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The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats.

Zheng Z, Sun Y, Liu Z, Zhang M, Li C, Cai H - Drug Des Devel Ther (2015)

Bottom Line: CM-Ns with a diameter of approximately 150 nm were successfully prepared, and the drug was well encapsulated into the Ns without degradation in simulated GI conditions.The area under the curve (AUC) and Cmax for the CM-Ns were more than threefold greater than those for the suspensions; moreover, similar decreases in the levels of TNF-α and interleukin-1β in both synovial fluid and blood serum were obtained from oral administration of CM-Ns and iv injection.CM was an effective antiarthritic agent, and the present N formulation appeared to be a promising system that allowed RA therapy with CM to be converted from iv to oral administration.

View Article: PubMed Central - PubMed

Affiliation: Department of Traditional Chinese Medicine, Dongying People's Hospital, Dongying, People's Republic of China.

ABSTRACT

Background: Rheumatoid arthritis (RA), induced by the prolonged inappropriate inflammatory responses, is one of the most prevalent of all chronic inflammatory joint diseases. Curcumin (CM), a yellow hydrophobic polyphenol derived from the herb turmeric, has various pharmacological activities against many chronic diseases and acts by inhibiting cell proliferation and metastasis and downregulating various factors, including nuclear factor kappa B, interleukin-1β and TNF-α. Given the pathogenesis of RA, we hypothesized that the drug also has antiarthritic effects. The aims of the present study included the following: 1) examining the therapeutic effect of CM administered via intravenous (iv) injection on RA and 2) formulating the drug into oil-water nanoemulsions (Ns) to overcome the low oral bioavailability of CM and achieve oral delivery of the drug.

Methods: The effect of CM administered through iv injection on adjuvant-induced arthritis in rats was studied in terms of paw swelling, weight indices of the thymus and spleen, and pathological changes in nuclear factor kappa B expression and inflammatory cytokines. Methotrexate was used as a positive control. The CM-Ns were prepared using a high-pressure homogenizing method and characterized with respect to the particle size and morphology. The stability of the CM-Ns in simulated gastrointestinal (GI) fluids and in vitro release were also investigated. A pharmacokinetic study of the CM-Ns and suspensions in which the plasma levels were determined using an high performance liquid chromatography method and the pharmacokinetic parameters were calculated based on a statistical moment theory was also performed in rats.

Results: CM administered via iv injection had a therapeutic effect on RA similar to methotrexate. CM-Ns with a diameter of approximately 150 nm were successfully prepared, and the drug was well encapsulated into the Ns without degradation in simulated GI conditions. The area under the curve (AUC) and Cmax for the CM-Ns were more than threefold greater than those for the suspensions; moreover, similar decreases in the levels of TNF-α and interleukin-1β in both synovial fluid and blood serum were obtained from oral administration of CM-Ns and iv injection.

Conclusion: CM was an effective antiarthritic agent, and the present N formulation appeared to be a promising system that allowed RA therapy with CM to be converted from iv to oral administration.

No MeSH data available.


Related in: MedlinePlus

Characterization of CM-Ns.Notes: (A) Particle size and size distribution and (B) a TEM image.Abbreviations: CM, curcumin; CM-Ns, CM-nanoemulsions; TEM, transmission electron microscope.
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f5-dddt-9-4931: Characterization of CM-Ns.Notes: (A) Particle size and size distribution and (B) a TEM image.Abbreviations: CM, curcumin; CM-Ns, CM-nanoemulsions; TEM, transmission electron microscope.

Mentions: CM had good solubility in the oil phase: approximately 100 mg/mL. The CM-Ns were prepared via a high-pressure homogenizing method with Solutol-HS 15 as an emulsifier, and no drug precipitation was observed during the preparation procedure. The drug could be successfully formulated into Ns with an entrapment efficiency of more than 90%. The particle size of the CM-Ns was approximately 150 nm, with a polydispersity index of 0.21 (less than 0.3) (Figure 5A), thus indicating a homogeneous dispersion.26 To confirm the hydrodynamic diameter of the Ns obtained by DLS and determine the morphology of Ns, TEM analysis was performed. As shown in Figure 5B, uniform and spherical particles with a diameter of approximately 150 nm were observed in the TEM image, which was consistent with the DLS results.


