Encapsulation of
hydrophilic and amphiphilic drugs in appropriate
colloidal carrier systems for sustained release is an emerging problem.
In general, hydrophobic bioactive substances tend to accumulate in
water-immiscible polymeric domains, and the release process is controlled
by their low aqueous solubility and limited diffusion from the nanocarrier
matrix. Conversely, hydrophilic/amphiphilic drugs are typically water-soluble
and insoluble in numerous polymers. Therefore, a core–shell
approach—nanocarriers comprising an internal core and external
shell microenvironments of different properties—can be exploited
for hydrophilic/amphiphilic drugs. To produce colloidally stable poly(lactic-
co
-glycolic) (PLGA) nanoparticles for mitomycin C (MMC)
delivery and controlled release, a unique class of amphiphilic polymers—hydrophobically
functionalized polyelectrolytes—were utilized as shell-forming
materials, comprising both stabilization via electrostatic repulsive
forces and anchoring to the core via hydrophobic interactions. Undoubtedly,
the use of these polymeric building blocks for the core–shell
approach contributes to the enhancement of the payload chemical stability
and sustained release profiles. The studied nanoparticles were prepared
via nanoprecipitation of the PLGA polymer and were dissolved in acetone
as a good solvent and in an aqueous solution containing hydrophobically
functionalized poly(4-styrenesulfonic-
co
-maleic acid)
and poly(acrylic acid) of differing hydrophilic–lipophilic
balance values. The type of the hydrophobically functionalized polyelectrolyte
(HF-PE) was crucial for the chemical stability of the payload—derivatives
of poly(acrylic acid) were found to cause very rapid degradation (hydrolysis)
of MMC, in contrast to poly(4-styrenesulfonic-
co
-maleic
acid). The present contribution allowed us to gain crucial information
about novel colloidal nanocarrier systems for MMC delivery, especially
in the fields of optimal HF-PE concentrations, appropriate core and
shell building materials, and the colloidal and chemical stability
of the system.