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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

Thioredoxin-albumin fusion protein prevents copper enhanced zinc-induced neurotoxicity via its antioxidative activity
In this study, we examined the effect of HSA-Trx on Cu2+/Zn2+-induced neurotoxicity. Firstly, HSA-Trx was found to clearly suppress Cu2+/Zn2+-induced neuronal cell death in mouse hypothalamic neuronal cells (GT1-7 cells). Moreover, HSA-Trx markedly suppressed Cu2+/Zn2+-induced ROS production and the expression of oxidative stress related genes, such as heme oxygenase-1. In contrast, HSA-Trx did not affect the intracellular levels of both Cu2+ and Zn2+ after Cu2+/Zn2+ treatment. Finally, HSA-Trx was found to significantly suppress endoplasmic reticulum (ER) stress response induced by Cu2+/Zn2+ treatment in a dose dependent ...
Source: International Journal of Pharmaceutics - November 9, 2017 Category: Drugs & Pharmacology Source Type: research

Ionic liquid – microemulsions assisting in the transdermal delivery of Dencichine: Preparation, in-vitro and in-vivo evaluations, and investigation of the permeation mechanism
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Chengxiao Wang, Junxiao Zhu, Ding Zhang, Ye Yang, Luyao Zheng, Yuan Qu, Xiaoyan Yang, Xiuming Cui A novel microemulsion was developed and characterized for topical delivery of Dencichine (Den). Two imidazaolium ionic liquid, 1-hydroxyethyl-3-methylimidazolium chloride ([HOEIM]Cl) and 1-butyl-3-methylimidazolium dodecanesulfate ([BMIM]C12SO3) were incorporated into the aqueous and surfactant phases respectively for the remarkable enhancement on skin permeation. The nano-carrier was developed and optimize...
Source: International Journal of Pharmaceutics - November 9, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro and preclinical assessment of an intranasal spray formulation of parathyroid hormone PTH 1 –34 for the treatment of osteoporosis
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Allan J. Williams, Faron Jordan, Gareth King, Andrew L. Lewis, Lisbeth Illum, Tahir Masud, Alan C. Perkins, Richard G. Pearson Osteoporosis treatment with PTH 1–34 injections significantly reduces the incidence of bone fracture. Potential further reductions in fracture rate should be observed through nasal spray delivery to address the poor compliance associated with patient dislike of repeated PTH 1–34 subcutaneous injections. In vitro human osteoblast-like Saos-2 cell intracellular cAMP le...
Source: International Journal of Pharmaceutics - November 9, 2017 Category: Drugs & Pharmacology Source Type: research

The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems: Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Katarzyna Gniado, Pól MacFhionnghaile, Patrick McArdle, Andrea Erxleben The amorphization of 18 different drugs on milling with one mole equivalent sodium taurocholate (NaTC) was investigated. In all cases the X-ray powder pattern showed an amorphous halo after milling at room temperature or after cryomilling and 14 of the 18 coamorphous drug-NaTC systems were physically stable for between one to eleven months under ambient storage conditions. In three cases, namely carbamazepine-NaTC, indomethac...
Source: International Journal of Pharmaceutics - November 9, 2017 Category: Drugs & Pharmacology Source Type: research

On the role of salt formation and structural similarity of co-formers in co-amorphous drug delivery systems
In conclusion, structural similarity of the co-formers does not lead to similar co-former performance for a given drug. Salt formation is not a prerequisite for the formation of a co-amorphous system, but if a co-amorphous salt system is formed, improved dissolution rate and physical stability are observed. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

DNA interaction, anti-proliferative effect of copper oxide nanocolloids prepared from metallosurfactant based microemulsions acting as precursor, template and reducing agent
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Gurpreet Kaur, Varsha Dogra, Rajeev Kumar, Sandeep Kumar, Gaurav Bhanjana, Neeraj Dilbaghi, Nitin Kumar Singhal In the present study, we have synthesized mixed cuprous/copper oxide nanosuspensions by metallosurfactant based microemulsion technique. Three metallosurfactants were synthesized which includes two non-ionic double chained metallosurfactants with C12, C16 chains with coordinated copper i.e. Cudda and Cuhexa, respectively. Another cationic double chained metallosurfactant with loosely bound met...
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

Demonstration of pharmaceutical tablet coating process by injection molding technology
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Vibha Puri, David Brancazio, Eranda Harinath, Alexander R. Martinez, Parind M. Desai, Keith D. Jensen, Jung-Hoon Chun, Richard D. Braatz, Allan S. Myerson, Bernhardt L. Trout We demonstrate the coating of tablets using an injection molding (IM) process that has advantage of being solvent free and can provide precision coat features. The selected core tablets comprising 10% w/w griseofulvin were prepared by an integrated hot melt extrusion-injection molding (HME-IM) process. Coating trials were conducted...
Source: International Journal of Pharmaceutics - November 8, 2017 Category: Drugs & Pharmacology Source Type: research

