title: Novel curcumin-loaded human serum albumin nanoparticles surface functionalized with folate: characterization and in vitro/vivo evaluation.
abstract: Folate-conjugated, curcumin-loaded human serum albumin nanoparticles (F-CM-HSANPs) were obtained by the chemical conjugation of folate to the surface of the curcumin (CM)-loaded human serum albumin nanoparticles (NPs). The NPs were characterized by various parameters, including size, polydispersity, zeta potential, morphology, encapsulation efficiency, and drug release profile. The mean particle size of F-CM-HSANPs was 165.6±15.7 nm (polydispersity index <0.28), and the average encapsulation efficiency percentage and drug loading percentage of the F-CM-HSANPs were 88.7%±4.8% and 7.9%±0.4%, respectively. Applied in vitro, the CM NPs, after conjugation with folate, maintained sustained release, and a faster release of CM was more visibly observed than the unconjugated NPs. F-CM-HSANPs can prolong the retention time of CM significantly in vivo. However, after intravenous injection of F-CM-HSANPs, the pharmacokinetic parameters of CM were not significantly different from those of CM-loaded human serum albumin NPs. The improved antitumor activity of F-CM-HSANPs may be attributable to the protection of drug from enzymatic deactivation followed by the selective localization at the desired site. These results suggest that the intravenous injection of F-CM-HSANPs is likely to have an advantage in the current clinical CM formulation, because it does not require the use of a solubilization agent and it is better able to target the tumor tissue.
authors: Breast Cancer Center.
authors: Zhiwang
authors: Z
authors: Song
authors: Breast Cancer Center.
authors: Yonglin
authors: Y
authors: Lu
authors: Breast Cancer Center.
authors: Xia
authors: X
authors: Zhang
authors: Department of Pharmacy.
authors: Haiping
authors: H
authors: Wang
authors: Department of Gastrointestinal Surgery, Shanghai East Hospital, Tongji University, Shanghai, People's Republic of China.
authors: Junyi
authors: J
authors: Han
authors: Breast Cancer Center.
authors: Chunyan
authors: C
authors: Dong
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000008:administration & dosage* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry* / Q000494:pharmacology; D005492:Folic Acid / Q000737:chemistry* / Q000494:pharmacology; D019073:HT29 Cells; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry*; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D051381:Rats; D012709:Serum Albumin / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013499:Surface Properties; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D012709:Serum Albumin; D005492:Folic Acid; D003474:Curcumin
keywords: HSA nanoparticles; curcumin; folate; pharmacokinetic parameters