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Drug delivery skin

Jonas G Croissant, Jeffrey I Zink, Laurence Raehm, Jean-Olivier Durand
Coherent two-photon-excited (TPE) therapy in the near-infrared (NIR) provides safer cancer treatments than current therapies lacking spatial and temporal selectivities because it is characterized by a 3D spatial resolution of 1 µm3 and very low scattering. In this review, the principle of TPE and its significance in combination with organosilica nanoparticles (NPs) are introduced and then studies involving the design of pioneering TPE-NIR organosilica nanomaterials are discussed for bioimaging, drug delivery, and photodynamic therapy...
January 18, 2018: Advanced Healthcare Materials
Nataša Z Bubić Pajić, Marija N Todosijević, Gordana M Vuleta, Nebojša D Cekić, Vladimir D Dobričić, Sonja R Vučen, Bojan R Čalija, Milica Ž Lukić, Tanja M Ilić, Snežana D Savić
Two types of biocompatible surfactants were evaluated for their capability to formulate skin-friendly/non-irritant microemulsions as vehicles for two poorly water-soluble model drugs differing in properties and concentrations: alkyl polyglucosides (decyl glucoside and caprylyl/capryl glucoside) and ethoxylated surfactants (glycereth-7-caprylate/ caprate and polysorbate 80). Phase behavior, structural inversion and microemulsion solubilization potential for sertaconazole nitrate and adapalene were found to be highly dependent on the surfactants structure and HLB value...
December 20, 2017: Acta Pharmaceutica
Michele Campos Alves, Priscila Aparecida de Almeida, Hudson Caetano Polonini, Carla Aparecida Pereira Bhering, Anderson de Oliveira Ferreira, Marcos Antonio Fernandes Brandao, Nadia Rezende Barbosa Raposo
BACKGROUND: Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract...
January 15, 2018: Current Drug Delivery
Gentry T King, Keith D Eaton, Brandon R Beagle, Christopher J Zopf, Gilbert Y Wong, Heike I Krupka, Steven Y Hua, Wells A Messersmith, Anthony B El-Khoueiry
Purpose and Methods Trop-2 is a glycoprotein over-expressed in many solid tumors but at low levels in normal human tissue, providing a potential therapeutic target. We conducted a phase 1 dose-finding study of PF-06664178, an antibody-drug conjugate that targets Trop-2 for the selective delivery of the cytotoxic payload Aur0101. The primary objective was to determine the maximum tolerated dose and recommended phase 2 dose. Secondary objectives included further characterization of the safety profile, pharmacokinetics and antitumor activity...
January 15, 2018: Investigational New Drugs
Willi Cawello, Marina Braun, Jens-Otto Andreas
BACKGROUND AND OBJECTIVE: Pharmacokinetic studies using deconvolution methods and non-compartmental analysis to model clinical absorption of drugs are not well represented in the literature. The purpose of this research was (1) to define the system of equations for description of rotigotine (a dopamine receptor agonist delivered via a transdermal patch) absorption based on a pharmacokinetic model and (2) to describe the kinetics of rotigotine disposition after single and multiple dosing...
January 13, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Vic A Narurkar, Tina S Alster, Eric F Bernstein, Tina J Lin, Anya Loncaric
<p>BACKGROUND: Fractional photothermolysis (FP) is a popular treatment option for photodamaged skin and addresses shortcomings of ablative skin resurfacing and nonablative dermal remodeling. Previous studies have demonstrated that FP using the 1550nm wavelength has led to improvement of ultrastructural changes and clinical effects associated with photodamaged skin in the deeper dermal structures, while treatment with the 1927nm wavelength has shown clinical effects in the superficial dermis. Both wavelengths produce precise microscopic treatment zones (MTZs) in the skin...
January 1, 2018: Journal of Drugs in Dermatology: JDD
E Carazo, A Borrego-Sánchez, F García-Villén, R Sánchez-Espejo, P Cerezo, C Aguzzi, C Viseras
On/into/through the skin drug delivery represents an attractive alternative for the oral route, providing local and/or systemic drug delivery. Due to its complex and well-organised structure, most of the drugs show difficulties to penetrate the human skin. Therefore, enormous efforts have been invested to develop intelligent drug delivery systems overcoming the skin barrier with particular emphasis on increasing therapeutic activity and minimizing undesirable side-effects. Most of these strategies require the use of singular materials with new properties...
January 5, 2018: Chemical Record: An Official Publication of the Chemical Society of Japan ... [et Al.]
