ABSTRACT
The article was to study the effect of local photodynamics therapy combined with carbon dioxide lattice laser - "light needles" for the treatment of basal cell carcinoma (BCC). 5-Aminolevulinic acid (5-ALA) cubic liquid crystal using glyceryl monostearate (GMO) as the substrate was prepared. The cytotoxicity of 5-ALA cubic liquid crystal combined with light needles in vitro were evaluated. The pharmacodynamics study of 5-ALA cubic liquid crystal combined with light needles of high or low energy for BCC was carried out based on the pathological changes, tumor volume, vascular endothelial growth factor (VEGF) expression and the recurrence rate, which has been approved by the Ethics Committee of Beijing Institute of Radiation Medicine. The cubic liquid crystal was isotropic with the lattice of PN3M. The cytotoxicity of 5-ALA cubic liquid crystal combined with light needles was much higher than that of 5-ALA or light needles alone. Compared with light needles or photodynamic therapy alone, 5-ALA cubic liquid crystal combined with light needles of high energy could prevent the BCC metastasis and of low energy could inhibit BCC growth. It demonstrated the obvious therapeutical effects for BCC. 5-ALA cubic liquid crystal combined with light needles can effectively treat BCC, which provides a new choice for clinical BCC treatment.
ABSTRACT
OBJECTIVE: To prepare and characterize triptolide cubic liquidcrystal,study the rheological properties and in vitro transdermal properties. METHODS: Cubic liquid crystal (V2) was prepared by using phytantriol-carbitol-water three-component system. Using the ternary phase diagram method to optimize the target area. V2 was characterized by small-angle X-ray scattering, infrared spectroscopy and differential scanning calorimetry. Rheological properties of V2 was studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using improved Franz diffusion cell method. RESULTS: SAXS is shown as double-diamond lattice cubic liquid crystal; rheological parameters are good; DSC results show V2 can be converted into a hexagonal phase at 65.5 ℃ and converted into a layered liquid crystal at 90 ℃, and the addition of the drug does not change the liquid crystal structure. In vitro transdermal cumulative permeation amount is about 1.54 times that of the gel, and the sustained release of triptolide can be as long as 48 h. CONCLUSION: The prepared triptolide liquid crystal has good appearance and suitable rheology, and its cumulative permeation amount and infiltration rate of V2 are superior to the hydrophilic gel, which provides theoretical reference for triptolide percutaneous administration.
ABSTRACT
Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64:16:20, w/w/w) loaded with 6 mg·g-1 of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8:3.2:16:20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC0-∞ of ISH2 group were increased significantly compared with that of SMH solution group and the AUC0-∞ of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis.