Search results for "Conjugates"

Chemical conjugation of dexamethasone to a polyaspartamide and in vitro evaluation studies

2004

Two macromolecular conjugates of dexamethasone containing different drug amounts were synthesized using PHEA as the polymeric carrier and a succinic group as spacer. The content of linked drug was equal to 25.3% w/w (conjugate A) and 12.7% w/w (conjugate B). Both polymeric conjugates, unlike the free drug, were water-soluble and the amount of unlinked drug was evaluated to be approximately about 0.01% w/w. Both conjugates were relatively stable in vitro at pH 7.4 whereas in the presence of esterase only the conjugate B was able to release drug under the used experimental conditions. This dissimilar behavior has been attributed to the distinct macromolecular conformations assumed in aqueous …

Glycoconjugate expression and cartilage development of the cranial skeleton.

1998

Only few detailed investigations have focused on the glycobiology of cranial development. The functional elements in most inductive and morphogenetic processes are not individual cells, but rather collectives of interacting populations and extracellular matrix components that give rise to specific tissues and organs. Experimental evidence strongly suggests that sugar chains not only confer morphological characteristics. Complex carbohydrate molecules and their corresponding receptors are involved in recognition processes decoding biological information during cranial morphogenesis. The distribution patterns of glycoconjugates are highly dynamic and show a clear correlation with characterist…

Structure and properties of pharmacologically active polymers

1975

Although the concept of using pharmacologically active macromolecular compounds as drugs is still regarded with much skepticism for both theoretical and practical reasons, interest in this field has grown in recent years because of the opportunity to take advantage of the specific properties of polymeric materials. For low molecular weight drugs, changes in structure often lead to a loss of specific activity. On the other hand, the properties of macromolecular drugs depend on the structure of the polymer used and this can be varied over a wide range by the incorporation of comonomer units, by the application of polymer-analogous reactions, or by related structural changes. A new model is pr…

PHEA-Dox nanoparticles as pH-sensitive model for drug delivery in tumour treatment.

2015

PHEA-Dox nanoparticles as pH-sensitive model for drug delivery in tumour treatment. S. Camporaa, G. Adamoa, N. Maurob, C. Scialabbab, M. Licciardib, G. Giammonab and G. Ghersia. aDipartmento di “Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche” (STEBICEF), Università di Palermo, Viale delle Scienze Ed. 16, 90128 Palermo, Italy. bLaboratory of Biocompatible Polymers, Dipartmento di “Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche” (STEBICEF), Università di Palermo, Via Archirafi, 32 90123 Palermo, Italy. Classical chemotherapeutic applications, using molecules such as doxorubicin (Dox), have side effects due to an unspecific action. In order to obtain a specific release of…

An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety

2020

The rapid growth of serious infections caused by antibiotic resistant bacteria, especially the nosocomial ESKAPE pathogens, has been acknowledged by Governments and scientists and is one of the world’s major health problems. Various strategies have been and are currently investigated and developed to reduce and/or delay the bacterial resistance. One of these strategies regards the design and development of antimicrobial hybrids and conjugates. This unprecedented critical review, in which our continuing interest in the synthesis and evaluation of the bioactivity of imidazole derivatives is testified, aims to summarise and comment on the results obtained from the end of the 1900s until Februa…

Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging.

2017

Background In this work, the in vitro and in vivo stabilities and the pharmacology of HPMA-made homopolymers were studied by means of radiometal-labeled derivatives. Aiming to identify the fewer amount and the optimal DOTA-linker structure that provides quantitative labeling yields, diverse DOTA-linker systems were conjugated in different amounts to HPMA homopolymers to coordinate trivalent radiometals Me(III)* = gallium-68, scandium-44, and lutetium-177. Results Short linkers and as low as 1.6% DOTA were enough to obtain labeling yields > 90%. Alkoxy linkers generally exhibited lower labeling yields than alkane analogues despite of similar chain length and DOTA incorporation rate. High sta…

Molecular modelling studies on dopamine-amino acid conjugates as potential dopaminergic modulators

2015

Polymer Drug Conjugates for the Treatment of Neurodegenerative Disorders

2013

Nanociencia y nanotecnología son la base de técnicas innovadoras para el transporte de fármacos con beneficios potenciales para el paciente y nuevos mercados para la industria. La obtención de nuevos sistemas de transporte de fármacos más efectivos es uno de los principales retos actuales, junto con la mejora del diagnóstico tanto in vitro como in vivo y el desarrollo de tecnologías para la ingeniería tisular y la medicina regenerativa. Además de ser necesario disponer de moléculas con actividad farmacológica para conseguir terapias efectivas se necesitan su transporte y liberación controlada para llegar a conseguir tratamientos con mayor índice terapéutico. El uso de estrategias de direcci…

ANTIBODY-DRUG CONJUGATES: A SYSTEMATIC REVIEW OF IN VITRO STUDIES IN ORAL CANCER

2021

DES-polyacetals as polymer therapeutics for the treatment of prostate cancer

2012

Esta tesis se centra en el diseño de nuevos conjugados polímero-fármaco sensibles a pH para usarse como agentes únicos o en terapia de combinación para el tratamiento del cáncer hormono-dependiente, en particular cáncer de próstata. Éstos conjugados se basan en sístemas poliacetalicos previamente descritos en los que el fármaco forma parte de la cadena principal del polímero. En el microambiente tumoral o después de la absorción celular por endocitosis, el descenso del pH encontrado en el compartimiento ácido del endosoma lisosomal, desencadena la degradación del polímero y como consecuencia la liberación del fármaco que se difunde fuera en el citosol. Para el diseño de éstos sistemas, la n…