The aim of this study was to develop and evaluate a curcumin (Cur) nanoemulsion (NE) and enhance transdermal drug delivery. The comparative effects of Cur-NE were evaluated in terms of wound healing and anti-inflammatory action. Clove oil (oil), Tween-80 (surfactant), and PEG-400 (co-surfactant) were selected on the basis of their solubility and maximum nanoemulsion region. An aqueous micro-titration method with high-energy ultrasonication was used for the preparation of Cur-NE. This method was optimized to find the best NE, followed by a five-factor, three-level, central composite design. % oil, % S_mix, ultrasonication time (min), ultrasonication intensity (%), and temperature (°C) were selected and optimized as independent variables. The optimized NE had parameters of 5.0% oil, 10% S_mix, ultrasonication time (10 min), 40% ultrasonication intensity and 50 °C temperature, which were applied as independent and dependent variables. On the basis of experimental data of the dependent variables, we calculated a hydrodynamic diameter of 93.64 ± 6.48 nm, transmittance of 98.64 ± 0.37%, and PDI of 0.263 ± 0.021. TEM and SEM results revealed the smooth and spherical shape of the particles in the NE, with a zeta potential of −11.67 ± 0.11, refractive index of 1.71 ± 0.034, viscosity of 37 ± 7 cp, pH of 7.4 ± 0.07, and drug content of 98.11 ± 0.16% for the optimized Cur-NE. Cur-NE optimization with clove oil, Tween-80, and PEG-400 might be useful for enhancing the skin permeation of Cur. In conclusion, Cur-NE played a significant role in wound healing and exhibited anti-inflammatory effects, demonstrating its potential as a nanoformulation for safe and nontoxic transdermal delivery.

Here, the aim is to improve the bioavailability of Naringenin (NRG) in brain and to establish the highest remedial benefit from a novel anti-ischemic medicine i.e. NRG. A novel Naringenin-loaded-nanoemulsion (NE)-(in situ)-gel (i.e. thermoresponsive), was formulated with the help of Poloxamer-407 (20.0% w/v). Chitosan (CS, 0.50% w/v) was used to introduce the mucoadhesive property of NE-(in situ)-gel and finally called as NRG-NE-gel + 0.50%CS. A novel UHPLC-ESI-Q-TOF-MS/MS-method was optimized and used for NRG-NE-gel + 0.50%CS to quantify the Pharmacokinetic-(PK)-parameters in plasma as well as brain and to evaluate the cerebral ischemic parameters after MCAO i.e. locomotor activity, grip strength, antioxidant activity, and quantity the infarction volume in neurons with the safety/toxicity of NRG-NE-gel + 0.50%CS after i.n. administration in the rats. The mucoadhesive potency and gelling temperature of NRG-NE-gel + 0.50%CS were observed 6245.38 dynes/cm2 and 28.3 ± 1.0 °C, respectively. Poloxamer-407 based free micelles size was observed 98.31 ± 1.17 nm with PDI (0.386 ± 0.021). The pH and viscosity of NRG-NE-gel + 0.50%CS were found to be 6.0 ± 0.20 and 2447 ± 24cp (at 35.0 ± 1.0 °C temperature), respectively. An elution time and m/z NRG were observed 1.78 min and 270.97/150.96 with 1.22 min and m/z of 301.01/150.98 for Quercetin (IS) respectively. Inter and intra %precision and %accuracy was validated 1.01-3.37% and 95.10-99.30% with a linear dynamic range (1.00 to 2000.00 ng/ml). AUC0-24 of plasma & brain were observed 995.60 ± 24.59 and 5600.99 ± 144.92 (ng min/ml g) in the rats after the intranasal (i.n.) administration of NRG-NE-gel + 0.50%CS. No toxicological response were not found in terms of mortalities, any-change morphologically i.e. in the microstructure of brain as well as nasal mucosa tissues, and also not found any visual signs in terms of inflammatory or necrosis. Intranasally administered NRG-NE-gel + 0.50%CS enhanced the bioavailability of Naringenin in the brain. In the cerebral ischemic rats, significantly improved the neurobehavioral activity (locomotor & grip strength) followed by antioxidant activity as well as infarction volume. Finally, the toxicity studies carried out and established the safe nature of optimized-NRG-NE-gel + 0.50%CS.

The aim of this study was to investigate the brain targeting potential of rasagiline-encapsulated chitosan-coated PLGA nanoparticles (RSG-CS-PLGA-NPs) delivered intranasally into the brain. Chitosan-coated PLGA nanoparticles (RSG-CS-PLGA-NPs) were developed through double emulsification-solvent evaporation technique. RSG-CS-PLGA-NPs were characterized for particle size, zeta potential, size distribution, encapsulation efficiency, and in vitro drug release. The mean particle size, polydispersity index, and encapsulation efficiency were found to be 122.38 ± 3.64, 0.212 ± 0.009, and 75.83 ± 3.76, respectively. High-performance liquid chromatography–mass spectroscopy and mass spectroscopy study showed a significantly high mucoadhesive potential of RSG-CS-PLGA-NPs and least for conventional and homogenized nanoformulation. Pharmacokinetic results of RSG-CS-PLGA-NPs in Wistar rat brain and plasma showed a significantly high (**p < 0.005) AUC_0-24 and amplified C_max over intravenous treatment group. Finally, the investigation demonstrated that intranasal delivery of mucoadhesive nanocarrier showed significant enhancement of bioavailability in brain, after administration of the RSG-CS-PLGA-NPs which could be a substantial achievement of direct nose to brain targeting in Parkinson’s disease therapy and related brain disorders.