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Drug delivery skin

R Petrilli, J O Eloy, J A R Paschoal, R F V Lopez
5-Fluorouracil (5-FU) is used for the topical treatment of pre-cancerous skin lesions. However, previous reports focus on 5-FU quantification in plasma samples, failing to provide information about drug quantification in the skin. Therefore, the aim of this work was to develop a simple and reliable analytical method employing HPLC-UV for 5-FU quantification in skin samples. Chromatographic separation was obtained using the commonly available Lichrospher RP-C18 endcapped column. Porcine ear skin matrix-based analytical curves with thymine, as internal standard, were used...
March 5, 2018: Die Pharmazie
Sarunya Tuntiyasawasdikul, Ekapol Limpongsa, Napaphak Jaipakdee, Bungorn Sripanidkulchai
RATIONAL: Phytoestrogens have been found to delay signs of skin aging in post-menopausal women, in a way similar to the effects of estrogens. Diarylheptanoids from a rhizome of traditional Thai herb named Curcuma comosa is considered to be a novel class of phytoestrogens. OBJECTIVES: The aims of this study were to prepare effective topical films using mixed types and vary ratios of hydrophobic (Eudragit RL, Eudragit RS, and Eudragit NE) and hydrophilic polymer (hydroxylpropyl methycellulose, HPMC) with Transcutol as a permeation enhancer for delivery of diarylheptanoids to improve signs of skin aging in post-menopausal women...
March 15, 2018: Drug Development and Industrial Pharmacy
Mayte Martinez-Martinez, Guillermo Rodriguez-Berna, Isabel Gonzalez Alvarez, M Jesus Hernandez, Avelino Corma, Marival Bermejo, Virginia Merino, Marta Gonzalez-Alvarez
In this work, 6-phosphogluconic trisodium salt (6-PG-Na+) is introduced as a new aqueous and non-toxic crosslinker agent to obtain ionic hydrogels. Here, it is shown the formation of hydrogels based on chitosan crosslinked with 6-PG-Na+. This formulation is obtained by ionic interaction of cationic groups of polymer with anionic groups of crosslinker. These hydrogels are non-toxic, do not cause dermal irritation, are easy to extend and have an adequate adhesion force to be applied as polymeric film over the skin...
March 14, 2018: Biomacromolecules
Michael A Luzuriaga, Danielle R Berry, John C Reagan, Ronald A Smaldone, Jeremiah J Gassensmith
Biodegradable polymer microneedle (MN) arrays are an emerging class of transdermal drug delivery devices that promise a painless and sanitary alternative to syringes; however, prototyping bespoke needle architectures is expensive and requires production of new master templates. Here, we present a new microfabrication technique for MNs using fused deposition modeling (FDM) 3D printing using polylactic acid, an FDA approved, renewable, biodegradable, thermoplastic material. We show how this natural degradability can be exploited to overcome a key challenge of FDM 3D printing, in particular the low resolution of these printers...
March 14, 2018: Lab on a Chip
Ana Claudia Pompeu Raminelli, Valeria Romero, Mohammad H Semreen, Gislaine Ricci Leonardi
The clinical efficacy of the topical tretinoin is widely studied and has been well established for many therapeutic interventions, among some, photoaging, acne, and melasma. However, the side effects, mainly cutaneous irritation, erythema, xerosis and peeling, remain major obstacle to the patient compliance. Besides, the insight regarding the drug delivery profile is essential to understand the therapeutic action of the drug. Herein we highlight further advances and an update on tretinoin delivery systems such as liposomes, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, cyclodextrins, nanostructured polymers and other technological systems that reduce its side effects and improve the permeation profile to potentiate efficacy and drug safety on the skin...
