<abstract xmlns="http://www.w3.org/1999/xhtml">

<p>Triptolide exerts strong anti-inflammatory and immunomodulatory effects; however, its oral administration might be associated with side effects. Transdermal administration can improve the safety of triptolide. In this study, glycerosomes were prepared as the transdermal vehicle to enhance the transdermal delivery of triptolide. With entrapment efficiency and drug loading as dependent variables, the glycerosome formulation was optimized using an orthogonal experimental design. Phospholipid-to-cholesterol and phospholipid-to-triptolide mass ratios of 30:1 and 5:1, respectively and a glycerol concentration of 20 % (<italic>V/V</italic>) were used in the optimization. The glycerosomes prepared with the optimized formulation showed good stability, with an average particle size of 153.10 ± 2.69 nm, a zeta potential of –45.73 ± 0.60 mV and an entrapment greater than 75 %. Glycerosomes significantly increased the transdermal delivery of triptolide compared to conventional liposomes. As efficient carriers for the transdermal delivery of drugs, glycerosomes can potentially be used as an alternative to oral triptolide administration.</p>
</abstract>

Triptolide exerts strong anti-inflammatory and immunomodulatory effects; however, its oral administration might be associated with side effects. Transdermal administration can improve the safety of triptolide. In this study, glycerosomes were prepared as the transdermal vehicle to enhance the transdermal delivery of triptolide. With entrapment efficiency and drug loading as dependent variables, the glycerosome formulation was optimized using an orthogonal experimental design. Phospholipid-to-cholesterol and phospholipid-to-triptolide mass ratios of 30:1 and 5:1, respectively and a glycerol concentration of 20 % (V/V) were used in the optimization. The glycerosomes prepared with the optimized formulation showed good stability, with an average particle size of 153.10 ± 2.69 nm, a zeta potential of –45.73 ± 0.60 mV and an entrapment greater than 75 %. Glycerosomes significantly increased the transdermal delivery of triptolide compared to conventional liposomes. As efficient carriers for the transdermal delivery of drugs, glycerosomes can potentially be used as an alternative to oral triptolide administration.

Optimizing glycerosome formulations <italic>via</italic> an orthogonal experimental design to enhance transdermal triptolide delivery

Shanghai University of Traditional, Chinese Medicine

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Optimizing glycerosome formulations  an orthogonal experimental design to enhance transdermal triptolide delivery

Triptolide exerts strong anti-inflammatory and immunomodulatory effects; however, its oral administration might be associated with side effects. Transdermal...

Optimizing glycerosome formulations via an orthogonal experimental design to enhance transdermal triptolide delivery

Published Online: Aug 30, 2021

Page range: 135 - 146

Accepted: Jan 21, 2021

DOI: https://doi.org/10.2478/acph-2022-0006

Keywords
nanocarriers, liposomes, glycerosomes, transdermal, rheumatoid arthritis

© 2022 Chunyun Zhu et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Optimizing glycerosome formulations via an orthogonal experimental design to enhance transdermal triptolide delivery

Published Online: Aug 30, 2021

Page range: 135 - 146

Accepted: Jan 21, 2021

DOI: https://doi.org/10.2478/acph-2022-0006

Keywordsnanocarriers, liposomes, glycerosomes, transdermal, rheumatoid arthritis

© 2022 Chunyun Zhu et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Keywords
nanocarriers, liposomes, glycerosomes, transdermal, rheumatoid arthritis