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Nanoscale Res Lett. 2017 Aug 23;12(1):504. doi: 10.1186/s11671-017-2256-9.

Effects of Micro-environmental pH of Liposome on Chemical Stability of Loaded Drug.

Author information

1
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, No. 14, Block 3, Renmin Road South, Chengdu, 610041, China.
2
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, No. 14, Block 3, Renmin Road South, Chengdu, 610041, China. dentistcai@hotmail.com.
3
State Key Laboratory of Oral Diseases, West China Hospital of Stomatology, Sichuan University, No. 14, Block 3, Renmin Road South, Chengdu, 610041, China. qiangpengzz@scu.edu.cn.

Abstract

Liposome is a promising carrier system for delivering bioactive molecules. However, the successful delivery of pH-sensitive molecules is still limited by the intrinsic instability of payloads in physiological environment. Herein, we developed a special liposome system that possesses an acidic micro-environment in the internal aqueous chamber to improve the chemical stability of pH-sensitive payloads. Curcumin-loaded liposomes (Cur-LPs) with varied internal pH values (pH 2.5, 5.0, or 7.4) were prepared. These Cur-LPs have similar particle size of 300 nm, comparable physical stabilities and analogous in vitro release profiles. Interestingly, the chemical stability of liposomal curcumin in 50% fetal bovine serum and its anticancer efficacy in vitro are both micro-environmental pH-dependent (Cur-LP-2.5 > Cur-LP-5.0 > Cur-LP-7.4). This serum stability still has space to be further enhanced to improve the applicability of Cur-LP. In conclusion, creating an acidic micro-environment in the internal chamber of liposome is feasible and efficient to improve the chemical stability of pH-sensitive payloads.

KEYWORDS:

Controlled release; Curcumin; Drug delivery; Liposomes; Nanoparticles

PMID:
28836126
DOI:
10.1186/s11671-017-2256-9

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