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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28645630/evolution-of-cyclodextrin-nanosponges
#1
Fabrizio Caldera, Maria Tannous, Roberta Cavalli, Marco Zanetti, Francesco Trotta
Cyclodextrin-based nanosponges (CD-NSs) are insoluble, highly cross-linked 3D network polymers used in several scientific and technological fields, the main area of investigation concerns the pharmaceutical applications, in which CD-NSs have been mostly employed as drug delivery systems. CD-NSs can be generally grouped into four consecutive generations, taking into account their chemical composition and properties. The 1st generation of NSs are plain nanosponges, subdivided into four main types: urethane, carbonate, ester and ether NSs, depending on the chemical nature of the functional group connecting the CD to the cross-linker...
June 20, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28645629/production-and-characterization-of-aluminium-oxide-nanoshells-on-spray-dried-lactose
#2
Joel Hellrup, Mårten Rooth, Anders Johansson, Denny Mahlin
Atomic layer deposition (ALD) enables deposition of dense nanometer thick metal oxide nanoshells on powder particles with precise thickness control. This leads to products with low weight fraction coating, also when depositing on nano- or micron sized powder particles. This study aimed at investigating the aluminium oxide nanoshell thickness required to prevent moisture sorption. The nanoshells were produced with ALD on spray-dried lactose, which is amorphous and extremely hygroscopic. The particles were studied with dynamic vapor sorption between 0 to 50% RH, light scattering, scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and polarized light microscopy...
June 20, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28642204/co-delivery-of-paclitaxel-and-anti-survivin-sirna-via-redox-sensitive-oligopeptide-liposomes-for-the-synergistic-treatment-of-breast-cancer-and-metastasis
#3
Xinyan Chen, Yidi Zhang, Chunming Tang, Chunli Tian, Qiong Sun, Zhigui Su, Lingjing Xue, YifanYin, Caoyun Ju, Can Zhang
The overexpression of survivin in breast cancer cells is an important factor of paclitaxel (PTX) resistance in breast cancer. To overcome PTX resistance and improve the antitumor effect of PTX, we developed a novel liposome-based nanosystem (PTX/siRNA/SS-L), composed of a redox-sensitive cationic oligopeptide lipid (LHSSG2C14) with a proton sponge effect, natural soybean phosphatidylcholine (SPC), and cholesterol for co-delivery of PTX and anti-survivin siRNA, which could specifically downregulate survivin overexpression...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28642203/developments-of-polysorbate-tween-based-microemulsions-preclinical-drug-delivery-toxicity-and-antimicrobial-applications
#4
REVIEW
Gurpreet Kaur, S K Mehta
The present review deals with the progress of Polysorbates (Tween) based microemulsions in drug delivery. PEGylated Sorbitan Fatty Acid Esters (Tweens/Polysorbates) are one of the most used non-ionic surfactants. Particularly Polysorbates based microemulsion has been widely used for enhancing solubilization of poorly soluble drugs. This article deals with underlying the preclinical factors which affect the solubilization efficacy of Tween formulations, implication of pharmaceutically accepted vectors in terms of absorption, bioavailability, biological fate and potential toxicity...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28642202/engineering-of-multifunctional-temperature-sensitive-liposomes-for-synergistic-photothermal-photodynamic-and-chemotherapeutic-effects
#5
Tuan Hiep Tran, Hanh Thuy Nguyen, Nam Van Le, Thi Thu Phuong Tran, Jong Seong Lee, Sae Kwang Ku, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Heterogeneity of cancer cells and drug resistance require multiple therapeutic approaches for comprehensive treatment. In this study, temperature-sensitive liposomes containing anti-cancer agent tanespimycin (17-AAG) and photosensitizer IR 820 were developed for combination of phototherapy and chemotherapy. The temperature-sensitive liposomes composed of DPPC, cholesterol, DSPE-PEG, 17-AAG, and IR 820 (LP-AI) at weight ratio of 35/15/3/2/2 were formulated as a thin film using extrusion and evaluated for particle size, morphology and drug release profile...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28642201/combination-of-coenzyme-q10-loaded-liposomes-with-ultrasound-targeted-microbubbles-destruction-utmd-for-early-theranostics-of-diabetic-nephropathy