March 12, 2018: Current Medicinal Chemistry
Yingying Liu, Yulong Sui, Chao Liu, Changqing Liu, Meiyan Wu, Bin Li, Youming Li
In this study, we reported a pH/near-infrared (NIR)-responsive hydrogel for on-demand drug delivery and wound healing. Cellulose nanofibrils (TOCNFs) were produced by 2, 2, 6, 6-tetramethylpiperidine-1-oxyl (TEMPO)-mediated oxidation method. Polydopamine (PDA) was introduced into TOCNFs network to fabricate a PDA/TOCNFs hydrogel through ion-crosslinking with calcium ion as a crosslinker. Then, tetracycline hydrochloride (TH) which loaded on PDA could be released from the prepared hydrogels in an on-demand fashion under NIR exposure or at lower pH conditions...
May 15, 2018: Carbohydrate Polymers
Mónika Bakonyi, Attila Gácsi, Anita Kovács, Mária-Budai Szűcs, Szilvia Berkó, Erzsébet Csányi
The application of local anesthetics, usually administered by subcutaneous injection, is common in the course of diagnostic, therapeutic, and cosmetic dermatology procedures. The effective dermal delivery of lidocaine could offer a solution to many adverse effects caused by needle insertion, such as pain, local reactions or toxicity, and additionally, it avoids the disruption of anatomical landmarks. Therefore, novel dermal formulations of local anesthetics are needed to overcome the barrier function of the skin and provide sufficient and prolonged anesthesia...
March 6, 2018: Journal of Pharmaceutical and Biomedical Analysis
Jung U Shin, Jung Dong Kim, Hong Kee Kim, Hong Kyu Kang, Chulmin Joo, Ju Hee Lee, Do Hyeon Jeong, Seungri Song, Howard Chu, Jung Soo Lee, Hemin Lee, Kwang Hoon Lee
BACKGROUND: The stratum corneum is an almost impermeable barrier. Recently, microneedles have been used to increase drug delivery passing the stratum corneum by incorporating the drug within the microneedle or by coating the surface of the microneedle with the drug. OBJECTIVE: This study was performed to investigate whether applying a biodegradable microneedle patch after topical steroid application increases penetration of the steroid in vitro, as well as treatment efficacy in patients with prurigo nodularis...
February 1, 2018: European Journal of Dermatology: EJD
Pablo Serrano-Castañeda, Jose Juan Escobar-Chavez, Isabel Marlen Rodriguez-Cruz, Luz Maria Melgoza, Jessica Martinez-Hernandez
The microneedles technology has found applications in many health-related fields. For example, their application in drugs and vaccines delivery as well, as the determination of biomarkers, has been reported. They also have a place in the dermatology and cosmetic areas such as the treatment of wounds from burns, scars, acne, depigmentation, and alopecia will be shown. Microneedles are used in therapeutic applications and are manufactured using materials such as metal (steel, titanium, nickel), polymer (oly-glycolic acid (PGA), poly-lactide-co-glycolide acid (PLGA), poly-L-lactic acid (PLA), chitosan), glass, silicon, ceramic, carbohydrates (trehalose, sucrose, mannitol)...
2018: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
Shayan Fakhraei Lahiji, Yoojung Jang, Yonghao Ma, Manita Dangol, Huisuk Yang, Mingyu Jang, Hyungil Jung
Dissolving microneedle (DMN) is referred to a microscale needle that encapsulates drug(s) within a biodegradable polymer matrix and delivers it into the skin in a minimally invasive manner. Although vast majority of studies have emphasized DMN as an efficient drug delivery system, the activity of DMN-encapsulated proteins or antigens can be significantly affected due to a series of thermal, physical and chemical stress factors during DMN fabrication process and storage period. The objective of this study is to evaluate the effects of DMN fabrication parameters including polymer type, polymer concentration, fabrication and storage temperature, and drying conditions on the activity of the encapsulated therapeutic proteins by employing lysozyme (LYS) as a model protein...
