Multifunctional nanoparticles have been identified as a promising drug-delivery system for sustainable drug release. The structural and size tunability and disease-targeting ability of nanoparticles have made them more suitable for multiple drug loading and delivery, thereby enhancing therapeutic results through synergistic effects. Nanoparticulate carriers with specific features such as target specificity and stimuli-responsiveness enable selective drug delivery with lower potential side effects. In this review we have classified the recently published articles on polymeric and inorganic nanoparticle-mediated drug delivery into three different categories based on functionality and discussed their efficiency for drug delivery and their therapeutic outcomes in preclinical models. Most of the drug-loaded nanodelivery systems discussed have demonstrated negligible or very low systemic toxicity throughout the experimental period in animal models compared with free drug administration. In addition, some challenges associated with the translation of nanoparticle-based drug carrier responses to clinical application are highlighted.
Aim: A novel thermosensitive in situ gel loaded with meropenem (MP) liposomes was designed to improve retention in the oral cavity as a prophylactic measure to prevent ventilator-acquired pneumonia in critically ill patients. Methodology & results: Meropenem liposomes were incorporated into poloxamer 407 gels and gamma irradiated. Mean size of liposome was 247 nm, polydispersity index < 0.3 and zeta potential >-25 mV; properties remained unaltered even post sterilization. Permeation study revealed that 75.26% and 34% of MPs were released from MP in situ gel and MP in situ liposomal gel, respectively. The relation between viscosity (cp) and shear rate (1/s) indicate that in situ gels exhibited non-Newtonian behavior at 37°C. The study using Pseudomonas aeruginosa confirmed the antimicrobial activity of meropenem. Conclusion: Prolonged in situ residence, because of rapid gelation process enables an easy administration of meropenem as liposomal suspension in critically ill patients.
Aim: Negatively charged deformable liposomes (DL) of ketoprofen were formulated to enhance transdermal delivery of ketoprofen (KP) under the influence of iontophoresis for intraarticular delivery. Methods: Conventional and deformable KP liposomes were prepared using thin film hydration, characterized and intraarticular delivery of KP was evaluated using Sprague-Dawley rats. Results: Vesicles displayed entrapment efficiency (>71%); zeta potential <-25 mV; size between 152.4 ± 12.42 nm to 220.4 ± 6.22 nm, KP-DL were stable under iontophoresis. Conventional and deformable liposomes exhibited relatively higher iontophoretic flux values than passive flux; Iontophoretic delivery enhanced KP availability in the synovial fluid (1.34 ± 0.12 μg.h/ml) fourfold over passive delivery (0.329 ± 0.15 μg.h/ml). Conclusion: Iontophoretic mediated transport of deformable liposomes could improve transdermal delivery of ketoprofen into the synovial joints than conventional liposomes.
Human immunodeficiency virus (HIV)-infected individuals display an enhanced production of reactive oxygen species (ROS). This reduction of antioxidant capacity in host tissues has been related to the decrease in total levels of ROS scavengers such as glutathione (GSH). Prevention of opportunistic infections due to a weakened immune system is becoming a key strategy along with HIV elimination. Research in these directions is clearly warranted, especially a combination of antiretrovirals and antioxidants to ameliorate oxidative stress, improve intracellular uptake and target viral reservoirs. Hence, we aimed to formulate liposomes loaded with the antiretroviral drug efavirenz (EFA) in the presence of glutathione, as these carriers can be engineered to enhance the ability to reach the target reservoirs. The goal of the present work was to investigate the intracellular uptake of EFA-loaded liposome (with and without GSH) by human monocytic leukemia cells (THP-1 cells) and examine cell viability and ROS scavenging activity. Results obtained provided significant data as follows: (i) treatment with EFA and GSH combination could enhance the uptake and reduce cytotoxicity; (ii) encapsulation of EFA into liposomes increased its levels in the macrophages, which was further enhanced in the presence of GSH; (iii) delivery of EFA in the presence of GSH quenched the intracellular ROS, which was significantly higher when delivered via liposomes. Data revealed that a combination of EFA and GSH encompasses advantages; hence, GSH supplementation could be a safe and cost-effective treatment to slow the development of HIV infection and produce an immune-enhancing effect.
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