#6
Ting Yue, He-Lin Xu, Pian-Pian Chen, Lei Zheng, Qun Huang, Wen-Shuang Sheng, Yuan-Di Zhuang, Li-Zhuo Jiao, Ting-Ting Chi, De-Li ZhuGe, Jin-Jin Liu, Ying-Zheng Zhao, Li Lan
Diabetic nephropathy (DN) is one of the most common and lethal microvascular complications of diabetes. This study aimed to explore whether coenzymeQ10 (CoQ10) as an antioxidant combined with ultrasound-targeted microbubble destruction (UTMD) could reverse the progress of early diabetic nephropathy (DN). CoQ10 has great potential to treat early DN. However, the clinical application of CoQ10 has been limited because of its low aqueous solubility and non-specific distribution. Therefore, CoQ10-loaded liposomes (CoQ10-lip) were prepared and combined with ultrasound microbubbles for the early theranostics of DN...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28642200/enhancement-of-solubility-and-dissolution-rate-of-baicalein-wogonin-and-oroxylin-a-extracted-from-radix-scutellariae
#7
Hang Yu, Jae-Sang Chang, Sun Young Kim, Yoon G Kim, Hoo-Kyun Choi
Baicalein, wogonin, and oroxylin A are three major hydrophobic components in the extract of Radix scutellariae with wide spectrum of pharmacological applications. The purpose of this study was to enhance the solubility, dissolution rate and stability of baicalein, wogonin and oroxylin A by solid dispersion (SD) technique. SD of the extract with various polymers was prepared to select the best carrier. Solubility study, chemical stability study and dissolution study were performed to characterize the SD. The solubility of all three components, after forming solid dispersion with povidone K-30 (PVP K-30) was significantly increased in pH 6...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28634141/one-step-preparation-of-spherical-drug-particles-by-contamination-free-dry-milling-technique-with-corn-starch-beads
#8
Toshiyuki Niwa, Maria Yoshida, Naoko Hayashi, Keita Kondo
The novel dry milling technique has been developed by using a mechanical powder processor for improving the dissolution properties of poorly water-soluble drugs. It was found that the drug crystals were well pulverized by co-processing with fine particles of corn starch (CS). The morphological observation and particle size evaluation revealed that the processed products formed the composite particles with ordered-mixed structure, having double-layered particles with a core of CS and a coating layer of phenytoin (Phe), as a model drug...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28636894/effects-of-hpmc-substituent-pattern-on-water-up-take-polymer-and-drug-release-an-experimental-and-modelling-study
#9
Diego Caccavo, Gaetano Lamberti, Anna Angela Barba, Susanna Abrahmsén-Alami, Anna Viridén, Anette Larsson
The purpose of this study was to investigate the hydration behavior of two matrix formulations containing the cellulose derivative hydroxypropyl methylcellulose (HPMC). The two HPMC batches investigated had different substitution pattern along the backbone; the first one is referred to as heterogeneous and the second as homogenous. The release of both the drug molecule theophylline and the polymer was determined. Additionally, the water concentrations at different positions in the swollen gel layers were determined by Magnetic Resonance Imaging...
June 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28636893/controlled-release-from-aspirin-based-linear-biodegradable-poly-anhydride-esters-for-anti-inflammatory-activity
#10
Queeny Dasgupta, Sahitya Movva, Kaushik Chatterjee, Giridhar Madras
This work reports the synthesis of a novel, aspirin-loaded, linear poly (anhydride ester) and provides mechanistic insights into the release of aspirin from this polymer for anti-inflammatory activity. As compared to conventional drug delivery systems that rely on diffusion based release, incorporation of bioactives in the polymer backbone is challenging and high loading is difficult to achieve. In the present study, we exploit the pentafunctional sugar alcohol (xylitol) to provide sites for drug (aspirin) attachment at its non-terminal OH groups...
