Curcumin and Quercetin-Loaded Lipid Nanocarriers: Development of Omega-3 Mucoadhesive Nanoemulsions for Intranasal Administration

Abstract

Curcumin (CUR) and quercetin (QU) are potential compounds for treatment of brain diseases such as neurodegenerative diseases (ND) because of their anti-inflammatory and antioxidant properties. However, low water solubility and poor bioavailability hinder their clinical use. In this context, nanotechnology arises as a strategy to overcome biopharmaceutical issues. In this work, we develop, characterize, compare, and optimize three different omega-3 (ω-3) fatty acids nanoemulsions (NEs) loaded with CUR and QU (negative, cationic, gelling) prepared by two different methods for administration by intranasal route (IN). The results showed that formulations prepared with the two proposed methods exhibited good stability and were able to incorporate a similar amount of CUR and QU. On the other side, differences in size, zeta potential, in vitro release kinetics, and permeation/retention test were observed. Considering the two preparation methods tested, high-pressure homogenization (HPH) shows advantages, and the CQ NE- obtained demonstrated potential for sustained release. Toxicity studies demonstrated that the formulations were not toxic for Caenorhabditis elegans. The developed ω-3 fatty acid NEs have shown a range of interesting properties for the treatment of brain diseases, since they have the potential to increase the nose-to-brain permeation of CUR and QU, enabling enhanced treatments efficiency.

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

“…The objective of X-ray powder diffractometry (XRPD) was to identify the changes in the crystalline structure of the MLX raw material and the possible dilution effect due to the addition of different excipients such as lactose, Eudragit ® and Metolose ® incorporated into the formulation CNM. Meanwhile, the grazing incidence X-ray diffraction (GID) was to perform a better evaluation of the surface of the selected formulation (CNM) due to its adequate MLX release profile [ 38 ].…”

“…The diffractograms obtained from the raw materials (MLX, lactose, Metolose ® and Eudragit ® ) and the CNM formulation and its placebo make it possible to know if the samples are crystalline or amorphous. GID method has also been used, which consists in that the angle of incidence (θ) remains fixed while the detector moves normally around the axis of the goniometer [ 38 ]. GID is a surface-sensitive technique that, allows the characterization of epitaxial films with thicknesses down to a few atomic layers.…”

Quercetin nanoformulations: recent advancements and therapeutic applications

“…In a study, Mahadev et al formulated the quercetin nanoemulsion that displayed 87.04% entrapment efficiency, significant therapeutic activity for the management of body weight, glucose level, lipid level, and also had a protective effect on hepatocytes and pancreatic cells [36]. In another study, Vaz et al formulated the quercetin nanoemulsion which displayed 7.90 ± 0.24 zeta potential, >99% encapsulation efficiency, and also showed sustained drug release, increased permeation and therapeutic efficiency [37]. Rehman et al prepared the quercetin nanoemulsion using modified emulsification-solvent evaporation method.…”

Potential of Lipid-Based Nanocarriers against Two Major Barriers to Drug Delivery—Skin and Blood–Brain Barrier

“…The study claimed the stability and sustained release behavior of the system as described above for the efficient treatment of neurodegenerative brain diseases. Furthermore, the toxicity of the formulations was tested in an animal model, C. elegans , and the results demonstrated no toxicity for all tested formulations in varieties of concentrations [ 153 ].…”