Construction of various lipid carriers to study the transdermal penetration mechanism of sinomenine hydrochloride

Abstract

Objective

To investigate the transdermal mechanisms and compare the differences in transdermal delivery of Sinomenine hydrochloride (SN) between solid lipid nanoparticles (SLN), liposomes (LS), and nanoemulsions (NE).

Methods

SN-SLN, SN-LS and SN-NE were prepared by ultrasound, ethanol injection and spontaneous emulsification, respectively. FTIR, DSC, in vitro skin penetration, activation energy (Ea) analysis were used to explore the mechanism of drug penetration across the skin.

Results

The particle size and encapsulation efficiency were 126.60 nm, 43.23 ± 0.48%(w/w) for SN-SLN, 224.90 nm, 78.31 ± 0.75%(w/w) for SN-LS, and 83.22 nm, 89.01 ± 2.16%(w/w) for SN-LS. FTIR and DSC showed the preparations had various levels of impacts on the stratum corneum’s lipid structure which was in the order of SLN > NE > LS. Ea values of SN-SLN, SN-LS, and SN-NE crossing the skin were 2.504, 1.161, and 2.510 kcal/mol, respectively.

Conclusion

SLN had a greater degree of alteration on the skin cuticle, which allows SN to permeate skin more effectively.

Keywords:

• Sinomenine hydrocohlride
• solid lipid nanoparticles
• liposomes
• nanoemulsion
• transdermal drug delivery systems

Acknowledgements

The content is solely the responsibility of the authors and does not necessarily represent the official views of Anhui University of Chinese Medicine.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Data availability statement

The datasets used or analysed during the current study are available from the corresponding author on reasonable request.

Additional information

Funding

The authors gratefully acknowledge support from the National Natural Science Foundation of China (No. 81803831), Anhui Province Science and Technology Major Project (201903a07020007), and Major Programs of Natural Science Research in Colleges and Universities in Anhui Province(2023AH040108).