Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES): Synthesis, cytotoxicity and inclusion of anaesthetic actives
نویسندگان
چکیده
The mono-6-deoxy-6-azides of 2,6-di-O-methyl-β-cyclodextrin (DIMEB) and randomly methylated-β-cyclodextrin (RAMEB) were conjugated to propargylated hydroxyethyl starch (HES) by Cu(+)-catalysed [2 + 3] cycloaddition. The resulting water soluble polymers showed lower critical solution temperatures (LCST) at 52.5 °C (DIMEB-HES) and 84.5 °C (RAMEB-HES), respectively. LCST phase separations could be completely avoided by the introduction of a small amount of carboxylate groups at the HES backbone. The methylated CDs conjugated to the HES backbone exhibited significantly lower cytotoxicities than the corresponding monomeric CD derivatives. Since the binding potentials of these CD conjugates were very high, they are promising candidates for new oral dosage forms of anaesthetic actives.
منابع مشابه
Preparationa and Characterization of domperidone Inclusion complexes with cyclodextrin: Influence of preparation method
Domperidone is a widely used antiemetic, poorly water soluble drug, erratically absorbed in stomach and possess several dissolution-related problems thus it has poor bioavailability. Solubility of a drug plays a very important role in dissolution and hence absorption of drug which ultimately affects its bioavailability. Hence, by considering the facts related to drug, attempts have been made to...
متن کاملPreparationa and Characterization of domperidone Inclusion complexes with cyclodextrin: Influence of preparation method
Domperidone is a widely used antiemetic, poorly water soluble drug, erratically absorbed in stomach and possess several dissolution-related problems thus it has poor bioavailability. Solubility of a drug plays a very important role in dissolution and hence absorption of drug which ultimately affects its bioavailability. Hence, by considering the facts related to drug, attempts have been made to...
متن کاملHydroxyethyl starch as an effective methotrexate carrier in anticancer therapy
At present, effective anticancer therapy remains one of the most challenging tasks facing the scientific community. A major limitation to most conventional low-molecular weight anticancer chemotherapeutics is their unfavourable uptake by healthy tissue, fast metabolism and lack of tumour cell selectivity. One way to solve this problem is the application of hybrid nanoparticles containing widely...
متن کاملThe effect of hydroxyethyl starches and crystalloid fluids on mortality and need for dialysis in vascular surgery patients
Introduction Previous research has indicated that fluid choice is an important component of the resuscitation of the critically-ill patient. Synthetic hydroxyethyl starches (HES) may remain within the intravascular space compared to crystalloid solutions, yet they have also been associated with acute kidney injury. Data comparing HES and crystalloid solutions in anesthesia is incomplete. The go...
متن کاملRapid exacerbation of renal function after administration of hydroxyethyl starch in a dog
Hydroxyethyl starches (HES) are commonly used synthetic colloidal solution in veterinary medicine. Despite of possible adverse effect to kidney injury in human, there is no report about nephrotoxic effects of HES in dogs. HES was administered to a Golden retriever (4-year-old, intact male) with ascites in order to increase plasma osmolality. Initially, the dog was mild azotemic, however, kidney...
متن کامل