Developments in drug delivery of bioactive alkaloids derived from traditional Chinese medicine

Drug Deliv. 2018 Nov;25(1):398-416. doi: 10.1080/10717544.2018.1431980.


The bioactive alkaloids (e.g. vincristine, hydroxycamptothecin, ligustrazine, and so on) from traditional Chinese medicine (TCM) have exerted potent efficacies (e.g. anti-tumor, anti-inflammation, immunosuppression, etc.). However, a series of undesirable physicochemical properties (like low solubility and weak stability) and baneful pharmacokinetic (PK) profiles (e.g. low bioavailability, short half time, rapid clearance, etc.) have severely restricted their applications in clinic. In addition, some side effects (like cumulative toxicities caused by high-frequency administration and their own toxicities) have recently been reported and also confined their clinical uses. Therefore, developments in drug delivery of such alkaloids are of significance in improving their drug-like properties and, thus, treatment efficiencies in clinic. Strategies, including (i) specific delivery via liposomes; (ii) sustained delivery via nanoparticles, gels, and emulsions; and (iii) transdermal delivery via ethosomes, solid lipid nanoparticles, and penetrating enhancers, have been reported to improve the pharmacokinetic and physicochemical characters of problematic TCM alkaloids, decline their adverse effects, and thus, boost their curative efficacies. In this review, the recent reports in this field were comprehensively summarized with the aim of providing an informative reference for relevant readers.

Keywords: Bioactive alkaloids; drug delivery; pharmacokinetics; toxicity; traditional Chinese medicine.

Publication types

  • Review

MeSH terms

  • Alkaloids / administration & dosage*
  • Alkaloids / metabolism
  • Animals
  • Drug Delivery Systems / methods
  • Drug Delivery Systems / trends*
  • Drugs, Chinese Herbal / administration & dosage*
  • Drugs, Chinese Herbal / metabolism
  • Humans
  • Medicine, Chinese Traditional / methods
  • Medicine, Chinese Traditional / trends*
  • Metabolic Clearance Rate / drug effects
  • Metabolic Clearance Rate / physiology
  • Skin Absorption / drug effects
  • Skin Absorption / physiology


  • Alkaloids
  • Drugs, Chinese Herbal

Grants and funding

This work was supported by Program for New Century Excellent Talents in University (NCET-13-0906); the funds from Shanghai Municipal Commission of Health and Family Planning (ZY3-CCCX-3-5001) and Science and Technology Commission of Shanghai Municipality (15DZ2292000); and the Xinglin Scholar Program of Shanghai University of Traditional Chinese Medicine.