Abstract:
:Introduction: Making selective inhibitors of novel Gram-negative targets is not a substantial challenge - getting them into Gram-negative bacteria to reach their lethal target is the bottleneck. Poor permeability of the antibiotic requires high concentration causing off target activity. The lack of simple experimental techniques to measure antibiotic uptake as well as the local concentration at the target site creates a particular bottleneck in understanding and in improving the antibiotic activity. Areas covered: Here we recall current approaches to quantify the uptake. For a few antibiotics with known evidence for channel-limited permeation, the flux across a single OmpF or OmpC channel has been measured. For a typical concentration gradient of 1 µM of antibiotics the uptake varies between one up to few hundred molecules per second and per channel. Expert opinion: The current research effort is on quantifying the flux for a larger list of compounds on a cellular (mass spectra, fluorescence) or at single channel level (electrophysiology). A larger dataset of single channel permeabilities under various condition will be a powerful tool for understanding and improving the activity of antibiotics.
journal_name
Expert Opin Drug Delivjournal_title
Expert opinion on drug deliveryauthors
Winterhalter Mdoi
10.1080/17425247.2021.1847080subject
Has Abstractpub_date
2020-11-13 00:00:00pages
1-9eissn
1742-5247issn
1744-7593pub_type
杂志文章abstract:INTRODUCTION:Gemcitabine, an anticancer drug, is a nucleoside analog deoxycytidine antimetabolite, which acts against a wide range of solid tumors. The limitation of gemcitabine is its rapid inactivation by the deoxycytidine deaminase enzyme following its in vivo administration. AREAS COVERED:One of the most promising...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2011.632630
更新日期:2011-12-01 00:00:00
abstract:INTRODUCTION:With the incorporation of edge activators into the lipid bilayer structure, elasticity properties are given to liposomes. Regardless of the debate over the precise permeation mechanism of elastic liposomes, these vesicles have been proven to enhance drug permeation into or through skin in most cases. AREA...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2013.779252
更新日期:2013-06-01 00:00:00
abstract::Introduction: Sativex® spray is clinically utilized to deliver delta9-tetrahydrocannabinol and cannabidiol to oral mucosa for systemic absorption. We challenge the consensus that the mechanism of absorption following the oro-mucosal application occurs via the buccal tissue. Areas covered: Correctness of the consensus ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2019.1653852
更新日期:2019-10-01 00:00:00
abstract:INTRODUCTION:Inflammatory bowel disease (IBD) is an exceptional scenario with regard to drug targeting, as oral administration has the potential to deliver the drug directly to the site(s) of action. Consequently, retention of the drug within the intestinal lumen and tissue, rather than systemic absorption, is frequent...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2013.800480
更新日期:2013-09-01 00:00:00
abstract:OBJECTIVES:Thermosensitive chitosan/glycerophosphate (C/GP) solutions exhibiting sol-gel transition around body temperature were prepared to develop a class of injectable hydrogel platforms for the imaging and loco-regional treatment of hepatocellular carcinoma (HCC). Indocyanine green (ICG) was loaded in the thermosen...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1517/17425247.2015.1042452
更新日期:2015-01-01 00:00:00
abstract::Introduction: Systemically administered non-viral gene delivery systems face multiple biological barriers that decrease their efficiency. These systems are rapidly cleared from the circulation and sufficient concentrations do not accumulate in diseased tissues. A number of targeting strategies can be used to provide f...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2019.1656196
更新日期:2019-10-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Drug combinations have been the standard of care in the treatment of cancer for > 50 years. Typically, combination chemotherapy uses agents with non-overlapping toxicities which are escalated to their maximum tolerated dose. However, emerging evidence indicates that this approach may not be prov...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2010.538678
更新日期:2010-12-01 00:00:00
abstract::In the last decade, interest in physical organogels has grown rapidly with the discovery and synthesis of a very large number of diverse molecules, which can gel organic solvents at low concentrations. The gelator molecules immobilise large volumes of liquid following their self-assembly into a variety of aggregates s...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2.3.489
