Abstract:
INTRODUCTION:The use of hydrophilic polymers as a substitute for the Fc-domain in immuno- or non-immuno-based binding proteins is accelerating. Chemical PEGylation has led the way and is still the most advanced and clinically-approved approach. Hydrophilic polymers act by maintaining a flexible conformation and hydrogen bonding to a network of water molecules to acquire a larger hydrodynamic volume and apparent mass than their actual molecular mass suggest. The benefits are increased blood half-life and bioavailability, stability and reduced immunogenicity. In the case of PEG, there is also evidence of enhanced targeting and reduced side effects, but drawbacks include the fact that PEG is non-biodegradable. AREAS COVERED:This report reviews the state of the art for antibody PEGylation in terms of approaches and effects. Additionally, non-biological (such as N-(2-hydroxypropyl)methacrylamide) and potentially superior biological alternatives (such as polysialylation) are described, ending with recombinant approaches (such as hydrophilic peptides and glyco-engineering), which promise to circumvent the need for chemical modification altogether. EXPERT OPINION:The emergence of many small, antibody fragment-like mimics will drive the need for such technologies, and PEGylation is still the choice polymer due to its established use and track record. However, there will be a place for many alternative technologies if they can match the pharmacokinetics of PEG-conjugates and bring addition beneficial features such as easier production.
journal_name
Expert Opin Drug Delivjournal_title
Expert opinion on drug deliveryauthors
Chen C,Constantinou A,Deonarain Mdoi
10.1517/17425247.2011.602399subject
Has Abstractpub_date
2011-09-01 00:00:00pages
1221-36issue
9eissn
1742-5247issn
1744-7593journal_volume
8pub_type
杂志文章,评审abstract::The field of infectious diseases is in crisis and there is a need for strategies that can facilitate the rapid development of new antimicrobial agents. Radioimmunotherapy (RIT), a therapeutic modality originally developed for cancer treatment, has recently been suggested as a novel therapy for the treatment of a varie...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2.6.1075
更新日期:2005-11-01 00:00:00
abstract::Objective: Conventional chloramphenicol (CHL) eye drops are widely used anti-infection formulations for acute bacterial conjunctivitis. However, the therapeutic effects are limited by insufficient concentration in the conjunctival sac. Hence, the objective of this study is to formulate and develop novel CHL eye drops ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2019.1609447
更新日期:2019-06-01 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
abstract:INTRODUCTION:Many drug candidates with high therapeutic efficacy have low water solubility, which limits the administration and transport across physiological barriers, for example, the tumor tissue barrier. Therefore, strategies are needed to permeabilize the physiological barriers safely so that hydrophobic drugs may...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2015.1021681
更新日期:2015-01-01 00:00:00
abstract::The treatment of genetic diseases using therapeutic gene transfer is considered to be a significant development. This development has brought with it certain limitations, and the process of overcoming these barriers has seen a drastic change in gene delivery. Many metal ions such as Mg2+, Mn2+, Ba2+ and, most importan...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1517/17425247.3.2.235
更新日期:2006-03-01 00:00:00
abstract:INTRODUCTION:The renaissance in drug delivery research during the past decade led to several new approaches toward vaccine development. Transdermal immunization (TI) is a promising modality with both practical and immunological merits. Compared with conventional routes of administration, this needle-free delivery appro...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2013.746660
更新日期:2013-02-01 00:00:00
abstract:BACKGROUND:The present work aims to formulate nanostructured lipid carriers (NLCs) exhibiting high skin deposition and high inherent antioxidant potential to repurpose the use of melatonin hormone and some antioxidant oils in the treatment of androgenic alopecia (AGA). RESEARCH DESIGN AND METHODS:NLCs were characteriz...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2018.1517740
更新日期:2018-10-01 00:00:00
abstract::Nitric oxide (NO), the 1992 'Molecule of the Year', is the focus of immense medical and scientific exploration. Interest in NO has grown exponentially since the initial and relatively recent discovery that NO is the long sought after endothelial relaxing factor. There is intense research that is continuing to expose t...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425240903196743
更新日期:2009-10-01 00:00:00
abstract:INTRODUCTION:Utilizing the prodrug approach as a method to overcome various pharmaceutical and pharmacokinetic barriers to drug delivery is significantly accelerating and achieving successes. In contrast to the older traditional prodrugs which suffer from decreased bioavailability and a high profile of side effects, du...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2016.1142527
更新日期:2016-01-01 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: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:INTRODUCTION:Harnessing RNA interference as a therapeutic approach has the potential to significantly expand the druggable target space, offering new hope for treatment of diseases that cannot be addressed with existing classes of drugs. A number of siRNA therapeutics have already progressed into preclinical and clinic...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2012.642363
更新日期:2012-02-01 00:00:00
abstract:INTRODUCTION:Topical drug delivery is a challenging area with many advantages such as avoidance of first passage effect, stabilization of blood concentrations and attainment of local therapeutic effect with fewer side effects. Despite all these advantages, topical drug delivery remains limited to few molecules, since s...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2016.1182489
更新日期:2016-08-01 00:00:00
