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Development of solidified self-microemulsifying drug delivery systems containing l-tetrahydropalmatine: Design of experiment approach and bioavailability comparison
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Nguyen-Thach Tung, Cao-Son Tran, Thi-Minh-Hue Pham, Hoang-Anh Nguyen, Tran-Linh Nguyen, Sang-Cheol Chi, Dinh-Duc Nguyen, Thi-Bich-Huong Bui The study first aimed to apply a design of experiment (DoE) approach to investigate the influences of excipients on the properties of liquid self-microemulsifying drug delivery system (SMEDDS) and SMEDDS loaded in the pellet (pellet-SMEDDS) containing l-tetrahydropalmatine (l-THP). Another aim of the study was to compare the bioavailability of l-THP suspension, liq...
Source: International Journal of Pharmaceutics - December 15, 2017 Category: Drugs & Pharmacology Source Type: research

Point of use production of liposomal solubilised products
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Swapnil Khadke, Peter Stone, Aleksey Rozhin, Jerome Kroonen, Yvonne Perrie With the progression towards personalised and age-appropriate medicines, the production of drug loaded liposomes at the point of care would be highly desirable. In particular, liposomal solubilisation agents that can be produced rapidly and easily would provide a new option in personalised medicines. Such a process could also be used as a rapid tool for the formulation and pre-clinical screening of low soluble drugs. Within this...
Source: International Journal of Pharmaceutics - December 14, 2017 Category: Drugs & Pharmacology Source Type: research

Conductive vancomycin-loaded mesoporous silica polypyrrole-based scaffolds for bone regeneration
In this study, we have developed bone scaffolds composed of hydroxyapaptite (HAp), gelatin and mesoporous silica, all recognized as promising materials in bone tissue engineering due to favorable biocompatibility, osteoconductivity and drug delivery potential, respectively. These materials were coupled with conductive polypyrrole (PPy) polymer to create a novel bone scaffold for regenerative medicine. Conductive and non-conductive scaffolds were made by slurry casting method and loaded with a model antibiotic, vancomycin (VCM). Their properties were compared in different experiments in which scaffolds containing PPy showed...
Source: International Journal of Pharmaceutics - December 6, 2017 Category: Drugs & Pharmacology Source Type: research

Multivariate modeling of diffuse reflectance infrared fourier transform (DRIFT) spectra of mixtures with low-content polymorphic impurities with analysis of outliers
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Slobodan Šašić, Andrew Gilkison, Mark Henson Diffuse Reflectance Fourier Transform Infrared Spectroscopy (DRIFTS)-based multivariate models were developed to quantify the content of two polymorphic impurities in mixtures with the desired active pharmaceutical ingredient (API) form, with the impurities not exceeding 2% wt/wt. In addition, close attention was paid to the outlier detection criteria: Q residuals; Hotelling T2; and score bi-plot. While reasonably accurate results were obtained for the ...
Source: International Journal of Pharmaceutics - December 6, 2017 Category: Drugs & Pharmacology Source Type: research

