Drug Delivery System Based on pH-Sensitive Biocompatible Poly(2-vinyl pyridine)-b-poly(ethylene oxide) Nanomicelles Loaded with Curcumin and 5-Fluorouracil

Abstract

<jats:p>Smart polymeric micelles (PMs) are of practical interest as nanocarriers for the encapsulation and controlled release of hydrophobic drugs. Two hydrophobic drugs, naturally-based curcumin (Cur) and synthetic 5-fluorouracil (5-FU), were loaded into the PMs formed by a well-defined pH-sensitive poly(2-vinyl pyridine)-b-poly(ethylene oxide) (P2VP90-b-PEO398) block copolymer. The influence of the drug loading on the micellar sizes was investigated by dynamic light scattering (DLS) and it appears that the size of the PMs increases from around 60 to 100 nm when Cur is loaded. On the contrary, the loading of the 5-FU has a smaller effect on the micellar sizes. This difference can be attributed to higher molar mass of Cur with respect to 5-FU but also to higher loading efficiency of Cur, 6.4%, compared to that of 5-FU, 5.8%. In vitro drug release was studied at pH 2, 6.8, and 7.4, and it was observed that the pH controls the release of both drugs. At pH 2, where the P2VP sequences from the “frozen-in” micellar core are protonated, the drug release efficiencies exceed 90%. Moreover, it was demonstrated, by in vitro assays, that these PMs are hemocompatible and biocompatible. Furthermore, the PMs protect the Cur against the photo-degradation, whereas the non-ionic PEO corona limits the adsorption of bovine serum albumin (BSA) protein on the surface. This study demonstrates that these pH-sensitive PMs are suitable for practical utilization as human-safe and smart, injectable drug delivery systems.</jats:p>

The Benefits of Smart Nanoparticles in Dental Applications

“…Atanase and collaborators [ 87 ] synthesized smart polymeric micelles (PMs) based on poly(2-vinyl pyridine)-b-poly(ethylene oxide) block copolymers as nanocarriers for the encapsulation and controlled release of natural and synthetic hydrophobic drugs. Studies have shown that PMs are sensitive to the pH and protect the natural drug (curcumin) against photodegradation.…”

Micellar Drug Delivery Systems Based on Natural Biopolymers

“…An ideal drug carrier must be biocompatible, biodegradable, non-toxic, and have the capability to release the loaded active principles at the desired site of action. Until now, a large number of inorganic and organic materials, which have been formulated as liposomes, organic and inorganic nanoparticles, and hydrogels, have been used as promising drug carriers [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. However, there is an increasing interest in using natural biopolymers for the elaboration of different types of drug delivery systems (DDS) due to their abundance in nature and characteristic features, such as sustainability, biocompatibility, and biodegradability [ 9 , 10 ].…”

Curcumin Loaded Nanoliposomes Localization by Nanoscale Characterization

“…To improve the bioavailability of fragile and hydrophobic drugs, nanocarriers have been developed to protect the encapsulated drug from enzymatic degradation, provide controlled release, alter their pharmacokinetics, prolong their residence in plasma, and improve their cytoprotective and antioxidant effects [ 12 , 13 ]. The targeted delivery and cellular internalization of curcumin are also improved by its encapsulation in nanoparticles and nanoemulsions [ 14 ].…”