Search results for "FARMACEUTICO"

Controlled delivery of naltrexone by an intraoral device: in vivo study on human subjects.

2013

Naltrexone is widely used in the treatment of opiate addiction but its current peroral administration is characterized by low bioavailability with various side effects. The development of a long-acting transbuccal delivery device (IntelliDrug) for NLX may be useful to improve patient compliance and the therapy effectiveness. The aims of the study are (a) to test basic safety and effectiveness of controlled transbuccal drug delivery on human subjects; (b) to compare NLX bioavailability following transbuccal delivery vs per os conventional delivery; and (c) to test the hypothesis that transbuccal delivery is more efficient than the conventional route. In this randomized cross-over pilot study…

Diffusion of naltrexone across reconstituted human oral epithelium and histomorphological features

2006

Abstract In transbuccal absorption a major limitation could be the low permeability of the mucosa which implies low drug bioavailability. The ability of naltrexone hydrochloride (NLX) to penetrate a resembling histologically human buccal mucosa was assessed and the occurrence of any histomorphological changes observed. We used reconstituted human oral (RHO) non-keratinised epithelium as mucosal section and a Transwell diffusion cells system as bicompartmental model. Buccal permeation was expressed in terms of drug flux ( J s ) and permeability coefficients ( K p ). Data were collected using both artificial and natural human saliva. The main finding was that RHO does not restrain NLX permeat…

Bioavailability in vivo of naltrexone following transbuccal administration by an electronically-controlled intraoral device: a trial on pigs.

2010

Naltrexone (NLX), an opioid antagonist, is widely used in the treatment of opiate addiction, alcoholism and smoking cessation. Its current peroral administration induces various adverse side effects and has limited efficacy since bioavailability and patient compliance are poor. The development of a long-acting drug delivery system of NLX may overcome the current drawbacks and help in the improvement of treatment of addiction. The primary endpoints of this study were: a) to compare the NLX bioavailability and pharmacokinetics after delivering a single transbuccal dose, released by a prototype of intraoral device, versus an intravenous (I.V.) bolus of the same drug dose; b) to verify the func…

Production of polymeric micro- and nanostructures with tunable properties as pharmaceutical delivery systems

2020

Abstract The production of novel graft copolymers based on poly-e-caprolactone (PCL) and polyaspartamide are useful to realize structures for potential biomedical applications. Here, the synthesis of pegylated PCL/polyhydroxyethyl aspartamide (PHEA) graft copolymers (PHEA-g-SUCC-PCL-g-PEG) with tunable composition, was achieved by followpling a synthetic strategy that involved first the grafting of preformed PCL on PHEA backbone, then polyethylen glycol (PEG), by using 1,1′-carbonyldiimidazole (CDI) to speed up the condensation reaction. Graft copolymers with a Derivatization Degree (DD) in PCL ranging between 1.1 and 4.4 mol% were obtained, and processable with different technologies for t…

CURCUMIN ENTRAPPED INTO LIPID NANOSYSTEMS IMPROVES INHIBITION OF NEUROBLASTOMA CANCER CELL GROWTH ACTIVATING HSP70 PROTEIN

2010

Lipid nanocarriers containing esters prodrugs of Flurbiprofen. Preparation, physical-chemical characterization and biological studies.

2013

In this paper, the preparation, chemical-physical, technological and in vitro characterization of nanostructured lipid carriers (NLC) carrying R-flurbiprofen ester prodrugs, were analyzed for a potential pharmaceutical application. R-flurbiprofen was chosen as a model drug because it has been found to play an effective role in counteracting secretases involved in neurodegenerative diseases, although it does not cross the Blood Brain Barrier (BBB). In this study, two R-flurbiprofen ester prodrugs (ethyl and hexyl) were successfully synthesized and entrapped into non-pegylated and pegylated NLC. The obtained systems showed average diameters in the colloidal size range, negative zeta potential…

Galactosylated polymeric carriers for liver targeting of sorafenib

2014

In this paper, we describe the preparation of liver-targeted polymeric micelles potentially able to carry sorafenib to hepatocytes for treatment of hepatocarcinoma (HCC), exploiting the presence of carbohydrate receptors, ASGPR. These micelles were prepared starting from a galactosylated polylactide-polyaminoacid conjugate. This latter was obtained by chemical reaction of α,β-poly(N-2-hydroxyethyl) (2-aminoethylcarbamate)-d,l-aspartamide (PHEA-EDA) with polylactic acid (PLA), and subsequent reaction with lactose, leading to PHEA-EDA-PLA-GAL copolymer. Liver-targeted sorafenib-loaded micelles were obtained in aqueous media at low PHEA-EDA-PLA-GAL copolymer concentration value with nanometer …

Lipid nanocarriers containing sorafenib inhibit colonies formation in human hepatocarcinoma cells

2015

Here, the potential of two nanostructured lipid carriers (NLC) for controlled release of sorafenib was evaluated. The obtained systems showed characteristics suitable as drug delivery systems for the treatment of hepatocellular carcinoma (HCC) through parenteral administration. The use of a mixture between a solid lipid (tripalmitin) with a liquid lipid (Captex 355 EP/NF or Miglyol 812) to prepare NLC systems could give a higher drug loading capacity and a longer term stability during storage than that obtained by using only solid lipids. The obtained nanoparticles showed a nanometer size and high negative zeta potential values. Scansion electron microscopy (SEM) of the sorafenib loaded NLC…

Nitrogen and sulfur co-doped carbon nanodots toward bovine hemoglobin: A fluorescence quenching mechanism investigation

2018

A deep understanding of the molecular interactions of carbon nanodots with biomacromolecules is essential for wider applications of carbon nanodots both in vitro and in vivo. Herein, nitrogen and sulfur co-doped carbon dots (N,S-CDs) with a quantum yield of 16% were synthesized by a 1-step hydrothermal method. The N,S-CDs exhibited a good dispersion, with a graphite-like structure, along with the fluorescence lifetime of approximately 7.50 ns. Findings showed that the fluorescence of the N,S-CDs was effectively quenched by bovine hemoglobin as a result of the static fluorescence quenching. The mentioned quenching mechanism was investigated by the Stern-Volmer equation, temperature-dependent…

STRATEGIE DI DIREZIONAMENTO ALL’EPATOCARCINOMA DI FARMACI ANTITUMORALI MEDIANTE SISTEMI NANOPARTICELLARI E DI VISUALIZZAZIONE IN CELLULE TUMORALI DEL…

Lo scopo di questo lavoro di tesi è stato quello di realizzare nuovi sistemi nanoparticellari per il direzionamento di farmaci o di agenti per l’imaging, potenzialmente utilizzabili per la terapia e/o per la diagnosi dell’epatocarcinoma (HCC), in particolare per quelle forme caratterizzate dall’overespressione del recettore di membrana degli epatociti ASGP-R o del recettore mitocondriale TSPO. In particolare, nel capitolo 2 sono state descritte la sintesi, la caratterizzazione chimico fisica, la capacità di internalizzazione cellulare e l’efficacia antitumorale di un nuovo sistema nanoparticellare, costituito da un dendrimero a struttura poli-amido-aminica (PAMAM) di quarta generazione, opp…