The efficiency and mechanism of N-octyl-O, N-carboxymethyl chitosan-based micelles to enhance the oral absorption of silybin
This study demonstrates the preparation of a silybin-loaded N-octyl-O, N-carboxymethyl chitosan micelle (OCC-SLB) to enhance the oral absorption efficiency of silybin (SLB) and investigate the related mechanisms of enhancement. Firstly, the physicochemical properties of OCC and OCC-SLB micelles, including critical micelle concentration (CMC), particle size, zeta potential, drug-loading, etc., were determined. Results of pharmacokinetic studies on rats then confirmed a desirable enhancement in the oral bioavailability of SLB by OCC-SLB micelles compared with a stock SLB suspension solution. Subsequently, uptake studies on t...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Mesoporous systems for poorly soluble drugs – recent trends
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Joakim Riikonen, Wujun Xu, Vesa-Pekka Lehto When poor aqueous solubility of active pharmaceutical ingredients is encountered during a drug formulation process, the toolbox typically utilized contains pharmaceutical salts, co-crystals, solid dispersions, cyclodextrins, lipids, liposomes and nanocrystals etc. Especially in the pharmaceutical industry, the option which confers the greatest benefit with the lowest risk is usually chosen. Several factors affect the final decision, but new technologies should also be ...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Novel sulforaphane-enabled self-microemulsifying delivery systems (SFN-SMEDDS) of taxanes: Formulation development and in vitro cytotoxicity against breast cancer cells
This study highlighted the unique properties of SFN and its potential use in reformulating taxanes with high drug load and significantly lower excipient content than the commercial products. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Multivariate analysis for the optimization of microfluidics-assisted nanoprecipitation method intended for the loading of small hydrophilic drugs into PLGA nanoparticles
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): E. Chiesa, R. Dorati, T. Modena, B. Conti, I. Genta Design of Experiment-assisted evaluation of critical process (total flow rate, TFR, flow rate ratio, FRR) and formulation (polymer concentration and structure, drug:polymer ratio) variables in a novel microfluidics-based device, a staggered herringbone micromixer (SHM), for poly(lactic-co-glycolic acid) copolymer (PLGA) nanoparticles (NPs) manufacturing was performed in order to systematically evaluate and mathematically describe their effects on NPs sizes and ...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

HPMA copolymer conjugate with pirarubicin: In vitro and ex vivo stability and drug release study
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Waliul Islam, Jun Fang, Tomas Etrych, Petr Chytil, Karel Ulbrich, Akihiro Sakoguchi, Katsuki Kusakabe, Hiroshi Maeda We have developed a tumor environment-responsive polymeric anticancer prodrug containing pirarubicin (THP) conjugated to N-(2-hydroxypropyl) methacrylamide copolymer (PHPMA), [P-THP], through a spacer containing pH-sensitive hydrazone bond, that showed remarkable therapeutic effect against various tumor models and in a human pilot study. Toward clinical development, here we report THP release prof...
Source: International Journal of Pharmaceutics - November 29, 2017 Category: Drugs & Pharmacology Source Type: research

Liposomes encapsulating native and cyclodextrin enclosed paclitaxel: Enhanced loading efficiency and its pharmacokinetic evaluation
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Priyanka Bhatt, Rohan Lalani, Imran Vhora, Sushilkumar Patil, Jitendra Amrutiya, Ambikanandan Misra, Rajashree Mashru Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded PEGylated liposomes (DLPLs) containing PTX and PTX-DMβCD complex were prepared by thin film hydration. Physicochemical characterization of comp...
Source: International Journal of Pharmaceutics - November 29, 2017 Category: Drugs & Pharmacology Source Type: research

