Novel curcumin-loaded human serum albumin nanoparticles surface functionalized with folate: characterization and in vitro/vivo evaluation

Figures & data

Figure 1 Transmission electron microscope images of CM-HSANPs (A) and F-CM-HSANPs (B) (×20,000).

Abbreviations: CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles.

Table 1 Storage stability of F-CM-HSANPs at 25°C and 60% RH (n=3)

	0 day	1 month	2 months	3 months
Particle size (nm)	165.6±15.7	165.9±16.2	167.3±15.5	168.4±14.9
DL%	5.5±0.7	5.6±0.8	5.5±0.5	5.4±0.6
EE%	83.2±6.9	81.8±7.2	82.1±6.4	80.3±5.6
PDI	<0.28	<0.30	<0.31	<0.33

Abbreviations: F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; RH, relative humidity; DL, drug loading; EE, encapsulation efficiency; PDI, polydispersity index.

Figure 2 In vitro release of CM from free CM, CM-HSANPs, and F-CM-HSANPs (n=3).

Abbreviations: CM, curcumin; CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; h, hours.

Table 2 Pharmacokinetic parameters of CM after IV administration of CM solution, CM-HSANPs, and F-CM-HSANPs to rats (n=6)

Parameter	IV administration
	Solution	CM-HSANPs	F-CM-HSANPs
t1/2 (h)	0.08±0.01	0.36±0.05*	0.43±0.07*
AUC0–t (ng⋅h/mL)	2,095.2±165.3	5,427.3±487.9*	6,450.9±632.2*
AUC0–∞ (ng⋅h/mL)	2,298.3±187.6	5,761.4±518.5*	6,721.6±643.1*
MRT (h)	2.9±0.8	13.7±1.4*	14.7±1.5*
CL (L/h)	16.7±1.8	3.2±0.6*	3.6±0.4*

Note:

* P<0.05 vs CM solution.

Abbreviations: CM, curcumin; IV, intravenous; CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; t_1/2, half-life; h, hours; AUC, area under the curve; MRT, mean residence time; CL, clearance.

Figure 3 Plasma concentration–time profiles of CM solution, CM-HSANPs, and F-CM-HSANPs after IV administration to rats (n=6).

Abbreviations: CM, curcumin; CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; IV, intravenous; h, hours.

Figure 4 The diagram of human colon cancer (HT 29 cells) xenograft models in vivo.

Figure 5 In vivo antitumor activities of free CM, CM-HSANPs, and F-CM-HSANPs (10 mg/kg) in human colon cancer (HT29 cells) xenograft models after the IV administration (n=8).

Abbreviations: CM, curcumin; CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; IV, intravenous; PBS, phosphate-buffered saline.

Figure 6 Body weight changes of free CM, CM-HSANPs, and F-CM-HSANPs (10 mg/kg) in human colon cancer (HT29 cells) xenograft models after the IV administration (n=8).

Abbreviations: CM, curcumin; CM-HSANPs, curcumin-loaded, human serum albumin nanoparticles; F-CM-HSANPs, folate-conjugated, curcumin-loaded human serum albumin nanoparticles; IV, intravenous; PBS, phosphate-buffered saline.