Quality by Design-Driven Zeta Potential Optimisation Study of Liposomes with Charge Imparting Membrane Additives.

Autor: Németh Z; Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6, Eötvös Street, H-6720 Szeged, Hungary., Csóka I; Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6, Eötvös Street, H-6720 Szeged, Hungary., Semnani Jazani R; Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6, Eötvös Street, H-6720 Szeged, Hungary., Sipos B; Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6, Eötvös Street, H-6720 Szeged, Hungary., Haspel H; Department of Applied and Environmental Chemistry, Faculty of Science and Informatics, Institute of Chemistry, University of Szeged, 1, Rerrich Béla Sqare, H-6720 Szeged, Hungary., Kozma G; Department of Applied and Environmental Chemistry, Faculty of Science and Informatics, Institute of Chemistry, University of Szeged, 1, Rerrich Béla Sqare, H-6720 Szeged, Hungary., Kónya Z; Department of Applied and Environmental Chemistry, Faculty of Science and Informatics, Institute of Chemistry, University of Szeged, 1, Rerrich Béla Sqare, H-6720 Szeged, Hungary., Dobó DG; Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, 6, Eötvös Street, H-6720 Szeged, Hungary.
Jazyk: angličtina
Zdroj: Pharmaceutics [Pharmaceutics] 2022 Aug 26; Vol. 14 (9). Date of Electronic Publication: 2022 Aug 26.
DOI: 10.3390/pharmaceutics14091798
Abstrakt: Liposomal formulations, as versatile nanocarrier systems suitable for targeted delivery, have a highly focused role in the therapy development of unmet clinical needs and diagnostic imaging techniques. Formulating nanomedicine with suitable zeta potential is an essential but challenging task. Formulations with a minimum ±30 mV zeta potential are considered stable. The charge of the phospholipid bilayer can be adjusted with membrane additives. The present Quality by Design-derived study aimed to optimise liposomal formulations prepared via the thin-film hydration technique by applying stearylamine (SA) or dicetyl phosphate (DCP) as charge imparting agents. This 3 2 fractional factorial design-based study determined phosphatidylcholine, cholesterol, and SA/DCP molar ratios for liposomes with characteristics meeting the formulation requirements. The polynomials describing the effects on the zeta potential were calculated. The optimal molar ratios of the lipids were given as 12.0:5.0:5.0 for the SA-PBS pH 5.6 (optimised sample containing stearylamine) and 8.5:4.5:6.5 for the DCP-PBS pH 5.6 (optimised sample containing dicetyl phosphate) particles hydrated with phosphate-buffered saline pH 5.6. The SA-PBS pH 5.6 liposomes had a vesicle size of 108 ± 15 nm, 0.20 ± 0.04 polydispersity index, and +30.1 ± 1.2 mV zeta potential, while these values were given as 88 ± 14 nm, 0.21 ± 0.02, and -36.7 ± 3.3 mV for the DCP-PBS pH 5.6 vesicles. The prepared liposomes acquired the requirements of the zeta potential for stable formulations.
Databáze: MEDLINE
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