Oral bacterial infections are fairly common in patients with diabetes mellitus; however, due to limited treatment options, herbal medicines are considered an alternate solution. This study aimed to formulate a stable essential-oil-loaded nanoemulsion for the treatment of oral bacterial infections. Essential oils from edible sources including coriander, clove, cinnamon and cardamom were extracted by hydrodistillation. The response surface methodology was used to optimize the nanoemulsion formulation by applying the Box–Behnken design. The oil concentration, surfactant concentration and stirring speed were three independent factors, and particle size and polydispersity index were two responses. The particle size, polydispersity index and zeta potential of the optimized formulation were 130 mm, 0.222 and −22.9, respectively. The ATR-FTIR analysis revealed that there was no incompatibility between the active ingredients and the excipients. A significant release profile in active ingredients of nanoemulsion, i.e., 88.75% of the cinnamaldehyde and 89.33% of eugenol, was recorded after 24 h. In the ex vivo goat mucosal permeation study, 71.67% of the cinnamaldehyde permeated and that of the eugenol 70.75% from the nanoemulsion. The optimized formulation of the essential-oil-loaded nanoemulsion showed a 9 mm zone of inhibition against Staphylococcus aureus and Staphylococcus epidermidis, whereas in anti-quorum sensing analysis, the optimized nanoemulsion formulation showed an 18 mm zone of inhibition. It was concluded that formulated essential-oil-loaded nanoemulsion can be used against S. epidermidis and S. aureus infections in oral cavity.
Nanoparticles are used increasingly for the treatment of different disorders, including burn wounds of the skin, due to their important role in wound healing. In this study, acriflavine-loaded poly (ε-caprolactone) nanoparticles (ACR-PCL-NPs) were prepared using a double-emulsion solvent evaporation method. All the formulations were prepared and optimized by using a Box–Behnken design. Formulations were evaluated for the effect of independent variables, i.e., poly (ε-caprolactone) (PCL) amount (X1), stirring speed of external phase (X2), and polyvinyl alcohol (PVA) concentration (X3), on the formulation-dependent variables (particle size, polydispersity index (PDI), and encapsulation efficiency) of ACR-PCL-NPs. The zeta potential, PDI, particle size, and encapsulation efficiency of optimized ACR-PCL-NPs were found to be −3.98 ± 1.58 mV, 0.270 ± 0.19, 469.2 ± 5.6 nm, and 71.9 ± 5.32%, respectively. The independent variables were found to be in excellent correlation with the dependent variables. The release of acriflavine from optimized ACR-PCL-NPs was in biphasic style with the initial burst release, followed by a slow release for up to 24 h of the in vitro study. Morphological studies of optimized ACR-PCL-NPs revealed the smooth surfaces and spherical shapes of the particles. Thermal and FTIR analyses revealed the drug–polymer compatibility of ACR-PCL-NPs. The drug-treated group showed significant re-epithelialization, as compared to the controlled group.
This study aimed to synthesise montelukast-loaded polymeric nanoparticles via the ionic gelation method using chitosan as a natural polymer and tripolyphosphate as a crosslinking agent. Tween 80, hyaluronic acid and leucine were added to modify the physicochemical properties of nanoparticles, reduce the nanoparticles’ uptake by alveolar macrophages and improve powder aerosolisation, respectively. The nanoparticles ranged from 220 nm to 383 nm with a polydispersity index of ≤0.50. The zeta potential of nanoparticles ranged from 11 mV to 22 mV, with a drug association efficiency of 46–86%. The simple chitosan nanoparticles (F2) were more spherical in comparison to other formulations (F4–F6), while the roughness of hyaluronic acid (F5) and leucine (F6) added formulations was significantly high er than F2 and Tween 80 added formulation (F4). The DSC and FTIR analysis depict that the physical and chemical properties of the drug were preserved. The release of the drugs from nanoparticles was more sustained in the case of F5 and F6 when compared to F2 and F4 due to the additional coating of hyaluronic acid and leucine. The nanoparticles were amorphous and cohesive and prone to exhalation due to their small size. Therefore, nanoparticles were admixed with lactose microspheres to reduce particle agglomeration and improve powder dispersion from a dry powder inhaler (DPI). The DPI formulations achieved a dispersed fraction of 75 to 90%, a mass median aerodynamic diameter (MMAD) of 1–2 µm and a fine particle fraction (FPF) of 28–83% when evaluated using the Anderson cascade impactor from Handihaler®. Overall, the montelukast-loaded nanoparticles physically admixed with lactose microspheres achieved optimum deposition in the deep lung for potential application in asthmatic patients.
1. IntroductionTypically, the design and characterization of drug delivery systems are based on the synthetic features of the drug, such as particle size, morphology, surface charge, composition, l...