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Drug Delivery and Translational Research

Amarjitsing Rajput, Aditi Bariya, Ahmed Allam, Sarah Othman, Shital B Butani
The purpose of conducting the present research work was to develop resveratrol nanostructured in situ gel for the treatment of Alzheimer's disease. Resveratrol loaded lipid carrier was prepared by melt emulsification-probe sonication method, and the final product was evaluated for particle size (132 ± 11.90 nm), polydispersity index (0.209 ± 0.005), zeta potential (- 23 ± 3.79 mV), drug loading (9.26 ± 3.79%), and entrapment efficiency (74 ± 11.40%). Following incorporation of the resveratrol nanostructured lipid carrier in gellan gum and xanthan gum, in situ gel was formulated and characterized...
May 21, 2018: Drug Delivery and Translational Research
Yingchao Li, Yongjun Wang, Ran Zhang, Cuiru Liu, Yue Wei, Jin Sun, Zhonggui He, Youjun Xu, Tianhong Zhang
Tapentadol suffers from rapid clearance due to extensive metabolism in vivo, which results in low oral bioavailability. In the present study, three novel prodrugs of tapentadol (WWJ01, WWJ02, and WWJ03) were synthesized to improve its metabolic stability and thereby improve its oral bioavailability. They all exhibited good stability in phosphate buffers, simulated gastrointestinal fluids, rat plasma, and intestinal and liver homogenates. Disappointingly, the N,N-diethylcarbamate prodrug of tapentadol (WWJ02) and the N,N-diisopropylcarbamate prodrug of tapentadol (WWJ03) were metabolized into inactive metabolites when incubated with liver microsomes...
May 17, 2018: Drug Delivery and Translational Research
Lara E Pereira, Tyana Singletary, Amy Martin, Chuong T Dinh, Frank Deyounks, Angela Holder, Janet McNicholl, Karen W Buckheit, Robert W Buckheit, Anthony Ham, David F Katz, James M Smith
This study evaluated effects of differing gel volumes on pharmacokinetics (PK). IQB4012, a gel containing the non-nucleoside reverse transcriptase inhibitor IQP-0528 and tenofovir (TFV), was applied to the pigtailed macaque vagina and rectum. Vaginal gel volumes (1% loading of both drugs) were 0.5 or 1.5 ml; following wash-out, 1 or 4 ml of gel were then applied rectally. Blood, vaginal, and rectal fluids were collected at 0, 2, 4, and 24 h. Vaginal and rectal tissue biopsies were collected at 4 and 24 h...
May 14, 2018: Drug Delivery and Translational Research
Nils K Prenzler, Rolf Salcher, Max Timm, Lutz Gaertner, Thomas Lenarz, Athanasia Warnecke
Suppression of foreign body reaction, improvement of electrode-nerve interaction, and preservation of residual hearing are essential research topics in cochlear implantation. Intracochlear pharmaco- or cell-based therapies can open new horizons in this field. Local drug delivery strategies are desirable as higher local concentrations of agents can be realized and side effects can be minimized compared to systemic administrations. When administered locally at accessible, basal parts of the cochlea, drugs reach apical regions later and in much lower concentrations due to poor diffusion patterns in cochlear fluids...
May 14, 2018: Drug Delivery and Translational Research
Alexis Guionet, S Moosavi Nejad, Justin Teissié, Takashi Sakugawa, Sunao Katsuki, Hidenori Akiyama, Hamid Hosseini
Pulsed electric fields (PEFs) are applied as physical stimuli for DNA/drug delivery, cancer therapy, gene transformation, and microorganism eradication. Meanwhile, calcium electrotransfer offers an interesting approach to treat cancer, as it induces cell death easier in malignant cells than in normal cells. Here, we study the spatial and temporal cellular responses to 10 μs duration PEFs; by observing real-time, the uptake of extracellular calcium through the cell membrane. The experimental setup consisted of an inverted fluorescence microscope equipped with a color high-speed framing camera and a specifically designed miniaturized pulsed power system...
May 11, 2018: Drug Delivery and Translational Research
Chandra Bhushan Tripathi, Poonam Parashar, Malti Arya, Mahendra Singh, Jovita Kanoujia, Gaurav Kaithwas, Shubhini A Saraf
Breast cancer is the most common cancer of occurrence in women and has the highest mortality incidence rate therein. The present study envisaged to develop doxorubicin (Dox) loaded folate functionalized nanoemulsion (NE) for profound therapeutic activity against mammary gland cancer. NE was prepared using pseudo-ternary phase diagrams utilizing α-linolenic acid (ALA) as lipid phase, to further enhance the anticancer potential of Dox. Box-Behnken design was employed to systematically develop the NE. Optimized NE (f-Dox-NE) was evaluated for in vitro and in vivo performance...
