Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

Rassu, Giovanna; Sorrenti, Milena; Catenacci, Laura; Pavan, Barbara; Ferraro, Luca; Gavini, Elisabetta; Bonferoni, Maria Cristina; Giunchedi, Paolo; Dalpiaz, Alessandro

doi:10.3390/pharmaceutics13081180

Cited by 26 publications

(10 citation statements)

References 102 publications

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“…Cytotoxicity measurement revealed that the noncytotoxic concentrations are 1.03 mg/mL HPβCD_MEL-P_PVA_spd and 0.38 mg/mL αCD_MEL-P_PVA_spd. These results corresponded to the literature data, where a higher tolerable concentration was detected for HPβCD than αCD [46]. LPS was not cytotoxic to the cells.…”

Section: In Vitro Cytotoxicity and Il-6 Cox-2 Il-1b Expressionsupporting

confidence: 92%

Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

et al. 2021

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Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The application of mucoadhesive polymers can increase the contact time with the nasal mucosa, and permeation enhancers can enhance the absorption of the drug. We aimed to produce nanoparticles containing meloxicam potassium (MEL-P) by spray drying intended for nasal application. Various cyclodextrins (hydroxypropyl-β-cyclodextrin, α-cyclodextrin) and biocompatible polymers (hyaluronic acid, poly(vinylalcohol)) were used as excipients to increase the permeation of the drug and to prepare mucoadhesive products. Physico-chemical, in vitro and ex vivo biopharmaceutical characterization of the formulations were performed. As a result of spray drying, mucoadhesive nanospheres (average particle size <1 µm) were prepared which contained amorphous MEL-P. Cyclodextrin-MEL-P complexes were formed and the applied excipients increased the in vitro and ex vivo permeability of MEL-P. The highest amount of MEL-P permeated from the α-cyclodextrin-based poly(vinylalcohol)-containing samples in vitro (209 μg/cm2) and ex vivo (1.47 μg/mm2) as well. After further optimization, the resulting formulations may be promising for eliciting a rapid analgesic effect through the nasal route.

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Section: In Vitro Cytotoxicity and Il-6 Cox-2 Il-1b Expressionsupporting

confidence: 92%

Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

et al. 2021

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“…The formation of inclusion complexes with organic molecules, which can be included wholly or partially in the hydrophobic cavity, is favored by this conformation. CD complexation can be exploited, primarily to enhance the guest's solubility but also to ameliorate other properties of the drug such as chemical stability, to prevent adverse side effects (e.g., gastrointestinal irritation), to mask unpleasant odors and flavors, and to prevent drug interactions with other components of the formulation (e.g., drug, active molecule and excipients) [18,19].…”

Section: Introductionmentioning

confidence: 99%

Native Cyclodextrins as Complexation Agents for Pterostilbene: Complex Preparation and Characterization in Solution and in the Solid State

et al. 2021

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Pterostilbene (3,5-dimethoxy-4′-hydroxystilbene, PTB) is a natural dietary stilbene, occurring primarily in blueberries and Pterocarpus marsupium heartwood. The interest in this compound is related to its different biological and pharmacological properties, such as its antioxidant, anti-inflammatory, and anticarcinogenic activities and its capacity to reduce and regulate cholesterol and blood sugar levels. Nevertheless, its use in therapy is hindered by its low aqueous solubility; to overcome this limitation we studied the feasibility of the use of cyclodextrins (CDs) as solubility-enhancing agents. CDs are natural macrocyclic oligomers composed of α-d-glucose units linked by α-1,4 glycosidic bonds to form torus-shaped molecules, responsible for inclusion complex formation with organic molecules. In particular, the aim of this study was to evaluate the feasibility of complexation between PTB and native CDs using various preparative methods. The isolated solid products were characterized using differential scanning calorimetry (DSC), simultaneous thermogravimetric/DSC analysis (TGA/DSC), Fourier transform infrared (FT-IR) spectroscopy, and X-ray diffraction (XRD) on powder and single crystals. The results indicated little or no evidence of the affinity of PTB to complex with α-CD using the kneading method. However, with β-CD and γ-CD thermal analysis revealed an interaction which was also corroborated by FT-IR and 1H-NMR spectroscopy. With β-CD, a hydrated complex of PTB was isolated and its characterization by single-crystal XRD revealed, for the first time, the mode of inclusion of the PTB molecule in the cavity of a CD. To complement the solid-state data, liquid-phase studies were carried out to establish the effect of CDs on the aqueous solubility of PTB and to determine the complex stoichiometries and the association constants for complex formation. Phase-solubility studies showed AL-type profiles for α- and β-CD and a BS profile for γ-CD, with K1:1 values of 1144, 4950, and 133 M−1 for α-CD·PTB, β-CD·PTB, and γ-CD·PTB, respectively. The stoichiometry of CD·PTB complexes, determined by Job’s method, revealed for each system a 1:1 molar ratio. The dissolution rate of PTB was approximately doubled just by employing simple physical mixtures, but the best performance was achieved by products obtained via kneading and co-precipitation, which effected the complete dissolution of PTB in 40 and 20 min for β-CD and γ-CD, respectively.

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“…Cyclodextrins are cyclic compounds composed of D-glucose molecules connected by 1,4-glycosidic bonds; they are water-soluble, non-reducing, molecules that take the form of a white crystalline powder ( Rassu et al, 2021 ). Commonly used α-, β-, and γ-cyclodextrins are composed of six, seven, and eight glucose molecules, respectively ( Papakyriakopoulou et al, 2021 ).…”

Section: Methods To Improve Brain-targeted Nasal Mucosal Drug Deliver...mentioning

confidence: 99%

Research progress in brain-targeted nasal drug delivery

Huang,

Chen,

et al. 2024

Front. Aging Neurosci.

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The unique anatomical and physiological connections between the nasal cavity and brain provide a pathway for bypassing the blood–brain barrier to allow for direct brain-targeted drug delivery through nasal administration. There are several advantages of nasal administration compared with other routes; for example, the first-pass effect that leads to the metabolism of orally administered drugs can be bypassed, and the poor compliance associated with injections can be minimized. Nasal administration can also help maximize brain-targeted drug delivery, allowing for high pharmacological activity at lower drug dosages, thereby minimizing the likelihood of adverse effects and providing a highly promising drug delivery pathway for the treatment of central nervous system diseases. The aim of this review article was to briefly describe the physiological structures of the nasal cavity and brain, the pathways through which drugs can enter the brain through the nose, the factors affecting brain-targeted nasal drug delivery, methods to improve brain-targeted nasal drug delivery systems through the application of related biomaterials, common experimental methods used in intranasal drug delivery research, and the current limitations of such approaches, providing a solid foundation for further in-depth research on intranasal brain-targeted drug delivery systems (see Graphical Abstract).

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Versatile Nasal Application of Cyclodextrins: Excipients and/or Actives?

Cited by 26 publications

References 102 publications

Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

Native Cyclodextrins as Complexation Agents for Pterostilbene: Complex Preparation and Characterization in Solution and in the Solid State

Research progress in brain-targeted nasal drug delivery

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