Challenges in Coopted Hydrophilic and Lipophilic Herbal Bioactives in the Same Nanostructured Carriers for Effective Bioavailability and Anti-Inflammatory Action.

Teodora-Alexandra Iordache,Ioana Lacatusu,Nicoleta Badea,Mirela Mihaila,Simona Crisan,Anca Lucia Pop

doi:10.3390/nano11113035

Teodora-Alexandra Iordache, Ioana Lacatusu + Show 4 more

Open Access

https://doi.org/10.3390/nano11113035

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Abstract

There is ongoing research on various herbal bioactives and delivery systems which indicates that both lipid nanocarriers and herbal medicines will be fine tunned and integrated for future bio-medical applications. The current study was undertaken to systematically develop NLC-DSG-yam extract for the improved efficacy of herbal Diosgenin (DSG) in the management of anti-inflammatory disorders. NLCs were characterized regarding the mean size of the particles, morphological characteristics, physical stability in time, thermal behaviour, and entrapment efficiency of the herbal bioactive. Encapsulation efficiency and in vitro antioxidant activity measured the differences between the individual and dual co-loaded-NLC, the co-loaded one assuring a prolonged controlled release of DSG and a more emphasized ability of capturing short-life reactive oxygen species (ROS). NLCs safety properties were monitored following the in vitro MTS ((3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay) and RTCA (Real-Time Cell Analysis) assays. Concentrations less than 50 μg/mL showed no cytotoxic effects during in vitro cytotoxicity assays. Besides, the NLC-DSG-yam extract revealed a great anti-inflammatory effect, as the production of pro-inflammatory cytokines (TNF-alpha, IL-6) was significantly inhibited at 50 μg/mL NLC (e.g., 98.2% ± 1.07 inhibition of TNF-α, while for IL-6 the inhibition percentage was of 62% ± 1.07). Concluding, using appropriate lipid nanocarriers, the most desirable properties of herbal bioactives could be improved.

Highlights

Herbal bioactives are gaining more interest as components of novel formulations, adding health beneficial properties due to their reduced toxicity compared with synthetic ingredients
nanostructured lipid carriers (NLC) are appropriate carriers for hydrophobic drugs, this study demonstrated the adaptability of these lipophilic delivery systems for effectively capturing the hydrophilic principles as wild yam extract (Yam)
The size and morphology of the lipid nanocarriers loaded with DSG and wild yam extract were provided by the ZC phase contrast micrographs (Figure 1)

Summary

Introduction

Herbal bioactives are gaining more interest as components of novel formulations, adding health beneficial properties due to their reduced toxicity compared with synthetic ingredients. The bioactive phytochemicals from various plants have been used to treat health problems for a long time [1]. Many bioactive phytochemicals, such as polyphenols, flavonoids, steroids, terpenoids, and alkaloids from medicinal plants, have been used as precursors for several synthetic and semisynthetic drugs [2]. Administration of herbal drugs, is not always the most efficacious approach. The effectiveness of herbal bioactives depends on the active compound’s bioavailability over a sustained period. Most herbal bioactives manifest low bioavailability [3].

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