Investigation of the Absorption of Nanosized lamotrigine Containing Nasal Powder via the Nasal Cavity

Ambrus, Rita; Gieszinger, Péter; Gáspár, Róbert; Sztojkov‐Ivanov, Anita; Ducza, Eszter; Márki, Árpád; Janáky, Tamás; Tömösi, Ferenc; Kecskeméti, Gábor; Szabó‐Révész, Piroska; Bartos, Csilla

doi:10.3390/molecules25051065

Cited by 12 publications

(6 citation statements)

References 45 publications

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“…Nasal administration offers a non-invasive pathway to delivery drugs for treating both local and systemic diseases, with several advantages of bypassing the blood-brain barrier, avoiding hepatic first-pass elimination, and reducing side effects [ 1 , 2 , 3 ]. Particularly aiming at central nervous system (CNS) diseases, including schizophrenia, migraines, Parkinson’s, etc., intranasal drug delivery via the olfactory and trigeminal routes directly to the brain is capable of providing much more effective drug concentration at lower doses and reduced risk for adverse reactions [ 4 , 5 , 6 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

Spray Dried Levodopa-Doped Powder Potentially for Intranasal Delivery

Liu

Shen

et al. 2022

Pharmaceutics

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This work was aimed to develop levodopa (L-dopa) nasal powder to achieve controllable drug release and high nasal deposition efficiency. A series of uniform microparticles, composed of amorphous L-dopa and excipients of hydroxypropyl methyl cellulose (HPMC), polyvinylpyrrolidone (PVP), or hydroxypropyl-β-cyclodextrin (CD), were fabricated by a self-designed micro-fluidic spray dryer. The effects of excipient type and drug/excipient mass ratio on the particle size, morphology, density, and crystal property, as well as the in vitro performance of drug release, mucoadhesion, and nasal deposition, were investigated. Increased amounts of added excipient, regardless of its type, could accelerate the L-dopa release to different extent. The addition of CD showed the most obvious effect, i.e., ~83% of L-dopa released in 60 min for SD-L1CD2, compared to 37% for raw L-dopa. HPMC could more apparently improve the particle mucoadhesion than PVP and CD, with respective adhesive forces of ~269, 111, and 26 nN for SD-L1H2, -L1P2, and -L1CD2. Nevertheless, the deposition fractions in the olfactory region for such samples were almost the same (~14%), probably ascribable to their quite similar particle aerodynamic diameter (~30 μm). This work demonstrates a feasible methodology for the development of nasal powder.

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Section: Introductionmentioning

confidence: 99%

Spray Dried Levodopa-Doped Powder Potentially for Intranasal Delivery

Liu

Shen

et al. 2022

Pharmaceutics

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“…Furthermore, the usage of mucoadhesive additives allows the delivery of nanosized drugs intranasally to overcome the limitations of the particle size requirements for nasal formulations. Based on our previous experience, it can be concluded that the bioavailability of an active pharmaceutical ingredient is increased by decreasing its particle size [18,19].…”

Section: Introductionmentioning

confidence: 99%

Comparison of Modern In Vitro Permeability Methods with the Aim of Investigation Nasal Dosage Forms

et al. 2021

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Nowadays, the intranasal route has become a reliable alternative route for drug administration to the systemic circulation or central nervous system. However, there are no official in vitro diffusion and dissolution tests especially for the investigation of nasal formulations. Our main goal was to study and compare a well-known and a lesser-known in vitro permeability investigation method, in order to ascertain which was suitable for the determination of drug permeability through the nasal mucosa from different formulations. The vertical diffusion cell (Franz cell) was compared with the horizontal diffusion model (Side-Bi-Side). Raw and nanonized meloxicam containing nasal dosage forms (spray, gel and powder) were tested and compared. It was found that the Side-Bi-Side cell was suitable for the investigation of spray and powder forms. In contrast, the gel was not measurable on the Side-Bi-Side cell; due to its high viscosity, a uniform distribution of the active substance could not be ensured in the donor phase. The Franz cell, designed for the analysis of semi-solid formulations, was desirable for the investigation of nasal gels. It can be concluded that the application of a horizontal cell is recommended for liquid and solid nasal preparations, while the vertical one should be used for semi-solid formulations.

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“…In particular, drug transport to brain across the nasal epithelium could be further improved by using nasal powders (Ambrus et al, 2020;Rassu et al, 2018;Tanaka et al, 2016). The solid particle dissolution and drug release in the fluid lining the nasal epithelium sustain the drug passive diffusion rate, owing to the saturation concentration in contact with the tissue (Colombo et al, 2016;Giuliani et al, 2018;Pozzoli et al, 2017).…”

Section: Introductionmentioning

confidence: 99%