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Drug Delivery and Translational Research

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https://www.readbyqxmd.com/read/28432657/in-vitro-assay-for-measuring-real-time-topotecan-release-from-liposomes-release-kinetics-and-cellular-internalization
#1
Roger Gilabert-Oriol, Lina Chernov, Malathi Anantha, Wieslawa H Dragowska, Marcel B Bally
Topotecan is a drug that is under investigation for the treatment of neuroblastoma and has been encapsulated into liposomes to improve its therapeutic efficacy. However, liposomal formulations still need to be optimized for drug retention and new techniques to measure drug release are required to better understand this process. Here, a novel in vitro method based on fluorescence de-quenching and an automated microscopy imaging platform were developed for monitoring, in real time, the release of topotecan from a liposomal formulation...
April 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28429276/enhancing-thermal-stability-of-a-highly-concentrated-insulin-formulation-with-pluronic-f-127-for-long-term-use-in-microfabricated-implantable-devices
#2
Jason Li, Michael K Chu, Brian Lu, Sako Mirzaie, Kuan Chen, Claudia R Gordijo, Oliver Plettenburg, Adria Giacca, Xiao Yu Wu
Development of highly concentrated formulations of protein and peptide drugs is a major challenge due to increased susceptibility to aggregation and precipitation. Numerous drug delivery systems including implantable and wearable controlled-release devices require thermally stable formulations with high concentrations due to limited device sizes and long-term use. Herein we report a highly concentrated insulin gel formulation (up to 80 mg/mL, corresponding to 2200 IU/mL), stabilized with a non-ionic amphiphilic triblock copolymer (i...
April 20, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28417445/chemopreventive-efficacy-of-curcumin-loaded-plga-microparticles-in-a-transgenic-mouse-model-of-her-2-positive-breast-cancer
#3
Alex E Grill, Komal Shahani, Brenda Koniar, Jayanth Panyam
Curcumin has shown promising inhibitory activity against HER-2-positive tumor cells in vitro but suffers from poor oral bioavailability in vivo. Our lab has previously developed a polymeric microparticle formulation for sustained delivery of curcumin for chemoprevention. The goal of this study was to examine the anticancer efficacy of curcumin-loaded polymeric microparticles in a transgenic mouse model of HER-2 cancer, Balb-neuT. Microparticles were injected monthly, and mice were examined for tumor appearance and growth...
April 17, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28389859/a-method-to-slow-down-the-ionization-dependent-release-of-risperidone-loaded-in-a-thermoresponsive-poly-n-acryloyl-glycinamide-hydrogel
#4
Mahfoud Boustta, Michel Vert
Poly(N-acryloyl glycinamide) polymers are soluble in hot aqueous media that gel rapidly on cooling. This gelatin-like behavior was previously compared with drug delivery requirements. Slow releases were demonstrated in vitro using different model molecules and macromolecules and in vivo using methylene blue. Risperidone is a weak basic drug sparingly soluble in water frequently used to treat patients suffering of schizophrenia. A standard risperidone-poly(N-acryloyl glycinamide) hydrogel formulation was selected from which the drug was allowed to release comparatively in buffered and non-buffered isotonic media at 37 °C under pseudo sink conditions...
April 7, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28386870/two-release-rates-from-monolithic-carboxymethyl-starch-tablets-formulation-characterization-and-in-vitro-in-vivo-evaluation
#5
Tien Canh Le, Mircea Alexandru Mateescu
Most of non-steroidal anti-inflammatory drugs (NSAIDs) including ibuprofen at more than 1200 mg/day may generate gastrointestinal and cardiovascular side effects. Bilayer or multiparticulate devices have been developed for controlled release in order to prevent undesired side effects. A new "two release rate (2RR) monolithic tablets" approach is now proposed for controlled release of poorly soluble drugs, particularly NSAIDs. Ibuprofen was used as model drug. This concept is based on a calcium carboxymethyl-starch (CaCMS) complex as a novel, low-cost excipient for monolithic dosage forms easy to manufacture by direct compaction...
