Amphotericin B is an antifungal drug used for the treatment of invasive fungal infections. However, its clinical use is limited due to its serious side effects, such as renal and cardiovascular toxicity. Furthermore, amphotericin B is administered in high doses due to its poor water solubility. Hence, it is necessary to develop an on-demand release strategy for the delivery of amphotericin B to reduce cytotoxicity. The present report describes a novel encapsulation of amphotericin B into lipase-sensitive polycaprolactone to form a nanocomposite. Nanocomposites were produced by the oil-in-water method and their physicochemical properties such as size, hydrodynamic diameter, drug loading, and zeta potential were determined. The in vitro release of amphotericin B was characterized in the presence and absence of lipase. The antifungal activity of the nanocomposites was verified against lipase-secreting Candida albicans, and cytotoxicity was tested against primary human dermal fibroblasts. In the absence of lipase, the release of amphotericin B from the nanocomposites was minimal. However, in the presence of lipase, an enzyme that is abundant at infection sites, a fungicidal concentration of amphotericin B was released from the nanocomposites. The antifungal activity of the nanocomposites showed an enhanced effect against the lipase-secreting fungus, Candida albicans, in comparison to the free drug at the same concentration. Furthermore, nanoencapsulation significantly reduced amphotericin B-related cytotoxicity compared to the free drug. The synthesized nanocomposites can serve as a potent carrier for the responsive delivery of amphotericin B in antifungal applications.
Ultrasmall cationic silver nanoparticles (AgNPs) have recently emerged as highly potent antimicrobial agents for the treatment of multidrug‐resistant bacteria and their biofilms. However, the clinical application of these cationic AgNPs is hampered by their poor stability and high reactivity in solution, leading to uncontrolled release of toxic silver ions. An ideal platform featuring broad‐spectrum antibacterial activity and high biocompatibility that prevents overexposure to silver ions, is therefore highly desirable. Herein, we explored a biocompatible and biodegradable polymer, poly(lactic‐co‐glycolic) acid (PLGA) as an effective carrier for the recently discovered polycationic silver nanoclusters (pAgNCs). These pAgNCs impregnated PLGA nanocomposites (pAgNCs@PLGA) were developed by water‐in‐oil‐in‐water (W1/O/W2) emulsion method and characterized by various analytical techniques. Our experimental results reveal that pAgNCs@PLGA had spherical morphology with an average diameter of ∼188 nm and consists of multiple ultrasmall (∼2 nm) pAgNCs at the polymeric core. The minimum inhibitory concentration of pAgNCs for Staphylococcus aureus and Pseudomonas aeruginosa were found to be 6.9 μg/mL. After impregnation within PLGA, the antimicrobial efficacy of our pAgNCs against Staphylococcus aureus and Pseudomonas aeruginosa remained consistent, while the nanocomposites were biocompatible at the minimum inhibitory concentration (MIC) against both bacteria. The pAgNCs@PLGA nanocomposite developed in this work may present a path forward to bring these highly potent pAgNCs into medical practice.
Rifampicin (RFP) is a first‐line drug used to treat a variety of infections, including wound infections but has limitations in its use due to its toxicity. Hence, an urgent need exists for the development of suitable carriers for the delivery of the antibiotic. In this study, a novel approach is introduced for drug administration, employing stimulus‐responsive carriers to achieve an on‐demand strategy. This innovative method aims to minimize the dosage and frequency of drug administration, consequently lowering cytotoxicity levels. We used the lipases‐sensitive polycaprolactone (PCL) to produce nanocomposites loaded with rifampicin (PCL−RFP NPs). Nanoparticles were prepared by a single‐step emulsion solvent evaporation method. The size distribution of blank nanoparticles (PCL NPs) and PCL−RFP NPs were 172±30 nm and 229±58 nm, respectively. The liberation of RFP from PCL−RFP NPs was monitored over a period of 72 h in the absence and the presence of lipase was 9.46±0.24 % and 53.3±3.33 %, respectively, indicating responsive behavior. The minimum inhibitory concentration to lipase‐expressing Staphylococcus aureus (S. aureus) of PCL−RFP NPs was significantly improved compared to the free drug. Cytotoxicity tests using human dermal fibroblasts showed that the nanocomposites had better biocompatible when compared to the free drug. These findings indicate that the developed nanocomposite carriers have the potential to be promising candidates for delivering antibiotics in the field of biomedicine.
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