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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28445768/polymer-free-electrospun-nanofibers-from-sulfobutyl-ether7-beta-cyclodextrin-sbe7-%C3%AE-cd-inclusion-complex-with-sulfisoxazole-fast-dissolving-and-enhanced-water-solubility-of-sulfisoxazole
#1
Zehra Irem Yildiz, Asli Celebioglu, Tamer Uyar
In this study, our aim was to develop solid drug-cyclodextrin inclusion complex system having nanofibrous morphology in order to have fast-dissolving property and enhanced water-solubility of poorly water-soluble drug. Here, we prepared a highly concentrated aqueous solution of inclusion complex between sulfisoxazole and sulfobutyl ether7-beta-cyclodextrin (SBE7-β-CD, Captisol(®)), and then, without using any polymeric matrix, the electrospinning of sulfisoxazole/SBE7-β-CD-IC nanofibers was performed in order to obtain free-standing and handy nanofibrous web...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28445767/the-visualized-macrocycles-chemistry-and-application-of-fluorophore-tagged-cyclodextrins
#2
Gábor Benkovics, Milo Malanga, Éva Fenyvesi
Cyclodextrins are macrocyclic molecules able to form host-guest complexes due to their hydrophobic cavity. Because of their carbohydrate nature they do not absorb light in the UV-vis region (200-800nm), but they can be converted into spectroscopically active compounds via modification with a chromophore unit. Among the chromophores, the group of fluorophores can provide high sensitivity in analytical applications (chemosensing) and low detection limit in optical imaging methods (fluorescent microscopy). Fluorophore-tagged cyclodextrins therefore combine interesting spectroscopic properties with promising supramolecular features which make these conjugates widely applicable in various pharmaceutical fields...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28445766/inhibitory-effect-of-emulsifiers-in-sedds-on-protease-activity-just-an-illusion
#3
Noemi Lupo, Una Fidahic, Gergely Hetényi, Janine Griesser, Andreas Bernkop-Schnürch
AIM: Evaluation of inhibitory effect of emulsifiers on pancreatic trypsin and α-chymotrypsin. METHODS: The inhibitory effect of Cremophor EL, Cremophor RH 40, Brij O10, Tween 20, polyethylene glycol 8000, polyethylene glycol 400, Carbitol, Pemulen TR-1, Pemulen TR-2, Carbopol Ultrez 20 and Carbopol Ultrez 21 on pancreatic trypsin and α-chymotrypsin was tested. BAEE (Nα-Benzoyl-L-arginine ethyl ester), BTEE (N-Benzoyl-L-tyrosine ethyl ester), casein and insulin were used as substrates for trypsin and α-chymotrypsin...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28445765/in-line-monitoring-and-optimization-of-powder-flow-in-a-simulated-continuous-process-using-transmission-near-infrared-spectroscopy
#4
Md Anik Alam, Zhenqi Shi, James K Drennen, Carl A Anderson
In-line monitoring of continuous powder flow is an integral part of the continuous manufacturing process of solid oral dosage forms in the pharmaceutical industry. Specifically, monitoring downstream from loss-in-weight (LIW) feeders and/or continuous mixers provides important data about the state of the process. Such measurements support control of the process and thereby enhance product quality. Near Infrared Spectroscopy (NIRS) is a potential PAT tool to monitor the homogeneity of a continuous powder flow stream in pharmaceutical manufacturing...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28445764/development-of-light-driven-gas-forming-liposomes-for-efficient-tumor-treatment
#5
Jae Min Lee, Yu Seok Youn, Eun Seong Lee
In this study, we report a gas-forming liposome containing 1H-1H-2H-perfluoro-1-hexene (PFH) and gold nanoparticles (AuNPs). These liposomes were rapidly destabilized by external near-infrared (NIR) light, as a result of the vaporization of PFH influenced by an AuNPs-mediated photothermal event. In particular, these liposomes showed the triggered release of the encapsulated D-(KLAKLAK)2 peptide drug. The experimental results demonstrated that the light-irradiated liposomes significantly enhanced in vitro photothermal and D-(KLAKLAK)2 peptide-mediated cell death of CAOV-3 tumor cells...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28442269/enhanced-adhesion-and-in-situ-photothermal-ablation-of-cancer-cells-in-surface-functionalized-electrospun-microfiber-scaffold-with-graphene-oxide
#6
Nicolò Mauro, Cinzia Scialabba, Giovanna Pitarresi, Gaetano Giammona
The physicochemical characteristics of a biomaterial surface highly affect the interaction with living cells. Recently, much attention has been focused on the adhesion properties of functional biomaterials toward cancer cells, since is expected to control metastatic spread of a tumor, which is related to good probability containing the progression of disease burden. Here, we designed an implantable poly(caprolactone)-based electrospun microfiber scaffold, henceforth PCLMF-GO, to simultaneously capture and kill cancer cells by tuning physicochemical features of the hybrid surface through nitrogen plasma activation and hetero-phase graphene oxide (GO) covalent functionalization...