March 2, 2018: European Journal of Pharmaceutical Sciences
Vivian Saez, Ingrid D L de Souza, Cláudia Regina Elias Mansur
The antioxidative and photoprotective properties of vitamin E have caused it to be included as an active agent in various pharmaceutical and cosmetic products. However, its lipophilicity, chemical instability, and poor skin penetration have limited the effectiveness of these formulations. For that reason, many attempts to include it in different drug delivery systems have been made. In recent decades, lipid nanoparticles have received special attention due to their advantages of compatibility with the skin, ability to enhance penetration of drugs in the stratum corneum, protection of the encapsulated substance against degradation induced by the external medium, and control of drug release...
March 5, 2018: International Journal of Cosmetic Science
Irhan Ibrahim Abu Hashim, Noha Fawzy Abo El-Magd, Ahmed Ramadan El-Sheakh, Mohammed Fawzy Hamed, Abd El-Gawad Helmy Abd El-Gawad
The goal of the current study was to explore the potential benefits of Acitretin (Act) nanovesicular gel as a prospective antipsoriatic topical delivery system counteracting the drug challenges in terms of its extremely low aqueous solubility, instability, skin irritation, and serious systemic adverse effects. Act-loaded niosomes were successfully developed, entirely characterized, and optimized. Further evaluation of the optimized formula was conducted regarding its stability and ex vivo cytotoxicity on different cell lines...
2018: International Journal of Nanomedicine
Muhammad Rouf Akram, Mahmood Ahmad, Asad Abrar, Rai Muhammad Sarfraz, Asif Mahmood
Background: The present work was conducted to prepare and evaluate transdermal patches with optimization of suitable polymeric blend of poly(meth) acrylates (Eudragit® ) (Ammonio Methacrylate Copolymer Ph Eur) for sustained transdermal delivery of glimepiride. Method: Polymeric matrix transdermal films were prepared by using Ammonio Methacrylate Copolymer Ph Eur RL 100 and Ammonio Methacrylate Copolymer Ph Eur RS 100 as the film former, and dibutyl phthalate (30% w/w) as the plasticizer...
2018: Drug Design, Development and Therapy
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
Konstantina Karamanou, Gwenn Perrot, Francois-Xavier Maquart, Stéphane Brézillon
Wound healing, a complex physiological process, is responsible for tissue repair after exposure to destructive stimuli, without resulting in complete functional regeneration. Injuries can be stromal or epithelial, and most cases of wound repair have been studied in the skin and cornea. Lumican, a small leucine-rich proteoglycan, is expressed in the extracellular matrices of several tissues, such as the cornea, cartilage, and skin. This molecule has been shown to regulate collagen fibrillogenesis, keratinocyte phenotypes, and corneal transparency modulation...
March 1, 2018: Advanced Drug Delivery Reviews
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
Rakesh Gupta, Beena Rai
Nanoparticles are used in the medical field for various applications like cell imaging, drug delivery, gene and si-RNA delivery, to name a few. Designing nanoparticles for a given application, purely based on the trial and error experimentation, requires a lot of time and effort. In this study we show that computer simulations could help in designing nanoparticles for drug delivery thus reducing the time and cost associated with their design, development and deployment. The permeation of nanoparticles, having various surface chemistries and patterns, through the skin lipid bilayer was studied using constrained and unconstrained molecular dynamics simulations...
February 27, 2018: Nanoscale
Thaiene Avila Reis, Ana Elise Jaculi, Rubens da Costa Alves, Tais Gratieri, Ricardo Bentes Azevedo, Graziella Anselmo Joanitti, Guilherme Martins Gelfuso, Marcilio Cunha-Filho
Considering the feasibility of the aluminum phthalocyanine chloride (AlPcCl) application in the topical photodynamic therapy of cutaneous tumors and the lack of HPLC methods capable of supporting skin permeation experiments using this compound, the aim of this study was to obtain a simple and selective chromatographic method for AlPcCl determination in skin matrices. A HPLC-UV/Vis method was developed using a normal-phase column operating at 30°C, an isocratic mobile phase of methanol : phosphoric acid (0...
2018: Journal of Analytical Methods in Chemistry
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
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