Environmental-sensitive micelles based on poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) diblock copolymer for application in drug delivery.
Anticancer drug doxorubicin (DOX) was physically loaded into the micelles prepared from poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) diblock copolymers (PEOz-PLLA). PEOz-PLLA consists of hydrophilic segment PEOz and hydrophobic segment PLLA showed pH-sensitivity in the aqueous solution. The DOX-loaded micelle exhibited a narrow size distribution with a mean diameter around 170 nm. The micellar structure can preserve hydrophobic drug DOX under the physiological condition (pH 7.4) and selectively release DOX by sensing the intracellular pH change in late endosomes and secondary lysosomes (pH 4-5). At 37 degrees C, the cumulated released rate of DOX from micelles was about 65% at pH 5.0 in the initial 24 h. Additionally, polymeric micelles had low cytotoxicity in human normal fibroblast HFW cells for 72 h by using MTT assay. Moreover, DOX-loaded micelles could slowly and efficiency decrease cell viability of non-small-cell lung carcinoma CL3 cells. Taken together, PEOz-b-PLLA diblock polymeric micelles may act as useful drug carriers for cancer therapy.
Hsiue
Ging-Ho
GH
Department of Chemical Engineering, National Tsing Hua University, Hsinchu, 300 Taiwan, ROC. ghhsiue@nx.nthu.edu.tw
Wang
Chun-Hung
CH
Lo
Chun-Liang
CL
Wang
Chau-Hui
CH
Li
Ju-Pi
JP
Yang
Jia-Ling
JL
D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D002289:Carcinoma, Non-Small-Cell Lung; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems; D006801:Humans; D008823:Micelles; D010080:Oxazoles / Q000737:chemistry; D011073:Polyamines; D011091:Polyesters / Q000737:chemistry; D011108:Polymers / Q000737:chemistry
D000903:Antibiotics, Antineoplastic; D008823:Micelles; D010080:Oxazoles; D011073:Polyamines; D011091:Polyesters; D011108:Polymers; C511916:poly(2-ethyl-2-oxazoline); C033616:poly(lactide); D004317:Doxorubicin