April 6, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28364197/the-role-of-particle-size-of-glyburide-crystals-in-improving-its-oral-absorption
#6
Yongjun Wang, Wenqian Yang, Qiang Fu, Zhibin Guo, Bingjun Sun, Wen Liu, Yaxuan Liu, Simeng Mu, Mengran Guo, Jingru Li, Xiaohui Pu, Zhonggui He
Currently, nanosizing is becoming increasingly prevalent as an efficient way for the improvement of oral drug absorption. This study mainly focuses on two points, namely the crystal properties, and the in vitro and in vivo characterizations of drug crystals during the nanosizing process. We used glyburide, an oral type 2 diabetes (T2D) medication, as our model drug. We sought to reduce the crystalline size of this drug and evaluate its absorption properties by comparing it with the original coarse drug because of previous reports about its gastrointestinal absorption insufficiency...
March 31, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28349343/characterization-and-evaluation-of-a-peptide-based-sirna-delivery-system-in-vitro
#7
Baoling Chen, Kimoon Yoo, Wen Xu, Ran Pan, Xiao Xia Han, P Chen
Since its inception more than a decade ago, gene silencing mediated by double-stranded small interfering RNA (siRNA) has been widely investigated as a potential therapeutic approach for a variety of diseases. However, the use of siRNA is hampered by its rapid degradation and poor cellular uptake in vitro and in vivo. Recently, peptide-based carriers have been applied to siRNA delivery, as an alternative to the traditional delivery systems. Here, a histidine-containing amphipathic amino acid pairing peptide, C6M3, which can form complexes with siRNA, was used as a new siRNA delivery system...
March 27, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28324320/tailoring-the-properties-of-mpeg-plla-nanoparticles-for-better-encapsulation-and-tuned-release-of-the-hydrophilic-anticancer-drug
#8
Sachin S Surwase, Neha M Munot, Bhaskar B Idage, Susheela B Idage
Gemcitabine is used as a first-line drug for treating many solid tumours. However, it suffers from a major drawback of strong side effects and short plasma half-life because of degradation by enzyme when administered intravenously. Polyesters and copolyesters are the most widely used and preferred class of biodegradable polymer. In the present work, efforts have been made to prepare poly(ethylene glycol) monomethoxy ether-poly(L-lactide) (mPEG-PLLA), a biodegradable amphiphilic copolymer with a view to improve the entrapment and tuned release of hydrophilic drug gemcitabine...
March 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28321676/transdermal-delivery-of-human-growth-hormone-via-laser-generated-micropores
#9
Yang Song, Karishma Hemmady, Ashana Puri, Ajay K Banga
The epidermal skin barrier plays an important role in protecting underlying structures. It allows the passage of low molecular weight lipophilic molecules, but restricts the passage of hydrophilic molecules and macromolecules. The objective of this study was to investigate the feasibility of transdermal delivery of human growth hormone (hGH) through laser-microporated dermatomed porcine ear skin. The permeation of hGH was evaluated at different laser fluences and micropore densities. In vitro permeation studies were performed on vertical Franz diffusion cells using dermatomed porcine ear skin treated with ablative laser (2940 nm; P...
March 20, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28315051/development-of-antibody-modified-chitosan-nanoparticles-for-the-targeted-delivery-of-sirna-across-the-blood-brain-barrier-as-a-strategy-for-inhibiting-hiv-replication-in-astrocytes
#10
Jijin Gu, Karam Al-Bayati, Emmanuel A Ho
RNA interference (RNAi)-mediated gene silencing offers a novel treatment and prevention strategy for human immunodeficiency virus (HIV) infection. HIV was found to infect and replicate in human brain cells and can cause neuroinfections and neurological deterioration. We designed dual-antibody-modified chitosan/small interfering RNA (siRNA) nanoparticles to deliver siRNA across the blood-brain barrier (BBB) targeting HIV-infected brain astrocytes as a strategy for inhibiting HIV replication. We hypothesized that transferrin antibody and bradykinin B2 antibody could specifically bind to the transferrin receptor (TfR) and bradykinin B2 receptor (B2R), respectively, and deliver siRNA across the BBB into astrocytes as potential targeting ligands...
