Development of Innovative Polymer-Based Matricial Nanostructures for Ritonavir Oral Administration

Abstract

Ritonavir is used in the treatment of pediatric human immunodeficiency virus infection. The aim of this study was to develop and evaluate innovative polymer-based matricial nanostructures containing ritonavir for a sustained delivery. Two formulations were prepared by interfacial deposition of preformed polymers using Eudragit® RS100 in combination with Polycaprolactone triol 300 (NPR-300) or Polycaprolactone triol 900 (NPR-900). Ritonavir (1 mg mL-1) was incorporated in the formulations. NPR-300 showed a mean size of 559 nm, SPAN of 1.66, zeta potential of 5.9 mV, pH of 4.23, drug content of 73%, and stability under storage for 15 days. NPR-900 showed a mean size of 120 nm, SPAN of 0.83, zeta potential of 7.0 mV, pH of 4.2, drug content of 81%, and stability under storage for 60 days. The ritonavir content was 100% incorporated in both formulations. TEM images demonstrated spherical matricial structures. The ritonavir release in the simulated gastric medium was controlled by incorporation into the nanoparticles, especially into NPR-900. The formulations showed mucoadhesive properties, and the taste evaluation by an in vivo sensory panel indicated that particle size might influence taste perception since the formulation with the larger size of the nanoparticles (NPR-300) worsened the taste of the suspension. The NPR-900 was the most promising nanoparticle formulation for oral delivery of ritonavir.

Nanocapsules containing Saussurea lappa essential oil: Formulation, characterization, antidiabetic, anti-cholinesterase and anti-inflammatory potentials

“…Simultaneously with the emergence of plant-based drug formulations, the pharmaceutical field has known during the last era a steady growth in investment in nanotechnology in order to improve existing treatments and develop novel therapies (Matteucci et al, 2018). Polymeric nanoparticles (NP) have been proposed as a novel approach to overcome difficulties encountered in traditional drug delivery such as poor aqueous solubility, low bioavailability, poor stability and bitter taste (Giaretta et al, 2019;Ma and Williams, 2018;Umerska et al, 2018). Sonaje et al (2010) noticed an enhanced intestinal absorption of insulin, a prolonged reduction in blood glucose levels and an increased bioavailability upon insulin encapsulation in chitosan/ poly(γ-glutamic acid) based NP.…”

Lamivudine and Zidovudine-Loaded Nanostructures: Green Chemistry Preparation for Pediatric Oral Administration

“…The formulation MN, on the other hand, did not demonstrate mucoadhesiveness (MI = 0.99). An increase in particle size indicates the nanoformulation aggregated with the mucin particles, thus having an affinity for them [ 18 , 58 ]. The results indicate that the mucin is partially adsorbed on the surface of the nanostructures, while a remaining amount was kept free in the solution, with respect to the PN formulation.…”

“…Mucin solution was prepared in water at 0.25 % ( w/v ) concentration under magnetic stirring at room temperature. Aliquots of nanostructures were mixed with mucin solution (1:1) at 37 °C for 2 h. The resulting solutions were evaluated regarding mucoadhesion index (MI) [ 18 ]. The MI were calculated according to Equation (3): MI = Dh2/Dh0 where Dh0 and Dh2 are the average particle sizes before and after contact with mucin, respectively.…”

Advanced 3D Electrospinning “Xspin” System: Fabrication of Bifiber Floating Oral Pharmaceutical Scaffolds for Controlled Drug Delivery

“…Additionally, researchers such as Sinha et al formed a solid dispersion (SD) of RTV and Gelucire through a eutectic mixture in a 1:4 ratio . Giaretta et al investigated polymer-based matricial nanostructures containing RTV, achieving sustained delivery with over 60% dissolution within the first 2 h . Karakucuk et al explored a nanosuspension dosage form that improved RTV solubility to 100% within the first hour, although it did not provide a sustaining effect. , …”