<p>Modification of fliposomes with a polycation can enhance the control of pH-induced release</p>

Abstract

PurposeNowadays, the development of stimuli-sensitive nanocontainers for targeted drug delivery is of great value. Encapsulation of a drug in a pH-sensitive liposomal container not only provides protective and transport functions, but also helps to create a system with a controlled release mechanism.MethodsIn this study, we investigated the influence of a cationic polypeptide on the pH-induced release of anticancer drug doxorubicin (DXR) from the anionic fliposomes – liposomes consisting of a neutral lipid, an anionic lipid (prone to interact with a polycation), and a lipid trigger (imparting the pH-sensitivity).ResultsFirst, we showed the possibility to control the pH-induced release by the simple modification of the anionic fliposomes with linear polylysine. Second, we optimized the fliposomal composition such that the obtained fliposomes responded to the pH changes only when complexed with the polycation (“turning on” the release). Finally, pH-induced release from the polylysine-modified anionic fliposomes was tested on an anticancer drug DXR.ConclusionWe have succeeded in developing “smart” stimuli-sensitive nanocontainers capable of tunable controlled release of a drug. Moreover, based on the data on release of a low molecular salt, one can predict the release profile of DXR.

Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir

“…For instance, the combination of a highly mucoadhesive polymer to increase vaginal retention [11] with another polymer capable of modulating the release of the drug [12] can achieve effective and long-lasting drug release in the vaginal mucosa. The combination of polyanionic polymeric layers with polycationic polymeric layers by means of this technique also produces polyelectrolyte multilayers (PEM) [13,14], with the advantage that these polymers have a pH-dependent behaviour [15,16]. This is of great interest when developing formulations for the prevention of sexual transmission of HIV, since accelerating vaginal drug release at the time of ejaculation can increase the effectiveness of the protection [17].…”

As1411-modified liposomes to enhance drug utilization and augment the anti-tumor efficacy

“…Nevertheless, their particle size of ~ 100 nm makes them susceptible to being captured by the liver's vascular network system, thereby reducing drug enhancement and utilization. In response, various Liposome nanoparticles that respond to the tumor microenvironment have been developed, including pH (Ibrahim et al 2014;Lokova and Zaborova 2019) and temperature-responsive nano-systems (Fu et al 2019;Bing et al 2018), that release drugs according to the tumor microenvironment, effectively mitigating premature drug release, leakage, and related issues. Although these designs reduce toxic drug side effects, the overall utilization rate remains low.…”