Nanoparticle-Based Rifampicin Delivery System Development

Abstract

The alkaline milieu of chronic wounds severely impairs the therapeutic effect of antibiotics, such as rifampicin; as such, the development of new drugs, or the smart delivery of existing drugs, is required. Herein, two innovative polyelectrolyte nanoparticles (PENs), composed of an amphiphilic chitosan core and a polycationic shell, were synthesized at alkaline pH, and in vitro performances were assessed by 1H NMR, elemental analysis, FT-IR, XRD, DSC, DLS, SEM, TEM, UV/Vis spectrophotometry, and HPLC. According to the results, the nanostructures exhibited different morphologies but similar physicochemical properties and release profiles. It was also hypothesized that the simultaneous use of the nanosystem and an antioxidant could be therapeutically beneficial. Therefore, the simultaneous effects of ascorbic acid and PENs were evaluated on the release profile and degradation of rifampicin, in which the results confirmed their synergistic protective effect at pH 8.5, as opposed to pH 7.4. Overall, this study highlighted the benefits of nanoparticulate development in the presence of antioxidants, at alkaline pH, as an efficient approach for decreasing rifampicin degradation.

Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

“…The FTIR spectra of the drug (rifampicin), formulated rifampicin microfibers and polymers used are shown in Figure 4 . The FTIR drug rifampicin spectrum showed a peak of 3472 cm −1 (NH stretching), 2894 cm −1 (C-H bonding), 1629 cm −1 (C=O), 1478 cm −1 (C=C), 1379 cm −1 (CH2, C=C), 1059 cm −1 (-CH, CO, C-H), and 987 cm −1 (≡C-H, C-H) [ 18 ]. The IR range of alginate had characteristic absorption peaks at 3311 cm −1 , which showed OH stretching, 1612 cm −1 , which showed carboxylic C=O, 1298 cm −1 , which possessed C-CH, 1086 and 1059 cm −1 , ascribed to C-O stretching, 1032 cm −1 , which represented C-C, 942 cm −1 , which showed C-O, 888 cm −1 , which manifested CH, and 822 cm −1 , which represented Na-O [ 19 ].…”

Effect of CYP3A4 Inhibitors and Inducers on Pharmacokinetics and Pharmacodynamics of Saxagliptin and Active Metabolite M2 in Humans Using Physiological-Based Pharmacokinetic Combined DPP-4 Occupancy

“…The input parameters of saxagliptin and metabolite M2 for the PBPK-DO model are given in Table 1 ( Rodgers et al, 2005 ; Kim et al, 2006 ; Rodgers and Rowland, 2006 ; Su et al, 2012 ; Qian et al, 2019 ). The corresponding parameters of inhibitors/inducers are listed in Supplementary Tables S1–S3 ( Rodgers et al, 2005 ; Zhou et al, 2005 ; Rodgers and Rowland, 2006 ; Usach et al, 2013 ; Qian et al, 2019 ; Motiei et al, 2021 ; Lanni et al, 2021 ). The physiological parameters in humans are presented in Supplementary Table S4 ( Li et al, 2012 and Qian et al, 2019 ) 6 .…”

In SituBiosynthesis of a Metal Nanoparticle Encapsulated in Alginate Gel for Imageable Drug-Delivery System

“…We adopted rifampicin (RIF) and doxorubicin (DOX) as the model drugs to prove that the developed drug-delivery system is applicable regardless of solubility in aqueous solution. Although these drugs are effective chemotherapeutic agents (RIF for antituberculosis and DOX for anticancer), they are mainly administered intravenously due to poor solubility and rapid hydrolysis in gastric conditions. − Normally, oral drugs go through the hostile surroundings of the acidic gastric media (pH 1.0–3.0), which deteriorates their pharmaceutical property due to the reaction with gastric acid, while they should have reached the intestine (pH 6.0–7.0) to work . Fortunately, alginate gel has the capability to retain its containing substances under an acidic environment but quickly diffuses in the intestinal media where the pH ranges from 6.0 to 7.0 as a consequence of its changeable network structure depending on the surrounding pH. , …”