Exploring combined herbal extract-loaded phytoniosomes for antimalarial and antibacterial activity against methicillin-resistant Staphylococcus aureus.

Antibiotic resistance in the context of treating malarial infections is a major challenge in India. Home remedies such as thulasi leaves (Ocimum tenuiflorum), black pepper seeds (Piper nigrum), clove buds (Syzygium aromaticum), cinnamon bark (Cinnamomum verum), and nilavembu whole plant powder (Andrographis paniculata) were taken to explore antimalarial and methicillin-resistant Staphylococcus aureus (MRSA) activity. Among the five extracts, the best two extracts, C. verum and P. nigrum extract, showed the presence of Quercetin. Phytoniosomes were prepared by simple probe sonication with the two extracts and the resultant vesicles were in the size range of (319.7 nm). They showed significant (P < 0.001) antimalarial potency IC50 at 5.25 µg/ml against P. falciparum 3D7. In addition, their cytotoxicity (TC50) against Vero cell line was found to be > 100 µg/ml. The therapeutic index was found to be > 32 µg/ml. Phytoniosomes were converted to a capsule dosage form by lyophilization and this capsule was stable up to 90 days.

Phytochemical screening and cytotoxicity evaluation of crude extracts: Toxicity comparison of crude extracts and its ethosomal formulations.

BACKGROUND: Combined plant extracts of Phyllanthus niruri, Croton tiglium, and Zingiber officinale are reported to have potential pharmacological applications. Ethosomes have a unique ability of encapsulating drugs or plant extracts with varying hydrophobicities in the phospholipid bilayer. AIM: To explore cytotoxicity of the combined plant extracts and ethosome loaded combined plant extracts for topical delivery. To study effect of ethosomes loaded combined plant extracts using HaCaT cells model treated with testosterone. METHODS: Dried powder of plant was extracted with ethanol using Soxhlet and cold macerations. Total phenolic and flavonoid contents were also determined using established methods. The combined extract loaded ethosome formulation was prepared by solvent dispersion method. RESULTS: The plant extracts loaded ethosomes formulation with a vesicle size range 1524.6-167.7 nm was prepared. HaCaT cells treated with testosterone negative control showed an IC50 value of 27 ± 1.0. Thw standard marketed topical minoxidil (1% solution) treated cells with testosterone showed an IC50 value 33 ± 1.0 and the combined plant extracts loaded ethosomes with testosterone showed an IC50 value 30 ± 1.0. Morphological alterations of rat skin exposed to the combined plant extract loaded ethosomes solution were assessed and compared with untreated skin and negative control. CONCLUSION: The preclinical safety was investigated employing an in vitro cytotoxicity and histopathological study. The cell line study results confirmed that the combined plant extracts loaded ethosomes inhibits testosterone and increase cell viability closer to that of standard drug minoxidil. According to our histopathological study, the combined plant extract loaded ethosomal formulations did not cause any damage to the rat skin layer.