March 17, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28303451/improved-intestinal-absorption-of-water-soluble-drugs-by-acetylation-of-g2-pamam-dendrimer-nanocomplexes-in-rat
#11
Chengyun Yan, Jiwei Gu, Yuguang Lv, Weiguo Shi, Hongying Jing
In search of an effective and less toxic absorption enhancer, we synthesized primary amine acetylation of generation 2 polyamidoamine (G2 PAMAM) dendrimer (Ac-G2) by the reaction of G2 PAMAM dendrimer with acetic anhydride, and evaluated the effects of Ac-G2 on the intestinal absorption of poorly absorbable water-soluble drugs using an in situ closed-loop method in rats. The results indicated that Ac50-G2 had a greatest absorption enhancing effect for 5(6)-carboxyfluorescein (CF) in various acetylation levels of G2 PAMAM dendrimers...
March 16, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28299722/a-versatile-method-for-the-preparation-of-particle-loaded-microbubbles-for-multimodality-imaging-and-targeted-drug-delivery
#12
Joshua Owen, Calum Crake, Jeong Yu Lee, Dario Carugo, Estelle Beguin, Alexandre A Khrapitchev, Richard J Browning, Nicola Sibson, Eleanor Stride
Microbubbles are currently in clinical use as ultrasound contrast agents and under active investigation as mediators of ultrasound therapy. To improve the theranostic potential of microbubbles, nanoparticles can be attached to the bubble shell for imaging, targeting and/or enhancement of acoustic response. Existing methods for fabricating particle-loaded bubbles, however, require the use of polymers, oil layers or chemical reactions for particle incorporation; embed/attach the particles that can reduce echogenicity; impair biocompatibility; and/or involve multiple processing steps...
March 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28299721/pro-np%C3%A2-protect-against-tio2-nanoparticle-induced-phototoxicity-in-zebrafish-model-exploring-potential-application-for-skin-care
#13
Min-Sik Kim, Melinda Stees, Bala Vamsi K Karuturi, Sivakumar Vijayaraghavalu, Richard E Peterson, Gary L Madsen, Vinod Labhasetwar
Titanium dioxide nanoparticles (TiO2NPs) are used in sunscreen products to protect the skin from the sun's ultraviolet rays. However, following exposure to sunlight, the photocatalytic activity of TiO2NPs can produce an excess of reactive oxygen species (ROS), causing skin cell damage, triggering an inflammatory response. In zebrafish model, we evaluated how well Pro-NP™ (biodegradable NPs containing superoxide dismutase and catalase) could protect them from TiO2NP-induced photo-oxidative stress. We hypothesized that the antioxidant properties of Pro-NP™ would protect zebrafish embryos from the phototoxic effects of TiO2NPs, improving overall survival and growth...
March 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28290050/micellar-nano-carriers-for-the-delivery-of-stat3-dimerization-inhibitors-to-melanoma
#14
Amir H Soleimani, Shyam M Garg, Igor M Paiva, Mohammad R Vakili, Abdulraheem Alshareef, Yung-Hsing Huang, Ommoleila Molavi, Raymond Lai, Afsaneh Lavasanifar
The objective of this research was to develop polymeric micellar formulations of inhibitors of signal transducer and activator of transcription 3 (STAT3) dimerization, i.e., S3I-1757 and S3I-201, and evaluate the activity of successful formulations in B16-F10 melanoma, a STAT3 hyperactive cancer model, in vitro and in vivo. STAT3 inhibitory agents were encapsulated in methoxy poly(ethylene oxide)-b-poly(ε-caprolactone) (PEO114-b-PCL22) and methoxy poly(ethylene oxide)-b-poly(α-benzyl carboxylate-ε-caprolactone) (PEO114-b-PBCL20) micelles using co-solvent evaporation...
March 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28283842/a-pharmaceutical-study-on-lornoxicam-fast-disintegrating-tablets-formulation-and-in-vitro-and-in-vivo-evaluation
#15
Mohamed Yousif Moutasim, Aliaa Nabil ElMeshad, Mohamed Ahmed El-Nabarawi
Lornoxicam is an anti-inflammatory drug used to relieve rheumatoid arthritis pain, but the low water solubility and bitter taste of the drug present challenges for formulation as fast disintegrating tablets (FDTs). Complexation of the drug with β-cyclodextrin was initially carried out to increase the drug solubility and to mask its bitter taste. Tablets were prepared by direct compression of drug complex (DC), F-Melt, mannitol, crospovidone, and sodium starch glycolate (SSG). FDTs were characterized in terms of disintegration time (DT) and dissolution...