Rational design of polysorbate 80 stabilized human serum albumin nanoparticles tailored for high drug loading and entrapment of irinotecan
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Neetika Taneja, Kamalinder K. Singh Human serum albumin (HSA) nanoparticles are considered to be versatile carrier of anticancer agents in efficiently delivering the drug to the tumor site without causing any toxicity. The aim of the study was to develop stable HSA nanoparticles (NPs) of drug irinotecan (Iro) having slightly water solubility and moderate HSA binding. A novel strategy of employing a hydrophilic non-ionic surfactant polysorbate 80 which forms protein-polysorbate 80 complex with increased affinity ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Nanoparticle-loaded hydrogels as a pathway for enzyme-triggered drug release in ophthalmic applications
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Michelle Åhlén, Gopi Krishna Tummala, Albert Mihranyan The aim of this study was to develop nanoparticle loaded hydrogel based contact lenses that could be used for ocular drug delivery. Two potential contact lens platforms for controlled ophthalmic drug delivery were developed by incorporating chitosan-poly (acrylic acid) nanoparticles into polyvinyl alcohol (PVA) hydrogels and in-situ gelled nanoparticles and cellulose nanocrystals (CNC) in PVA lenses. The nanoparticles were shown to disintegrate ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Reclaiming hijacked phagosomes: Hybrid nano-in-micro encapsulated MIAP peptide ensures host directed therapy by specifically augmenting phagosome-maturation and apoptosis in TB infected macrophage cells
We describe the potential of nano-encapsulated synthetic Magainin-I analog peptide (MIAP) as Host Directed Therapy against TB. Micron-sized inhalable platform “Porous Nanoparticle Aggregates Particles (PNAP)” with nano-scale physiognomies were developed to improve the delivery of MIAP-peptide to the lungs and enhance its stability. This particle engineering enabled more control over aerodynamic characteristics and bioactive release. Antimicrobial and mechanistic studies were carried out against virulent H37Rv TB bacteria. These MIAP-PNAP nano-assemblies demonstrated dose and time dependent antibacterial action ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Failure of active targeting by a cholesterol-anchored ligand and improvement by altering the lipid composition to prevent ligand desorption
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Shoshiro Yamamoto, Yu Sakurai, Hideyoshi Harashima Although anti-angiogenic therapy is predicted to be an effective therapy for treating cancer, selectively targeting tumor endothelial cells (TECs), and not normal endothelial cells, remains a major obstacle. Modifying a drug carrier with a targeting ligand is a popular strategy for developing an active-targeting type drug delivery system (DDS). We previously reported that a cyclo(Arg-Gly-Asp-D-Phe-Lys) (cRGD)-equipped liposome that contains encapsulated siRNA (R...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained-release multiparticulates for oral delivery of a novel peptidic ghrelin agonist: Formulation design and in vitro characterization
This study describes the generation of a high load capacity pellet formulation for sustained release of a freely water-soluble dairy-derived hydrolysate, FHI-2571. The activity of this novel peptidic ghrelin receptor agonist is reported using in vitro calcium mobilization assays. Conventional extrusion spheronization was then used to prepare peptide-loaded pellets which were subsequently coated with ethylcellulose (EC) film coats using a fluid bed coating system in bottom spray (Wurster) mode. Aqueous-based EC coating dispersions produced mechanically brittle coats which fractured due to osmotic pressure build-up within pe...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

A simple and rapid measurement method of encapsulation efficiency of doxorubicin loaded liposomes by direct injection of the liposomal suspension to liquid chromatography
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Eiichi Yamamoto, Shota Miyazaki, Chiaki Aoyama, Masaru Kato A simple and rapid chromatographic measurement method for determining doxorubicin (DOX) encapsulation efficiency (EE) into PEGylated liposomes using nanoparticle exclusion chromatography (nPEC) was developed. In this work, Doxil® and two PEGylated liposomes spiked with DOX were employed as model liposomes, and unencapsulated DOX was measured by high performance liquid chromatography with diode-array detector using an N-vinylpyrrolidone modified nPEC...
Source: International Journal of Pharmaceutics - November 26, 2017 Category: Drugs & Pharmacology Source Type: research

Temperature-sensitive copolymer-coated fluorescent mesoporous silica nanoparticles as a reactive oxygen species activated drug delivery system
In this study, a temperature and ROS-responsive drug delivery system ROSP@MSN based on mesoporous silica nanoparticles has been designed and synthesized by taking advantage of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acrylate modified polymers (ROSP) as “nano-valve”, which can respond selectively to cancer exclusive microenvironment and implement targeted drug release. Due to the superior temperature-sensitive properties of ROSP, ROSP@MSN could achieve cargo loading in cold water, and subsequently close the pore by raising temperature to obtain ROSP@MSN@DOX. Upon the stimulus of ROS, ROSP@MSN@DOX s...
Source: International Journal of Pharmaceutics - November 25, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced glioma therapy by synergistic inhibition of autophagy and tyrosine kinase activity
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Xuhui Wang, Yue Qiu, Qianwen Yu, Hui Li, Xiaoxiao Chen, Man Li, Yang Long, Yayuan Liu, Libao Lu, Jiajing Tang, Zhirong Zhang, Qin He Autophagy is a lysosomal degradation pathway that acts as a cytoprotective mechanism causing treatment resistance in various cancer cells. Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor. However, the nonselective distribution of ZD6474 in vivo and the low ...
Source: International Journal of Pharmaceutics - November 25, 2017 Category: Drugs & Pharmacology Source Type: research

