Pharmaceutical Sciences and Health Technologies 4.
Dr. Budavári, Bálint
OUC5ML
Semmelweis University, Department of Biophysics and Radiation Biology
+36309562776
budavari.balint.peter@semmelweis.hu
Development of corticosteroid-loaded liposomes for inhalation
Bálint Budavári1, Krsiztina S. Nagy1, Angéla Jedlovszky-Hajdú1
1: Semmelweis University, Department of Biophysics and Radiation Biology
Szóbeli
Pharmaceutical Sciences and Health Technologies 4.
English
Pharmaceutical Sciences and Health Technologies
Introduction
Liposomes are nanoscale drug-carrier systems capable of incorporating both hydrophilic and hydrophobic molecules. They can be characterised by size and lamellarity, such as multilamellar vesicles (MLVs) or small unilamellar vesicles (SUVs). In the current market, liposomal drugs focus either on intravenous or per os administration. Our main goal was to develop a liposomal drug for potential inhalation use.
Aims
Our goal was to create corticosteroid-loaded liposomes with long shelf-life and high entrapment efficiency that can be internalised by cells, representing the potential future target area in the human body. Furthermore, we optimised the freeze-drying process and characterised the basic physical and chemical properties of the vesicles, such as size distribution, cytotoxicity, and potential chemical interactions between their compounds.
Methods
The liposomes were prepared by thin-layer hydration followed by extrusion to obtain SUVs. Their size distribution was measured by dynamic light scattering to determine their stability. We have also determined the entrapment efficiency (EE%) by size-exclusion gel chromatography and the effect on cell viability on the EBC-1 cell line. Different disaccharides were used in a wide range of mass ratios to optimise the freeze-drying process. Potential chemical interactions were assessed by infrared spectroscopy.
Results
SUVs with a diameter of 100 nm were synthesised from a DPPC-DMPC-DSPC mixture combined with prednisolone (Pred) or budesonide (Bud). They were stable for 6 months in PBS solution, and the EE% was above 70% for Pred and 86% for Bud. Neither sample was cytotoxic to the EBC-1 human lung carcinoma cell line during the 72-hour observation period. The ideal settings for freeze drying are: 10 m/m% Bud and a 1:15 lipid-to-trehalose mass ratio. No chemical interactions happened between the components.
Conclusion
We could successfully prepare corticosteroid-loaded liposomes with high stability and EE% for potential therapy in asthma or COPD. The liposomes were not cytotoxic, and no chemical interactions disturbed the process. We could also successfully freeze-dry the samples for optimised storage, transportation and application.
Funding
TKP2021-EGA-24
NKFIH FK 137749
EFOP-3.6.3-VEKOP-16-2017-00009
Semmelweis University
Krisztina S. Nagy, PhD
I do not give consent to the publication of my abstract on the website of the congress.
after finishing doctoral studies with absolutorium (PhD)
Szabad
elfogadva
szóbeli
nem rendelkezett róla
6089
16:00
16:10