Preparation of Cell Penetrating Peptides-Mediated Targeting Drug Liposomes

Biological membrane is the inevitable barrier needed to cross when liposomes try delivering drugs into cells, tissues, and organs for their biological actions. One of the most promising methods to overcome this barrier is based on the use of cell penetrating peptides (CPPs). Development of CPPs mediated targeting drug liposomes has focused on creating approaches for delivering bioactive molecules, especially for proteins and gene drugs, to cells and for enhancing their stability in vitro and in vivo. The most common type of various CPPs is cationic CPPs, which are positively charged and can enter cells when added exogenously. Here, we describe a mature approach based on thin film hydration method for cationic CPPs modified targeting drug liposomes (drug/CPPs-Lip) preparation. The formation of drug/CPPs-Lip depends on a number of experimental variables. The grafting method and location as well as the modification density of CPPs on liposomes strongly affect the activity and transmembrane capability of CPPs-drug/Lip. In addition, the control of experimental parameters such as temperature, hydration time, and sonicating frequency influences the final characteristics of the CPPs-drug/Lip, such as size, surface zeta potential, drug encapsulation efficiency, drug loading amount, stability, and reproducibility. The method presented in this chapter could be helpful to prepare reliable and reproducible drug/CPPs-Lip and according experimental results.