April 22, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28438698/chitosan-and-hyaluronan-coated-liposomes-for-pulmonary-administration-of-curcumin
#7
Maria Manconi, Maria Letizia Manca, Donatella Valenti, Elvira Escribano, Hervé Hillaireau, Anna Maria Fadda, Elias Fattal
Aiming at improving the nebulization performances and lung antioxidant protection of curcumin, chitosan or hyaluronan-coated liposomes were prepared and their characteristics and performances were compared with that of uncoated liposomes. Curcumin loaded liposomes displayed a diameter lower than 100nm, the coating with both polymers led to a small increase of vesicle size around 130nm and the zeta potential turned to positive values using chitosan while remained negative using hyaluronan. Chitosan allowed the formation of more lamellar and stiffer vesicles with a higher bilayer thickness (dB∼59Ǻ) with respect to the uncoated liposomes, whereas hyaluronan allowed the interdigitation of the bilayers (dB∼47Ǻ) due to the polymer intercalation between phospholipid head groups resulting in vesicles mainly organized in uncorrelated bilayers...
April 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28438697/predicting-drug-loading-in-pla-peg-nanoparticles
#8
M Meunier, A Goupil, P Lienard
Polymer nanoparticles present advantageous physical and biopharmaceutical properties as drug delivery systems compared to conventional liquid formulations. Active pharmaceutical ingredients (APIs) are often hydrophobic, thus not soluble in conventional liquid delivery. Encapsulating the drugs in polymer nanoparticles can improve their pharmacological and bio-distribution properties, preventing rapid clearance from the bloodstream. Such nanoparticles are commonly made of non-toxic amphiphilic self-assembling block copolymers where the core (poly-[D,L-lactic acid] or PLA) serves as a reservoir for the API and the external part (Poly-(Ethylene-Glycol) or PEG) serves as a stealth corona to avoid capture by macrophage...
April 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28434935/solid-nanofoams-based-on-cellulose-nanofibers-and-indomethacin-the-effect-of-processing-parameters-and-drug-content-on-material-structure
#9
J Bannow, J-W Benjamins, J Wohlert, K Löbmann, A J Svagan
The unique colloidal properties of cellulose nanofibers (CNF), makes it a very interesting new excipient in pharmaceutical formulations, as CNF in combination with some poorly-soluble drug can create nanofoams with closed cells. Previous nanofoams, created with the model drug indomethacin, demonstrated a prolonged release compared to films, owing to the tortuous diffusion path that the drug needs to take around the intact air-bubbles. However, the nanofoam was only obtained at a relatively low drug content of 21wt% using fixed processing parameters...
April 20, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28434934/introducing-a-novel-gravitation-based-high-velocity-compaction-analysis-method-for-pharmaceutical-powders
#10
Timo Tanner, Osmo Antikainen, Henrik Ehlers, Jouko Yliruusi
With modern tableting machines large amounts of tablets are produced with high output. Consequently, methods to examine powder compression in a high-velocity setting are in demand. In the present study, a novel gravitation-based method was developed to examine powder compression. A steel bar is dropped on a punch to compress microcrystalline cellulose and starch samples inside the die. The distance of the bar is being read by a high-accuracy laser displacement sensor which provides a reliable distance-time plot for the bar movement...
