Construction and evaluation of charge-reversal nanocarrier loaded with hematoporphyrin monomethyl ether
10.16438/j.0513-4870.2017-0431
- VernacularTitle:载血卟啉单甲醚电荷反转型纳米载体构建及评价
- Author:
Ai-ren XU
1
;
Jian-hui RONG
1
;
Meng-jia CHEN
1
;
Zheng-hong FENG
1
;
Wei-cheng MA
1
;
Song SHEN
2
;
Yi JIN
3
Author Information
1. Ningbo Urinary and Renal Diseases Hospital, Ningbo 315100, China
2. School of Pharmacy, Jiangsu University, Zhenjiang 212013, China
3. Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
charge conversion;
lysosomal escape;
hematoporphyrin monomethyl ether;
sonodynamic therapy;
targeted delivery
- From:
Acta Pharmaceutica Sinica
2017;52(10):1605-1610
- CountryChina
- Language:Chinese
-
Abstract:
Charge-reversal nanocarrier was constructed to enhance lysosomal escape and improve an-titumor effect. We synthesized the cholesterol-polyethyleneimine-hexahydrophthalic anhydride (Chol-PEI-HHPA) polymer and characterized by 1H NMR. The charge-reversal liposomes (Lipo-HHPA) were synthesized and the hematoporphyrin monomethyl ether (HMME) was loaded. pH-triggered charge conversion was determined at different pH values. The lysosomal escape and cytotoxicity of the Lipo-HHPA were evaluated in MCF-7 cells. The Lipo-HHPA was uniform with an average particle size of 102 nm. Upon the irradiation of ultrasound, burst release of HMME could be observed. The zeta potential of Lipo-HHPA changed sharply from negative (-23.5 mV) to positive (+21.2 mV) over the pH range of 7.4-4.5. In the cellular uptake experiment, the lysosomal escape of Lipo-HHPA was observed. HMME loaded Lipo-HHPA displayed obviously enhanced cytotoxicity towards MCF-7 cells. These results indicate that the charge-reversal liposomes hold a great potential in improving the cytotoxicity and antitumor effect.
