pH-Responsive Controlled-Release Nanocarriers


CD Bioparticles offers custom services to stimuli-responsive controlled-release nanocarriers using advanced techniques. Our experienced scientists have created a comprehensive platform to design the pH-responsive of controlled-release nanocarriers in order to improve the capability of controlled-release drug delivery system.

Introduction to pH-responsive Controlled-release Nanocarriers

To protect healthy tissues from toxic drugs and to prevent drug decomposition, controlled drug delivery systems has been designed to control drug release at special time and space on demand. Biological pH responsive drug delivery system is easy to achieve because human body exists variations in pH. In addition, cancer cells have a more acidic environment compared with normal cells. Furthermore, tumor and inflammatory tissues are more acidic than normal tissues and blood which is mainly caused by high glycolysis rate and high level of CO2. Therefore, the abnormal pH gradients provide opportunities to achieve pH-responsive controlled drug delivery systems for cancer treatment.

In general, either or both of the corona and core part of the pH-responsive nanoparticles will respond to the external pH to change their soluble/insoluble or charge states. A series of MSN-based stimuli-responsive systems have been shown as a good example. The caps such as polyamine and DNA were linked on the surface of MSNs through electrostatic attraction and were uncapped from MSNs under low pH condition. By contrast, the caps including supramolecular stoppers and inorganic nanoparticles were anchored on the surface of the MSNs by acid-labile bonds such as in acetals. The third gating mechanism involves the reversible reaction between polyalcohols and boronic acids to form boronate esters. While at pH 2.0-4.0, the hydrolysis of the boroester bond took place and thus resulted in a rapid release of the entrapped drug.

Figure 1. Graphical representation of the pH-responsive MSNs capped with polymers (A) and nanoparticles (B) that linked to the surface of MSNs via pH-sensitive linkers. (Ke-Ni Yang, et al. Cancer Biol Med. 2014,11:34-43.)

Key Features of pH-responsive Controlled-release Nanocarriers

  • Controlled-release nanocarriers can protect healthy tissues from toxic drugs and decrease the side-effects by releasing in target tissues.
  • pH-responsive controlled-release is easy to achieve for cancer treatment due to its more acidic environment.
  • Controlled drug release at special time and space on demand.
  • Controlled-release can be achieved with a ‘zero release’ effect in blood circulation.
  • Controlled-release can prevent drug decomposition.

pH-responsive Controlled-release Nanocarriers Applications

Various materials can be used as gatekeepers to control drug release under acidic conditions to broaden the application of nanoparticles in pH-responsive controlled-release system. This technology has great potential for application in tumor therapy and for improving anti-cancer drug efficiency and decreasing side effects. However, most work is focused on in vitro studies, more customized manipulation of the pH-responsive drug delivery system in vivo via pH change need to be done to improve its therapeutic application.

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References:
1. Chun-Ling Z., et al. Cell microenvironment stimuli-responsive controlled-release delivery systems based on mesoporous silica nanoparticles. Journal of food and drug analysis. 2014, 22: 18-28.
2. Ke-Ni Yang, et al. pH-responsive mesoporous silica nanoparticles employed in controlled drug delivery systems for cancer treatment. Cancer Biol Med. 2014,11: 34-43.
3. Weiwei G. et al. pH-responsive nanoparticles for drug delivery. Molecular Pharmaceutics. 2010, 7(6): 1913–1920.

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