Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles

We firstly investigated the interactions between PTX and glycyrrhizic acid and designed a nano-sized formulation that could largely increase the solubility of PTX using GA, a hypotoxic or even therapeutic material, as a carrier

Fu-Heng Yang

2015

Scholarcy highlights

  • Paclitaxel is a natural terpenoid compound, extracted from the bark of Western Taxus brevifolia, that has excellent antitumor activities against a wide range of solid tumors, including refractory human ovarian, breast cancers and non-small-cell lung carcinoma
  • The data obtained from this study indicated that the PTX-loaded glycyrrhizic acid micelles led to a 6-fold enhancement in the oral bioavailability of PTX
  • On account of the amphiphilic characteristics of GA, the combination could form micelles in aqueous medium to enhance the solubility of PTX
  • In vitro release study showed that PTX-loaded GA micelles could be considered as a delayed drug release system
  • Compared with Taxol®, PTX-loaded GA micelles demonstrated a notable improvement of oral bioavailability in vivo, which could be largely due to the enhancement of the PTX absorption in jejunum and colon intestine
  • The encapsulation efficiency was about 90%, and the drug loading rate could reach up to 7.90%
  • The increased absorption of PTX may be attributed to a comprehensive effect of GA on the following aspects: the enhancement of PTX solubility, the nanosize drug delivery system, the inhibition of P-gp efflux and the inhibition on CYP3A
  • Unlike many other new dosage forms of PTX, of which various materials are still a long way to go to verify their clinical use, glycyrrhizic acid could be a very promising carrier for the oral delivery system of PTX, since GA itself has been used in clinic for years

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