Lipid coated chitosan-DNA nanoparticles for enhanced gene delivery
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Elias Baghdan, Shashank Reddy Pinnapireddy, Boris Strehlow, Konrad H. Engelhardt, Jens Schäfer, Udo Bakowsky Chitosan as a polycationic non-viral vector for gene delivery has the advantage of being a biocompatible and biodegradable polymer. However, without laborious chemical modifications to its structure, it is of limited use as a gene delivery vehicle due to its low ability to efficiently transfect under physiological conditions. To address this problem, we developed novel liposome encapsulated ...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Incorporation of surface-modified dry micronized poorly water-soluble drug powders into polymer strip films
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Lu Zhang, Yidong Li, Manal Abed, Rajesh N. Davé Recent work has established polymer strip films as a robust platform for delivery of poorly water-soluble drugs via slurry casting, in particular using stable drug nanosuspensions. Here, a simpler, robust method to directly incorporate dry micronized poorly water-soluble drug, fenofibrate (FNB), is introduced. As a major novelty, simultaneous surface modification using hydrophilic silica along with micronization was done using fluid energy mill (FEM...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Protein-alginate complexes as pH-/ion-sensitive carriers of proteins
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Vida Rahmani, Heather Sheardown Protein-alginate complexes were prepared with the objective of quantifying the influence of the parameters such as protein characteristics on the final complex properties and their dissociation rates. Cytochrome C, lysozyme, myoglobin, chymotrypsin, and bovine serum albumin were used as model proteins for preparing the complexes and physical properties such as composition, average diameter, and zeta potential of the complexes formed were measured. In addition, protein rel...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Polymer-based nanoparticles loaded with a TLR7 ligand to target the lymph node for immunostimulation
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Jérôme Widmer, Cédric Thauvin, Inès Mottas, Van Nga Nguyen, Florence Delie, Eric Allémann, Carole Bourquin Small-molecule agonists for the Toll-like receptors (TLR) 7 and 8 are effective for the immunotherapy of skin cancer when used as topical agents. Their systemic use has however been largely unsuccessful due to dose-limiting toxicity. We propose a polymer-based nanodelivery system to target resiquimod, a TLR7 ligand, to the lymph node in order to focus the immunosti...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring gold nanoparticles interaction with mucins: A spectroscopic-based study
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Nadia Barbero, Martina Coletti, Federico Catalano, Sonja Visentin The interaction between two mucin types (mucin from porcine stomach – PGM and mucin from bovine submaxillary glands – BSM) and gold nanoparticles (GNPs) of various size (5, 20 and 40 nm) and functionalization (with cysteamine or thioglycolic acid) was studied under physiological conditions, in order to investigate the affinity of the nanoparticles to the proteins. Different methods are employed to monitor the interactio...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Penta-block copolymer microspheres: Impact of polymer characteristics and process parameters on protein release
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Minh-Quan Le, Fabien Violet, Cédric Paniagua, Xavier Garric, Marie-Claire Venier-Julienne Here, we aimed to develop protein loaded microspheres (MSs) using penta-block PLGA-based copolymers to obtain sustained and complete protein release. We varied MS morphology and studied the control of protein release. Lysozyme was used as a model protein and MSs were prepared using the solid-in-oil-in-water emulsion solvent extraction method. We synthesized and studied various penta-block PLGA-based copolyme...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Anti-Adherent Biomaterials for Prevention of Catheter Biofouling
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Colin P. McCoy, Nicola J. Irwin, Louise Donnelly, David S. Jones, John G. Hardy, Louise Carson Medical device-associated infections present a leading global healthcare challenge, and effective strategies to prevent infections are urgently required. Herein, we present an innovative anti-adherent hydrogel copolymer as a candidate catheter coating with complementary hydrophobic drug-carrying and eluting capacities. The amphiphilic block copolymer, Poloxamer 188, was chemically-derivatized with methacryloyl...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Development and characterization of an organic solvent free, proliposomal formulation of Busulfan using quality by design approach
