Cubic and hexagonal liquid crystals as drug carriers for the transdermal delivery of triptolide

Abstract

The purpose of this study was to develop and evaluate triptolide-loaded cubic and hexagonal liquid crystals for transdermal drug delivery systems (TDDSs). We prepared and characterized triptolide-loaded lyotropic liquid crystals and evaluated for their percutaneous permeation properties in vitro and in vivo . We then used the adjuvant arthritic rat model and HaCaT cells to analyze the pharmacodynamics and conduct cell-stimulating studies of these liquid crystals. The optimized preparations were identified as cubic and hexagonal phase structures, respectively. Moreover, the in vitro percutaneous penetration studies demonstrated that compared to the homemade triptolide gel, cubic and hexagonal liquid crystals could significantly increase the percutaneous cumulative penetration of drugs within 48 h. Besides, the results of skin-blood synchronous microdialysis showed that the triptolide concentration in skin was higher than that in blood, and the cubic and hexagonal liquid crystals significantly increased the bioavailability of triptolide. Triptolide-loaded cubic and hexagonal liquid crystals presented excellent anti-arthritic effects, alleviating paw swelling and inhibiting inflammation by downregulating the levels of TNF-α and IL-1β. In vitro cell-stimulating studies displayed that triptolide-loaded cubic and hexagonal liquid crystals exhibited no obvious toxicity, which exhibited that triptolide-loaded cubic and hexagonal liquid crystals were remarkable biocompatibility. Collectively, triptolide-loaded cubic and hexagonal liquid crystals represented a promising candidate for rheumatoid arthritis therapy.

Hexosomes as Efficient Platforms for Possible Fluoxetine Hydrochloride Repurposing with Improved Cytotoxicity against HepG2 Cells

“…The black view under the cross-polarized optical microscope indicates the isotropic phase of the cubosomes as previously reported. 20 , 38 Consequently, the presence of OA alters the GMO effective packing parameter that induces the phase transition from the cubic phase (cubosomes) to the 2D hexagonal phase (hexosomes) 17 , 39 as shown in Figure S2B , which indicates the anisotropic phase with a fanlike structure of hexosomes as previously reported. 38 , 40 The obtained hexosomes appeared as a homogenous milky-like dispersion.…”

Transdermal delivery of inflammatory factors regulated drugs for rheumatoid arthritis

“…Patch refers to a flake preparation made of drugs and suitable materials that can be pasted on the skin for topical administration. Transdermal patches are usually composed of four layers, the impermeable backing layer, drug containing matrix layer, adhesive layer, and peelable anti adhesion protective layer (Pastore et al., 2015 ). The patch can slowly release the drug, allowing it to penetrate the skin and maintain a constant plasma concentration (Nalamachu & Gudin, 2020 ).…”

Therapeutic potential of triptolide in autoimmune diseases and strategies to reduce its toxicity

“…Their structures and chemical properties of V 2 and H 2 phases are similar to those of cell membranes, allowing drugs to penetrate stratum corneum for transdermal delivery [ 145 ]. Shan et al [ 146 ] reported that the IC 50 of triptolide-loaded V 2 group and H 2 group in HaCaT cells were respectively 158 and 23 times that of free triptolide group, indicating their excellent anti-arthritic effects with low skin irritation.…”