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

• Published in: Colloids and surfaces, B, Biointerfaces Vol. 140; pp. 74 - 82
• Main Authors: Chen, Yiyin, Minh, Le Van, Liu, Jianwen, Angelov, Borislav, Drechsler, Markus, Garamus, Vasil M., Willumeit-Römer, Regine, Zou, Aihua
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-04-2016
• Subjects: Anti-Inflammatory Agents, Non-Steroidal - chemistry; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Baicalin; Bioavailability; Carriers; Cell Survival - drug effects; Cellular; Cryo-TEM; Cryoelectron Microscopy; Drug Liberation; Drug Stability; Drugs; Female; Flavonoids - chemistry; Flavonoids - pharmacokinetics; Flavonoids - pharmacology; Folate receptor; Folate Receptors, GPI-Anchored - antagonists & inhibitors; Folate Receptors, GPI-Anchored - metabolism; Folic Acid - analogs & derivatives; Folic Acid - chemistry; HeLa Cells; Humans; In vitro testing; Liposomes; Liposomes - chemistry; Liposomes - ultrastructure; Microscopy, Confocal; Microscopy, Electron, Transmission; Morphology; Polyethylene Glycols - chemistry; SAXS; Scattering, Small Angle; Stability; Targeting drug delivery; Uterine Cervical Neoplasms - metabolism; Uterine Cervical Neoplasms - pathology; X-Ray Diffraction; Folate receptor; Liposomes; Targeting drug delivery; Cryo-TEM; Baicalin; SAXS
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2015.11.018

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).
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•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 80nm in diameter with proper zeta potentials about −25mV 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.