May 10, 2018: Drug Delivery and Translational Research
Wei Wei, Zhonggui He, Jincheng Yang, Mengchi Sun, Jin Sun
Rational design of anticancer prodrugs for efficient albumin binding can show distinct advantages in drug delivery in terms of high drug availability, long systemic circulation, potential targeting effect, and enhanced chemotherapy effect. In the present study, we reported a cytosine arabinoside (Ara-C) prodrug which could well formulate in solution and instantly transform into long-circulating nanocomplexes by hitchhiking blood-circulating albumin after i.v. administration. Specifically, Ara-C was conjugated with an albumin-binding maleimide derivative, the resulting Ara-C maleimide caproic acid conjugate (AM) was well formulated in aqueous solution, conferring high albumin-binding ability in vitro albumin-binding studies...
May 10, 2018: Drug Delivery and Translational Research
Yinxian Yang, Hailing Gao, Shuang Zhou, Xiao Kuang, Zhenjie Wang, Hongzhuo Liu, Jin Sun
Parenteral therapy for severe and complicated malaria is necessary, but currently available parenteral antimalarials have their own drawbacks. As for recommended artemisinin-based combination therapy, antimalarial artemether and lumefantrine are limited in parenteral delivery due to their poor water solubility. Herein, the aim of this study was to develop the lipid-based emulsions for intravenous co-delivery of artemether and lumefantrine. The lipid emulsion was prepared by high-speed shear and high-pressure homogenization, and the formulations were optimized mainly by monitoring particle size distribution under autoclaved conditions...
May 10, 2018: Drug Delivery and Translational Research
Mohd Cairul Iqbal Mohd Amin, Lik Voon Kiew, Benjamin Boyd
No abstract text is available yet for this article.
May 10, 2018: Drug Delivery and Translational Research
K Madhumathi, Y Rubaiya, Mukesh Doble, R Venkateswari, T S Sampath Kumar
A dual local drug delivery system (DDS) composed of calcium phosphate bioceramic nanocarriers aimed at treating the antibacterial, anti-inflammatory, and bone-regenerative aspects of periodontitis has been developed. Calcium-deficient hydroxyapatite (CDHA, Ca/P = 1.61) and tricalcium phosphate (β-TCP) were prepared by microwave-accelerated wet chemical synthesis method. The phase purity of the nanocarriers was confirmed by x-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR), while the transmission electron microscopy (TEM) confirmed their nanosized morphology...
May 1, 2018: Drug Delivery and Translational Research
Pushkar Kulkarni, Marina Rajadurai, Aarti Sevilimedu, Surendar Basaveni, Swapna Yellanki, Raghavender Medishetti, Uday Saxena
Lung cancer is the single largest cause of cancer related deaths in the world. Current treatments include surgery, radiation therapy, chemotherapy using cytotoxic drugs, and monoclonal antibodies. Such treatments have limited efficacy due to diverse nature of lung cells involved and lack of tissue penetration. Cytotoxic drugs, while potent, have the enormous drawback of limited entry into the lung selectively, thus causing collateral damage to other tissues. To overcome these shortcomings, we report here the development of new magnetic irinotecan containing nanoparticles (NPs), which target the lung over other tissues by over 5-fold...
May 1, 2018: Drug Delivery and Translational Research
Zhen Li, Min Song, Zhun He, Ling Zong, Bo Jiang, Tao Zhang, Zhiliang Hu
Systematic chemotherapy has required high time span for recovery in cancer patients, serious toxic effects, and increased the time of cancer-free survival of patient but decreased the overall survival time of patients irrespective of diseased condition(s). To compare the quick recovery of inhalable doxorubicin and cisplatin in the lung cancer patients. A total of 240 patients with non-small cell lung cancer (NSCLC) patients were randomly divided into two groups of 120 each. Patients had inhaled 25 mg/m2 doxorubicin (DON group) or 10 mg/m2 cisplatin (CPN group) once in a day for 21 days...
May 1, 2018: Drug Delivery and Translational Research
Anurag Pramanik, Sanjeev Garg
An in silico approach is proposed to first predict the partition coefficient of the model drug, paclitaxel, in different biocompatible and biodegradable polymer versus the blood plasma using artificial neural networks (ANNs) and semi-empirical quantitative structure property relationships (QSPRs). A simplified molecular-input line-entry system (SMILES) notation is used to represent the structures of the different polymers and the drug. The SMILES notation is then used to calculate the various structure-based descriptors...
