L'Importanza della Farmacovigilanza in pediatria

Safety data concerning drugs usage in children are often inadequate, because most of marketed medicines have not undergone clinical trials involving children: therefore many drugs used in children are used “off-label” or “off-licence” in paediatric population. Furthermore, Adverse Drug Reactions (ADRs) are a significant problem in paediatric patients, and can be different from those observed in adults, because of the different weight and the incomplete maturity of organs and systems. Clinical trials involving children have been started only few years ago, and their results will be available in a long time; clinical trials will identify the more common and predictable side effects of medicines, but the rarest ones will be seen only when the drug will be used in larger numbers of patients, under the conditions of every day use. For these reasons, paediatric pharmacovigilance is essential, providing data on ADRs and drugs safety from both spontaneous reports and active surveillance program, e.g. post-marketing safety studies, and ad hoc epidemiological studies

Flavonoid microparticles by spray-drying: Influence of enhancersof the dissolution rate on properties and stability

Naringenin (Nn) and Quercetin (Q) have numerous health benefits particularly due to their antioxidant properties. However, their low solubility, bioavailability and stability limit their use as components for functional foods, nutraceuticals and pharmaceutical agents. In this research, Nn- and Q-microparticles were produced by a spray-drying process using a combination of cellulose acetate phthalate (CAP) as coating gastroresistant polymer and swelling or surfactant agents as enhancers of dissolution rate. Raw materials and microparticles produced were all characterized by particle size analysis, differential scanning calorimetry, X-ray diffraction, and imaged by electron and fluorescence microscopy. During 12 months, storage stability was evaluated by analyzing drug content, HPLC and DSC profiles, as well as antioxidant activity (DPPH test). In vitro dissolution tests, using a pH-change method, were carried out to investigate the influence of formulative parameters on flavonoid release from the microparticles. Presence of a combination of CAP and surfactants or swelling agents in the formulations produced microparticles with good resistance at low pH of the gastric fluid and complete flavonoid release in the intestinal environment. The spray-drying technique and the process conditions selected have given satisfying encapsulation efficiency and product yield. The microencapsulation have improved the technological characteristics of the powders such as morphology and size, have given long-lasting storage stability and have preserved the antioxidant properties

Editorial of Special Issue "Botanicals: innovative tools for pharmaceutical, cosmetic and nutraceutical"

FDA defined “botanicals” as products of plant materials, algae, macroscopic fungi, and their combinations and considered them as finished, labeled products containing vegetables as ingredients, that can be used as conventional foods, dietary supplements, drugs, cosmetics, or medical devices depending on its route of administration, formulation, safety and intended use [1, 2]. Today, the use of medicinal plant remains widespread, and a significant portion of the world's population utilizes herbal natural products and supplements as the primary mode of healthcare [3,4]. In the United States, for instance, nearly 20% of adults and 5% of children utilize botanical supplements to treat different diseases. The increase in adoption of herbal remedies may be ascribed to: a general preference of natural therapies and aversion for other interventions like surgery, allopathic medicines etc; inclination towards self-medication based upon experience; affordable cost of herbal medicines and ease of availability; side effects associated with conventional medicines (especially in cases of chronic problems) and growing promotion of herbal medicines [4]. Botanicals in medicine are usually recommended for disease prevention and to maintain good health, while rarely their use is suggested for acute and/or life-threatening problems. More recently, it is observed a growing use of herbal medicine when conventional medicine is ineffective or for pain palliation in case of long-standing problems like cancer, arthritis, etc. [5]. Also the cosmetic market has been influenced by botanicals. In particular, it has been observed a growing trend in incorporating antioxidants in sunscreens and skincare products to replenish the natural reservoirs in the skin [6]. This “new renaissance” of herbal product obliges us to employ them with a real scientific method. Researchers having access to innovative technologies can optimize the use of herbal ingredients in natural formulations, to give safety and efficacy to the formulation across a scientific view, validating the traditional use, with no previous scientific evidence. On these bases, this special issue is aimed to give an overview of the current state of botanicals research, in order to collect recent scientific data on the development of pharmaceutical products, cosmetics, and nutraceuticals. The attention is focused on the chemical composition, biological activities [7-11] and nutritional aspects of new herbal products and on the application of innovative technologies or formulative approaches to improve their stability and bioavailability [8-10, 12-15]. Readers will find information about new natural products endowed with healthy activities. Flaxseed oil, for instance, is a very important product characterized by anti-oxidant, anti- inflammatory and anti-dysmetabolic effects and has been evaluated for a potential application in different diseases [8]. Brassica vegetables also possess anti-oxidative properties and are associated with the risk reduction of chronic diseases including cardiovascular diseases and cancer. The focus of the present special issue is also on some indigenous underutilized wild edible plants, such as Pereskia aculeate, a natural diet supplement studied as “novel food” in virtue of its high nutritional value [10] and Momordica cochinchinensis, a super fruit, of the functional food industry [11]. Finally, our readers will find interesting examples of innovative delivery strategies to increase the bioavailability of natural active compounds from vegetable sources. Extensive discussion on this special issue about different nanocarriers for the delivery of natural products, functional foods, dietary supplements, and herbal medicinal products is also addressed

