery technologies for patient-centred treatment of radiation-induced xerostomia (dry mouth)
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Osamah S. Malallah, Cristina M. Aller Garcia, Gordon B. Proctor, Ben Forbes, Paul G. Royall Radiotherapy is a life-saving treatment for head and neck cancers, but almost 100% of patients develop dry mouth (xerostomia) because of radiation-induced damage to their salivary glands. Patients with xerostomia suffer symptoms that severely affect their health as well as physical, social and emotional aspects of their life. The current management of xerostomia is the application of saliva substitutes or systemic ...
Source: International Journal of Pharmaceutics - February 25, 2018 Category: Drugs & Pharmacology Source Type: research

Relationships between surface coverage ratio and powder mechanics of binary adhesive mixtures for dry powder inhalers
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Jonas Rudén, Göran Frenning, Tobias Bramer, Kyrre Thalberg, Göran Alderborn The aim of this paper was to study relationships between the content of fine particles and the powder mechanics of binary adhesive mixtures and link these relationships to the blend state. Mixtures with increasing amounts of fine particles (increasing surface coverage ratios (SCR)) were prepared using Lactopress SD as carrier and micro particles of lactose as fines (2.7 µm). Indicators of unsettled bulk de...
Source: International Journal of Pharmaceutics - February 24, 2018 Category: Drugs & Pharmacology Source Type: research