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https://www.readbyqxmd.com/read/28088574/time-dependence-of-the-enhancement-effect-of-chemical-enhancers-molecular-mechanisms-of-enhancing-kinetics
#1
Xiaochang Liu, Peng Quan, Shanshan Li, Chao Liu, Yuan Zhao, Yongshan Zhao, Liang Fang
Chemical enhancers are widely used for facilitating drug penetration in transdermal drug delivery system (TDDS). However, there is a lack of knowledge about how the enhancement effect changes over time. In this study, on the basis of kinetic parameters of enhancement effect, molecular details of the dynamic enhancement process was described and a new hypothesis of the recovery mechanism of the skin barrier function was proposed. Using pretreated skin and flurbiprofen patch, the effects of Azone (AZ) and menthol decanoate (MT-10) were evaluated with in vitro permeation experiment and further confirmed by confocal laser scanning microscopy (CLSM) and TEWL...
January 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28077264/self-assembly-of-green-tea-catechin-derivatives-in-nanoparticles-for-oral-lycopene-delivery
#2
Weikun Li, Murat Yalcin, Qishan Lin, Mohammed-Salleh M Ardawi, Shaker A Mousa
Lycopene is a natural anti-oxidant that has attracted much attention due to its varied applications such as protection against loss of bone mass, chronic diseases, skin cancer, prostate cancer, and cardiovascular disease. However, high instability and extremely low oral bioavailability limits its further clinical development. We selected a green tea catechin derivative, oligomerized (-)-epigallocatechin-3-O-gallate (OEGCG) as a carrier for oral lycopene delivery. Lycopene-loaded OEGCG nanoparticles (NPs) were prepared by a nano-precipitation method, followed by coating with chitosan to form a shell...
January 7, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28071597/three-dimensional-printing-of-a-microneedle-array-on-personalized-curved-surfaces-for-dual-pronged-treatment-of-trigger-finger
#3
Seng Han Lim, Jian Yao Ng, Lifeng Kang
The hand function of patients who suffer from trigger finger can be impaired by the use of traditional splints. There is also a risk of systemic side effects with oral non-steroidal anti-inflammatory drugs (NSAIDs) used for pain relief. Microneedle-assisted transdermal drug delivery offers an attractive alternative for local delivery of NSAIDs. However, traditional microneedle arrays fabricated on flat surfaces are unable to deliver drugs effectively across the undulating skin surface of affected finger(s)...
January 10, 2017: Biofabrication
https://www.readbyqxmd.com/read/28071592/development-and-evaluation-of-zinc-phthalocyanine-nanoemulsions-for-use-in-photodynamic-therapy-for-leishmania-spp
#4
Luciana Betzler de Oliveira de Siqueira, Verônica da Silva Cardoso, Igor Almeida Rodrigues, Ana Lúcia Vazquez-Villa, Elisabete Pereira Dos Santos, Bruno da Costa Leal Ribeiro Guimarães, Cristal Dos Santos Cerqueira Coutinho, Alane Beatriz Vermelho, Eduardo Ricci Junior
Photodynamic therapy (PDT) combines light with photosensitizers (PS) for production of reactive oxygen species (ROS) that can kill infectious microorganisms such as bacteria, fungi and protozoa. The application of nanotechnology has enabled the advancement of PDT because many PS are insoluble in water, necessitating a nanocarrier as a physiologically acceptable carrier. Nanoemulsions are efficient nanocarriers for solubilizing liposoluble drugs, like the PS, in water. Cutaneous (CL) and mucocutaneous leishmaniasis (ML) are caused by different species of the genus Leishmania, transmitted to humans by sandfly bites...
