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transdermal delivery system

Hisako Ibaraki, Takanori Kanazawa, Yuuki Takashima, Hiroaki Okada, Yasuo Seta
Nucleic acid-based targeting of nuclear factor kappaB (NF-κB) is gaining attention as a treatment option for skin diseases like atopic dermatitis (AD). Transdermal administration improves patient quality of life because of non-invasive; however, siRNA delivery into the skin can be challenging owing to the barrier of tight junctions in the granular layer. Therefore, we aimed to develop a delivery system of siRNA for topical skin application using functional peptides. We previously reported that combined treatment with a cytoplasm-responsive stearylated-arginine-rich peptide (STR-CH2 R4 H2 C) and a tight junction opening peptide (AT1002) showed high siRNA permeability in the skin of AD-induced and normal mice...
March 15, 2018: International Journal of Pharmaceutics
Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
Sabine Szunerits, Rabah Boukherroub
Advances in materials science and bionanotechnology have allowed the refinements of current drug delivery systems, expected to facilitate the development of personalized medicine. While dermatological topical pharmaceutical formulations such as foams, creams, lotions, gels, etc., have been proposed for decades, these systems target mainly skin-based diseases. To treat systemic medical conditions as well as localized problems such as joint or muscle concerns, transdermal delivery systems (TDDSs), which use the skin as the main route of drug delivery, are very appealing...
2018: Frontiers in Bioengineering and Biotechnology
Emma L Tombs, Vasiliki Nikolaou, Gabit Nurumbetov, David M Haddleton
Purpose: The main objective of this present study was the investigation of potential novel transdermal patch technology (TEPI®) delivering ibuprofen as the active pharmaceutical ingredient (API) using a novel poly(ether-urethane)-silicone crosslinked pressure-sensitive adhesive (PSA) as the drug reservoir in a solvent-free manufacturing process. Methods: The patch was synthesized utilizing the hot-melt crosslinking technique without the addition of solvents at 80 °C in 100% relative humidity...
2018: Journal of Pharmaceutical Innovation
Ying Hao, Wei Li, XingLi Zhou, Fan Yang, ZhiYong Qian
A microneedle (MN) is a micron-sized needle with a height of 10-2000 μm and a width of 10-50 μm, which can penetrate through the epidermis layer to dermal tissue directly without pain. Microneedles are widely used in transdermal drug delivery systems (TDDS) because they are efficient, safe, convenient and painless. Morphologically, microneedles are divided into four types: solid microneedles, coated microneedles, dissolving microneedles, and hollow microneedles. Different types of microneedles play different roles in different research fields...
December 1, 2017: Journal of Biomedical Nanotechnology
Swati Jagdale, Gokul Deore, Anuruddha Chabukswar
Background Nabumetone is biopharmaceutics classification system (BCS) class II drug, widely used in the treatment of osteoarthritis and rheumatoid arthritis. The most frequently reported adverse reactions for the drug involve disturbance in gastrointestinal tract , diarrhea, dyspepsia and abdominal pain. Microemulgel has advantages of microemulsion for improving solubility for hydrophobic drug. Patent literature had shown that the work for drug has been carried on spray chilling, enteric coated tablet, and topical formulation which gave idea for present research work for development of transdermal delivery...
February 26, 2018: Recent Patents on Drug Delivery & Formulation
Dhaval R Kalaria, Mayank Singhal, Vandana Patravale, Virginia Merino, Yogeshvar N Kalia
Effective treatment of Parkinson's disease (PD) involves administration of therapeutic agents with complementary mechanisms of action in order to replenish, sustain or substitute endogenous dopamine. The objective of this study was to investigate anodal co-iontophoresis of pramipexole (PRAM; dopamine agonist) and rasagiline (RAS; MAO-B inhibitor) in vitro and in vivo. Passive permeation of PRAM and RAS (20 mM each) across porcine skin after 6 h was 15.7±1.9 and 16.0±2.9 µg/cm2 , respectively. Co-iontophoresis at 0...
February 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Hongwei Lin, Qingchun Xie, Xin Huang, Junfeng Ban, Bo Wang, Xing Wei, Yanzhong Chen, Zhufen Lu
Aim: The aim of this work was to develop a novel vesicular carrier, ultradeformable liposomes (UDLs), to expand the applications of the Chinese herbal medicine, imperatorin (IMP), and increase its transdermal delivery. Methods: In this study, we prepared IMP-loaded UDLs using the thin-film hydration method and evaluated their encapsulation efficiency, vesicle deformability, skin permeation, and the amounts accumulated in different depths of the skin in vitro. The influence of different charged surfactants on the properties of the UDLs was also investigated...
2018: International Journal of Nanomedicine
Zhan Tang, Qiao Wang, Zhifen He, Lina Yin, Yawen Zhang, Shenghao Wang
Matrine is contained in several herbs used in traditional Chinese medicine, named Sophora alopecuroides, Sophora flavescens or Sophora subprostrata. In vitro and in vivo studies have focused on the treatment of chronic hepatitis or liver fibrosis using matrine. However, little is known about its liver pharmacokinetic profile. In this study pharmacokinetics of matrine in rat organs and tissues, such as liver, blood and skin were studied after intravenous (40 mg/kg) or transdermal administration (6 mg/cm2, 5 cm2)...
