Abstract:
:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular systems can be obtained exploiting the capability of CDs to form inclusion complexes. (i) The threading of free CDs on certain blocks or side chains of copolymers leads to polypseudorotaxanes, which can assembly via regular stacking of the threaded CDs. The resultant assemblies can be reversible broken under a certain shear stress and reformed at rest, exhibiting thixotropy that enables the flow through the syringe and the gel recovery in the implantation site. (ii) CDs grafted to polymer chains can develop their ability to form inclusion complexes with complementary guest moieties in other polymeric structures. The result is a ladder- or zipper-like arrangement, which can be also broken and reformed under certain stress conditions. Both types of CDsupramolecular gels can load and stabilize a variety of drugs via interaction with available polymer functional groups or with the CDs that are not participating in other complexes. Moreover, since the complex formation depends on various external and internal variables of the body, the syringeable CD gels can also provide stimuli-responsive drug release. This review focuses on the two main types of syringeable CD gels, prepared via self-aggregation of poly(pseudo)rotaxanes and via zipper-like assembly of CD-functionalized and guest-functionalized macromolecules, and analyzes the mechanisms and variables involved in the gelling processes and the most recent applications in the drug delivery field.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo Cdoi
10.2174/1568026613666131219124308subject
Has Abstractpub_date
2014-01-01 00:00:00pages
494-509issue
4eissn
1568-0266issn
1873-4294pii
CTMC-EPUB-58181journal_volume
14pub_type
杂志文章,评审abstract::Interest in the chemistry and biological properties of non-nucleoside N-glycosidic compounds has gathered pace over the past several years; the occurrence of the N-glycoside moiety in glycoproteins and a range of active natural products has prompted the synthesis of a diverse spectrum of related materials with promisi...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802608783378837
更新日期:2008-01-01 00:00:00
abstract::This chapter describes the life cycle, general morphology and ultrastructure of the larval and adult stages of Taenia solium, a parasitic flatworm of humans found in underdeveloped countries. Experimental results describing the role of proteins and glycoproteins in the host-parasite relationship, as well as the variou...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802608783790875
更新日期:2008-01-01 00:00:00
abstract::Research over the years has gradually and sequentially highlighted contributory role of hypothalamic- based kisspeptin-signaling axis as a major positive modulator of the neuroendocrinological reproductive axis in mammals. However, a series of landmark studies provided convincing evidence of role of this signaling in ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026616666160212123309
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abstract::Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addr...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802610790725461
更新日期:2010-01-01 00:00:00
abstract::An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802611794785163
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abstract::Many efforts are currently being made to connect small molecules to target proteins by extracting pharmacological data from bibliographic sources and storing them in annotated chemical libraries. Here, small molecules are further connected to biological pathways, with particular focus to pathways involving members of ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/156802607782194671
更新日期:2007-01-01 00:00:00
abstract::In medical oncology, targeted therapy has emerged over the last decade, as the most promising strategy to fight cancer. In addition, a more complete understanding of tumor heterogeneity and pharmacology of the more conventional anti-cancer agents has led to development of metronomic chemotherapy (MC) (i.e. a more freq...
journal_title:Current topics in medicinal chemistry
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abstract:: ...
journal_title:Current topics in medicinal chemistry
pub_type: 社论
doi:10.2174/156802661921191024120954
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abstract::Pyrimidine and purine nucleosides and their derivatives have critical functions and pharmacological applications in the brain. Nucleosides and nucleobases are precursors of nucleotides, which serve as the energy-rich currency of intermediary metabolism and as precursors of nucleic acids. Nucleosides (e.g., adenosine) ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802611795347582
更新日期:2011-01-01 00:00:00
abstract::Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2002-10-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 社论
doi:10.2174/1568026615666150413161707
更新日期:2015-01-01 00:00:00
abstract::Antiplatelets represent a diverse group of agents that share the ability to reduce platelet activity through a variety of mechanisms. Antithrombotic agents are effective in the secondary prevention of ischemic strokes. Most strokes are caused by a sudden blockage of an artery in the brain (called an ischaemic stroke) ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802609789869664
更新日期:2009-01-01 00:00:00
abstract::Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used drugs but their use is hampered by gastrointestinal side effects. Cyclo-oxygenase Inhibitor Nitric Oxide Donors (CINODs) are a new class of anti-inflammatory and analgesic drugs generated by adding a nitric oxide generating moiety to the parent NSAID via a...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802607779941350
更新日期:2007-01-01 00:00:00