June 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28636892/topical-bioavailability-of-diclofenac-from-locally-acting-dermatological-formulations
#11
S F Cordery, A Pensado, W S Chiu, M Z Shehab, A L Bunge, M B Delgado-Charro, R H Guy
Assessment of the bioavailability of topically applied drugs designed to act within or beneath the skin is a challenging objective. A number of different, but potentially complementary, techniques are under evaluation. The objective of this work was to evaluate in vitro skin penetration and stratum corneum tape-stripping in vivo as tools with which to measure topical diclofenac bioavailability from three approved and commercialized products (two gels and one solution). Drug uptake into, and its subsequent clearance from, the stratum corneum of human volunteers was used to estimate the input rate of diclofenac into the viable skin layers...
June 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28634142/cysteamine-polysaccharide-hydrogels-study-of-extended-ocular-delivery-and-biopermanence-time-by-pet-imaging
#12
Andrea Luaces-Rodríguez, Victoria Díaz-Tomé, Miguel González-Barcia, Jesús Silva-Rodríguez, Michel Herranz, María Gil-Martínez, María Teresa Rodríguez-Ares, Carla García-Mazás, José Blanco-Mendez, María Jesús Lamas, Francisco Javier Otero-Espinar, Anxo Fernández-Ferreiro
Cystinosis is a rare autosomal recessive disorder in which cystine crystals accumulate within the lysosomes of various organs, including the cornea. Ocular treatment is based on the administration of cysteamine eye drops, requiring its instillation several times per day. We have introduced the cysteamine in two types of previously developed ocular hydrogels (ion sensitive hydrogel with the polymers gellan gum and kappa-carrageenan and another one composed of hyaluronic acid), aiming at increasing the ocular retention in order to extend the dosing interval...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28634140/novel-nanoparticles-based-on-chitosan-dicarboxylate-conjugates-via-tandem-ionotropic-covalent-crosslinking-with-tripolyphosphate-and-subsequent-evaluation-as-drug-delivery-vehicles
#13
Isra Dmour, Mutasem O Taha
Chitosan-based nanoparticles prepared by ionotropic gelation are prone to stability issues. The aim of this work is to chemically modify chitosan by grafting to succinate, phthalate, glutarate and phenylsuccinate moieties and to investigate the suitability of the resulting polymers as covalently-crosslinked nanocarriers. Corresponding nanoparticles (NPs) were formulated by ionotropic gelation using tripolyphosphate (TPP) anion then they were covalently crosslinked using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (EDC)...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28634139/ocular-disposition-of-ciprofloxacin-from-topical-pegylated-nanostructured-lipid-carriers-effect-of-molecular-weight-and-density-of-poly-ethylene-glycol
#14
Sai Prachetan Balguri, Goutham R Adelli, Karthik Yadav Janga, Prakash Bhagav, Soumyajit Majumdar
Ciprofloxacin (CIP) is an antibacterial agent prescribed for the treatment of ocular infections. The objective of the present project is to investigate the effect of surface PEG functionalization of the Nano structured lipid carriers (NLCs) on formulation stability, ocular penetration and distribution. CIP NLCs were tested with different molecular weight (poly ethylene glycol) PEGs ranging from (2K to 20K) grafted onto the phospholipid and with different chain lengths (14-18 carbons) of phospholipids derivatized with PEG-2K...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28634138/intracellular-and-transdermal-protein-delivery-mediated-by-non-covalent-interactions-with-a-synthetic-guanidine-rich-molecular-carrier
#15
Jungkyun Im, Sanket Das, Dongjun Jeong, Chang-Jin Kim, Hyun-Suk Lim, Ki Hean Kim, Sung-Kee Chung
The impermeability of the cell plasma membrane is one of the major barriers for protein transduction into mammalian cells, and it also limits the use of proteins as therapeutic agents. Protein transduction has usually been achieved based on certain invasive processes or cell penetrating peptides (CPP). Herein we report our study in which a synthetic guanidine-rich molecular carrier is used as a delivery vector for intracellular and transdermal delivery of proteins. First a sorbitol-based molecular carrier having 8 guanidine units (Sor-G8) was synthesized, and then was simply mixed with a cargo protein of varying sizes to form the non-covalent complex of carrier-cargo proteins...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28633107/effects-of-chemical-and-physical-enhancement-techniques-on-transdermal-delivery-of-3-fluoroamphetamine-hydrochloride
