The Role of Amphiphilic Compounds in Nasal Nanoparticles

Abstract

Nasal medications hold significant importance and are widely utilized due to their numerous advantageous properties, offering a compelling route for both local and systemic therapeutic effects. Nowadays, the development of nasal particles under 1 micrometer is in the focus of much scientific research. In our experiments, the use of innovative nanotechnology to increase the effectiveness of the active substance was of paramount importance. Our aim was to create solid nanoparticles that enable targeted and effective delivery of the active ingredient into the body.

The innovation of this experimental series lies not only in highlighting the importance of amphiphilic compounds in enhancing penetration, but also in the fact that while most nasally administered formulations are in liquid form, our formulation is solid. Liquid formulations frequently suffer from the disadvantage of possible leakage during administration, which can reduce the bioavailability of the active ingredient. In our experiments we created novel drug delivery systems of finely divided powders, which, thanks to the penetration enhancers, can be successfully administered. These enhancers facilitate the swift disintegration and penetration of the particles through the membrane. This represents a new direction in nasal drug delivery methods.

The results of our trials are promising in the development of innovative pharmaceutical products and outline the role of amphiphilic compounds in more efficient utilization and targeted application of active substances. According to our results it can be concluded that this innovative approach not only addresses the common issues associated with liquid nasal formulations but also paves the way for more stable and effective delivery methods. The use of finely divided powders for nasal delivery, enabled by penetration enhancers, represents a major breakthrough in the field, providing a dependable alternative to conventional liquid formulations and ensuring improved therapeutic results.

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Materials

Chlorpromazine (CPZ), Kolliphor RH 40, Poloxamer 470, polyvinyl alcohol (PVA), Hexane and bovine serum albu-min were obtained from Sigma-Aldrich (St. Louis, MI,USA). 2-hydroxylpropyl-β-cyclodextrin (HPBCD) was purchased from Cyclolab (Budapest, Hungary). Transcultol HP, and Labrasol were kind gifts from Gattefossé (Lyon,France). The human nasal epithelial cell line (RPMI 2650) and the human colon adenocarcinoma Caco-2 cell linewere sourced from the American Type Culture Collec-tion (ATCC, Manassas, Virginia, USA). The MTT paint,3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bro-mide, along with buffer solutions such as Hank’s BalancedSalt Solution (HBSS) and phosphate-buffered saline (PBS),were procured from Sigma-Aldrich (St. Louis, MI, USA).The RPMI and Caco-2 cell culture maintenance medium,TrypLE™ Express Enzyme, was supplied by Thermo FisherScientific (Waltham, MA, USA). Ninety-six-well cell platesand culture flasks were acquired from VWR International(Debrecen, Hungary).

Quoc, T.T., Bíró, K., Pető, Á. et al. The Role of Amphiphilic Compounds in Nasal Nanoparticles. AAPS PharmSciTech 25, 269 (2024). https://doi.org/10.1208/s12249-024-03000-8

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