Targeted regulation of macrophage polarization by RGD/PS co-modified liposomes loaded with cryptotanshinone:An in vitro study
GUO Zi-yan
WANG Zhong-shan
WU Le-le
WU Zhi-yong
LI Feng-lan
Abstract：AIM:To investigate the effects of cryptotanshinone(CTS)-loaded,RGD peptide-and phosphatidylserine(PS)-co-modified liposomes(RGD-PSL)on the inflammatory status of macrophages under lipopolysaccharide(LPS)stimulation in vitro.METHODS:Cryptotanshinone(CTS)-loaded liposomes co-modified with RGD peptide and phosphatidylserine(PS)(termed CTS@RGD-PSL)were prepared via the thin-film hydration method.Physicochemical characterizations,including dynamic light scattering(DLS)and cryogenic transmission electron microscopy(Cryo-TEM),were performed.RAW 264.7 macrophages were used to evaluate biocompatibility through CCK-8 and live/dead cell staining assays.The expression of M1/M2 phenotypic markers(CD86,CD206,Arg-1,IL-10,IL-6,TNF-α,iNOS)was analyzed by qRT-PCR and immunofluorescence RESULTS:CTS@RGD-PSL exhibited uniform particle size(234±5)nm and good dispersion,enabling efficient CTS delivery.qRT-PCR results demonstrated that CTS@RGD-PSL significantly upregulated anti-inflammatory factors(Arg-1,IL-10,CD206;P＜0.05)and suppressed pro-inflammatory cytokines(IL-6,TNF-α,iNOS;P＜0.05)compared to free CTS and unmodified liposomes.Immunofluorescence analysis revealed that CTS@RGD-PSL markedly reduced the expression of M1 marker CD86(P＜0.05)and enhanced M2 marker CD206(P＜0.001)in lipopolysaccharide-stimulated macrophages.CONCLUSION:Both CTS,RGD-PSL and CTS@RGD-PSL promoted macrophage M2 polarization,with CTS@RGD-PSL demonstrating the most potent anti-inflammatory effects,thereby proposing a potential therapeutic strategy for oral and maxillofacial inflammatory diseases.
Keywords：cryptotanshioneRGD peptidephosphatidylserineRAW264.7 macrophagespolarization
Publication Date：2025-06-28
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：9( 311-319 )