[Tumor cell targetability of folate receptor-mediated mitoxantrone albumin nanoparticles].
OBJECTIVE
To study the tumor cell targetability of folate-conjugated mitoxantone-loaded albumin nanoparticles (MTO-BSANP-folate).


METHODS
Bovine albumin nanoparticles were prepared by desolvation method. The activated folic acid (N-hydroxysuccinimide ester of folic acid) was conjuated to the surface of BSANP via the amino groups. The MTO-BSANP-folate was prepared by mixing folate-conjugated albumin nanoparticles with mitoxantrone and then cross-linked by glutaraldehyde. 3HTdR and flow cytometry were used to evaluate the targetability of MTO-BSANP-folate.


RESULTS
The encapsulation rate of folate-conjugated mitoxantrone albumin nanoparticles was (96.55 +/- 0.96)% and the drug loading was (9.66 +/- 0.10)%. The results of 3HTdR showed that the efficacy of MTO-BSANP-folate in killing SKOV3 cells was higher than that of MTO-BSANP-folate, and the results of flow cytometry showed that the apoptosis-promoting effect of MTO-BSANP-folate was 3.5-4.5 times higher than that of MTO-BSANP.


CONCLUSIONS
MTO-BSANP-folate could be targeted, via folate receptor, to the tumor cells rich in folate receptors.
Zhang
Liang-ke
LK
Department of Pharmacy, Chongqing University of Medical Sciences, Chongqing 400016, China.
Hou
Shi-xiang
SX
Mao
Sheng-jun
SJ
Wei
Da-peng
DP
Song
Xiang-rong
XR
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D002352:Carrier Proteins / Q000378:metabolism; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D008942:Mitoxantrone / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D053758:Nanoparticles; D010051:Ovarian Neoplasms / Q000378:metabolism / Q000473:pathology; D011956:Receptors, Cell Surface / Q000378:metabolism; D012710:Serum Albumin, Bovine / Q000737:chemistry / Q000493:pharmacokinetics*
D000970:Antineoplastic Agents; D002352:Carrier Proteins; D058973:Folate Receptors, GPI-Anchored; D011956:Receptors, Cell Surface; D012710:Serum Albumin, Bovine; D005492:Folic Acid; D008942:Mitoxantrone