Preparation and in-vitro/in-vivo evaluation of curcumin nanosuspension with solubility enhancement.
OBJECTIVE
We developed Cur nanosuspension (Cur-NS) with PVPK30 and SDS as stabilizers to improve poor water solubility and short biological half-time of Cur.


METHODS
Physicochemical characterization of Cur-NS was characterized systematically. The in-vitro dissolution, cytotoxicity and in-vivo pharmacokinetic experiments of Cur-NS were also evaluated.


RESULTS
Scanning electron microscope indicated that the morphologies of Cur-NS were spherical or ellipsoidal in shape. X-ray diffraction verified that Cur was successfully developed as nanoparticles with an amorphous phase in Cur-NS. Fourier transform infrared spectroscopy suggested there was no degradation about Cur in the Cur-NS. Furthermore, the in-vitro study showed that the cumulative release of the Cur-NS was 82.16 ± 2.62% within 34 h and the cytotoxicity of the Cur-NS against HepG2 cells was much better than raw Cur. Besides, in-vivo pharmacokinetics in rats by intravenous injection displayed that the in-vivo process of Cur-NS pertained to two-compartment model. Meanwhile, the t1/2 and AUC0-t of Cur-NS were enhanced by 11.0-fold and 4.2-fold comparing to Cur solution.


CONCLUSIONS
The Cur-NS significantly increased the water solubility and half-time of Cur, suggesting its potential as a nanocarrier in the delivery of Cur for future clinical application.
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Xin
X
Li
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Huiling
H
Yuan
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Caiyun
C
Zhang
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Weidong
W
Chen
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Weiye
W
Cheng
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Xin
X
Chen
College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui, China.
Xi
X
Ye
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D030024:Curcuma / Q000737:chemistry; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods* / Q000592:standards; D005260:Female; D056945:Hep G2 Cells; D018197:Hepatoblastoma / Q000188:drug therapy; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D019999:Pharmaceutical Solutions / Q000737:chemistry; D011145:Polyvinyls; D017207:Rats, Sprague-Dawley; D012967:Sodium Dodecyl Sulfate / Q000031:analogs & derivatives; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water; D014961:X-Ray Diffraction
D000972:Antineoplastic Agents, Phytogenic; D019999:Pharmaceutical Solutions; D011145:Polyvinyls; C488580:poly(vinyl phenyl ketone); C542100:sodium dodecyl dioxyethylene sulfate; D014867:Water; D012967:Sodium Dodecyl Sulfate; D003474:Curcumin
curcumin; cytotoxicity; intravenous injection; nanosuspension; pharmacokinetics