#16
Ashana Puri, Kevin S Murnane, Bruce E Blough, Ajay K Banga
The present study investigated the passive transdermal delivery of 3-fluoroamphetamine hydrochloride (PAL-353) and evaluated the effects of chemical and physical enhancement techniques on its permeation through human skin. In vitro drug permeation studies through dermatomed human skin were performed using Franz diffusion cells. Passive permeation of PAL-353 from propylene glycol and phosphate buffered saline as vehicles was studied. Effect of oleic acid, maltose microneedles, ablative laser, and anodal iontophoresis on its transdermal permeation was investigated...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28629984/the-contribution-of-the-in-vivo-fate-of-an-oil-depot-to-drug-absorption
#17
R W Kalicharan, C Oussoren, P Schot, E de Rijk, H Vromans
Sustained release of lipophilic compounds can be achieved with oil depots. These parenteral formulations are generally injected in the vastus lateralis and deltoid muscle. It is known that the absorption rate differs between these two muscles. The reason for this is not fully understood. The aim of the current study was to investigate the fate of an oil depot in different tissues to elucidate whether the disappearance rate of oil is the cause of observed differences in absorption rate. A study with healthy volunteers was conducted to determine 1...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28629983/self-assembly-nanostructure-controlled-sustained-release-activity-and-stability-of-peptide-drugs
#18
Xi-Rui Zhou, Yimeng Cao, Qiang Zhang, Xi-Bo Tian, He Dong, Long Chen, Shi-Zhong Luo
Peptides are considered as a new generation of drugs due to their high structural and functional diversity. However, the development of peptide drugs is always limited by their poor stability and short circulation time. Carriers are applied for peptide drug delivery, but there may be problems like poor loading efficiency and undesired xenobiotic toxicity. Peptide self-assembly is an effective approach to improve the stability and control the release of peptide drugs. In this study, two self-assembling anticancer peptides are designed by appending a pair of glutamic acid and asparagine to either the N-terminus or the C-terminus of a lytic peptide...
June 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28629982/polymeric-nanoparticles-promising-platform-for-drug-delivery
#19
REVIEW
Khalid M El-Say, Hossam S El-Sawy
Nano medicine had viewed countless breakthroughs in drug delivery implementations. The main objective of nanotechnology application in delivering and carrying many promising therapeutics is to assure drugs carriage to their action sites, to maximize the pharmacological desired influence of remedies and to overcome their limitations and drawbacks that would hinder the required effectiveness. One of these applications was the particulates type of nano-range in size and tremendous impact in achievement. About this specific diversity of particulates, the different elaboration methodologies, mandatory and elementary components for design, and examples of splendid success stories for these particulates were emphasized in this humble review...
June 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28629981/retrospective-quality-by-design-rqbd-applied-to-the-optimization-of-orodispersible-films
#20
Branca M A Silva, Sílvia Vicente, Sofia Cunha, Jorge F J Coelho, Cláudia Silva, Marco Seabra Reis, Sérgio Simões
The study demonstrates the application of QbD based on historical data for a product at a later development stage - retrospective QbD (rQbD). More specifically, it is investigated the root-cause for the observed slower drug release in Orodispersible Films (ODFs) during storage. Risk assessment tools were used to identify parameters affecting ODFs critical quality attributes, namely percent drug release and residual water content. The parameters room temperature, room relative humidity, drying temperature and mixing equipment were used in the statistical modeling of the available data...
June 16, 2017: International Journal of Pharmaceutics
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