The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats.

Zheng Z, Sun Y, Liu Z, Zhang M, Li C, Cai H - Drug Des Devel Ther (2015)

Characterization of CM-Ns.Notes: (A) Particle size and size distribution and (B) a TEM image.Abbreviations: CM, curcumin; CM-Ns, CM-nanoemulsions; TEM, transmission electron microscope.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4555965&req=5

f5-dddt-9-4931: Characterization of CM-Ns.Notes: (A) Particle size and size distribution and (B) a TEM image.Abbreviations: CM, curcumin; CM-Ns, CM-nanoemulsions; TEM, transmission electron microscope.
Mentions: CM had good solubility in the oil phase: approximately 100 mg/mL. The CM-Ns were prepared via a high-pressure homogenizing method with Solutol-HS 15 as an emulsifier, and no drug precipitation was observed during the preparation procedure. The drug could be successfully formulated into Ns with an entrapment efficiency of more than 90%. The particle size of the CM-Ns was approximately 150 nm, with a polydispersity index of 0.21 (less than 0.3) (Figure 5A), thus indicating a homogeneous dispersion.26 To confirm the hydrodynamic diameter of the Ns obtained by DLS and determine the morphology of Ns, TEM analysis was performed. As shown in Figure 5B, uniform and spherical particles with a diameter of approximately 150 nm were observed in the TEM image, which was consistent with the DLS results.

Bottom Line: CM-Ns with a diameter of approximately 150 nm were successfully prepared, and the drug was well encapsulated into the Ns without degradation in simulated GI conditions.The area under the curve (AUC) and Cmax for the CM-Ns were more than threefold greater than those for the suspensions; moreover, similar decreases in the levels of TNF-α and interleukin-1β in both synovial fluid and blood serum were obtained from oral administration of CM-Ns and iv injection.CM was an effective antiarthritic agent, and the present N formulation appeared to be a promising system that allowed RA therapy with CM to be converted from iv to oral administration.

View Article: PubMed Central - PubMed

Affiliation: Department of Traditional Chinese Medicine, Dongying People's Hospital, Dongying, People's Republic of China.

ABSTRACT

Background: Rheumatoid arthritis (RA), induced by the prolonged inappropriate inflammatory responses, is one of the most prevalent of all chronic inflammatory joint diseases. Curcumin (CM), a yellow hydrophobic polyphenol derived from the herb turmeric, has various pharmacological activities against many chronic diseases and acts by inhibiting cell proliferation and metastasis and downregulating various factors, including nuclear factor kappa B, interleukin-1β and TNF-α. Given the pathogenesis of RA, we hypothesized that the drug also has antiarthritic effects. The aims of the present study included the following: 1) examining the therapeutic effect of CM administered via intravenous (iv) injection on RA and 2) formulating the drug into oil-water nanoemulsions (Ns) to overcome the low oral bioavailability of CM and achieve oral delivery of the drug.

Methods: The effect of CM administered through iv injection on adjuvant-induced arthritis in rats was studied in terms of paw swelling, weight indices of the thymus and spleen, and pathological changes in nuclear factor kappa B expression and inflammatory cytokines. Methotrexate was used as a positive control. The CM-Ns were prepared using a high-pressure homogenizing method and characterized with respect to the particle size and morphology. The stability of the CM-Ns in simulated gastrointestinal (GI) fluids and in vitro release were also investigated. A pharmacokinetic study of the CM-Ns and suspensions in which the plasma levels were determined using an high performance liquid chromatography method and the pharmacokinetic parameters were calculated based on a statistical moment theory was also performed in rats.

Results: CM administered via iv injection had a therapeutic effect on RA similar to methotrexate. CM-Ns with a diameter of approximately 150 nm were successfully prepared, and the drug was well encapsulated into the Ns without degradation in simulated GI conditions. The area under the curve (AUC) and Cmax for the CM-Ns were more than threefold greater than those for the suspensions; moreover, similar decreases in the levels of TNF-α and interleukin-1β in both synovial fluid and blood serum were obtained from oral administration of CM-Ns and iv injection.

Conclusion: CM was an effective antiarthritic agent, and the present N formulation appeared to be a promising system that allowed RA therapy with CM to be converted from iv to oral administration.

No MeSH data available.


Related in: MedlinePlus