Extraction, Isolation, Characterization, and Development of Phospholipids Complex Nanocarrier for Improved Solubility, Antiasthmatic, and Pharmacokinetic Potential of Curcuminoids.

BACKGROUND

Curcuma longa Linn. (Zingiberaceae) is a medicinal plant with significant biological activities owing to curcuminoids (CURs). Nevertheless, its low oral bioavailability because of low water solubility, inadequate absorption, short half-life, and rapid clearance hampered its clinical applications.

OBJECTIVE

The study aimed to extract, isolate, characterize, and formulate the Phospholipon ®90H complex and evaluate for improved solubility, antiasthmatic and pharmacokinetic potential of CURs.

METHODS

Phospholipon®90H-based complex of curcuminoids (CPLC) was synthesized via solvent evaporation technique and reported an improvement of solubility, antiasthmatic, and pharmacokinetic potential of CURs. CPLC was physico-chemically and functionally evaluated by Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, oral bioavailability, and antiasthmatic activity.

RESULTS

Ethyl acetate rhizome extracts (EARE) displayed ~17.42 % w/w extraction yield of CURs. CPLC revealed high entrapment of CURs (~ 92.55 % w/w) within the polar head of phospholipids. Small particle size ~ 194 nm with zeta potential value ~ -20.4 mV suggests the physical stability of CPLC. Physical analysis evidenced the formation of stable and amorphous CPLC by establishing hydrophobic and weak intermolecular forces between CURs and Phospholipon ®90H. Undoubtedly, the amorphous CPLC raised the aqueous solubility of CURs (~2-fold) compared to pure CURs. CPLC formulations (~ 20 mg/kg of CURs, p.o.) significantly lowered the leucocyte and eosinophil count compared to pure CURs. CPLC improved the oral bioavailability of CURs compared to pure CURs.

CONCLUSION

Results highlight that CPLC could be established as a breakthrough respiratory nanocarrier for CURs and other phytocompounds with respiratory potential.