The present study aims to investigate the major constituents of the essential oil from Zingiber cassumunar rhizome (EO) and to develop microemulsions with enhanced chemical stability and anti-inflammatory activity of EO. The major constituents of EO were terpinen-4-ol (40.5 ± 6.6%) and sabinene (17.4 ± 1.4%) as determined by gas chromatography-mass spectrometry. These compounds were responsible for the anti-inflammatory activities of EO. Sabinene and terpinen-4-ol significantly reduced nuclear factor-kappa B (NF-kB) expression by 47 ± 5 and 78 ± 8%, respectively (p < 0.001) and significantly reduced the interleukin-6 (IL-6) secretion levels to 64 ± 4% (p < 0.05) and 50 ± 1% (p < 0.001), respectively. EO microemulsions, developed using the system of EO/Tween 20 and propylene glycol (2:1)/water, showed the internal droplet size in the range of 211.5 ± 63.3 to 366.7 ± 77.8 nm. Both EO and EO microemulsions were shown to be safe for human use since there was no apparent toxic effect on human peripheral blood mononuclear cells. Interestingly, EO microemulsion could significantly protect sabinene from the evaporation after heating-cooling stability test, which leads to a good stability and high efficacy. Moreover, EO microemulsions significantly enhanced the anti-inflammatory effect comparing to the native EO. Therefore, microemulsions were attractive delivery system for natural anti-inflammatory compounds since they could enhance both efficacy and stability of EO.
The aims of the present study were to develop olive oil microemulsions and characterize their antioxidant and skin moisturizing properties. The acid, iodine, and saponification values of olive oil were 0.38 + 0.01 mg potassium hydroxide/g, 88.2 + 5.9 mg iodine/g, and 192.2 + 1.4 mg potassium hydroxide/g, respectively. Pseudoternary phase diagrams, constructed using the water titration method, produced suitable microemulsions: microemulsion 1 (10% olive oil, 64% Tween 85, 16% propylene glycol, and 10% water) and microemulsion 2 (10% olive oil, 64% Tween 85, 16% ethanol, and 10% water). Microemulsions 1 and 2 exhibited Newtonian flow behavior with internal droplet sizes of 443.60 + 27.66 nm and 139.37 + 12.15 nm, respectively. Their in vitro antioxidant and skin moisturizing properties were investigated in comparison with native olive oil. Microemulsion 2 possessed the highest significant antioxidant effect (p < 0.05) giving half maximal inhibitory concentration values in radical-scavenging activity against 1,1-diphenyl-2-picrylhydrazyl and 2,2 0 -azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) of 4.78 + 1.25 mg/mL and 14.85 + 11.18 mg/mL, respectively. The lipid peroxidation inhibition of microemulsion 2 was comparable to native olive oil, whereas the skin moisturizing effect of microemulsion 1 was comparable to the well-known skin moisturizer, hyaluronic acid. In conclusion, microemulsions enhanced both antioxidant and skin moisturizing effects and were attractive formulations for using as a cosmetic or drug delivery system.
Leukemia therapeutics are aiming for improved efficacy by targeting molecular markers differentially expressed on cancerous cells. Lymphocyte function-associated antigen-1 (LFA-1) expression on various types of leukemia has been well studied. Here, the role and expression of LFA-1 on leukemic cells and the possibility of using this integrin as a target for drug delivery is reviewed. To support this rationale, experimental results were also included where cIBR, a cyclic peptide derived from a binding site of LFA-1, was conjugated to the surface of polymeric nanoparticles and used as a targeting ligand. These studies revealed a correlation of LFA-1 expression level on leukemic cell lines and binding and internalization of cIBR-NPs suggesting a differential binding and internalization of cIBR-NPs to leukemic cells overexpressing LFA-1. Nanoparticles conjugated with a cyclic peptide against an accessible molecular marker of disease hold promise as a selective drug delivery system for leukemia treatment.
Curcumin is one of the most promising natural therapeutics for use against Alzheimer’s disease. The major limitations of curcumin are its low oral bioavailability and difficulty in permeating the blood–brain barrier. Therefore, designing a delivery system of curcumin to overcome its limitations must be employed. KLVFF, a peptide known as an amyloid blocker, was used in this study as a targeting moiety to develop a targeted drug delivery system. A prototype of transnasal KLVFF conjugated microemulsions containing curcumin (KLVFF-Cur-ME) for the nose-to-brain delivery was fabricated. The KLVFF-Cur-ME was developed by a titration method. A conjugation of KLVFF was performed through a carbodiimide reaction, and the conjugation efficiency was confirmed by FTIR and DSC technique. KLVFD-Cur-ME was characterized for the drug content, globule size, zeta potential, and pH. A transparent and homogeneous KLVFF-Cur-ME is achieved with a drug content of 80.25% and a globule size of 76.1 ± 2.5 nm. The pH of KLVFF-Cur-ME is 5.33 ± 0.02, indicating non-irritation to nasal tissues. KLVFD-Cur-ME does not show nasal ciliotoxicity. An ex vivo diffusion study revealed that KLVFF-Cur-ME partitions the porcine nasal mucosa through diffusion, following the Higuchi model. This investigation demonstrates the successful synthesis of a bifunctional KLVFF-Cur-ME as a novel prototype to deliver anti-Aβ aggregation via an intranasal administration.
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