Correlation between Biophysical Properties of Niosomes Elaborated with Chloroquine and Different Tensioactives and Their Transfection Efficiency

Pharmaceutics

Santiago Grijalvo¹  Ramón Eritja¹  Laura Lagartera²  Nuseibah AL Qtaish³  Gustavo Puras³  Ilia Villate-Beitia³  Myriam Sainz-Ramos³  Idoia Gallego³  José Luis Pedraz³  Margarita Menéndez⁴ 

[1] Biomedical Research Networking Centre in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Institute of Health Carlos III, Av. Monforte de Lemos 3–5, 28029 Madrid, Spain;Institute of Medicinal Chemistry (IQM-CSIC), Calle Juan de la Cierva 3, 28006 Madrid, Spain;Laboratory of Pharmacy and Pharmaceutical Technology, NanoBioCel Research Group, Faculty of Pharmacy, University of the Basque Country (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain;Rocasolano Physical Chemistry Institute, Superior Council of Scientific Investigations (IQFR-CSIC), Calle Serrano 119, 28006 Madrid, Spain;

关键词: chloroquine;    niosomes;    gene delivery;    biophysical properties;    surfactants;   

DOI  :  10.3390/pharmaceutics13111787

来源: DOAJ

【 摘 要 】

Lipid nanocarriers, such as niosomes, are considered attractive candidates for non-viral gene delivery due to their suitable biocompatibility and high versatility. In this work, we studied the influence of incorporating chloroquine in niosomes biophysical performance, as well as the effect of non-ionic surfactant composition and protocol of incorporation in their biophysical performance. An exhaustive comparative evaluation of three niosome formulations differing in these parameters was performed, which included the analysis of their thermal stability, rheological behavior, mean particle size, dispersity, zeta potential, morphology, membrane packing capacity, affinity to bind DNA, ability to release and protect the genetic material, buffering capacity and ability to escape from artificially synthesized lysosomes. Finally, in vitro biological studies were, also, performed in order to determine the compatibility of the formulations with biological systems, their transfection efficiency and transgene expression. Results revealed that the incorporation of chloroquine in niosome formulations improved their biophysical properties and the transfection efficiency, while the substitution of one of the non-ionic surfactants and the phase of addition resulted in less biophysical variations. Of note, the present work provides several biophysical parameters and characterization strategies that could be used as gold standard for gene therapy nanosystems evaluation.

【 授权许可】

Unknown