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Dhawal Chobisa, Ketan Patel, Jasmin Monpara, Mayank Patel, Pradeep Vavia Parenteral administration of Busulfan (BU) conquers the bioavailability and biovariability related issues of oral BU by maintaining the plasma drug concentration in therapeutic range with minimal fluctuations thereby significantly reducing the side effects. Busulfex® is the only commercially available parenteral formulation of BU composed of organic solvents N, N-dimethylacetamide and polyethylene glycol 400. Since, BU is highl...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Particle agglomeration of chitosan –magnesium aluminum silicate nanocomposites for direct compression tablets
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Rapee Khlibsuwan, Thaned Pongjanyakul Exfoliated nanocomposites of chitosan-magnesium aluminum silicate (CS-MAS) particles are characterized by good compressibility but poor flowability. Thus, the aims of this study were to investigate agglomerates of CS-MAS nanocomposites prepared using the agglomerating agents water, ethanol, or polyvinylpyrrolidone (PVP) for flowability enhancement and to evaluate the agglomerates obtained as direct compression fillers for tablets. The results showed that the additio...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Investigating cascade impactor performance using a modified 3D printed induction port
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Kai Berkenfeld, Michael Bernauer, Jason T. McConville, Alf Lamprecht Based on a computer tomographic scan of a human trachea, a modified induction port (mIP), for use with the Next Generation Cascade Impactor, was manufactured using 3D printing technology. Standard United States Pharmacopoeia IP (USPIP) was compared to the mIP and a 3D printed version of the USPIP (USP3DIP) by analyzing different types of commercial salbutamol formulations for inhalation. Increased retention of particles in the mIP was ...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Interactions between a poorly soluble cationic drug and sodium dodecyl sulfate in dissolution medium and their impact on in vitro dissolution behavior
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Zongyun Huang, Shuchi Parikh, William P. Fish In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The aim of this study is toevaluate the effects ofsodium dodecyl sulfate (SDS) mediated medium onthe dissolution behaviors of a poorly soluble cat...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Improvement of intestinal absorption of curcumin by cyclodextrins and the mechanisms underlying absorption enhancement
In this study, the effects of various cyclodextrins on the intestinal absorption of curcumin were evaluated in rat intestine by an in situ closed-loop method. Among the tested cyclodextrins, 50 mM α-cyclodextrin significantly enhanced the absorption of curcumin without inducing any intestinal toxicity. The analysis of cellular transport across Caco-2 cell monolayers showed that 50 mM α-cyclodextrin reduced the transepithelial electrical resistance value of cell monolayers and improved the permeability of 5(6)-carboxyfluorescein, a poorly absorbable drug, which is mainly transported via a paracellu...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Hyaluronan-decorated liposomes as drug delivery systems for cutaneous administration
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Silvia Franzé, Alessandro Marengo, Barbara Stella, Paola Minghetti, Silvia Arpicco, Francesco Cilurzo The work aimed to evaluate the feasibility to design hyaluronic acid (HA) decorated flexible liposomes to enhance the skin penetration of nifedipine. Egg phosphatidylcholine (e-PC) based transfersomes (Tween 80) and transethosomes (ethanol) were prepared. HA was reacted with 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (HA-DPPE) and two molar ratios (0.5 and 3%) of conjugate with respect to e...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Novel cremochylomicrons for improved oral bioavailability of the antineoplastic phytomedicine berberine chloride: Optimization and pharmacokinetics
In conclusion, berberine-loaded cremochylomicron could be considered as a promising nanoplatform for targeting lymphatic system and improving BER oral bioavailability with lower dose and side effects. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Cyclodextrins: structure, physicochemical properties and pharmaceutical applications
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Phatsawee Jansook, Noriko Ogawa, Thorsteinn Loftsson Since their discovery over 100 years ago cyclodextrins (CDs) have been the subject of numerous scientific publications. In 2016 alone CDs were the subject of over 2200 research articles published in peer-reviewed journals and mentioned in over 2300 patents and patent applications, many of which were on pharmaceutical applications. Natural CDs and their derivatives are used as enabling pharmaceutical excipients that enhance aqueous solubility of poorly...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

