Development and Optimization of Nanoemulsion from Ethanolic Extract of Centella asiatica (NanoSECA) Using D-Optimal Mixture Design to Improve Blood-Brain Barrier Permeability

Abstract

The evidence on the neuroprotective impact of Centella asiatica (C. asiatica) has been greatly documented in recent years. However, a major obstacle that remains to be overcome is the capacity of the active molecules in C. asiatica to cross the blood-brain barrier (BBB). In this study, we explored the possibilities of using a D-optimal mixture design to fabricate nanoemulsion of C. asiatica (NanoSECA) for better brain bioavailability. The parameters for optimization were the percentage of water (10–80% w/v) and virgin coconut oil (VCO) (10–80% w/v). Nanoemulsions were formulated using a high-pressure homogenization approach and were characterized for their physicochemical properties. The optimal VCO-based nanoemulsion (VBN: F2) conditions were found at 80% (w/v) of water and 10% (w/v) of VCO. Subsequently, viability tests were conducted on neuroblastoma (SH-SY5Y) and macrophage (RAW 264.7) cell lines. NanoSECA was distinguished for its antioxidant, acetylcholinesterase (AChE), anti-inflammatory, and parallel artificial membrane permeability assay (PAMPA) activities in vitro. The NanoSECA has a particle size of 127.833 ± 8.280 nm, zeta potential (ZP) of −24.9 ± 0.011 mV, polydispersity index (PDI) of 0.493 ± 4.681, percentage prediction error (PPE) of −12.02%, and pH of 6.0 ± 0.006 and is also stable under different storage conditions. Cell viability was improved in a dose-dependent manner on SH-SY5Y and RAW 264.7 cell lines. In addition, NanoSECA significantly reduced the AChE activity, suppressing the level of proinflammatory mediators and oxidative stress. Moreover, NanoSECA showed high BBB permeation with a high value of experimental permeability to cross the BBB. Thus, NanoSECA could efficiently potentiate the central nervous system (CNS) therapeutic activities through enhanced penetration of BBB. These nano-delivery systems are crucial to unlock the full potential of C. asiatica for treating numerous CNS disorders.

Quantification of Xanthone and Anthocyanin in Mangosteen Peel by UPLC-MS/MS and Preparation of Nanoemulsions for Studying Their Inhibition Effects on Liver Cancer Cells

“…Comparatively, the mean particle sizes of xanthone and anthocyanin nanoemulsions prepared in our study were smaller than those reported by Jusril [ 36 ] and Bamba et al [ 37 ], with the former using coconut oil, Tween 80, Span 80, and ethyl acetate extract from mangosteen peel to prepare a xanthone nanoemulsion with the mean particle size at 181 nm, and the latter using corn oil, polyglycerol polyricinoleate, and ethanol extract from blueberry pomace to prepare a water-in-oil-in-water anthocyanin nanoemulsion with the mean particle size at 400 nm. Obviously, the difference in mean particle size of the nanoemulsion can be attributed to the variation in oil, surfactant and solvent varieties as well as the extraction method.…”

Nanotechnology-driven wound healing potential of asiaticoside: a comprehensive review

“…346 Advanced nanotechnological approaches, such as stimulus-responsive or smart delivery systems, may enable the on-demand release of AC, responding to specific cues present in the wound microenvironment for precise and timely therapeutic interventions. 347 Moreover, the incorporation of innovative biomaterials and bioengineering techniques may facilitate the development of multifunctional scaffolds or dressings capable of simultaneously providing structural support, promoting tissue regeneration, and delivering AC in a controlled manner. 348 Additionally, combining AC with other bioactive agents or growth factors within nanocarriers could potentially create synergistic therapeutic effects, accelerating wound closure, reducing inflammation, and minimizing scar formation.…”

Formulation and Characterization of Non-Toxic, Antimicrobial, and Alcohol-Free Hand Sanitizer Nanoemulgel Based on Lemon Peel Extract

“…The PDI is a valuable parameter to evaluate the stability of the nanoemulgel formulation, representing the distribution of a population's size within a given sample [48]. Since all LN formulations presented a PDI value lower than 0.5, it indicates a narrow and uniform particle size distribution within all samples [49]. On the other hand, the zeta potential is a relevant factor to assess the stability of nanosuspensions.…”