April 20, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28433532/exci-cest-exploiting-pharmaceutical-excipients-as-mri-cest-contrast-agents-for-tumor-imaging
#11
Dario Livio Longo, Fatima Zzahra Moustaghfir, Alexandre Zerbo, Lorena Consolino, Annasofia Anemone, Martina Bracesco, Silvio Aime
Chemical Exchange Saturation Transfer (CEST) approach is a novel tool within magnetic resonance imaging (MRI) that allows visualization of molecules possessing exchangeable protons with water. Many molecules, employed as excipients for the formulation of finished drug products, are endowed with hydroxyl, amine or amide protons, thus can be exploitable as MRI-CEST contrast agents. Their high safety profiles allow them to be injected at very high doses. Here we investigated the MRI-CEST properties of several excipients (ascorbic acid, sucrose, N-acetyl-d-glucosamine, meglumine and 2-pyrrolidone) and tested them as tumor-detecting agents in two different murine tumor models (breast and melanoma cancers)...
April 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432020/surface-modification-of-acetaminophen-particles-by-atomic-layer-deposition
#12
Tommi O Kääriäinen, Marianna Kemell, Marko Vehkamäki, Marja-Leena Kääriäinen, Alexandra Correia, Hélder A Santos, Luis M Bimbo, Jouni Hirvonen, Pekka Hoppu, Steven M George, David C Cameron, Mikko Ritala, Markku Leskelä
Active pharmaceutical ingredients (APIs) are predominantly organic solid powders. Due to their bulk properties many APIs require processing to improve pharmaceutical formulation and manufacturing in the preparation for various drug dosage forms. Improved powder flow and protection of the APIs are often anticipated characteristics in pharmaceutical manufacturing. In this work, we have modified acetaminophen particles with atomic layer deposition (ALD) by conformal nanometer scale coatings in a one-step coating process...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432019/feasibility-of-mini-tablets-as-a-flexible-drug-delivery-tool
#13
Biplob Mitra, Jessica Chang, Sy-Juen Wu, Chad N Wolfe, Robert L Ternik, Thomas Z Gunter, Michael C Victor
Mini-tablets have potential applications as a flexible drug delivery tool in addition to their generally perceived use as multi-particulates. That is, mini-tablets could provide flexibility in dose finding studies and/or allow for combination therapies in the clinic. Moreover, mini-tablets with well controlled quality attributes could be a prudent choice for administering solid dosage forms as a single unit or composite of multiple mini-tablets in patient populations with swallowing difficulties (e.g., pediatric and geriatric populations)...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432018/on-the-role-of-api-in-determining-porosity-pore-structure-and-bulk-modulus-of-the-skeletal-material-in-pharmaceutical-tablets-formed-with-mcc-excipient
#14
Cathy Ridgway, Prince Bawuah, Daniel Markl, J Axel Zeitler, Jarkko Ketolainen, Kai-Erik Peiponen, Patrick Gane
The physical properties and mechanical integrity of pharmaceutical tablets are of major importance when loading with active pharmaceutical ingredient(s) (API) in order to ensure ease of processing, control of dosage and stability during transportation and handling prior to patient consumption. The interaction between API and excipient, acting as functional extender and binder, however, is little understood in this context. The API indomethacin is combined in this study with microcrystalline cellulose (MCC) at increasing loading levels...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432017/dual-functional-nanoparticles-for-precise-drug-delivery-to-alzheimer-s-disease-lesions-targeting-mechanisms-pharmacodynamics-and-safety
#15
Xiaoyao Zheng, Chi Zhang, Qian Guo, Xu Wan, Xiayan Shao, Qingfeng Liu, Qizhi Zhang
Alzheimer's disease (AD) is the most common form of dementia and is characterized by the cerebral accumulation of extracellular amyloid plaques. In a previous study, this histopathological hallmark was used as a target on a dual-functional nanoparticle (TQNP) to deliver biotechnological drugs, such as the H102 peptide, a β-sheet breaker, to AD lesions precisely. This delivery system could reduce the amyloid-β (Aβ) burden in the brains of AD model mice, as well as ameliorated the memory impairment of the mice...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432016/inkjet-printing-of-antiviral-pcl-nanoparticles-and-anticancer-cyclodextrin-inclusion-complexes-on-bioadhesive-film-for-cervical-administration