April 26, 2018: Drug Delivery and Translational Research
M R Fontanilla, S Casadiegos, R H Bustos, M A Patarroyo
Cytokines, chemokines, and growth and remodeling factors orchestrate wound healing when skin damage occurs. During early stages, when the wound is still open, detection and quantification of these compounds might provide biomarkers of skin wound healing, which could aid to complete the scenario provided by clinical follow-up data and histological and histomorphometric analyses. This work assessed and compared the healing of full-thickness skin wounds grafted with artificial dermis made with autologous skin fibroblasts and unidirectional or multidirectional type I collagen scaffolds to test this hypothesis...
April 24, 2018: Drug Delivery and Translational Research
Azren Aida Asmawi, Norazlinaliza Salim, Cheng Loong Ngan, Haslina Ahmad, Emilia Abdulmalek, Mas Jaffri Masarudin, Mohd Basyaruddin Abdul Rahman
Docetaxel has demonstrated extraordinary anticancer effects on lung cancer. However, lack of optimal bioavailability due to poor solubility and high toxicity at its therapeutic dose has hampered the clinical use of this anticancer drug. Development of nanoemulsion formulation along with biocompatible excipients aimed for pulmonary delivery is a potential strategy to deliver this poorly aqueous soluble drug with improved bioavailability and biocompatibility. In this work, screening and selection of pharmaceutically acceptable excipients at their minimal optimal concentration have been conducted...
April 24, 2018: Drug Delivery and Translational Research
Mridul Majumder, Saeid Rajabnezhad, Ali Nokhodchi, Mohammed Maniruzzaman
The current study explores the first case of the implementation of solution calorimetry (SolCal) in order to determine the amorphous content of crystalline benzoyl-methoxy-methylindol-acetic acid (BMA)-a model poorly soluble drug, in the amorphous granules prepared via single-step continuous twin-screw dry granulations (TSG). Amorphous magnesium aluminometasilicate (Neusilin®) (US2) was used as a novel inorganic carrier via a TwinLab 10 mm twin-screw extruder. The BMA/US2 blends were processed at 180 °C and varying drug: carrier ratios of 1:4, 1:2...
April 24, 2018: Drug Delivery and Translational Research
Ruby Bansal, Brashket Seth, Shashikant Tiwari, Sadaf Jahan, Manisha Kumari, Aditya Bhushan Pant, Rajnish Kumar Chaturvedi, Pradeep Kumar, Kailash Chand Gupta
Development of efficient and safe nucleic acid carriers is one of the most challenging requirements to improve the success of gene therapy. Here, we synthesized a linker, 3-(hexadecyloxy)-1-chloropropan-2-ol, and grafted it onto linear polyethylenimine in varying amounts to obtain a series of HD-lPEI polymers that were able to form self-assembled nanoparticles (SN). 1 H-NMR spectrometry was used to determine the extent of grafting of the linker, HD, on to the lPEI backbone. We further complexed the SN of HD-lPEI with plasmid DNA (pDNA) and the resultant nanoplexes were characterized by their size and zeta potential and further evaluated for their transfection ability and cytotoxicity in MCF-7 cells...
April 18, 2018: Drug Delivery and Translational Research
Wan Maznah Wan Ishak, Haliza Katas, Ng Pei Yuen, Maizaton Atmadini Abdullah, Mohd Hanif Zulfakar
Wound healing is a physiological event that generates reconstitution and restoration of granulation tissue that ends with scar formation. As omega fatty acids are part of membrane phospholipids and participate in the inflammatory response, we investigated the effects of omega-3, omega-6, and omega-9 fatty acids in the form of oils on wound healing. Linseed (LO), evening primrose (EPO), and olive oils (OO) rich in omega-3, omega-6, and omega-9 fatty acids were formulated into emulsions and were topically applied on rats with excision wounds...
April 17, 2018: Drug Delivery and Translational Research
Hans F Fritz, Andrea C Ortiz, Sitaram P Velaga, Javier O Morales
High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsulate a poorly water-soluble drug, nifedipine (NFD), by hot-melt emulsification, a low-energy method. LCMs are self-assembling colloidal particles composed of a hydrophobic core and a hydrophilic shell...
April 16, 2018: Drug Delivery and Translational Research
María Florencia Sanchez, Susana Andrea Breda, Elio Andrés Soria, Luis Ignacio Tártara, Rubén Hilario Manzo, María Eugenia Olivera
The purpose of this work was to develop an effective carbomer hydrogel to be used to treat second-degree burns that combined ciprofloxacin and lidocaine (CbCipLid hydrogel). Its antibiotic and anesthetic efficacy and the physical and chemical properties of the CbCipLid hydrogel (release rate and kinetics, rheology, appearance, and drug content) were evaluated both before and after a sterilization cycle and also after 6 months of storage. For the in vivo studies, second-degree burns were developed in a rat model...
April 13, 2018: Drug Delivery and Translational Research
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