March 10, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28243978/evaluation-of-in-vitro-and-in-vivo-anti-urolithiatic-activity-of-silver-nanoparticles-containing-aqueous-leaf-extract-of-tragia-involucrata
#16
Vinodhini Velu, Moonjit Das, Arunai Nambi Raj N, Kamal Dua, Himaja Malipeddi
The present investigation is focused on exploring the anti-urolithiatic potential of aqueous leaf extract of Tragia involucrata (TIA) and its silver nanoparticles (AgNPs) and to quantify the total phenol, flavonoid, terpenoid and sterol contents present in TIA. Quantification results suggested TIA to be a rich source of phenol, flavonoid and terpenoid and less of sterol content. The AgNPs were synthesized by a simple green method using aqueous extract of T. involucrata. The formation of AgNPs was confirmed through UV spectroscopy, particle size analysis, zeta potential, X-ray diffraction and transmission electron microscopy...
February 27, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28243977/recent-advances-in-hemophilia-b-therapy
#17
REVIEW
Sarena D Horava, Nicholas A Peppas
Hemophilia B is a hereditary bleeding disorder caused by the deficiency in coagulation factor IX. Understanding coagulation and the role of factor IX as well as patient population and diagnosis are all critical factors in developing treatment strategies and regimens for hemophilia B patients. Current treatment options rely on protein replacement therapy by intravenous injection, which have markedly improved patient lifespan and quality of life. However, issues with current options include lack of patient compliance due to needle-based administration, high expenses, and potential other complications (e...
February 27, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28224375/lanolin-based-organogel-of-salicylic-acid-evidences-of-better-dermatokinetic-profile-in-imiquimod-induced-keratolytic-therapy-in-balb-c-mice-model
#18
Gajanand Sharma, Neelam Devi, Kanika Thakur, Ashay Jain, O P Katare
The primary aim of the present study was to develop lanolin-based organogel with enhanced delivery potential and reduced skin irritation for the treatment of hyperkeratotic lesions and scaling. The drug was encapsulated in the lipidic bilayers of organogel. The values of particle size, polydispersity index (PDI), and zeta potential of the developed carrier system was found to be 257.5 nm, 0.272, and -24.9 mV, respectively. The system was pseudoplastic in nature with the yield value of 2.3078 Pa. The skin permeation studies exhibited superiority of the prepared lanolin-based organogel formulation over the conventional gel formulation (CGF)...
February 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28194730/preparation-and-in-vitro-in-vivo-characterization-of-trans-resveratrol-nanocrystals-for-oral-administration
#19
Sandeep K Singh, Vishal Makadia, Shweta Sharma, Mamunur Rashid, Sudhir Shahi, Prabhat R Mishra, Mohammed Wahajuddin, Jiaur R Gayen
Trans -resveratrol (t-RES) is a natural polyphenolic compound with extensive therapeutic activities; however, its clinical application is circumscribed due to its poor solubility and low bioavailability. The purpose of this study was to prepare stable t-RES nanocrystals (t-RES-NCs) with different stabilizers to improve its oral bioavailability. t-RES-NCs were fabricated by the probe sonication method and optimized by particles size, poly dispersive index and zeta potential. The pharmaceutical characterization of t-RES-NCs was further performed systematically...
February 13, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28160258/effect-of-microneedles-on-transdermal-permeation-enhancement-of-amlodipine
#20
Buchi N Nalluri, Chandrateja Uppuluri, Jyothirmayee Devineni, Atul Nayak, Karthik J Nair, Benjamin R Whiteside, Diganta B Das
The present study aimed to investigate the effect of microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation enhancement of amlodipine (AMLO). Two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PM) of 0.6 mm length were employed. In the case of PMs, arrays were applied thrice at different places within a 1.77-cm(2) skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Scaling analyses were done using dimensionless parameters like concentration of AMLO (Ct/Cs), thickness (h/L) and surface area of the skin (Sa/L(2))...
February 3, 2017: Drug Delivery and Translational Research
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