Pharmaceutical Sciences and Health Technologies II.
Dr. Budavári, Bálint
OUC5ML
Department of Biophysics and Radiation Biology
+36309562776
budavari.balint.peter@semmelweis.hu
Development of liposomal corticosteroids
Bálint Budavári1, Dr. S. Nagy Krisztina1, Dr. Jedlovszky-Hajdú Angéla1
1: Department of Biophysics and Radiation Biology
Szóbeli
Pharmaceutical Sciences and Health Technologies II.
English
Pharmaceutical Sciences and Health Technologies
Introduction: Liposomes offer many advantages as nanoscale drug delivery systems regarding several pharmaceutical aspects. Since corticosteroids are lipophilic, they integrate into the lipid bilayer. This novel approach can improve the efficacy of several anti-inflammatory therapies.
Aims: Our goals were to create liposomes with long-term stability and the capability of transporting and releasing corticosteroids at inflamed body temperature. Considering the possible future application in asthma therapy, we also aimed at reaching high entrapment efficacy and slight drug leakage of the vesicles.
Methods: Liposome samples with two compositions were prepared from 3 different types of phospholipids in combination with Prednisolone (Pred) and budesonide (Bud) by the commonly used thin layer hydration method followed by extrusion to get small unilamellar vesicles (SUVs). Dynamic light scattering was applied for stability tests regularly and size-exclusion gel chromatography for the determination of drug entrapment efficacy. The effect of liposomal drugs on cell viability was assessed on the EBC-1 human lung carcinoma cell line. The combination of flow cytometry and fluorescence microscopy was applied to study the internalization of liposomes.
Results: SUVs with 100-120 nm in hydrodynamic diameter were successfully prepared. Their size-distribution has remained in the desired range through several months regarding most of the samples. In terms of stability, the presence of the corticosteroids was found to be more important than their type. The entrapment efficiency was between 70-85% and the drug leakage was 35-40 % for Pred and 6-8 % for Bud in the first 30 min. Neither the free corticosteroids nor their liposomal form affected significantly the cell viability. Both the microscopy images and flow cytometry results proved the internalization of the vesicles by the cells.
Conclusion: We have successfully created corticosteroid-loaded liposomes with long-term stability (6 months) and excellent entrapment efficiency due to the lipophilic character of the applied drugs. Furthermore, these liposomes are not toxic and can be internalized by the investigated pulmonary cells.
Funding:
Semmelweis 250+ Excellence PhD Scholarship, EFOP-3.6.3-VEKOP-16-2017-00009, NKFI FK 137749, TKP2021-EGA-23
Semmelweis University
Dr. Simonné Dr. Nagy Krisztina
I do not give consent to the publication of my abstract on the website of the congress.
Szabad
elfogadva
szóbeli
nem rendelkezett róla
6089
09:45
09:55