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

Resveratrol-loaded nanoparticles based on polymeric blend for prostsate cancer treatment

The trans-resveratrol (RSV) has been reported to act as an antiproliferative and chemopreventive agent against a wide variety of tumors, including prostate cancer (PCa)I,2. Nanoencapsulation of RSV represents a powerful strategy to provide protection of degradation, enhancement of bioavailability, improvement of intracellular penetration and control delivery,4. We developed novel polymeric nanoparticles (NPs) encapsulating RSV (nano-RSV), based on a polymeric blend, as effective prototypes for PCa treatment. Our results support the potential use of these prototypes for the controlled delivery ofRSV for PCa treatment

<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

Microencapsulation of <i>Bacillus thuringiensis</i> and insecticidal activity evaluation on larvae of lepidoptera

Bacillus thuringiensis (Bt) is one of the bacterial entomopathogens most frequently studied as a toxin producer. Its insecticidal activity was attributed to the parasporal crystals formed during the stationary phase of its growth cycle, and released during sporulation. The efficacy of Bt is highly sensitive to the environmental conditions; when exposed to UV light, the insecticidal proteins undergoes to rapid degradation. Considerable research has attempted to improve Bt field persistence using ultraviolet absorbers, encapsulation and addition of clay granules to spray formulations. The aim of this study was to investigate different encapsulation processes in order to obtain the Bt-based formulations consisting of matrix-type microcapsules

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

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

Development of a Raltegravir-based Photoaffinity-Labeled Probe for Human Immunodeficiency Virus-1 Integrase Capture

Photoaffinity labeling (PAL) is one of the upcoming and powerful tools in the field of molecular recognition. It includes the determination of dynamic parameters, such as the identification and localization of the target protein and the site of drug binding. In this study, a photoaffinity-labeled probe for full-length human immunodeficiency virus-1 integrase (HIV-1 IN) capture was designed and synthesized, following the structure of the FDA-approved drug Raltegravir. This photoprobe was found to retain the HIV IN inhibitory potential in comparison with its parent molecule and demonstrates the ability to label the HIV-1 IN protein. Putative photoprobe/inhibitor binding sites near the catalytic site were then identified after protein digestion coupled to mass and molecular modeling analyses

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

Inhibitory effect of 2,3,5,6-tetrafluoro-4-[4-(Aryl)-1H-1,2,3-triazol-1-yl]benzenesulfonamide derivatives on HIV reverse transcriptase associated rnase H activities

The HIV-1 ribonuclease H (RNase H) function of the reverse transcriptase (RT) enzyme catalyzes the selective hydrolysis of the RNA strand of the RNA:DNA heteroduplex replication intermediate, and represents a suitable target for drug development. A particularly attractive approach is constituted by the interference with the RNase H metal-dependent catalytic activity, which resides in the active site located at the C-terminus p66 subunit of RT. Herein, we report results of an in-house screening campaign that allowed us to identify 4-[4-(aryl)-1H-1,2,3-triazol-1-yl]benzenesulfonamides, prepared by the “click chemistry” approach, as novel potential HIV-1 RNase H inhibitors. Three compounds (9d, 10c, and 10d) demonstrated a selective inhibitory activity against the HIV-1 RNase H enzyme at micromolar concentrations. Drug-likeness, predicted by the calculation of a panel of physicochemical and ADME properties, putative binding modes for the active compounds, assessed by computational molecular docking, as well as a mechanistic hypothesis for this novel chemotype are reported