更新日期:2005-05-01 00:00:00
abstract::Functionalised carbon nanotubes (f-CNTs) are emerging as new tools in the field of nanobiotechnology and nanomedicine. This is because they can be easily manipulated and modified by encapsulation with biopolymers or by covalent linking of solubilising groups to the external walls and tips. The possibility of incorpora...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.1.1.57
更新日期:2004-11-01 00:00:00
abstract:INTRODUCTION:Apart from statins, anti-platelet agents and invasive procedures, the anti-atherosclerotic medical weaponry for coronary heart disease (CHD) is scarce and only partially protects CHD patients from major adverse cardiac events. AREAS COVERED:Several novel non-invasive strategies are being developed to wide...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2015.999663
更新日期:2015-07-01 00:00:00
abstract::Introduction: Poloxamer based in situ gelling systems offer numerous advantages in drug delivery; however, their application as prolonged-release delivery platforms is limited mainly due to their weak mechanical properties and the interconnected aqueous network causing fast gel erosion and drug diffusion.Area covered:...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2020.1731469
更新日期:2020-04-01 00:00:00
abstract:INTRODUCTION:Calcium channel blockers are a very important class of antihypertensive drugs. Most calcium channel blockers (CCBs) exhibiting low oral bioavailability are required to be taken more than once a day due to their short half-lives which result in poor patient compliance. There is an ineluctable requirement fo...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2013.783562
更新日期:2013-08-01 00:00:00
abstract::FlexTouch® (FT) is a new prefilled insulin pen with the unique characteristic of no extendable push button at any dose setting and consequently a low activation force. Its technical features along with health care professionals' and patients' preferences in comparison to other traditionally used devices for insulin de...
journal_title:Expert opinion on drug delivery
pub_type: 社论
doi:10.1517/17425247.2014.894505
更新日期:2014-05-01 00:00:00
abstract::Devices for the aqueous delivery of intranasal corticosteroids to patients with allergic rhinitis have been available since 1984, so there is a need for new devices to be developed to provide ease of use, efficacy and safety. A novel drug delivery system has been developed for fluticasone furoate (FF; GlaxoSmithKline)...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.4.6.689
更新日期:2007-11-01 00:00:00
abstract:BACKGROUND:The advent of therapeutic proteins highlights the need for delivery systems that protect and extend the duration of its action. Ranibizumab-VEGF is one such drug used for treating wet AMD. This paper describes a facile method to sustain bioactive ranibizumab release from PLGA-based particles. METHODS:Two em...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2018.1538209
更新日期:2018-12-01 00:00:00
abstract::Background: Anti-tumor necrosis factor (anti-TNF) adherence is suboptimal. ava®, a reusable electromechanical self-injection device (e-Device) developed for certolizumab pegol (CZP) administration, aims to overcome some barriers to increase adherence. This study evaluates patient experience of the e-Device and its tra...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2020.1736552
更新日期:2020-05-01 00:00:00
abstract:INTRODUCTION:In the therapy of clinical diseases such as cancer, it is important to deliver drugs directly to tumor sites in order to maximize local drug concentration and reduce side effects. This objective may be realized by using 'smart' nanoparticles (NPs) as drug delivery systems, because they enable dramatic conf...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2015.1071352
更新日期:2015-01-01 00:00:00
abstract:INTRODUCTION:Topically applied small interfering RNA (siRNA) can be an effective treatment for skin disorders. Using noninvasive strategies can be a safe and effective siRNA-permeation-enhancement approach for facilitating skin delivery. It has been demonstrated that noninvasive approaches for enhancing siRNA transport...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2016.1121988
更新日期:2016-01-01 00:00:00
abstract::Cationic lipid/DNA complexes (lipoplexes) represent an attractive alternative to viral vectors for cell transfection in vitro and in vivo but still suffer from relatively low efficiency. Comprehension of the interactions between vectors and DNA as well as cellular pathways and mechanisms in DNA entry into cells and ul...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425240903287153
