Abstract
A large number of drugs are administered on different mucosal surfaces. However, due to the poor mucoadhesion of the current formulations, their bioavailability is often very low. The development of efficient mucoadhesive drug delivery systems is thus crucial for improving the performance of these drugs. The mucoadhesive properties of gold nanoparticles were investigated. First, two types of gold nanoparticles were synthesized: AuNP1 and AuNP2. AuNP1 only contain internal thiol groups on their metallic core, and AuNP2 contain both internal and peripheral thiol groups. Different protocols based on an adapted quantitative colorimetric method, UV-visible and fluorescence spectroscopies were then developed to gather information on their mucoadhesive properties. Moreover, a global correction factor for the inner filter effect in spectrofluorimetry was proposed, and the data obtained were compared to those commonly used in the literature. Mucins deeply interact with AuNP1, perturbing their core, whereas they remain at the periphery of AuNP2. The quantitative method suggests that a larger number of mucins interact with AuNP2. The establishment of this protocol could be applied to assess the mucoadhesive properties of other stable molecules. This mucoadhesive property of gold nanoparticles could be combined with their drug delivery ability in order to improve the medication administered on mucosa.
Highlights
Mucoadhesion is the ability to adhere to mucosal tissues, such as oral, buccal, nasal, vaginal and ocular mucosa
The Brust synthesis method is based on the use of thiolated ligands, allowing a rapid and strong stabilization of the gold core by thiol groups[34]
The AuNP synthesized using a modified Brust method do not require the use of tetraoctylammonium bromide (TOAB), an ionic stabilizing/phase transfer agent, as their synthesis is performed in water where both gold salt (HAuCl4) and polyethylene glycol (PEG) are soluble
Summary
Mucoadhesion is the ability to adhere to mucosal tissues, such as oral, buccal, nasal, vaginal and ocular mucosa (for reviews, see[1,2,3,4,5]). Mucoadhesive systems can be used to increase the retention time of drugs near the mucosa and improve their efficacy[6]. The development of efficient mucoadhesive drug delivery systems is a crucial area to improve the bioavailability and therapeutic performance of these drugs. Interactions between thiol groups and mucins suggest that functionalized gold nanoparticles (AuNP) could be mucoadhesive due to the multiple thiol groups present on their metallic surface. Thiol groups stabilizing the gold core could interact with mucins and improve their mucoadhesive properties. The thiol groups of mucins could interact directly with the gold core to form gold-sulfur bonds (Au-S). Different types of AuNP have been developed to treat cancerous tumors by thermal phototherapy[30]. A global formalism was described for the inner filter effect, allowing the correction of the re-absorption of the light by AuNP during fluorescence measurements
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