Optimization of PEGylated nanoemulsions for improved pharmacokinetics of BCS class II compounds

Drug Delivery
Harikrishna DevalapallySvitlana Silchenko

Abstract

The objective of the study was the optimization of nanoemulsion formulations to prevent their rapid systemic clearance after intravenous administration. An amphiphilic PEG derivative DSPE-PEG (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(polyethylene glycol) with different chain lengths and concentration was used as a nanoemulsion droplet surface modifier. The danazol loading in all nanoemulsions was kept on the same level of ∼2 mg/mL. In the present investigation, PEGylated and non-PEGylated nanoemulsions were compared in vitro phagocytosis by incubating with lung macrophages and in vivo after intravenous administration in rats. Danazol-containing nanoemulsions (NE) modified with various PEG chain lengths (2000-10 000) and concentrations (3-12 mg/mL) were prepared and characterized. Nanoemulsion droplets were reproducibly obtained in the size range of 213-340 nm. The non-PEGylated NE had the surface charge of -25.4 mV. This absolute charge value decreased with increasing chain length and concentration. With increase in chain length and density the macrophage uptake decreased which could be due to decrease in surface charge and hydrophilicity of droplets. The greatest shielding of the NE droplets was reached w...Continue Reading

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Citations

Jan 19, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·René HolmPeter Westh
Nov 7, 2016·Regulatory Toxicology and Pharmacology : RTP·Bapi GorainTapan Kumar Pal
Aug 8, 2021·International Journal of Molecular Sciences·Jelena B ĐokovićSnežana D Savić
Feb 14, 2019·Langmuir : the ACS Journal of Surfaces and Colloids·Amanda L MartinNaomi Matsuura

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