更新日期:2009-12-01 00:00:00
abstract:INTRODUCTION:In situ gel systems refer to a class of novel delivery vehicles, composed of natural, semisynthetic or synthetic polymers, which present the unique property of sol-gel conversion on receipt of biological stimulus. AREAS COVERED:The present review summarizes the latest developments in in situ gel technolog...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2012.665367
更新日期:2012-04-01 00:00:00
abstract:BACKGROUND:The lung comprises an interesting route of administration not only for topical drugs but also for systemically acting drugs. Over the last years, several models have been developed in order to study the efficacy and safety of pulmonary drug delivery. OBJECTIVE:This review describes relevant drug delivery mo...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425240903241788
更新日期:2009-11-01 00:00:00
abstract:INTRODUCTION:Most pathogens colonize and invade the host at mucosal surfaces, such as the lung and the intestine. To combat intestinal pathogens the induction of local adaptive immune responses is required, which is mainly achieved through oral vaccination. However, most vaccines are ineffective when given orally owing...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2011.561312
更新日期:2011-04-01 00:00:00
abstract:BACKGROUND:Although various injected peptide and protein therapeutics have been developed successfully over the past 25 years, several pharmacokinetic and immunological challenges are still encountered that can limit the efficacy of both novel and established biotech molecules. OBJECTIVE AND METHOD:PEGylation is a pop...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.5.4.371
更新日期:2008-04-01 00:00:00
abstract:BACKGROUND:Efficient and minimally invasive vector systems appear to be the most appropriate for both gene therapy and drug delivery. Numerous viral and non-viral vectors have been developed. Each vector has its own advantages and limitations. OBJECTIVE:New vectors have been required for overcoming the limitations of ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.5.2.221
更新日期:2008-02-01 00:00:00
abstract:INTRODUCTION:Radioimmunotherapy (RIT) with monoclonal antibodies and their fragments labelled with radionuclides emitting α -particles, β-particles or Auger electrons have been used for many years in the development of anticancer strategies. While RIT has resulted in approved radiopharmaceuticals for the treatment of h...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2018.1378180
更新日期:2018-02-01 00:00:00
abstract:INTRODUCTION:The work presents the development of acellular scaffolds extemporaneously embedded with platelet lysate (PL), as an innovative approach in the field of tissue regeneration/reparation. PL embedded scaffolds should have a tridimensional architecture to support cell migration and growth, in order to restore s...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1517/17425247.2015.961421
更新日期:2015-04-01 00:00:00
abstract:INTRODUCTION:The emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) is a major health issue and continues to be a global health concern. Despite significant advancements in treatment modalities, ~1.6 million deaths worldwide occur due to TB infection. This is bec...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2019.1609937
更新日期:2019-05-01 00:00:00
abstract:INTRODUCTION:Over the past several decades, liposomes have been used in a variety of applications, from delivery vehicles to cell membrane models. In terms of pharmaceutical use, they can offer control over the release of active agents encapsulated into their lipid bilayer or aqueous core, while providing protection fr...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2012.647908
更新日期:2012-02-01 00:00:00
abstract:INTRODUCTION:A major problem in ocular therapeutics with classical formulations is the maintenance of an effective drug concentration at the site of action for a long period of time. Enhancement of ocular bioavailability with increased dose penetration and longer retention time at desired sites can be achieved by recen...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2012.681775
更新日期:2012-06-01 00:00:00
abstract::Oral colon-targeted drug delivery systems have gained enormous attention among researchers in the last two decades. The significance of this site-specific drug delivery system can be measured by its usefulness for delivering a variety of therapeutic agents, both for the treatment of local diseases or for systemic ther...
journal_title:Expert opinion on drug delivery
pub_type: 社论
doi:10.1517/17425247.2011.597739
更新日期:2011-10-01 00:00:00