Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management

Abstract

The role of mycobacterial efflux pumps in drug-resistant tuberculosis has been widely reported. Recently, a new compound, named SS13, has been synthesized, and its activity as a potential efflux inhibitor has been demonstrated. In this work, the chemical–physical properties of the SS13 were investigated; furthermore, a formulative study aimed to develop a formulation suitable for oral administration was performed. SS13 shows nonintrinsic antitubercular activity, but it increases the antitubercular activity of all the tested drugs on several strains. SS13 is insoluble in different simulated gastrointestinal media; thus, its oral absorption could be limited. Solid lipid nanoparticles (SLNs) were, therefore, developed by using two different lipids, Witepsol and/or Gelucire. Nanoparticles, having a particle size (range of 200–450 nm with regards to the formulation composition) suitable for intestinal absorption, are able to load SS13 and to improve its permeation through the intestinal mucosa compared to the pure compound. The cytotoxicity is influenced by the concentration of nanoparticles administered. These promising results support the potential application of these nanocarriers for increasing the oral permeation of SS13 in multidrug-resistant tuberculosis management.

Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin

“…The above results demonstrated that QT–NSSPE could significantly improve the oral bioavailability of QT, which may be responsible for the follow reasons: (a) Most of QT in QT–NSSPE was in the form of nanocrystals, the smaller size and larger surface area of nanocrystals lead to higher dissolution rate, hence increasing the oral bioavailability of poorly water-soluble drugs [ 52 , 53 ]. (b) With an oily inner core of emulsion droplets, QT–NSSPE had partially characteristic of type I lipid formulations [ 54 ].…”

Transmucosal Solid Lipid Nanoparticles to Improve Genistein Absorption via Intestinal Lymphatic Transport

“…Alongside this, an untreated intestinal mucosa was used as a control. The intestine sections were placed on a 12-well cell culture plate that had been suitably modified (project INCREASE SARDINIA 2016-17, protocol number 31351, University of Sassari) [ 31 ] and previously filled with PBS (pH 6.8). An exact amount of sample (200 µl of F-SLN and fluorescein solution, corresponding to 0.1 mg of fluorescein) was placed on the mucosal surface of the intestine segments, and the plate was positioned in the incubator shaker apparatus at 25 °C and 150 rpm.…”

Surfactant-Free Chitosan/Cellulose Acetate Phthalate Nanoparticles: An Attempt to Solve the Needs of Captopril Administration in Paediatrics

“…The NP-C spectrum exhibits similar bands to NP-Cb, and it does not show the characteristic peak of CAT at 2566 cm −1 which is, however, visible in the physical mixture. This absence could be ascribed to the loading of CAT in the polymer matrix [37] or molecular interactions with the NP components that are not developed in the physical mixture and could be responsible for the shoulder at 2600-2450 cm −1 (Figure 3). In the physical mixture, the peak at 1747 cm −1 related to the carboxylic group of CAT is also evident.…”