Improved transdermal permeability of tanshinone IIA from cataplasms by loading onto nanocrystals and porous silica

Abstract

Novel transdermal cataplasms have been designed to improve permeability of poorly soluble drugs by different pretreatments. Nanocrystal and porous silica solid dispersions were loaded with Tanshinone IIA and incorporated into a cross-linked hydrogel matrix of cataplasm. It was shown that the small particle size and improved dissolution would increase dermal bioavailability. The adhesion, rheological properties, drug release, skin permeation, skin deposition and in vivo skin absorption of the different formulations were investigated. In an in vitro experiment using mouse skin, cumulative amount of drug permeated within 24 h was 7.32 ± 0.98 μg/cm² from conventional cataplasm, 13.14 ± 0.70 μg/cm² from nanocrystal-loaded cataplasm and 11.40 ± 0.13 μg/cm² from porous silica solid dispersion-loaded cataplasm. In vitro dissolution profiles showed that drug release was 76.5% and 74.9% from two optimized cataplasms within 24 h, while conventional cataplasm was 55.0%. The cross-linking characteristics of the cataplasms were preserved after incorporation of different drug forms, while the elastic and viscous behaviors of the hydrogel layers increased. In vivo evaluation by CLSM showed the more favorable skin permeation for two optimized cataplasms. These findings suggest that applications of nanocrystal and porous silica systems on cataplasms enable effective transdermal delivery of poorly soluble drugs. The resulting drug delivery and rheological properties are desirable for transdermal application.

Abbreviation

• All the abbreviations that appear in this article are shown in Table 1.

Graphical Abstract

Keywords:

• Transdermal
• tanshinone IIA
• nanocrystal
• porous silica
• cataplasm

Disclosure statement

The authors declare that we do not have any commercial or associated interests that constitute a conflict of interest in connection with the work submitted.

Additional information

Funding

This work was financially supported by Key Research Funding of Ningxia Province [No.2017BY084].