A novel formulation of [6]-gingerol: Proliposomes with enhanced oral bioavailability and antitumor effect
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Qilong Wang, Qiuyu Wei, Qiuxuan Yang, Xia Cao, Qiang Li, Feng Shi, Shan Shan Tong, Chunlai Feng, Qingtong Yu, Jiangnan Yu, Ximing Xu [6]-Gingerol, one of the components of the rhizome of Ginger, has a variety of biological activities such as anticoagulant, antioxidative, antitumor, anti-inflammatory, antihypertensive, and so forth. However, as one of the homologous phenolic ketones, [6]-gingerol is insoluble in water which limits its applications. Herein, we prepared [6]-gingerol proliposomes through mo...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

In-vitro and in-vivo cytotoxicity and efficacy evaluation of novel glycyl-glycine and alanyl-alanine conjugates of chitosan and trimethyl chitosan nano-particles as carriers for oral insulin delivery
Conclusion It seems that glycyl-glycine and alanyl-alanine conjugate nanoparticles of trimethyl chitosan have met the aim of this research work and have been able to orally deliver insulin with more than one mechanism in animal model. Hence, they are promising candidates for further research studies. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Investigating phase separation in amorphous solid dispersions via Raman mapping
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Christian Luebbert, Christian Klanke, Gabriele Sadowski The bioavailability of poorly-water-soluble active pharmaceutical ingredients (APIs) can be significantly improved by so-called amorphous solid dispersions (ASDs). However, the long-term stability of ASDs might be impaired by API recrystallization and/or amorphous phase separation (APS). So far, no methods have been reported to quantify APS in ASDs. In this work, phase-separation kinetics as well as the compositions of the two amorphous phases evol...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Oral hepatitis B vaccine: chitosan or glucan based delivery systems for efficient HBsAg immunization following subcutaneous priming
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Edna Soares, Sandra Jesus, Olga Borges The World Health Organization encourages “the development of oral formulations to simplify their transport, storage and administration in poor countries”, and to “facilitate an effective immunization program to prevent sexually transmitted hepatitis B”. Thus, two distinct and promising delivery systems were developed: recombinant hepatitis B surface antigen (HBsAg) encapsulated into alginate-coated chitosan particles (AlgChiPs) and into gluc...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and investigation of novel gastro-floating tablets with 3D extrusion-based printing
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Qijun Li, Xiaoying Guan, Mengsuo Cui, Zhihong Zhu, Kai Chen, Haoyang Wen, Danyang Jia, Jian Hou, Wenting Xu, Xinggang Yang, Weisan Pan Three dimensional (3D) extrusion-based printing is a paste-based rapid prototyping process, which is capable of building complex 3D structures. The aim of this study was to explore the feasibility of 3D extrusion-based printing as a pharmaceutical manufacture technique for the fabrication of gastro-floating tablets. Novel low-density lattice internal structure gastro-flo...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Orodispersible films: Product transfer from lab-scale to continuous manufacturing
In this study, a continuous coating machine was qualified in regards of the process conditions for film compositions and their effects on the formed films. To investigate differences between both manufacturing processes, various film formulations of hydrochlorothiazide and hydroxypropylcellulose (HPC) or hydroxypropylmethycellulose (HPMC) as film formers were produced and the resulting films were characterized. The qualification of the continuously operating coating machine reveals no uniform heat distribution during drying. Coating solutions for continuous manufacturing should provide at least a dynamic viscosity of 1&thi...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancement of tioconazole ungual delivery: Combining nanocapsule formulation and nail poration approaches
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Fernanda C. Flores, Wing Sin Chiu, Ruy C.R. Beck, Cristiane B. da Silva, M. Begoña Delgado-Charro This work investigated the impact of formulation including in vitro release profile, repeated dosing, and nail poration on the ex vivo nail delivery performance of antifungal formulations. Chitosan coated and uncoated tioconazole-loaded nanocapsules and a nano-based film-forming vehicle were assessed via in vitro release and in vitro permeation tests using an artificial membrane and human nail clippi...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the direct penetration into tissues underneath the skin with iontophoresis delivery of a ketoprofen cationic prodrug
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Shabbir Lobo, Guang Yan Current topical nonsteroidal anti-inflammatory drugs (NSAIDs) showed marginal efficacy in treatment of musculoskeletal disorders due to their fast clearance by skin blood flow and thus little direct penetration into the underlying muscle and joint tissues. Using ketoprofen (Kt) as a model NSAID and converting it to a cationic ester prodrug ketoprofen choline chloride (KCC), this study was to investigate the iontophoresis delivery of the prodrug KCC for improving the drug retentio...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