Natural Antioxidant Polyphenols On Inflammation Management: Anti-glycation Activity Vs Metalloproteinases Inhibition.

The diet polyphenols are a secondary metabolites of plants able to act on inflammation process. Their anti-inflammatory activity is articulated through several mechanisms that are related to their antioxidative and radical scavengers properties. Our work is focused on a novel approach to inflammatory disease management, based on anti-glycative and matrix metalloproteinases (MMPs) inhibition effects, as a connected phenomena. To better understand these correlation, polyphenols Structure-Activity Relationship (SAR) studies were also reported. The antioxidant polyphenols inhibit the AGEs at different levels of the glycation process in the following ways: 1) prevention of Amadori adduct oxidation; 2) trapping reactive dycarbonyl compounds; 3) attenuation of receptor for AGEs (RAGE) expression. Moreover, several flavonoids with radical scavenging property showed also MMPs inhibition interact directly with MMPs or indirectly via radical scavengers and AGEs reduction. The essential polyphenols features involved in these mechanisms are C2-C3 double bond and number and position of hydroxyl, glycosyl and O-methyl groups. These factors induce a change in molecular planarity interfering with the hydrogen bond formation, electron delocalization and metal ion chelation. In particular, C2-C3 double bond improve the antioxidant and MMPs inhibition, while the hydroxylation, glycosylation and methylation induce a positive and negative correlation respectively

POLYMERIC COLLOIDAL CARRIERS FOR NATURAL POLYPHENOLIC COMPOUNDS

Natural polyphenolic compounds are major micronutrients in our diet. They possess interesting antioxidant properties and play an important dietary role in reducing the risk of inflammation, neurodegenerative, and chronic diseases such as dysmetabolic pathologies. These abilities make polyphenols interesting for pharmaceutical, cosmetic, and nutraceutical fields. Unfortunately, they have a series of drawbacks that reduce their use such as high molecular weight, complex chemical structure, low water solubility, sensitivity to light and heat with consequently limited stability, and product shelf life. All these factors reduce bioavailability; limited dissolution rate and degradation at extreme pH values, resulting in less or no therapeutic effects. Besides that, polyphenols have extensive phase II metabolism and rapid elimination. Oral use and patient compliance are often limited by their astringent and bitter taste. The formulation of polymeric colloidal carriers could overcome these drawbacks allowing more efficient and stable products. This chapter will focus on the relevant recent scientific literature in the past few years regarding this topic. In particular, we analyzed the use of biocompatible natural and synthetic polymers able to formulate micro- and nanosystems with an improvement of the physicochemical, biological, and technological polyphenolic characteristics

Polyhydroxylated triterpenes from senecio pseudotites

Abstract: Three new polyhydroxylatedtriterpenes were isolated from the chloroform-methanol extract of the leaves of Seneciopseudotites. Their structures were elucidated as 2α,3β,23-trihydroxy-urs-12,19(29)-dien-28-oic-acid; 2α,3β,23-trihydroxy-urs-12,19(29)-dien-28-oic-acid-23-acetyl ester; 23-(trans-p-coumaroyloxy)-2α,3β-dihydroxy-urs-12,19(29)-dien-28-oic-acid by NMR spectroscopy