Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 535, Issue 1-2, Pages 18-26Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.10.053
Keywords
Celastrol; Herbal drugs; Oral bioavailability; Phospholipid complex; Phytosomes
Categories
Ask authors/readers for more resources
Celastrol (CST) is a promising natural drug of herbal origin that gained a great interest in the recent years by virtue of its wide variety of pharmacological actions. Nowadays, CST is extensively studied as a natural anticancer surrogate with a potential activity against various types of cancers. However, CST suffers from many limitations that handicapped its clinical utility such as limited aqueous solubility and poor gastrointestinal absorption which resulted into its low oral bioavailability. This work spotlights, for the first time, development of self-assembled phytosomal nanocarriers (CST-PHY) for improving CST solubility and oral bioavailability. First CST-phospholipid complex was prepared by a simple solvent evaporation technique. Formation of CST-phospholipid complex was confirmed by differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (XRD) and partition coefficient determination. After dispersion into deionized water, CST-phospholipid complex was self-assembled to form CST-PHY. The optimized CST-PHY demonstrated a nanometric particle size of 178.4 +/- 7.07 nm and a negative zeta potential of -38.7 +/- 3.61 mV. Comparative in-vitro release study showed the ability of phytosomes to significantly enhance CST release compared with crude drug and physical mixture. Pharmacokinetic studies in rabbits revealed significant improvement in CST-PHY oral bioavailability compared with crude CST evidenced by 4-fold increase in AUC(0-8) and 5-fold increase in C-max of CST-PHY compared with crude CST. Conclusively, the results confirmed the potential of phytosomal nanocarriers to improve CST oral delivery paving the way for its use for oral cancer therapy.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available