Drug development and industrial pharmacy · 2025
Preparation and evaluation of gastrodin-ferulic acid co-loaded liposome gel patches for the treatment of migraine.
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Wang Jie, Gu Xuemei, Gao Xia, Gao Huifang, Chen Jing, Lv Zhiyang, Chen Lei, Xu Yunzhu, Chen Xialin, Cao Liang, Wang Zhenzhong, Tian Jinzhou, Xiao Wei
Аннотация
OBJECTIVE: Gastrodin (GA) and ferulic acid (FA) are the main active ingredients of the traditional Chinese medicine Da Chuan Xiong formula for migraine treatment. This study aimed to develop a gastrodin-ferulic acid co-loaded liposomal gel patch (GA/FA-Lip-GelP) as a transdermal drug delivery system (TDDS) for migraine management.
SIGNIFICANCE: TDDS overcomes the limitations of first-pass metabolism associated with oral administration and is particularly suitable for migraine patients experiencing nausea and vomiting. The system contains three key components: sodium polyacrylate (hydrophilic gel matrix), laurocapram (Azone, permeation enhancer), and GA/FA-loaded liposomes (nanocarrier). This combination enables effective systemic drug delivery.
METHODS: The GA/FA-Lip was prepared using central composite design optimization. Subsequently, the GA/FA-Lip-GelP formulation was developed through single-factor screening and Box-Behnken designs. The optimized GA/FA-Lip-GelP was systematically evaluated via in vitro release studies, ex vivo transdermal permeation experiments, and in vivo pharmacokinetic/pharmacodynamic analyses.
RESULTS: The GA/FA-Lip was prepared via thin-film dispersion, forming uniform spherical nanoparticles (146.34 ± 1.35 nm). These nanoparticles achieved high encapsulation efficiencies (GA: 85.26 ± 1.90%; FA: 86.92 ± 2.23%) and demonstrated excellent stability. The final GA/FA-Lip-GelP demonstrated optimal adhesion, sustained drug release, and content uniformity under low-temperature storage. Compared to oral administration and non-liposomal gel patches, GA/FA-Lip-GelP showed significantly enhanced transdermal permeation, improved pharmacokinetic profiles, and superior therapeutic efficacy.
CONCLUSIONS: GA/FA-Lip-GelP demonstrated potential as an effective migraine treatment by overcoming first-pass metabolism, thereby improving bioavailability and enabling sustained drug release.
SIGNIFICANCE: TDDS overcomes the limitations of first-pass metabolism associated with oral administration and is particularly suitable for migraine patients experiencing nausea and vomiting. The system contains three key components: sodium polyacrylate (hydrophilic gel matrix), laurocapram (Azone, permeation enhancer), and GA/FA-loaded liposomes (nanocarrier). This combination enables effective systemic drug delivery.
METHODS: The GA/FA-Lip was prepared using central composite design optimization. Subsequently, the GA/FA-Lip-GelP formulation was developed through single-factor screening and Box-Behnken designs. The optimized GA/FA-Lip-GelP was systematically evaluated via in vitro release studies, ex vivo transdermal permeation experiments, and in vivo pharmacokinetic/pharmacodynamic analyses.
RESULTS: The GA/FA-Lip was prepared via thin-film dispersion, forming uniform spherical nanoparticles (146.34 ± 1.35 nm). These nanoparticles achieved high encapsulation efficiencies (GA: 85.26 ± 1.90%; FA: 86.92 ± 2.23%) and demonstrated excellent stability. The final GA/FA-Lip-GelP demonstrated optimal adhesion, sustained drug release, and content uniformity under low-temperature storage. Compared to oral administration and non-liposomal gel patches, GA/FA-Lip-GelP showed significantly enhanced transdermal permeation, improved pharmacokinetic profiles, and superior therapeutic efficacy.
CONCLUSIONS: GA/FA-Lip-GelP demonstrated potential as an effective migraine treatment by overcoming first-pass metabolism, thereby improving bioavailability and enabling sustained drug release.