Sequential therapy with redox-responsive glucolipid nanocarrier separately delivering siRNA and doxorubicin to overcome multidrug resistance
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Tingting Meng, Binbin Lu, Shihong Shao, Ming Yuan, Xuan Liu, Hong Yuan, Xuan Huang, Fuqiang Hu P-glycoprotein (P-gp) is a major efflux transporter overexpressed on multidrug resistant tumor cells and responsible for pumping drugs out. If anti-tumor drugs are given when P-gp level is low, satisfactory treatment efficiency may be achieved. Thus, a P-gp down-regulating siRNA (siMDR1) and doxorubicin (DOX) were applied to eliminate multidrug resistant breast cancer cells (MCF-7/ADR). A redox-responsive glu...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Development of pre-activated α-cyclodextrin as a mucoadhesive excipient for intra-vesical drug delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Muhammad Ijaz, Maximilian Prantl, Noemi Lupo, Flavia Laffleur, Mulazim Hussain Asim, Barbara Matuszczak, Andreas Bernkop-Schnürch The study was designed to synthesize and characterize pre-activated α-cyclodextrin (α-CD) derivatives as mucus adhering excipients for intra-vesical drug delivery. Sodium periodate (NaIO4) was used to oxidize α-CD and subsequently cysteamine was covalently attached to carbonyl groups of oxidized α-CD via reductive amination to produce thiolated &...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Chitosan based Pickering emulsion as a promising approach for topical application of rutin in a solubilized form intended for wound healing: In vitro and in vivo study
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Marwa Hasanein Asfour, Heba Elmotasem, Dina Mahmoud Mostafa, Abeer A.A. Salama The aim of the present study is to formulate the hydrophobic drug rutin in a solubilized form, intended for wound healing, via its loading into a novel Pickering emulsion stabilized by self aggregated chitosan particles (SACP). Rutin-loaded Pickering emulsion formulae were prepared using a high speed homogenizer. They were characterized by drop test, optical microscopy, droplet size and zeta potential determination. The resu...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

