Neuroprotective Effects of Resveratrol Against Aβ Administration in Rats are Improved by Lipid-Core Nanocapsules

Abstract

Alzheimer's disease (AD), a neurodegenerative disorder exhibiting a gradual decline in cognitive function, is characterized by the presence of neuritic plaques composed of neurofibrillary tangles and amyloid-β (Aβ) peptide. Available drugs for AD therapy have small effect sizes and do not alter disease progression. Several studies have been shown that resveratrol is associated with anti-amyloidogenic properties, but therapeutic application of its beneficial effects is limited. Here we compared the neuroprotective effects of free resveratrol treatment with those of resveratrol-loaded lipid-core nanocapsule treatment against intracerebroventricular injection of Aβ1-42 in rats. Animals received a single intracerebroventricular injection of Aβ1-42 (2 nmol), and 1 day after Aβ infusion, they were administered either free resveratrol (RSV) or resveratrol-loaded lipid-core nanocapsules (5 mg/kg, each 12 h, intraperitoneally), for 14 days. Aβ1-42-infused animals showed a significant impairment on learning memory ability, which was paralleled by a significant decrease in hippocampal synaptophysin levels. Furthermore, animals exhibited activated astrocytes and microglial cells, as well as disturbance in c-Jun N-terminal kinase (JNK) and glycogen synthase kinase-3β (GSK-3β) activation, beyond destabilization of β-catenin levels. Our results clearly show that by using lipid-core nanocapsules, resveratrol was able to rescue the deleterious effects of Aβ1-42 while treatment with RSV presented only partial beneficial effects. These findings might be explained by the robust increase of resveratrol concentration in the brain tissue achieved by lipid-core nanocapsules. Our data not only confirm the potential of resveratrol in treating AD but also offer an effective way to improve the efficiency of resveratrol through the use of nanodrug delivery systems.

α-bisabolol-loaded lipid-core nanocapsules reduce lipopolysaccharide-induced pulmonary inflammation in mice

“…The mechanisms of encapsulation and release of several drugs from nanoparticle-based systems have been extensively studied by our group. 25,[35][36][37][38] Here, the high α-bis loading capacity of LNCs was a consequence of its concomitant use as a core constituent and active ingredient, leading to an apparent solubility in water of ~10 mg mL −1 in the α-bis-LNCs.…”

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

“…34,152,162 Resveratrol has multiple health benefits, including antiaging, anticancer, cardioprotective, and PD protective effects. 66,68,145 Resveratrol exists in cis and trans forms, in which trans-resveratrol is more stable than cis-resveratrol which is pharmacologically less active.…”

“…9,11,60,66,[149][150][151] Nanosizing of phytobioactive compounds along with suitable protective agents enhances the bioavailability of the compound to the brain. 24,72,95,145,152 A few of the bioactive nanosize compounds with enhanced bioactivity and less toxicity are discussed in this section. Some of these nanobioactive compounds are listed in Table 1.…”

Amino Acid-PEGylated Resveratrol and Its Influence on Solubility and the Controlled Release Behavior

“…After stirring for another 30 min, the organic phase was separated, neutralized and washed with brine, dried by anhydrous sodium sulfate, filtered and condensed. The residue was recrystallized by ether to obtain PEG2000-carboxylmethyl active ester (10,16.71 g, 73.7%). Compound 10 (6 g, 2.6 mmol) was dissolved in 60 mL DMF and cooled to 0-5°C.…”

“…[1][2][3] RES has received much attention in recent years because of its various health functions and its potential for use in medicinal applications. 4,5) Many studies have demonstrated that RES has significant pharmacological activity 6) and potential to be a chemopreventive and therapeutic agent for cancers, [7][8][9] Alzheimer's disease, 10) cardiovascular disease, 11) hyperlipidemia, 12) ischemia disease and other diseases. 13) Recently, RES has seen widespread use as a food ingredient and nutraceutical supplement in bread, cake and beverage products.…”