February 10, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28070753/dodecyl-amino-glucoside-enhances-transdermal-and-topical-drug-delivery-via-reversible-interaction-with-skin-barrier-lipids
#5
Monika Kopečná, Miloslav Macháček, Eva Prchalová, Petr Štěpánek, Pavel Drašar, Martin Kotora, Kateřina Vávrová
PURPOSE: Skin permeation/penetration enhancers are substances that enable drug delivery through or into the skin. METHODS: To search for new enhancers with high but reversible activity and acceptable toxicity, we synthesized a series of D-glucose derivatives, both hydrophilic and amphiphilic. RESULTS: Initial evaluation of the ability of these sugar derivatives to increase permeation and penetration of theophylline through/into human skin compared with a control (no enhancer) or sorbitan monolaurate (Span 20; positive control) revealed dodecyl 6-amino-6-deoxy-α-D-glucopyranoside 5 as a promising enhancer...
January 9, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28070698/drug-coated-microneedles-for-rapid-and-painless-local-anesthesia
#6
Sung-Hyun Baek, Ju-Hyung Shin, Yeu-Chun Kim
This study showed that drug-coated PLLA (Poly (L-lactide)) microneedle arrays can induce rapid and painless local anesthesia. Microneedle arrays were fabricated using a micro-molding technique, and the needle tips were coated with 290.6 ± 45.9 μg of lidocaine, the most widely used local anesthetic worldwide. A dip-coating device was newly designed for the coating step using an optimized coating formulation. Lidocaine coated on the arrays was released rapidly into PBS within 2 min, and its stability in storage lasted 3 weeks at 4, 25, and 37°C...
March 2017: Biomedical Microdevices
https://www.readbyqxmd.com/read/28069552/longitudinal-monitoring-of-skin-accumulation-of-nanocarriers-and-biologicals-with-fiber-optic-near-infrared-fluorescence-spectroscopy-fonirs
#7
James I Griffin, Michael J Benchimol, Dmitri Simberg
Systemically injected drug delivery systems distribute into various organs and tissues, including liver, spleen and kidneys. Recent reports pointed out a significant accumulation of systemically injected nanoparticles in the skin. Skin constitutes the largest organ in the body with important immune functions, and accumulation of drug delivery systems could have significant implications for skin toxicity in living subjects. Fiber optic-based near-infrared spectroscopy (FONIRS) setup was developed and tested for measuring of NIR (760nm excitation) emission spectra in the skin...
January 6, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28069427/fabrication-of-topical-metered-dose-film-forming-sprays-for-pain-management
#8
Sneha Ranade, Amrita Bajaj, Vaishali Londhe, Najib Babul, Danny Kao
Topical film-forming metered dose spray formulations were designed for management of pain. Ropivacaine, a local anesthetic is explored for its topical efficacy in alleviating pain. Metered dose spray containers, organic solvents, film forming polymers and permeation enhancers were utilized to fabricate the Metered Dose topical spray. Factors like viscosity, spray pattern, spray angle, volume of actuation, droplet size distribution of the metered dose spray formulation and drying time, flexibility and wash-ability of the film formed after spraying were assessed...
January 6, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28068767/microneedle-assisted-skin-permeation-by-non-toxic-bioengineerable-gas-vesicle-nanoparticles
#9
Abhay U Andar, Ram Karan, Wolf T Pecher, Priya DasSarma, William D Hedrich, Audra L Stinchcomb, Shiladitya DasSarma
Gas vesicle nanoparticles (GVNPs) are hollow, buoyant protein organelles produced by the extremophilic microbe Halobacterium sp. NRC-1 and are being developed as bioengineerable and biocompatible antigen and drug-delivery systems (DDS). Dynamic light scattering measurements of purified GVNP suspensions showed a mean diameter of 245 nm. In vitro diffusion studies using Yucatan miniature pig skin showed GVNP permeation to be enhanced after MN-treatment compared to untreated skin. GVNPs were found to be non-toxic to mammalian cells (human kidney and rat mycocardial myoblasts)...
January 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28063969/hii-mesophase-as-a-drug-delivery-system-for-topical-application-of-methyl-salicylate
#10
Xin Liang, Yu-Lin Chen, Xiao-Jing Jiang, Sheng-Mei Wang, Ji-Wen Zhang, Shuang-Ying Gui
The main objective of this study was to develop reversed hexagonal (HII) mesophase for transdermal delivery of methyl salicylate. The formulation was prepared, characterized and evaluated for its skin penetration in vitro and skin retention in vivo. Preliminary pharmacodynamics and skin irritation were also investigated. The formulation was identified as hexagonal structure. In vitro study exhibited that HII mesophase enhanced the skin permeation by delivering 2.61 times more methyl salicylate than the commercially available cream...
