Dataset Information

Influence of drug loading on the physical stability of phospholipid-stabilised colloidal lipid emulsions.

ABSTRACT: When poorly water-soluble drugs are formulated in colloidal lipid emulsions, adequate stability of the emulsion must be ensured. The aim of this work was to investigate different aspects related to drug loading in order to gain a better understanding on how drugs affect the stability of phospholipid-stabilised emulsions. To obtain information on emulsion stability, a rapid and reproduceable shaking test was developed. A passive loading approach was applied for drug loading of the commercially available nanoemulsion Lipofundin® MCT/LCT 10% with seven drugs of different charge and localisation tendency within the emulsion system. Localisation of drug molecules in the droplet interface did not generally lead to destabilisation of the emulsion, whereas the charge of the drug was of decisive importance. Aspects such as the drug concentration, its influence on the pH and the impact of zeta potential changes had an influence on emulsion stability as well. Certain destabilising effects of drugs could be counteracted by modification of the pH. Lipofundin® MCT/LCT 10%, passively loaded with propofol, was compared with two commercially available propofol preparations. No negative effect of the passive loading procedure could be detected.

SUBMITTER: Francke NM

PROVIDER: S-EPMC7711285 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Influence of drug loading on the physical stability of phospholipid-stabilised colloidal lipid emulsions.

Francke Nadine Monika NM Bunjes Heike H

International journal of pharmaceutics: X 20201120

When poorly water-soluble drugs are formulated in colloidal lipid emulsions, adequate stability of the emulsion must be ensured. The aim of this work was to investigate different aspects related to drug loading in order to gain a better understanding on how drugs affect the stability of phospholipid-stabilised emulsions. To obtain information on emulsion stability, a rapid and reproduceable shaking test was developed. A passive loading approach was applied for drug loading of the commercially av ...[more]

PMID: 33305256

Similar Datasets

Project description:Cisplatin-complexed gold nanoparticles (PtII-AuNP) provide a promising strategy for chemo-radiation-based anticancer drugs. Effective design of such platforms necessitates reliable assessment of surface engineering on a quantitative basis and its influence on drug payload, stability, and release. In this paper, poly(ethylene glycol) (PEG)-stabilized PtII-AuNP was synthesized as a model antitumor drug platform, where PtII is attached via a carboxyl-terminated dendron ligand. Surface modification by PEG and its influence on drug loading, colloidal stability, and drug release were assessed. Complexation with PtII significantly degrades colloidal stability of the conjugate; however, PEGylation provides substantial improvement of stability in conjunction with an insignificant trade-off in drug loading capacity compared with the non-PEGylated control (<20% decrease in loading capacity). In this context, the effect of varying PEG concentration and molar mass was investigated. On a quantitative basis, the extent of PEGylation was characterized and its influence on dispersion stability and drug load was examined using electrospray differential mobility analysis (ES-DMA) hyphenated with inductively coupled plasma mass spectrometry (ICP-MS) and compared with attenuated total reflectance-FTIR. Using ES-DMA-ICP-MS, AuNP conjugates were size-classified based on their electrical mobility, while PtII loading was simultaneously quantified by determination of Pt mass. Colloidal stability was quantitatively evaluated in biologically relevant media. Finally, the pH-dependent PtII release performance was evaluated. We observed 9% and 16% PtII release at drug loadings of 0.5 and 1.9 PtII/nm2, respectively. The relative molar mass of PEG had no significant influence on PtII uptake or release performance, while PEGylation substantially improved the colloidal stability of the conjugate. Notably, the PtII release over 10 days (examined at 0.5 PtII/nm2 drug loading) remained constant for non-PEGylated, 1K-PEGylated, and 5K-PEGylated conjugates.

Dataset Information

Influence of drug loading on the physical stability of phospholipid-stabilised colloidal lipid emulsions.

Publications

Influence of drug loading on the physical stability of phospholipid-stabilised colloidal lipid emulsions.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets