Preparation of Triptolide-Chuanxiong Rhizoma Extract Ethanol Transfersomes and Analysis on Its in Vitro Anti-inflammatory Mechanism
10.13422/j.cnki.syfjx.20252166
- VernacularTitle:雷公藤甲素-川芎提取物醇传递体的制备及其体外抗炎作用机制分析
- Author:
Ling TAO
1
;
Zhiyan WAN
1
;
Yidan LIU
1
;
Zhe LI
1
;
Zhenzhong ZANG
1
;
Weifeng ZHU
1
;
Yongmei GUAN
1
Author Information
1. Key Laboratory of Modern Preparation of Traditional Chinese Medicine（TCM），Ministry of Education，Jiangxi University of Chinese Medicine，Nanchang 330004，China
- Publication Type:Journal Article
- Keywords:
triptolide;
Chuanxiong Rhizoma;
ethanol transfersomes;
compatibility of components;
transdermal delivery;
Janus kinase 2/signal transducer and activator of transcription 3（JAK2/STAT3） signaling pathway;
nuclear transcription factor-κB（NF-κB）
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2026;32(10):210-218
- CountryChina
- Language:Chinese
-
Abstract:
ObjectiveTo prepare triptolide-Chuanxiong Rhizoma extract ethanol transfersomes（TP-CX@TESs）， conduct its quality evaluation， and investigate its in vitro anti-inflammatory efficacy and the underlying mechanisms. MethodsTP-CX@TESs was prepared via the ultrasonic injection method. With encapsulation efficiency and particle size as evaluation indicators， Box-Behnken design-response surface methodology（BBD-RSM） was employed to optimize the formulation process. The TP-CX@TESs prepared under the optimal process was characterized and evaluated for in vitro transdermal performance. A lipopolysaccharide（LPS）-induced RAW264.7 cell inflammation model was established. After 24 h of drug intervention， the levels of inflammatory factors such as nitric oxide（NO）， interleukin-6（IL-6）， and tumor necrosis factor-α（TNF-α） in the cell supernatant were detected. Western blot was used to determine the protein expression levels of Janus kinase 2（JAK2）， signal transducer and activator of transcription 3（STAT3）， and α7 nicotinic acetylcholine receptor（α7nAChR）， and real-time fluorescence quantitative polymerase chain reaction（Real-time PCR） was applied to measure the mRNA expression levels of JAK2， STAT3， the encoding gene of α7nAChR（CHRNA7）， and nuclear transcription factor-κB（NF-κB）. ResultsResults of BBD-RSM showed that the optimal formulation for preparing TP-CX@TESs was as follows：egg yolk lecithin content of 2.3%， ethanol volume fraction of 30%， and ratio of polysorbate-80 to egg yolk lecithin of 2∶5. Microscopic characterization revealed that TP-CX@TESs exhibited a spherical-like structure with a particle size of （105.60±3.85） nm， a polydispersity index of 0.19±0.03， and a Zeta potential of （-15.89±0.98） mV. The encapsulation efficiencies of triptolide， ferulic acid， and ligustilide were （76.88±4.40）%， （78.84±4.40）%， and （65.88±0.06）%， respectively. Both in vitro release and transdermal penetration of triptolide， ferulic acid， and ligustilide in TP-CX@TESs all followed the first-order kinetic model， showing a certain sustained-release property. Experimental results in RAW264.7 cells indicated that TP-CX@TESs significantly inhibited the release of NO， TNF-α， and IL-6（P<0.01）， remarkably upregulated the protein expression levels of STAT3 and α7nAChR（P<0.01）， increased the mRNA expression level of CHRNA7， and significantly downregulated the mRNA expression level of NF-κB（P<0.05， P<0.01）. ConclusionThe optimized formulation process of TP-CX@TESs is simple and feasible， along with favorable in vitro release property， good transdermal permeability， and excellent in vitro anti-inflammatory activity， the mechanism is related to the inhibition of NF-κB.