January 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28056749/development-and-evaluation-of-naproxen-sodium-gel-using-piper-cubeba-for-enhanced-transdermal-drug-delivery-and-therapeutic-facilitation
#11
Sunetra Kaustubh Patwardhan, Manohar J Patil, Anbazhagan Sockalingam
BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients...
January 5, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28052582/magnetically-driven-nanoparticles-18-fdg-radiolabelling-and-positron-emission-tomography-biodistribution-study
#12
Mariarosaria De Simone, Daniele Panetta, Emilia Bramanti, Cristiana Giordano, Maria C Salvatici, Lisa Gherardini, Arianna Menciassi, Silvia Burchielli, Caterina Cinti, Piero A Salvadori
Superparamagnetic iron oxide nanoparticles (SPIONs) have received increasing interest as contrast media in biomedical imaging and innovative therapeutic tools, in particular for loco-regional ablative treatments and drug delivery. The future of therapeutic applications would strongly benefit from improving the capability of the nanostructured constructs to reach the selected target, in particular beyond the intravascular space. Besides the decoration of SPIONs surface with ad hoc bioactive molecules, external magnetic fields are in principle able to remotely influence SPIONs' physiological biodistribution and concentrate them to a specific anatomical region or portion of a tissue...
January 4, 2017: Contrast Media & Molecular Imaging
https://www.readbyqxmd.com/read/28050929/development-and-optimization-of-apigenin-loaded-transfersomal-system-for-skin-cancer-delivery-in-vitro-evaluation
#13
Manmohan Singh Jangdey, Anshita Gupta, Shailendra Saraf, Swarnlata Saraf
The aim of this work is to apply Box-Behnken design to optimize the transfersomes were formulated by modified rotary evaporation sonication technique using surfactant Tween 80. The response surface methodology was used having three-factored with three levels. The prepared formulations were characterized for vesicle shape, size, entrapment efficiency (%), stability, and in vitro permeation. The result showed that drug entrapment of 84.24% with average vesicle size of 35.41 nm and drug loading of 8.042%. Thus, optimized formulation was found good stability and is a promising approach to improve the permeability of apigenin in sustained release for prolonged period of time...
January 4, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28040601/a-novel-elastic-liposome-for-skin-delivery-of-papain-and-its-application-on-hypertrophic-scar
#14
Yan-Yan Chen, Ye-Hui Lu, Chun-Hua Ma, Wei-Wei Tao, Jing-Juan Zhu, Xu Zhang
This study aims to investigate the therapeutic effects of papain elastic liposomes (PEL) on hypertrophic scar through topical application. PEL were prepared using the reverse-phase evaporation method and optimized by response surface methodology. The transdermal absorption of optimized PEL was tested by vertical Franz diffusion cells in vitro. The effects of PEL were investigated in rabbit model of hypertrophic scar in vivo, histological analysis and scar-related proteins were detected to reveal potential scar repair mechanism...
December 29, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28040458/a-novel-approach-for-the-development-of-a-nanostructured-lipid-carrier-formulation-by-hot-melt-extrusion-technology
#15
Ajinkya M Bhagurkar, Michael A Repka, S Narasimha Murthy
The main aim of this study was to investigate the feasibility of preparing nanostructured lipid carrier (NLC) utilizing hot-melt extrusion (HME) coupled with probe sonication. The process parameters for HME and sonication were optimized and a modified screw configuration was used for extrusion. Lidocaine loaded NLCs were successfully prepared by the proposed method with particle size lower than 50 nm and PDI less than 0.3. Transmission electron microscopy revealed the spherical nature of the particles. The second objective was to develop NLCs for topical controlled delivery of drug for pain management in cutaneous wounds...