#16
Cem Varan, Henrika Wickström, Niklas Sandler, Yeşim Aktaş, Erem Bilensoy
Personalized medicine is an important treatment approach for diseases like cancer with high intrasubject variability. In this framework, printing is one of the most promising methods since it permits dose and geometry adjustment of the final product. With this study, a combination product consisting of anticancer (paclitaxel) and antiviral (cidofovir) drugs was manufactured by inkjet printing onto adhesive film for local treatment of cervical cancers as a result of HPV infection. Furthermore, solubility problem of paclitaxel was overcome by maintaining this poorly soluble drug in a cyclodextrin inclusion complex and release of cidofovir was controlled by encapsulation in polycaprolactone nanoparticles...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28428090/preparation-and-characterization-of-lipid-nanoparticle-pdna-complexes-for-stat3-downregulation-and-overcoming-chemotherapy-resistance-in-lung-cancer-cells
#17
Mustafa Kotmakçı, Vildan Bozok Çetintaş, A Gülten Kantarcı
Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types. RNA interference (RNAi) is proven powerful tool for downregulating STAT3, allowing re-sensitization of resistant cancer cells. However, delivery of RNA interference-mediating molecules for STAT3 downregulation in lung cancer cells is limited to a small number of studies most of which employ commercially available transfection kits...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28428089/enhanced-anti-rheumatic-activity-of-methotrexate-entrapped-ultradeformable-liposomal-gel-in-adjuvant-induced-arthritis-rat-model
#18
Alam Zeb, Omer Salman Qureshi, Chan-Hee Yu, Muhammad Akram, Hyung-Seo Kim, Myung-Sic Kim, Jong-Ho Kang, Arshad Majid, Sun-Young Chang, Ok-Nam Bae, Jin-Ki Kim
The aim of this study is to investigate in vivo anti-rheumatic activity of methotrexate-entrapped ultradeformable liposomal gel (MTX-UDLs-gel) in adjuvant-induced arthritis rat model. Methotrexate-entrapped ultradeformable liposomes (MTX-UDLs) with the optimal phosphatidylcholine to Tween 80 ratio (7:3, w/w) were incorporated into 1% Carbopol gel. MTX-UDLs-gel was characterized in terms of appearance, clarity, homogeneity, pH and drug content. The permeation of MTX-UDLs-gel across rat skin was investigated using Franz diffusion cell...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28416402/improvement-of-skin-whitening-agents-efficiency-through-encapsulation-current-state-of-knowledge
#19
REVIEW
Elissa Ephrem, Hamid Elaissari, Hélène Greige-Gerges
Hyperpigmentation is one of the most common skin disorder that affects both men and women of all ethnic groups, caused by several factors, such as UV exposure and skin inflammation. Topical whitening agents were found to be the best and the least aggressive therapy for treating hyperpigmentation compared to instrumental approaches. However, topical treatment faces several obstacles due to the low stability of the whitening agents. Therefore, the encapsulation of these agents was found to be crucial as it enhances their physicochemical stability and increases their concentration at the targeted site via an improved skin permeation, penetration or distribution...
April 14, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28416401/polymeric-nanoparticles-for-sirna-delivery-production-and-applications
#20
Gennara Cavallaro, Carla Sardo, Emanuela Fabiola Craparo, Barbara Porsio E Gaetano Giammona
Gene therapy through the use of siRNA and a polymeric carrier are becoming an efficient therapeutic option to conventional pharmaceutical formulations for the treatment of deadly diseases, such as cancer, pulmonary, ocular and neurodegenerative diseases. However, several considerations regarding the stability, formulation, and efficacy have to be faced up until these systems could be considered to be a marketable pharmaceutical products for to extend siRNA application to clinical practice. This review is focused on the key challenges of siRNA therapeutics, with special attention on the faced obstacles and on the formulation-related difficulties, providing a list of requirements needed for obtaining an ideal carrier for siRNA...
April 14, 2017: International Journal of Pharmaceutics
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