Preparation and quality evaluation of fluorocarbon microemulsion-based gel loaded with both 5-aminolevulinic acid and carbon dioxide
10.16438/j.0513-4870.2020-1201
- VernacularTitle:共载5-氨基酮戊酸及二氧化碳的氟碳微乳凝胶的制备及质量评价
- Author:
Jiao LIN
1
,
2
;
Lu-yao LIN
3
;
Zheng WU
3
;
Xue-han YANG
1
;
Xin ZHOU
1
;
Jia-liang ZHANG
1
Author Information
1. Department of Pharmacy, Fuzong Clinical Medical College of Fujian Medical University
2. 900 Hospital of the Joint Logistics Team), Fuzhou 350025, China
3. 900 Hospital of the Joint Logistics Team), Fuzhou 350025, China
- Publication Type:Research Article
- Keywords:
5-aminolevulinic acid;
carbon dioxide;
fluorocarbon microemulsion-based gel;
transdermal drug delivery;
photodynamic therapy
- From:
Acta Pharmaceutica Sinica
2021;56(1):306-313
- CountryChina
- Language:Chinese
-
Abstract:
To improve the efficacy of 5-aminolevulinic acid (5-ALA)-mediated photodynamic therapy (PDT), a fluorocarbon microemulsion-based gel (FMBG) loaded with both 5-ALA and carbon dioxide (CO2) was prepared in this study. Its physical and chemical properties such as particle size, zeta potential, morphology, pH value and viscosity were characterized. Acid-base titration experiment was used to determine the CO2 loading, a fluorescence derivatization method was established to determine the content of 5-ALA, and the confocal laser scanning microscope and Franz diffusion cell method were carried out to investigate its transdermal ability. Through the laser speckle contrast imaging, the CO2-affected blood flow perfusion of skin was measured. Finally, the skin irritation test was tested by hematoxylin-eosin staining (H&E) method. These results showed that the prepared FMBG was a milky white gel, with an average particle size of 202.4 nm, a zeta potential of -25.3 mV, a pH of 6.0, and a viscosity of 1 062.0 mPa·s. It can be stored stably for seven days at room temperature. The 5-ALA content of FMBG was measured to be approximately equal to 20% (w/w). At room temperature and normal pressure, the CO2 loading content of FMBG was 5.016 mg·L-1, which was 1.5 times as much as that of water. The transdermal absorption experiment and blood perfusion results showed that the FMBG can effectively enable the transdermal delivery of 5-ALA and CO2, and significantly increased the blood perfusion of skin. H&E staining results indicated that FMBG had negligible skin irritation (all animal tests were approved by the Ethics Committee of 900 Hospital of the Joint Logistics Team). In this study, a safe and stable FMBG loaded with both 5-ALA and CO2 was successfully prepared. It was suitable for transdermal application, having the potential of enhancing the efficacy of 5-ALA-mediated PDT.
