Design and evaluation of dry-coated tablets for colonic delivery of diclofenac sodium

A colonic drug delivery system is required to protect a drug during its transit through the upper gastro-intestinal tract and allow its release in the colon. The aim of this study was the preparation of dry-coated tablets designed for colonic release of the model drug Diclofenac sodium (DS). The system consists of a drug-pectine (PC) mixture as the core and hydroxypropylmethylcellulose (HPMC) alone or mixed in different ratios with poly(ε-caprolactone) (CL) as the coat layer

Targeted nanoparticles for the delivery of novel bioactive molecules to pancreatic cancer cells

Pancreatic cancer (PaCa) is a multifaceted disorder with an extremely poor prognosis. There is an urgent need to identify new and safe drugs as well as to develop novel tumor-targeted controlled release systems for effective treatment of late stage and resistant PaCa. Active targeting via the inclusion of specific ligands on the nanoparticles (NPs) is envisioned to provide a powerful therapeutic strategy. Herein, we present a study on the design and the development of novel DFCencapsulated biocompatible polymeric NPs, functionalized with peptides to selectively bind to Plec-1 (PTP), or densely decorated by low molecular weight organic molecules as alternative targeting ligands (2-ABA), and evaluated a) the impact on ligand binding and b) the in vitro antiproliferative efficacy against a panel of PaCa cells

<i>In vitro</i> and <i>in vivo</i> studies of artichoke extract (<i>Cynara scolymus</i> L.) as ketoprofen skin penetration enhancer

In this study, the enhancing effect of artichoke extract containing cynaropicrin on the in vitro and in vivo percutaneous absorption of ketoprofen from gels has been investigated

Evaluation of the vehicle effect on release of diphenhydramine hydrochloride from topical formulations: in vitro and in vivo preliminary studies

Diphenhydramine hydrochloride (DPH) is a histamine H1-receptor antagonist, widely used as antiallergic, antiemetic and antitussive drug in many pharmaceutical preparations. The aim of this study was to evaluate the vehicle effect on in vitro diffusion of DPH from new five topical formulations: microemulsion, microemulsion+silica, Na Alginate emulgel, Carbopol cream and hydroxyethylcellulose gel

Spray-dried microspheres based on methylpyrrolidinone chitosan: <i>in-vitro</i> and <i>ex-vivo</i> studies

The purpose of this work was the preparation and the study of methypyrrolidinone chitosan spray-dried microspheres for the intranasal release of metoclopramide hydrochloride (Met). Chitosan (CH) microparticles were prepared as comparison

<i>Ex vivo</i> cutaneous penetration of econazole nitrate from SLN incorporated in hydrophilic gels

Solid lipid nanoparticles (SLN) are considered as innovative drug carrier for topical application. The small size of the lipid particles ensures close contact to the stratum corneum and can increase the amount of the drug penetrating into the skin and it allows controlled drug release. The aim of this study was to develop controlled release gels containing SLN dispersions loaded with Econazole Nitrate (ECN) and to evaluate ex vivo skin penetration of the drug released from the particles

Docking ligando-DNA e validazione della capacità intercalante di nuovi derivati "two-armed"

In questo contesto è risultato di grande interesse cercare di studiare la capacità intercalante e le modalità di binding di noti ligandi (Actinomicina D, Etidio bromuro, Distamicina) attraverso uno studio computazionale con tecniche di docking che potesse risultare di utile supporto nella ricerca di nuovi agenti intercalanti. E’ stato quindi messo a punto un versatile metodo di docking tramite l’utilizzo del programma AutoDock operando in diverse condizioni sperimentali

Study of hydrogels based on polyacrilamide as new controlled release dosage forms produced by frontal polymerization

The work purpose was the evaluation of the potential application of the Frontal Polymerization (FP) technique as a new method for the preparation of controlled release dosage forms based on polyacrilamide, in which the drug loading and the polymer preparation occur at the same time

Single-step green synthesis and characterization of gold-conjugated polyphenol nanoparticles with antioxidant and biological activities

Background: Gold nanoparticles (GNPs) are likely to provide an attractive platform for combining a variety of biophysicochemical properties into a unified nanodevice with great therapeutic potential. In this study we investigated the capabilities of three different natural polyphenols, epigallocatechin-3-gallate (EGCG), resveratrol (RSV), and fisetin (FS), to allow synergistic chemical reduction of gold salts to GNPs and stabilization in a single-step green process. Moreover, antioxidant properties of the nanosystems, as well as preliminary antiproliferative activity and apoptotic process investigation of model EGCG-GNPs on stable clones of neuroblastoma SH-SY5Y cells expressing CFP-DEVD-YFP reporter, were examined. Methods: The GNPs were characterized by physicochemical techniques, polyphenol content, and in vitro stability. The antioxidant activity of the GNPs was also determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) cation (ABTS) radical-scavenging assays. Stable clones of neuronal SH-SY5Y-CFP-DEVD-YFP were generated and characterized, and cell viability after treatment with EGCG-GNPs was assessed after 72 hours through a 3(4,5-dimethylthiazol-2yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assay. Activation of the apoptotic pathways was also investigated by Western blot analysis. Results: With a diameter in the size range of 10–25 nm, the obtained nanoparticles (NPs) were found to contain 2.71%, 3.23%, and 5.47% of EGCG, RSV, and FS, respectively. Nanoprototypes exhibited remarkable in vitro stability in various media, suggesting that NP surface coating with phytochemicals prevents aggregation in different simulated physiological conditions. The scavenging activities for DPPH and ABTS were highly correlated with EGCG, RSV, and FS content. Moreover, high correlation coefficients between the ABTS and DPPH values were found for the prepared nanosystems. EGCG-GNPs induce a dose-dependent reduction on SH-SY5Y-CFP-DEVD-YFP cell viability that is likely to involve the activation of the apoptotic pathways, similarly to free EGCG, as suggested by the processing of the CFP-DEVD-YFP reporter. Conclusion: These results prompted us to propose the ecofriendly synthesized EGCG-, RSV-, and FS-based nanogold conjugates as suitable carriers for bioactive polyphenols to be used for the treatment of disorders associated with oxidative stress, including neurodegenerative disorders, cardiovascular disease, and cancer.</br