Rasha R Radwan, Heba A Mohamed, H E Ali, Ghada A Mahmoud
In the present study, L-arginine/acrylic acid (Arg/AAc) batch hydrogel was successfully prepared by gamma irradiation for transdermal delivery of propranolol HCl in hypertensive rats. The resulted system has been characterized by FTIR to confirm the hydrogel formation. The swelling behavior of the prepared hydrogels was investigated as a function of time and pH. The kinetics of swelling has been investigated. In vivo pharmacokinetics evaluation, skin irritation test, and histopathological studies were investigated...
January 8, 2018: Drug Delivery and Translational Research
Yanlin Wang, Na Jing, Linlin Su, Changhe Shi, Pei Zhang, Zhilei Wang, Huifang Sun, Jing Yang, Yutao Liu, Xuejun Wen, Jin Zhang, Shoutao Zhang, Yuming Xu
Skin fibroblasts were obtained from a 42-year-old Alzheimer's disease (AD) patient carrying mutations in the PSEN1 gene. An iPSC line was successfully established using the Sendai-virus (SeV) delivery system. The patient-specific iPSCs were free of genomically integrated reprogramming genes, had the specific mutation, expressed the expected pluripotency markers, and had the potential to differentiate into cells of all three germ layers. Our model might offer a robust platform for further study of the pathomechanism of this disease as well as drug testing and gene therapy studies...
December 12, 2017: Stem Cell Research
Bo Zhi Chen, Mohammad Ashfaq, Xiao Peng Zhang, Jia Nan Zhang, Xin Dong Guo
Microneedles (MNs) system for transdermal drug delivery has the potential to improve therapeutic efficacy, proving an approach that is more convenient and acceptable than traditional medication systems. The present study systematically researched dissolving polymer MNs fabricated from various common FDA-approved biocompatible materials, including gelatin, chitosan, hyaluronic acid (HA) and polyvinyl alcohol (PVA). Upon application of MN patches to the porcine cadaver skin, the MNs effectively perforated the skin and delivered drugs to subcutaneous tissue on contact with the interstitial fluid...
January 5, 2018: Journal of Drug Targeting
Mohesh Moothanchery, Razina Z Seeni, Chenjie Xu, Manojit Pramanik
Microneedle technology allows micron-sized conduits to be formed within the outermost skin layers for both localized and systemic delivery of therapeutics including nanoparticles. Histological methods are often employed for characterization, and unfortunately do not allow for the in vivo visualization of the delivery process. This study presents the utilization of optical resolution-photoacoustic microscopy to characterize the transdermal delivery of nanoparticles using microneedles. Specifically, we observe the in vivo transdermal delivery of gold nanoparticles using microneedles in mice ear and study the penetration, diffusion, and spatial distribution of the nanoparticles in the tissue...
December 1, 2017: Biomedical Optics Express
Yiping Deng, Fengjian Yang, Xiuhua Zhao, Lu Wang, Weiwei Wu, Chang Zu, Mingfang Wu
Ibuprofen (IBU) is an effective analgesic, non-steroidal anti-inflammatory drug. Unfortunately, oral IBU can cause adverse gastrointestinal drug reactions, such as bleeding and ulcerations, and increases the risk for stomach or intestinal perforations. In this study, IBU nanoparticles (IBU-NPs) were prepared through emulsion solvent evaporation and freeze-drying to improve their solubility. IBU nanoemulsion and nanosuspension were optimized through a single-factor experiment. IBU-NPs with a mean particle size of 216...
December 27, 2017: European Journal of Pharmaceutical Sciences
Maria Natalia Calienni, Carlos Facundo Temprana, Maria Jimena Prieto, Donatella Paolino, Massimo Fresta, Ayse Begum Tekinay, Silvia Del Valle Alonso, Jorge Montanari
With the aim of improving the topical delivery of the antineoplastic drug 5-fluorouracil (5FU), it was loaded into ultradeformable liposomes composed of soy phosphatidylcholine and sodium cholate (UDL-5FU). The liposome populations had a mean size of 70 nm without significant changes in 56 days, and the ultradeformable formulations were up to 324-fold more elastic than conventional liposomes. The interaction between 5FU and the liposomal membrane was studied by three methods, and also release profile was obtained...
December 30, 2017: Drug Delivery and Translational Research
Tamara N Tarbox, Alan B Watts, Zhengrong Cui, Robert O Williams
Recently, results have been published for the first successful phase I human clinical trial investigating the use of dissolving polymeric microneedles… Even so, further clinical development represents an important hurdle that remains in the translation of microneedle technology to approved products. Specifically, the potential for accumulation of polymer within the skin upon repeated application of dissolving and coated microneedles, combined with a lack of safety data in humans, predicates a need for further clinical investigation...