Mechanisms of drug release in pH-sensitive micelles for tumour targeted drug delivery system: A review
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Zhe Wang, Xiangping Deng, Jinsong Ding, Wenhu Zhou, Xing Zheng, Guotao Tang During the past decades, chemotherapy has been regarded as the most effective method for tumor therapy, but still faces significant challenges, such as poor tumor selectivity and multidrug resistance. The development of targeted drug delivery systems brings certain dramatic advantages for reducing the side effects and improving the therapeutic efficacy. Coupling a specific stimuli-triggered drug release mechanism with these deli...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research

A comprehensive approach to qualify and validate the essential parameters of an in vitro release test (IVRT) method for acyclovir cream, 5%
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Katrin I. Tiffner, Isadore Kanfer, Thomas Augustin, Reingard Raml, Sam G. Raney, Frank Sinner The rate of release of an active pharmaceutical ingredient (API) from a topical semisolid dosage form can be influenced by its physical and structural properties. An In Vitro Release Test (IVRT) is an established method to characterize this rate of API release and compare the underlying sameness in product quality characteristics. The purpose of this work was to validate an IVRT method to compare acyclovir crea...
Source: International Journal of Pharmaceutics - November 15, 2017 Category: Drugs & Pharmacology Source Type: research

Ampholytic starch excipients for high loaded drug formulations: Mechanistic insights
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Khalil Sakeer, Pompilia Ispas-Szabo, Nassim Benyerbah, Mircea Alexandru Mateescu Ampholytic starch derivatives are proposed as a new class of excipients carrying simultaneously anionic carboxymethyl (CM) and cationic aminoethyl (AE) groups on starch (St) polymeric chains. Three different types of derivatives were obtained by using the same reagents and varying only the order of their addition in the reaction medium: in one step method (OS) the two reactants were added simultaneously, whereas in two step...
Source: International Journal of Pharmaceutics - November 15, 2017 Category: Drugs & Pharmacology Source Type: research