December 28, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28039091/evaluation-of-paeonol-loaded-transethosomes-as-transdermal-delivery-carriers
#16
Z X Chen, B Li, T Liu, X Wang, Y Zhu, L Wang, X H Wang, X Niu, Y Xiao, Q Sun
Paeonol shows effective anti-allergic, anti-inflammatory and analgesic activities. However, because of its poor solubility in water and high volatility at room temperature, the application of this drug is restricted in the clinic. The objective of this research was to develop a biocompatible paeonol formulation with improved stability, skin delivery and pharmacokinetic efficiency. In this paper, paeonol-loaded vesicles were prepared using an ethanol injection method. Nano-vesicles were characterized for their physical properties and encapsulation efficiency (EE)...
December 28, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28035957/in-vivo-assessment-of-clobetasol-propionate-loaded-lecithin-chitosan-nanoparticles-for-skin-delivery
#17
Taner Şenyiğit, Fabio Sonvico, Alessandra Rossi, Işıl Tekmen, Patrizia Santi, Paolo Colombo, Sara Nicoli, Özgen Özer
The aim of this work was to assess in vivo the anti-inflammatory efficacy and tolerability of clobetasol propionate (CP) loaded lecithin/chitosan nanoparticles incorporated into chitosan gel for topical application (CP 0.005%). As a comparison, a commercial cream (CP 0.05% w/w), and a sodium deoxycholate gel (CP 0.05% w/w) were also evaluated. Lecithin/chitosan nanoparticles were prepared by self-assembling of the components obtained by direct injection of soybean lecithin alcoholic solution containing CP into chitosan aqueous solution...
December 26, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28035612/transdermal-adhesive-patches-loaded-with-ketoprofen-evaluated-by-dynamic-detection-of-percutaneous-absorption
#18
Menglin Wang, Longwei Li, Junxia Xie, Yinghua Sun, Guixia Ling, Zhonggui He
Topical delivery has many benefits toward NSAIDs administration, and the best-selling transdermal preparation in 2015 was the NSAID patch MOHRUS®. Herein, we report a ketoprofen adhesive patch (KAP) and evaluate the penetration and absorption compared to MOHRUS®. Microdialysis sampling technique was applied to determine drug penetration in the dermis and subcutaneous tissue. Simultaneously, blood samples were withdrawn over time to obtain the drug absorption in plasma. The ketoprofen concentrations in the dermis, subcutaneous tissue, and plasma were compared with the commercially available patch (MOHRUS®)...
December 29, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028794/effect-of-liquid-crystalline-systems-containing-antimicrobial-compounds-on-infectious-skin-bacteria
#19
Carla Souza, Evandro Watanabe, Carolina Patrícia Aires, Marilisa Guimarães Lara
This study aimed (i) to prepare liquid crystalline systems (LCS) of glyceryl monooleate (GMO) and water containing antibacterial compounds and (ii) to evaluate their potential as drug delivery systems for topical treatment of bacterial infections. Therefore, LCS containing CPC (cetylpyridinium chloride) (LCS/CPC) and PHMB (poly(hexamethylene biguanide) hydrochloride) (LCS/PHMB) were prepared and the liquid crystalline phases were identified by polarizing light microscopy 24 h and 7 days after preparation...
December 27, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28028793/in-vitro-drug-transfer-due-to-drug-retention-in-human-epidermis-pretreated-with-application-of-marketed-estradiol-transdermal-systems
#20
Yellela S R Krishnaiah, Naresh Pavurala, Yang Yang, Prashanth Manda, Usha Katragadda, Yongsheng Yang, Rakhi Shah, Guodong Fang, Mansoor A Khan
Study objective was to assess skin-to-skin drug transfer potential that may occur due to drug retention in human epidermis (DRE) pretreated with application of estradiol transdermal drug delivery systems (TDDS) and other estradiol transdermal dosage forms (gels and sprays). TDDS (products-A, B, and C) with varying formulation design and composition, and other estradiol transdermal products (gel and spray) were applied to heat separated human epidermis (HSE) and subjected to in vitro drug permeation study. Amounts of DRE were quantified after 24 h...
December 27, 2016: AAPS PharmSciTech
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