Resveratrol is a polyphenol that among other sources occurs in grapes and for this reason, red wines also contain considerable amounts of this compound. Resveratrol is thought to be responsible for the ‘‘French Paradox’’ which associates red wine consumption to the low incidence of cardiovascular diseases. The interest in resveratrol has increased due to its pharmacological effects that include cardio and neuroprotection and several other benefic actions (e.g. antioxidant, anti-inflammatory, anti-carcinogenic and anti-aging). Despite the therapeutic effects of resveratrol, its pharmacokinetic properties are not favorable since this compound has poor bioavailability being rapidly and extensively metabolized and excreted. To overcome this problem, drug delivery systems have been developed to protect and stabilize resveratrol and to enhance its bioavailability. Herein is presented an up-to-date revision covering the literature reported for nano and microformulations for resveratrol encapsulation that include liposomes, polymeric nanoparticles, solid lipid nanoparticles, lipospheres, cyclodextrins, polymeric microspheres, yeast cells carriers and calcium or zinc pectinate beads. Regarding the interaction of resveratrol with cell membranes, only few studies have been published so far. However, it is believed that this interaction can be implied in the biological activities of resveratrol since transmembranar proteins are one of its cellular targets. Indeed, resveratrol presents the capacity to modulate the membrane organization which may consequently affect the protein functionality. Therefore, the intracellular effects of resveratrol and the effects of this compound at the membrane level were also revised since their knowledge is essential for understanding the pharmacological and therapeutic activities of this bioactive compound.

Introduction: Resveratrol is a polyphenol found in grapes and red wines. Interest in this polyphenol has increased due to its pharmacological cardio- and neuroprotective, chemopreventive, and antiaging effects, among others. Nevertheless, its pharmacokinetic properties are less favorable, since the compound has poor bioavailability, low water solubility, and is chemically unstable. To overcome these problems, we developed two novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance resveratrol's oral bioavailability for further use in medicines, supplements, and nutraceuticals. Methods and materials: Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) loaded with resveratrol were successfully produced by a modified hot homogenization technique. These were completely characterized to evaluate the quality of the developed resveratrol-loaded nanoparticles. Results: Cryo-scanning electron microscopy morphology studies showed spherical and uniform nanoparticles with a smooth surface. An average resveratrol entrapment efficiency of ~70% was obtained for both SLNs and NLCs. Dynamic light scattering measurements gave a Z-average of 150–250 nm, polydispersity index of ~0.2, and a highly negative zeta potential of around −30 mV with no statistically significant differences in the presence of resveratrol. These characteristics remained unchanged for at least 2 months, suggesting good stability. Differential scanning calorimetry studies confirmed the solid state of the SLNs and NLCs at both room and body temperatures. The NLCs had a less ordered crystalline structure conferred by the inclusion of the liquid lipid, since they had lower values for phase transition temperature, melting enthalpy, and the recrystallization index. The presence of resveratrol induced a disorder in the crystal structure of the nanoparticles, suggesting a favoring of its entrapment. The in vitro release studies on conditions of storage showed a negligible resveratrol release over several hours for both nanosystems and the in vitro simulation of gastrointestinal transit showed that the resveratrol remained mostly associated with the lipid nanoparticles after their incubation in digestive fluids. Conclusion: Both nanodelivery systems can be considered suitable carriers for oral administration, conferring protection to the incorporated resveratrol and allowing a controlled release after uptake.

Generally drugs can act on the level of different biological membranes as well as inside the cells that are limited by membranes. Even in the latter situation, drugs must still interact with the membrane in order to cross it and reach their targets. For this reason, the efficiency of drugs to interact with the membranes constitutes one of the most important pharmacological features playing an essential role in their biological activity. Membranes are the gathering place of many proteins and lipids, and are the structures where most cellular activities occur. Although drugs bind to proteins and regulate their activity, the membrane lipid phase is no less important. Great part of compounds studied induces structural changes in the lipid phase resulting structural defects, which in turn disturb membrane function and indirectly modulate membrane proteins. This paper reviews the clinical significance of drug-membrane interaction studies with a special focus in the lipidic components of the membrane and reinforcing the importance of these studies in the field of medicinal chemistry since they constitute stimulating opportunities for understanding drugs mode of action and toxic effects and cannot be overlooked during drug design and synthesis.

TB is an infectious disease that is far from being eradicated and controlled. The treatment for TB is associated with noncompliance to therapy because it consists of a long-term treatment with a multidrug combination and is associated with the appearance of several side effects. Liposomal formulations are being developed with first- and second-line antibiotics, and might be an extremely useful alternative to current therapies. This article will thus focus on the role of liposomes as nanodelivery systems for the treatment of TB. Among several advantages, these nanocarriers allow an increase in the bioavailability of antibiotics, which may lead to a reduction in the time of treatment. Results obtained with such nanosystems, although preliminary, are promising and are perspective of the use of inhalation for TB treatment.