Optimization, characterization and evaluation of liposomes from Malus hupehensis (Pamp.) Rehd. extracts

Abstract

The Malus hupehensis (Pamp.) Rehd. is a traditional medicine and edible plant. The previous study found that the extracts of M. hupehensis (Pamp.) Rehd. had a good antioxidant activity in vivo and in vitro. But its clinical application was limited by its poor solubility, rapidly metabolized and poor bioavailability. Hence, this article aimed at developing liposomes as a novel transdermal system for delivering M. hupehensis extracts efficiently. The prepared liposomes were characterized regarding their entrapment efficiency percentage (EE%), vesicle size (VS), polydispersity index (PDI), zeta potential (ZP) and drug loading (DL). Box-Behnken design response surface methodology and factorial design were used to optimize formulation and preparation process, respectively. The optimized liposomes had an EE of 77.29 ± 0.99%, VS of 102.74 ± 1.61 nm, ZP of −21.79 ± 1.43 mV, PDI of 0.291 ± 0.005 and DL was 6.68 ± 0.49%. Transmission electron microscopy showed liposomes had a regular spherical surface. In addition, liposomes exhibited superior skin permeation potential and retention capacity compared with solution. Histopathological study ensured the safety of liposome application. Meanwhile, the optimized liposome has a good stability. Hence, M. hupehensis extracts liposomes could be considered a promising vehicle for transdermal delivery.

Keywords:

• Malus hupehensis (Pamp.) Rehd. extracts
• liposome
• optimization
• characterization
• skin penetration

Author contributions

Conceptualization: J. L., D. G. and Y. S. Data curation: J. L., J. C., Y. S., J. Z. and X. Z. Funding acquisition: D. G. Investigation: J. C., Y. F., Y. S. and J. Z. Writing – original draft: J. L. and D. G. Writing – review and editing: J. L. and D. G.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the National Natural Science Foundation of China [NO. 81202905], Subject Innovation Team of Shaanxi University of Chinese Medicine [NO. 2019-YL11] and Scientific Research Project of Education Department of Shaanxi Provincial Government [NO. 15JF015].