Baicalin loaded in folate-PEG modified liposomes for enhanced stability and tumor targeting

• Stable baicalin-loaded folate-receptor-targeted liposomes were designed and prepared.
• DLS, cryo-TEM and SAXS were used to study the physicochemical properties.
• The drug loading of BAI in the liposomes was about 9.5%.
• Baicalin loaded FR-targeted liposomes showed higher cytotoxicity and cell uptake compared with non-targeted liposomes.

Bioavailability of baicalin (BAI), an example of traditional Chinese medicine, has been modified by loading into liposome. Several liposome systems of different composition i.e., lipid/cholesterol (L), long-circulating stealth liposome (L-PEG) and folate receptor (FR)—targeted liposome (L-FA) have been used as the drug carrier for BAI. The obtained liposomes were around 80 nm in diameter with proper zeta potentials about −25 mV and sufficient physical stability in 3 months. The entrapment efficiency and loading efficiency of BAI in the liposomes were 41.0–46.4% and 8.8–10.0%, respectively. The morphology details of BAI lipsosome systems i.e., formation of small unilamellar vesicles, have been determined by cryogenic transmission electron microscopy (cryo-TEM) and small angle X-ray scattering (SAXS). In vitro cytotoxicity of BAI liposomes against HeLa cells was evaluated by MTT assay. BAI loaded FR-targeted liposomes showed higher cytotoxicity and cellular uptake compared with non-targeted liposomes. The results suggested that L-FA-BAI could enhance anti-tumor efficiency and should be an effective FR-targeted carrier system for BAI delivery.

Cyro-TEM image (left) of baicalin loaded folate-receptor targeted liposomes; uptake of fluorescent non-targeted liposomes and fluorescent folate-receptor targeted liposomes by HeLa cells (right).Figure optionsDownload as PowerPoint slide