Chitosan/Cyclodextrin Nanospheres for Potential Nose-to-Brain Targeting of Idebenone

Gaetano, Federica De; d’Avanzo, Nicola; Mancuso, Antonia; Gaetano, Anna De; Paladini, Giuseppe; Caridi, F.; Venuti, Valentina; Paolino, Donatella; Ventura, Cinzia Anna

doi:10.3390/ph15101206

Cited by 16 publications

(13 citation statements)

References 71 publications

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“…Native β-CyD and sulfobutylether-β-CyD (SBE-β-CyD) effectively include the bioflavonoid, coumestrol, enhancing its water solubility [ 25 , 26 ] and potentially improving its antioxidant and anti-inflammatory activity. Recently, the important role played by drug/CyD inclusion complexes was demonstrated, in terms of improving the encapsulation parameters and release rate of hydrophilic and hydrophobic drugs from polymeric nanoparticles [ 27 , 28 ], as well as the ability of these macrocycles to self-assemble into nanoaggregates, improving the water solubility of drugs and potentiating their therapeutic efficacy [ 29 , 30 ].…”

Section: Introductionmentioning

confidence: 99%

Bicalutamide Anticancer Activity Enhancement by Formulation of Soluble Inclusion Complexes with Cyclodextrins

et al. 2022

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Bicalutamide (BCL) is a nonsteroidal antiandrogen drug that represents an alternative to castration in the treatment of prostate cancer, due to its relatively long half-life and tolerable side effects. However, it possesses a very low water solubility that can affect its oral bioavailability. In this work, we developed inclusion complexes of BCL with the highly soluble hydroxypropyl-β-cyclodextrin (HP-β-CyD) and sulfobutylether-β-cyclodextrin (SBE-β-CyD) to increase the water solubility and anticancer activity of BCL. The inclusion complexes were prepared using the freeze-drying method and were then characterized in a solid state via differential scanning calorimetry and X-ray analysis and in solution via phase-solubility studies and UV-vis and NMR spectroscopy. The BCL/HP-β-CyD and BCL/SBE-β-CyD inclusion complexes were amorphous and rapidly dissolved in water. Both the 1H-NMR spectra and molecular modeling studies confirmed the penetration of the 2-(trifluoromethyl)benzonitrile ring of BCL within the cavity of both cyclodextrins (CyDs). Due to the consistent improvement of the water solubility of BCL, the inclusion complexes showed higher antiproliferative activity toward the human prostate androgen-independent cell lines, DU-145 and PC-3, with respect to free BCL. These results demonstrate the ability of HP-β-CyD and SBE-β-CyD to complex BCL, permitting the realization of liquid formulations with potentially high oral bioavailability and/or possible parenteral administration.

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Section: Introductionmentioning

confidence: 99%

Bicalutamide Anticancer Activity Enhancement by Formulation of Soluble Inclusion Complexes with Cyclodextrins

et al. 2022

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“…In vitro study results displayed significant antibacterial activity against both gram-positive and gram-negative bacteria thus demonstrating it as a useful system for treating ocular infections [113]. In another study, CD-based chitosan nanospheres (CS NPs) were developed and evaluated as a potential carrier for nose-to-brain targeting of idebenone [114].…”

Section: Cyclodextrin-linked Chitosanmentioning

confidence: 99%

“…treating ocular infections [113]. In another study, CD-based chitosan nanospheres (CS NPs) were developed and evaluated as a potential carrier for nose-to-brain targeting of idebenone [114].…”

Section: Applications Of Chitosanmentioning

confidence: 99%

Chitosan: A Potential Biopolymer in Drug Delivery and Biomedical Applications

et al. 2023

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Chitosan, a biocompatible and biodegradable polysaccharide derived from chitin, has surfaced as a material of promise for drug delivery and biomedical applications. Different chitin and chitosan extraction techniques can produce materials with unique properties, which can be further modified to enhance their bioactivities. Chitosan-based drug delivery systems have been developed for various routes of administration, including oral, ophthalmic, transdermal, nasal, and vaginal, allowing for targeted and sustained release of drugs. Additionally, chitosan has been used in numerous biomedical applications, such as bone regeneration, cartilage tissue regeneration, cardiac tissue regeneration, corneal regeneration, periodontal tissue regeneration, and wound healing. Moreover, chitosan has also been utilized in gene delivery, bioimaging, vaccination, and cosmeceutical applications. Modified chitosan derivatives have been developed to improve their biocompatibility and enhance their properties, resulting in innovative materials with promising potentials in various biomedical applications. This article summarizes the recent findings on chitosan and its application in drug delivery and biomedical science.

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“…Other strategies are needed, and among them, intranasal administration can represent a valid alternative to other administration routes to improve brain biodistribution [ 18 ]. The intranasal administration of drugs permits the targeting of the brain by means of olfactory and trigeminal pathways, avoiding first-pass metabolism and improving drug effectiveness [ 19 , 20 , 21 ]. However, a particulate delivery system with mucoadhesive properties is needed to avoid the fast mucociliary clearance that characterizes the application on nose mucosa [ 22 ].…”

Section: Introductionmentioning

confidence: 99%

Amphiphilic Cyclodextrin Nanoparticles as Delivery System for Idebenone: A Preformulation Study

et al. 2023

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Idebenone (IDE), a synthetic short-chain analogue of coenzyme Q10, is a potent antioxidant able to prevent lipid peroxidation and stimulate nerve growth factor. Due to these properties, IDE could potentially be active towards cerebral disorders, but its poor water solubility limits its clinical application. Octanoyl-β-cyclodextrin is an amphiphilic cyclodextrin (ACyD8) bearing, on average, ten octanoyl substituents able to self-assemble in aqueous solutions, forming various typologies of supramolecular nanoassemblies. Here, we developed nanoparticles based on ACyD8 (ACyD8-NPs) for the potential intranasal administration of IDE to treat neurological disorders, such as Alzheimer’s Disease. Nanoparticles were prepared using the nanoprecipitation method and were characterized for their size, zeta potential and morphology. STEM images showed spherical particles, with smooth surfaces and sizes of about 100 nm, suitable for the proposed therapeutical aim. The ACyD8-NPs effectively loaded IDE, showing a high encapsulation efficiency and drug loading percentage. To evaluate the host/guest interaction, UV-vis titration, mono- and two-dimensional NMR analyses, and molecular modeling studies were performed. IDE showed a high affinity for the ACyD8 cavity, forming a 1:1 inclusion complex with a high association constant. A biphasic and sustained release of IDE was observed from the ACyD8-NPs, and, after a burst effect of about 40%, the release was prolonged over 10 days. In vitro studies confirmed the lack of toxicity of the IDE/ACyD8-NPs on neuronal SH-SY5Y cells, and they demonstrated their antioxidant effect upon H2O2 exposure, as a general source of ROS.

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Chitosan/Cyclodextrin Nanospheres for Potential Nose-to-Brain Targeting of Idebenone

Cited by 16 publications

References 71 publications

Bicalutamide Anticancer Activity Enhancement by Formulation of Soluble Inclusion Complexes with Cyclodextrins

Bicalutamide Anticancer Activity Enhancement by Formulation of Soluble Inclusion Complexes with Cyclodextrins

Chitosan: A Potential Biopolymer in Drug Delivery and Biomedical Applications

Amphiphilic Cyclodextrin Nanoparticles as Delivery System for Idebenone: A Preformulation Study

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