abstract:INTRODUCTION:Current treatment of malignant tumors relies predominantly on chemotherapy delivering a single antineoplastic drug or a combination of two or more drugs intravenously. Problems with such treatments can include the killing of healthy cells, adverse side effects and chemoresistance. As cancer basically resul...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1517/17425247.2011.554817
更新日期:2011-03-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Recently, there has been substantial progress in the development of integrin targeted pharmaceuticals and drug delivery systems. Integrin is an important member in the cell adhesion molecule family, which is involved in regulation of complex biological conditions, from keeping normal physiologic...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425240903468696
更新日期:2010-02-01 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::Skin diseases are prevalent and can significantly affect quality of life. Empirical mathematical models retrospectively analyse data to predict skin permeation from the physico-chemical properties of drugs. Quantitative structure permeability relationships are discussed, along with alternatives to linear modelling. Me...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425240902865561
更新日期:2009-04-01 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:Liposomes, phospholipids, nanosized bubbles with a bilayered membrane structure, have drawn a lot of interest as pharmaceutical carriers for drugs and genes. In particular, liposomes are widely used for drug delivery into tumors. OBJECTIVE:In many cases, to enhance the efficacy of the liposomal drugs, drug-...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.5.9.1003
更新日期:2008-09-01 00:00:00
abstract:BACKGROUND:Pressurized metered-dose inhalers (pMDIs) include hydrofluoroalkane (HFA) propellant to generate a drug aerosol upon actuation and drugs can be formulated as solution or suspension. Suspended particles can cream or sediment depending on density differences between drug and propellant and shaking the pMDI is ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2020.1767066
更新日期:2020-07-01 00:00:00
abstract:INTRODUCTION:For poorly soluble compounds, a good bioavailability is typically needed to assess the therapeutic index and the suitability of the compound for technical development. In industry, the selection of the delivery technology is not only driven by technical targets, but also by constraints, such as production ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2011.614228
更新日期:2011-11-01 00:00:00
abstract:INTRODUCTION:Use of pre-filled syringes as both a packaging and delivery system for pharmaceutical drug products is accelerating. Pre-filled syringes must meet the quality and suitability for use requirements for both systems, including compatibility with the drug product. Relevant incompatibilities between pre-filled ...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2014.928281
更新日期:2014-10-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Vascular delivery of several classes of therapeutic agents may benefit from carriage by red blood cells (RBC), for example, drugs that require delivery into phagocytic cells and those that must act within the vascular lumen. The fact that several protocols of infusion of RBC-encapsulated drugs a...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425241003610633
更新日期:2010-04-01 00:00:00
abstract:INTRODUCTION:In any manufacturing process, the success of producing an end product with the desired properties and yield depends on a range of factors that include the equipment, process and formulation variables. It is the interest of manufacturers and researchers to understand each manufacturing process better and as...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2014.915805
更新日期:2014-07-01 00:00:00
abstract:INTRODUCTION:Biopolymers have been used extensively in the pharmaceutical field. Pectin, a biopolymer, has several unique properties that enable it to be used as an excipient or carrier for oral drug delivery systems. Accordingly, several investigators have identified the benefits of pectin-based delivery systems for o...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2011.584867
更新日期:2011-08-01 00:00:00
abstract:INTRODUCTION:Macrophages are involved in the normal defense of the body; however, the varying phenotypes of macrophages and imbalance in their ratio lead to the impairment of immune response initiating the production of inflammation. As the role of macrophages in immunological disorders and their surface receptors modu...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2020.1783237
更新日期:2020-09-01 00:00:00
abstract:INTRODUCTION:A major problem with conventional antitumor therapeutics is nonselective delivery of cytotoxic drugs to normal vital organs and tissues but little delivery to tumor tissues. AREAS COVERED:Here, the authors describe the tumor selective delivery of antitumor drugs by taking advantage of nano-sized drugs and...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.2014.955011
更新日期:2015-01-01 00:00:00
abstract:INTRODUCTION:Research into oral delivery of biologics has a long and rich history but has not produced technologies used in the clinic. The area has evolved in terms of strategies to promote oral biologics delivery from early chemical absorption enhancers to nanomedicine to devices. Continued activity in this area is j...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1080/17425247.2018.1504017
更新日期:2018-08-01 00:00:00
abstract:BACKGROUND:The delivery of drugs through the buccal mucosa has received a great deal of attention over the last two decades, and yet there are not many buccal delivery products available on the market. OBJECTIVE:This review outlines the advantages and disadvantages of buccal drug delivery, provides a historical perspe...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章,评审
doi:10.1517/17425247.5.5.531
更新日期:2008-05-01 00:00:00
abstract:BACKGROUND:The present work focuses on the development of ultra-small solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) encapsulating cyclosporine and calcipotriol, further incorporated into gel, increasing their penetration through the skin. RESEARCH DESIGN AND METHODS:Developed SLN and NLC were...
journal_title:Expert opinion on drug delivery
pub_type: 杂志文章
doi:10.1080/17425247.2017.1264386
更新日期:2017-02-01 00:00:00