abstract::Computational toxicity modeling can have significant impact in the drug discovery process, especially when utilized as a sentinel filter for common drug safety liabilities, such as mutagenicity, carcinogenicity and teratogenicity. This review will focus on the strengths and limitations of the current computational mod...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026013395074
更新日期:2001-09-01 00:00:00
abstract::An intensive research effort during the last 25 years has generated an impressive number of alkaloids isolated from marine ascidians, which remain unique among marine invertebrates in that they overwhelmingly produce this kind of metabolites. The present review is focused on some major groups of ascidians' bioactive a...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026613666131213155813
更新日期:2014-01-01 00:00:00
abstract::Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) controlling physiological processes as learning and memory. However, the overactivation of glutamatergic neurotransmission is often related to various CNS chronic and acute diseases (epilepsy, ischaemia, Parkinson, etc.). ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802612800229242
更新日期:2012-01-01 00:00:00
abstract::In this review the conformational studies of natural enkephalins (H-Tyr-Gly-Gly-Phe-Met-OH; the [Met(5)]enkephalin and H-Tyr-Gly-Gly-Phe-Leu-OH; the [Leu(5)]enkephalin), their acyclic and cyclic analogues, including those carried out in our laboratory, performed by experimental and theoretical methods and their combin...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026043451591
更新日期:2004-01-01 00:00:00
abstract::PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802607780487623
更新日期:2007-01-01 00:00:00
abstract::Alzheimer's Disease (AD) once considered a rare disorder emerges as a major health concern in recent times. The disease pathogenesis is very complex and yet to be understood completely. However, "Amyloid Cascade" is the central event in disease pathogenesis. Several proteins of the amyloid cascade are currently being ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026618666180116122921
更新日期:2017-01-01 00:00:00
abstract::The task of rationally designing vaccines that can effectively impact on the survival of cancer patients remains challenging. Monoclonal antibodies and T cell receptors have proven to be viable templates for the application of pharmacophore design principles to develop antigens and immunogens as these immune system mo...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802605774370928
更新日期:2005-01-01 00:00:00
abstract::A better understanding of the biology and pathogenesis of hematological malignancies has led to the development of immunotherapeutic and immunoregulatory drugs. Many of these agents have revolutionized the current treatment modalities, while others are under investigation. Rituximab (anti-CD20 antibody) has been estab...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802606778194235
更新日期:2006-01-01 00:00:00
abstract::As the first stable tachysterol analogs, 14-epi-19-nortachysterol and its 2-substituted derivatives were synthesized using the Stille coupling reaction between the A-ring precursor (three vinylstannanes) and the CD-ring vinyl trifrate. Among them, the 2-methylidene group was hydrogenated with Wilkinson's catalyst regi...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1568026615666141208103741
更新日期:2014-01-01 00:00:00
abstract::Tuberculosis (TB) is caused by the bacterium Mycobacterium tuberculosis and is a common infectious disease with high mortality and morbidity. The increasing prevalence of drug-resistant strains of TB presents a major public health problem. Due to the lack of effective drugs to treat these drug-resistant strains, the d...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026613666131113155042
更新日期:2014-01-01 00:00:00
abstract::Plasmodium has a complex life cycle that spans between mosquito and human. For survival and pathogenesis it banks upon dynamic alterations in ionic transport across organelle and plasma membrane. Being a fundamental contributor of crucial biological processes in parasite, ionic balance facilitates parasite invasion, a...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2019-01-01 00:00:00
abstract::In the last decade, we have been developing some gold(III) derivatives showing interesting antitumor properties and reduced systemic and renal toxicity, compared to the clinically-established reference drug cisplatin. Starting from the rationale at the base of our investigations, this review has been divided into two ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026615666150827094500
更新日期:2016-01-01 00:00:00
abstract::It is well established that matrix metalloproteinases (MMPs) contribute to the degradation of the extracellular matrix of coronary plaque and contribute to the thinning of the fibrous cap. As a result, the atheromatous plaque becomes unstable and prone to rupture with consequent clinical manifestations including acute...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026611208011206
更新日期:2012-01-01 00:00:00
abstract::(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends lar...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026611313080002
更新日期:2013-01-01 00:00:00
abstract::Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inh...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1568026616666160414122644
更新日期:2016-01-01 00:00:00
abstract::A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802612800672844
更新日期:2012-01-01 00:00:00
abstract::Trichomoniasis, one of the most common non-viral sexually transmitted infections worldwide, is caused by the parasite Trichomonas vaginalis. The pathogen colonizes the human urogenital tract, and the infection is associated with complications such as adverse pregnancy outcomes, cervical cancer, and an increase in HIV ...
journal_title:Current topics in medicinal chemistry
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doi:10.2174/1568026620999200904122212
更新日期:2021-01-01 00:00:00