March 1, 2017: Die Pharmazie
Degong Yang, Xiaocao Wan, Peng Quan, Chao Liu, Liang Fang
Acrylic pressure sensitive adhesives (PSAs) are widely used in transdermal drug delivery system (TDDS). However, there was little research about the quantitative relationship between drug release and drug-PSAs interaction. In this study, five acrylic PSAs with different molar fraction of carboxyl group were designed and synthesized. Propranolol (PRO) was used as model drug to evaluate release profiles in the PSAs in vitro and in vivo. The drug release percent in the PSAs were 81.66, 78.22, 51.66, 21.81 and 11...
January 29, 2018: European Journal of Pharmaceutical Sciences
Yanqi Ye, Jicheng Yu, Di Wen, Anna R Kahkoska, Zhen Gu
The intrinsic properties of therapeutic proteins present a major impediment for transdermal delivery, including their relatively large molecule size and susceptibility to degradation. One solution is to utilize microneedles (MNs), which are capable of painlessly traversing the stratum corneum and directly translocating protein drugs into the systematic circulation. MNs can be designed to incorporate appropriate structural materials as well as therapeutics or formulations with tailored physicochemical properties...
January 30, 2018: Advanced Drug Delivery Reviews
Basant A Habib, Sinar Sayed, Ghada M Elsayed
This study aimed to formulate suitable nanovesicles (NVs) for transdermal delivery of Ondansetron. It also illustrated a practical example for the importance of Box-Cox transformation. A 23 full factorial design was used to enable testing transfersomes, ethosomes, and transethosomes of Ondansetron simultaneously. The independent variables (IVs) studied were sodium taurocholate amount, ethanol volume in hydration medium and sonication time. The studied dependent variables (DVs) were: particle size (PS), zeta potential (ZP) and entrapment efficiency (EE)...
January 30, 2018: European Journal of Pharmaceutical Sciences
Kimihiro Okubo, Eiji Uchida, Takaaki Terahara, Katsuhiko Akiyama, Shigeo Kobayashi, Yusuke Tanaka
BACKGROUND: Emedastine patch was developed in Japan as the first transdermal drug delivery system of emedastine difumarate for allergic rhinitis. METHODS: A multicenter, randomized, double-blind, placebo-controlled, parallel-group comparison was conducted in patients with seasonal allergic rhinitis. Patients were administered emedastine patches (4 or 8 mg), placebo, or levocetirizine hydrochloride (5 mg tablet) once daily for 2 weeks (double-dummy technique). The primary objective was superiority to placebo by the change of the total nasal symptom score (sneezing, rhinorrhea, and nasal congestion) in Week 2...
January 29, 2018: Allergology International: Official Journal of the Japanese Society of Allergology
Mohamed Ali, Amira Abdel Motaal, Mohammed A Ahmed, Abdulrhman Alsayari, Omaima N El-Gazayerly
The active compounds present in Hypericum perforatum L. (Hypericaceae) include hyperforin, hypericins and flavonoids, which are assumed to be responsible for the activity of the extract in the treatment of wounds and scars. The present study aimed to incorporate H. perforatum extract standardized to a known content of phloroglucinols, naphthodianthrones and polyphenolic compounds into an effective transdermal drug delivery system capable of entrapping both lipophilic and hydrophilic constituents in the form of niosomal gels for wound treatment...
November 2018: Drug Delivery
Sophia N Economidou, Dimitrios A Lamprou, Dennis Douroumis
The role of two and three-dimensional printing as a fabrication technology for sophisticated transdermal drug delivery systems is explored in literature. 3D printing encompasses a family of distinct technologies that employ a virtual model to produce a physical object through numerically controlled apparatuses. The applicability of several printing technologies has been researched for the direct or indirect printing of microneedle arrays or for the modification of their surface through drug-containing coatings...
January 17, 2018: International Journal of Pharmaceutics
Saikat Ghosh, Biswajit Mukherjee, Shreyasi Chaudhuri, Tanushree Roy, Alankar Mukherjee, Soma Sengupta
Aspasomes of methotrexate with antioxidant, ascorbyl palmitate, were developed and optimized using factorial design by varying parameters such as lipid molar ratio, drug to lipid molar ratio, and type of hydration buffer for transdermal delivery for disease modifying activity in rheumatoid arthritis (RA). Aspasomes were characterized by drug-excipients interaction, particle size analysis, determination of zeta potential, entrapment efficiency, and surface properties. The best formulation was loaded into hydrogel for evaluation of in vitro drug release and tested in vivo against adjuvant induced arthritis model in wistar rats, by assessing various physiological, biochemical, hematological, and histopathological parameters...
January 16, 2018: AAPS PharmSciTech
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
Morteza Amjadi, Sahar Sheykhansari, Bradley J Nelson, Metin Sitti
Wearable transdermal delivery systems have recently received tremendous attention due to their noninvasive, convenient, and prolonged administration of pharmacological agents. Here, the material prospects, fabrication processes, and drug-release mechanisms of these types of therapeutic delivery systems are critically reviewed. The latest progress in the development of multifunctional wearable devices capable of closed-loop sensation and drug delivery is also discussed. This survey reveals that wearable transdermal delivery has already made an impact in diverse healthcare applications, while several grand challenges remain...
January 8, 2018: Advanced Materials
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
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
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