December 29, 2017: Drug Delivery and Translational Research
Yutaka Inoue, Mitsue Hibino, Isamu Murata, Ikuo Kanamoto
PURPOSE: As trisodium L-ascorbyl 2-phosphate 6-palmitate (APPS), an ascorbic acid derivative, is an amphiphilic substance, it forms micelles in aqueous solutions. Micelles are used as drug carriers and can emulsify drugs that are poorly soluble in water, such as nadifloxacin (NDFX). The purpose of this study was to prepare nanocarriers using APPS to carry NDFX into Yucatan micropig skin. METHODS: After synthesis of the NDFX nanoparticles by using the hydration method, physical evaluations were carried out that included assessments of particle size and zeta potential, encapsulation efficiency, particle structure by transmission electron microscopy, 31P-NMR spectra, and particle stability...
December 28, 2017: Pharmaceutical Research
Luisa S Dolci, Anna Liguori, Silvia Panzavolta, Anna Miserocchi, Nadia Passerini, Matteo Gherardi, Vittorio Colombo, Adriana Bigi, Beatrice Albertini
In this paper we developed an innovative, effective and rapid one-step approach to crosslink mucoadhesive gelatin films for buccal drug delivery. The method, which involves the application of non-equilibrium pressure plasma for 3 or 5 minutes/side, was compared with a classical approach based on the use of a chemical crosslinking agent, namely genipin. Econazole nitrate (ECN), an imidazole antifungal agent used for the treatment of skin infections and mucosal candidiasis, was selected as model drug. X-Ray Diffraction characterization performed on the drug-containing gelatin films revealed that ECN undergoes to a topotactic transformation into Econazole (EC) immediately after mixing with gelatin suggesting the occurrence of an acid-base reaction between drug and gelatin during film processing...
December 19, 2017: Colloids and Surfaces. B, Biointerfaces
Reinhard H H Neubert, Elfi Sommer, Melanie Schölzel, Benjamin Tuchscherer, Yahja Mrestani, Johannes Wohlrab
Due to the lipophilic properties of the uppermost skin layer of the stratum corneum (SC) it is highly challenging to reach therapeutic concentrations of cosmetic actives and drugs. Particularly, the hydrophilic ones penetrate poorly across the SC. The purpose of this study was to improve the topical bioavailability of the hydrophilic, polar tetrapeptide PKEK (amino acid sequence in one-letter notation). A nano-sized carrier system (microemulsion, ME) was therefore developed since MEs provide excellent penetration enhancing properties...
December 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Hye-Gyeong Kim, Deborah L Gater, Yeu-Chun Kim
Although vitamin D3 (VD3), which is the main form of vitamin D, can be produced in human skin under the sunlight, vitamin D deficiency emerged as a major public health problem worldwide. Mainly, oral supplements or vitamin D-fortified foods are distributed to help supplementation of vitamin D. However, those oral methods are limitedly supplied in the Middle East countries, and oral absorption has low efficiency due to many barriers and various changes of conditions along the route. Then, it is recommended to take them every day in order to maintain the adequate serum level of vitamin D...
December 16, 2017: Drug Delivery and Translational Research
Kunat Suktham, Thongchai Koobkobkruad, Tuksadon Wutikhun, Suvimol Surassmo
Sericin protein nanoparticles are a biocompatible, bio-viable class of nanocarriers gaining prominence in drug delivery system. This research aimed to investigate the suitability fabrication of silk protein (SP) nanoparticles for loading with resveratrol (RSV) via a solventless precipitation technique. The addition of 0.5% (w/v) pluronic surfactant proved optimal for SP nanoparticle fabrication, with obtained nanoparticles being spherical, mono-dispersed and having mean size of approximately 200-400 nm. All exhibited negative surface charges, the extent of which being dependent on the SP concentration, and were non-toxic to normal skin fibroblasts (CRL-2522)...
December 8, 2017: International Journal of Pharmaceutics
M Giulbudagian, S Hönzke, J Bergueiro, D Işık, F Schumacher, S Saeidpour, S B Lohan, M C Meinke, C Teutloff, M Schäfer-Korting, G Yealland, B Kleuser, S Hedtrich, M Calderón
Highly hydrophilic, responsive nanogels are attractive as potential systems for the topical delivery of bioactives encapsulated in their three-dimensional polymeric scaffold. Yet, these drug carrier systems suffer from drawbacks for efficient delivery of hydrophobic drugs. Addressing this, β-cyclodextrin (βCD) could be successfully introduced into the drug carrier systems by exploiting its unique affinity toward dexamethasone (DXM) as well as its role as topical penetration enhancer. The properties of βCD could be combined with those of thermoresponsive nanogels (tNGs) based on dendritic polyglycerol (dPG) as a crosslinker and linear thermoresponsive polyglycerol (tPG) inducing responsiveness to temperature changes...
December 11, 2017: Nanoscale
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