A pH-responsive glycolipid-like nanocarrier for optimising the time-dependent distribution of free chemical drugs in focal cells

Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Bolin Cheng, Binbin Lu, Xuan Liu, Tingting Meng, Yanan Tan, Yun Zhu, Na Liu, Hong Yuan, Xuan Huang, Fuqiang Hu Though Drug delivery systems have achieved accumulation at tumor sites via passive targeting and active targeting, the therapeutic effects are far from perfect. The unsatisfactory results are mainly due to limited drug release from the nanocarriers at tumor sites, while the pharmacological activities of the drug are attributed to the concentration of the free drug and the time maintained at the pharmacological targets. A pH-responsive chitosan based glycolipid-like nanocarrier (CSO-FBA-SA) was fabricated by conjugating stearyl alcohol (SA) to chitosan oligosaccharide (CSO) with the linkage of 4-formylbenzoic acid (FBA). FBA was a kind of aromatic aldehyde carbonyl compounds, which can form the benzoic-imine bond. In the presence of a Schiff’s base structure, the carrier showed improved properties and could be quickly degraded in an acidic environment. In order to explore the process and mechanism of the nanocarriers in focal cells, the method for determining the intracellular concentration of released free doxorubicin was established, and the time-dependent change of the DOX-loaded micelles was revealed. The sight of drug release was also obtained with CLSM. The cytotoxicity of the CSO-FBA-SA/DOX against human breast cancer MCF-7 cells incr...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research