Amphiphilic poly-N-vinylpyrrolidone nanoparticles as carriers for non-steroidal anti-inflammatory drugs: Characterization and in vitro controlled release of indomethacin

Abstract

Abstract. Novel amphiphilic poly-N-vinylpyrrolidone derivatives with different molecular weight of hydrophilic PVP fragment and one secondary di-n-alkyl terminal hydrophobic fragment of different length were synthesized to compare their inclination for formation of nano-scaled micelle-like aggregates in aqueous media with previously studied primary n-alkyl terminated poly-N-vinylpyrrolidones. The behavior of amphiphilies in water solutions was studied and critical aggregation concentration values for prepared polymer samples were determined by fluorescence spectroscopy and compared with those for primary n-alkyl derivatives. Polymeric micelle-like particles with or without encapsulated drug were prepared using dialysis or solvent evaporation techniques. Indomethacin was incorporated into hydrophobic inner core of these nanoparticles as a typical model drug. Dynamic light-scattering studies determined that the average size of particles formed was from 90 nm up to 600 nm with monodisperse size distribution and the nanoparticle size slightly increased with the amount of indomethacin encapsulated into inner core of the particles. In vitro release experiments carried out at different medium pH values using indomethacin-loaded nanoparticles exhibited slow and steady drug release into the medium.

Amphiphilic Poly(N-vinylpyrrolidone) Nanoparticles Conjugated with DR5-Specific Antitumor Cytokine DR5-B for Targeted Delivery to Cancer Cells

“…For drugs entrapment or immobilization on the surface of the nanoparticles, the polymers are taken in concentrations several orders higher than their CMC (10 −6 -10 −4 M), when more complex aggregates of spherical morphology and larger sizes are formed [39]. The introduction of the drug into the system also influences the size of obtained nanoparticles [13,40]. Therefore, the obtained nanoparticle size (about 220 nm) correlates with our previous findings.…”

“…Amph-PVP-based nanocarriers were proposed for the delivery of non-steroidal antiinflammatory drugs [39,40] and for drug delivery into the cell nucleus [41]. Moreover, amphiphilic linear-dendritic block copolymers based on the linear PVP and dendritic phenylalanyl-lysine dipeptide were reported for the enzyme-responsive release of doxoru-bicin [42].…”

Biocompatible Colloidal Suspensions Based on Magnetic Iron Oxide Nanoparticles: Synthesis, Characterization and Toxicological Profile

“…This distribution of the cations is responsible for the total magnetization of the molecule (Marinca et al, 2016). Besides the metallic nanoparticles used as valuable tools to enhance the effectiveness of the current therapies and to increase the compliance of the patient to the treatments, there were described other types of nanoparticles engineered in this direction, such as: polymeric colloids, liposomes, solid lipid nanoparticles, cyclodextrins, and others (Kuskov et al, 2010; Medeiros et al, 2015; Soica et al, 2016). …”

Box–Behnken Design of Experiments of Polycaprolactone Nanoparticles Loaded with Irinotecan Hydrochloride

“…A high stability is achieved in the presence of an adequate level of the surfactant, which when increased beyond that level can lead to adverse effects on the size of the NPs [27]. Similarly, the interaction between the polymer and surfactant was shown to increase the size of the NPs, which is suggested to be due to increased hydrophobicity [28] The highest value of negative charge achieved in this model was −19.63 ± 2.56 mV by using 0, −1, and 1 levels equivalent to 108 mg, 3 mg, and 6% of the polymer, drug, and surfactant, respectively. The negative charge of the NPs could be due to the carbonyl groups of the PCL, which create a negative charge on the surface of the NPs.…”