Preparation of Lipid Cubic Liquid Crystalline Nanoparticles of Sinomenine Based on Molecular Dynamics Simulations and Investigation of the Efficacy Against Rheumatoid Arthritis
Jiaoyue Zhu, Jingying Li, Yunlu Zou, Xuehui Ding, Jixin Li, Jiahui Xu, Yinghao Xiao, Ye Qiu, Wei Xu
TL;DR
Researchers developed lipid nanoparticles to improve the solubility and effectiveness of sinomenine, a drug for rheumatoid arthritis.
Contribution
A novel formulation strategy using lipid cubic nanoparticles and molecular dynamics simulations to enhance drug delivery.
Findings
SIN-LCNPs showed high encapsulation efficiency and improved drug delivery to inflamed joints in rats.
The nanoparticles significantly reduced inflammation and disease progression in rheumatoid arthritis models.
LCNPs enhanced intestinal permeability and absorption of sinomenine in vivo.
Abstract
Sinomenine (SIN) is a promising candidate for the treatment of rheumatoid arthritis (RA). Although it possesses the advantage of being non-addictive, its poor aqueous solubility and low oral bioavailability have limited its clinical application. To address these issues, SIN was encapsulated into lipid cubic liquid crystal nanoparticles (LCNPs) and systematically characterized. Molecular dynamics (MD) simulations were first employed to screen suitable excipients for formulation development. Combined with single-factor optimization and Box–Behnken response surface design, the optimal composition and preparation process were determined. The resulting SIN-LCNPs exhibited a particle size of 149.7 ± 0.9 nm, a polydispersity index (PDI) of 0.223 ± 0.01, a zeta potential of −18.9 mV, and an encapsulation efficiency (EE%) of 92.2%. Spectroscopic analyses confirmed successful incorporation of SIN…
Genes, proteins, chemicals, diseases, species, mutations and cell lines named across the full text — each resolved to its canonical identifier and authoritative record.
Click any figure to enlarge with its caption.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9
Figure 10
Figure 11Peer Reviews
No public reviews on file for this paper yet. If you reviewed it on a platform where reviews are public (OpenReview, ICLR, NeurIPS, ICML), you can paste yours below so the community can read it here.
Videos
No videos yet. Explain this paper in a talk, walkthrough, or lecture? Add one.
Taxonomy
TopicsAdvancements in Transdermal Drug Delivery · Berberine and alkaloids research · Drug Solubulity and Delivery Systems