Taste evaluation of a novel midazolam tablet for pediatric patients: In vitro drug dissolution, in vivo animal taste aversion and clinical taste perception profiles
This study utilized in vitro, in vivo and clinical data to evaluate the palatability of a novel midazolam chocolate tablet. In vitro dissolution experiments showed the crushed tablet to release within 5 min 1.68 mg of midazolam into simulated saliva. This translated to a drug level of 0.84 mg/ml in the oral cavity, which would be higher than the midazolam bitterness detection threshold concentration of 0.03 mg/ml determined in a rat ‘brief access taste aversion’ (BATA) model. The visual analogue scale scores of patients aged 4–16 years prescribed with midazolam pre-surgery show...
Source: International Journal of Pharmaceutics - November 12, 2017 Category: Drugs & Pharmacology Source Type: research

Biocompatible fluorinated poly( β-amino ester)s for safe and efficient gene therapy
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Jia-Hui Gong, Yi Wang, Lei Xing, Peng-Fei Cui, Jian-Bin Qiao, Yu-Jing He, Hu-Lin Jiang Cationic polymers have been widely used as one of the most promising non-viral vehicles for gene delivery due to their potential safety and ease of large-scale production. Here, we report the design and synthesis of a series of novel biodegradable fluorinated poly(β-amino ester)s (FPBAEs) by simple Michael-addition reaction as safe and efficient gene carrier. The results of transfection efficacy assay demonstrate...
Source: International Journal of Pharmaceutics - November 11, 2017 Category: Drugs & Pharmacology Source Type: research

Acyclovir chemical kinetics with the discovery and identification of newly reported degradants and degradation pathways involving formaldehyde as a degradant and reactant intermediate
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Bhanu C. Bejgum, Paul R. Johnson, William C. Stagner The purpose of this research was to determine acyclovir (ACV) acidic degradation kinetics which is relevant to gastric retentive device product design. A stability-indicating method revealed two unknown degradation products which have been identified by mass spectrometry as ACV and guanine formaldehyde adducts. In addition to the formation of these adducts, a proposed degradation scheme identifies the formation of methyl acetal ethylene glycol, formal...
Source: International Journal of Pharmaceutics - November 11, 2017 Category: Drugs & Pharmacology Source Type: research

Solid lipid nanoparticles as carriers for oral delivery of hydroxysafflor yellow A
In this study, HSYA solid lipid nanoparticles (SLNs) with the structure of w/o/w were prepared by a warm microemulsion process using approved drug excipients for oral delivery to increase the oral absorption of HSYA. The optimized HSYA SLNs are spherical with an average size of 214nm and the encapsulation efficiency is 55%. HSYA SLNs exhibited little cytotoxicity in Caco-2 and Hela cells, but increased the oral absorption of HSYA about 3.97-fold in rats, compared to HSYA water solution. In addition, cycloheximide pretreatment significantly decreased the oral absorption of HSYA delivered by SLNs. Importantly, the pharmacody...
Source: International Journal of Pharmaceutics - November 10, 2017 Category: Drugs & Pharmacology Source Type: research

Octenylsuccinate hydroxypropyl phytoglycogen enhances the solubility and in-vitro antitumor efficacy of niclosamide
This study showed that the use of OHPP could provide strong support for the development of niclosamide-based drug formulations. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 10, 2017 Category: Drugs & Pharmacology Source Type: research

High payload nanostructured lipid carriers fabricated with alendronate/polyethyleneimine ion complexes
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Basma N. Abd El-Hamid, Nitin K. Swarnakar, Ghareb M. Soliman, Mohamed A. Attia, Giovanni M. Pauletti Oral bioavailability of the anti-osteoporotic drug alendronate (AL) is limited to ≤ 1% due to unfavorable physicochemical properties. To augment absorption across the gastrointestinal mucosa, an ion pair complex between AL and polyethyleneimine (PEI) was formed and incorporated into nanostructured lipid carriers (NLCs) using a modified solvent injection method. When compared to free AL, ion pairing wi...
Source: International Journal of Pharmaceutics - November 9, 2017 Category: Drugs & Pharmacology Source Type: research