An optimized two-vial formulation lipid nanoemulsion of paclitaxel for targeted delivery to tumor
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Lina Chen, Bingchen Chen, Li Deng, Baoan Gao, Yuansheng Zhang, Chan Wu, Nong Yu, Qinqin Zhou, Jianzhong Yao, Jianming Chen The discovery of new intravenous drug delivery carrier for water-insoluble drug is a challenging task. In this paper, novel two-vial formulation of paclitaxel (PTX)-loaded lipid nanoemulsions (TPLEs) with particle sizes of 110nm (TPLE-1), 220nm (TPLE-2) and 380nm (TPLE-3), which were formed by mixing a PEG400 solution of PTX and 10% (w/w) blank lipid emulsions (BLEs) with different...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and characterization of an amylase-triggered dextrin-linked graphene oxide anticancer drug nanocarrier and its vascular permeability
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Siaw Fui Kiew, Yan Teck Ho, Lik Voon Kiew, James Chen Yong Kah, Hong Boon Lee, Toyoko Imae, Lip Yong Chung We synthesized a dextrin (DEX)-conjugated graphene oxide (GO) nanocarrier (GO100-DEX) as a potential drug delivery system to respond to a tumor-associated stimulus, α-amylase, that has high permeability through the fenestrated endothelial barrier to the tumor site. At acidic pH and in the presence of α-amylase to simulate tumor conditions, GO100-DEX released a 1.5-fold higher amount of...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of factors affecting the stability of lysozyme spray dried from ethanol-water solutions
In this study, lysozyme was chosen as a model pharmaceutical protein to study these aspects when spray drying from water-ethanol mixtures. The effect of formulation additives (trehalose, Tween 20 and phosphate-buffered saline) and processing conditions (inlet temperature and storage time of lysozyme in the feed solution before the spray drying process) on the protein bioactivity was investigated. The results showed that the bioactivities of spray dried lysozyme with these additives were about 5–10% higher than that without additives. The bioactivity of the spray dried lysozyme was found to increase with a decrease in...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Bubble-generating nano-lipid carriers for ultrasound/CT imaging-guided efficient tumor therapy
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Nan Zhang, Jia Li, Ruirui Hou, Jiangnan Zhang, Pei Wang, Xinyang Liu, Zhenzhong Zhang Ideal therapeutic effectiveness of chemotherapy is obtained only when tumor cells are exposed to a maximal drug concentration, which is often hindered by dose-limiting toxicity. We designed a bubble-generating liposomal delivery system by introducing ammonium bicarbonate and gold nanorods into folic acid-conjugated liposomes to allow both multimodal imaging and the local release of drug (doxorubicin) with hyperthermia...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical properties of inclusion complexes of highly soluble β-cyclodextrins with highly hydrophobic testosterone propionate
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Christian Celia, Angela Scala, Rosanna Stancanelli, Emanuela Surdo, Donatella Paolino, Alessandro Grattoni, Nicola Micale, Vincenza Crupi, Domenico Majolino, Massimo Fresta, Silvana Tommasini, Valentina Venuti, Cinzia Anna Ventura Hydroxypropyl-β-cyclodextrin (HP-β-CyD) and sulfobutyl ether-β-cyclodextrin (SBE-β-CyD) were used to generate hydrophilic complexes of the poorly water-soluble drug testosterone propionate (TP). The inclusion complexes were obtained by freeze-drying, and t...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Novel dissolving microneedles for enhanced transdermal delivery of levonorgestrel: In vitro and in vivo characterization
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Gangtao Yao, Guilan Quan, Shiqi Lin, Tingting Peng, Qingqing Wang, Hao Ran, Hangping Chen, Qian Zhang, Lili Wang, Xin Pan, Chuanbin Wu Dissolving microneedles (DMN) have been studied as a drug delivery system to enhance the transport of drug molecules across the skin with almost no pain. However, the poor dissolving ability of microneedles in the skin and low drug loading have limited their potential application. The aim of this study was to develop a novel dissolving microneedle system with improved d...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Prediction of human percutaneous absorption from in vitro and in vivo animal experiments
In conclusion, minipigs appear to be a promising model animal for predicting percutaneous drug absorption in humans, however, more in vivo and in vitro studies are needed to improve predictability. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Simplified stratum corneum model membranes for studying the effects of permeation enhancers
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Barbora Amélie Čuříková, Kamila Procházková, Barbora Filková, Petra Diblíková, Jan Svoboda, Andrej Kováčik, Kateřina Vávrová, Jarmila Zbytovská The activity of transdermal permeation enhancers is usually evaluated in vitro on human or animal skin, but skin samples can be hard to source and highly variable. To provide a more consistent basis for evaluating the activity of permeation enhancers, we prepared relatively ...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Understanding die fill variation during mini-tablet production
In this study, flow properties of different types of granules were characterised. Mini-tablets of 1.8 and 3mm diameters were prepared from the granules using a rotary press with multiple-tip compression tooling. A methodology was established to evaluate mini-tablet die fill variation within and across compaction cycles using data from compression roller displacement and mini-tablet weight. Both sizes of mini-tablets showed similar extents of inter-cycle weight variation that could be associated with granules’ inter-particulate friction. However, smaller mini-tablets had higher intra-cycle weight variation due to thei...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Different effects of silica added internal or external on in vitro dissolution of indomethacin hot-melt extrudates
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Yulong Xia, Meng Yuan, Yueyang Deng, Xue Ke, Tianyuan Ci The purpose of this work was to investigate the effect on the dissolution behavior when silica was added in different ways. The solid dispersion was prepared by hot-melt extrusion (HME) using indomethacin (IND) as a model drug and Kollidon VA64 as a carrier. In order to change the dissolution behavior, the silica was added during or after the HME respectively, to obtain the corresponding silica internal-added solid dispersion (InSD) and silica ex...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Cationic nanoemulsions as nucleic acids delivery systems
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Helder Ferreira Teixeira, Fernanda Bruxel, Michelle Fraga, Roselena Silvestri Schuh, Giovanni Konat Zorzi, Ursula Matte, Elias Fattal Since the first clinical studies, knowledge in the field of gene therapy has advanced significantly, and these advances led to the development and subsequent approval of the first gene medicines. Although viral vectors-based products offer efficient gene expression, problems related to their safety and immune response have limited their clinical use. Thus, design and opt...
Source: International Journal of Pharmaceutics - November 6, 2017 Category: Drugs & Pharmacology Source Type: research

Melt extrusion with poorly soluble drugs – An integrated review
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Michael A. Repka, Suresh Bandari, Venkata Raman Kallakunta, Anh Q. Vo, Haley McFall, Manjeet B. Pimparade, Ajinkya M. Bhagurkar Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This review is focused on the recent reports on the solubility enhancem...
Source: International Journal of Pharmaceutics - November 5, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring the feasibility of the use of biopolymers as a carrier in the formulation of amorphous solid dispersions – Part I: Gelatin
This study shows the potential of gelatin as a carrier to formulate amorphous solid dispersions. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 4, 2017 Category: Drugs & Pharmacology Source Type: research