Colloids and Surfaces B: MTX+HCQ nanomicelles are three times more effective than traditional drug delivery methods

Rheumatoid arthritis (RA) is the most common inflammatory rheumatic disease, affecting nearly 1% of the world's population
.

Current treatments for RA aim to achieve prolonged active periods and early and sustained remission of the disease through the gradual use of different drugs

Rheumatoid arthritis (RA) is the most common inflammatory rheumatic disease, affecting nearly 1% of the world's population

In a study in Brazil, a new type of hydroxychloroquine and methotrexate co-loaded with Pluronic® F-127 nanomicelles was developed and its therapeutic effect on RA was evaluated

In this study, the researchers newly developed a new type of Pluronic® F-127 nanomicelles, the micelles are loaded with new hydroxychloroquine and methotrexate
.

Research results show that this drug-loaded nanomicelle can regulate the inflammatory process of RA and reduce osteoclast production, edema and cell migration to joints

In this study, the researchers newly developed a new type of Pluronic® F-127 nanomicelles, the micelles are loaded with new hydroxychloroquine and methotrexate

Nanomicelles are one of the most widely used nanoparticles, which can improve the blood circulation time, bioavailability and specificity of drugs
.

The therapeutic agent can be transported passively or actively after systemic administration, and selectively accumulate in the inflammation site.

Nanomicelles are one of the most widely used nanoparticles, which can improve the blood circulation time, bioavailability and specificity of drugs

Experimental contentExperimental content

Thirty-five C57BL/6 mice were divided into 7 experimental groups, each consisting of 5 animals
.

Thirty-five C57BL/6 mice were divided into 7 experimental groups, each consisting of 5 animals
.

Animal handling

Animal handling animal handling

Sham : 0.
1 mL saline and 0.
1 mL Freund's complete adjuvant

Sham : 0.
1 mL saline and 0.
1 mL Freund's complete adjuvant Sham

Saline：Equivalent normal saline

Saline：Equivalent saline Saline

mBSA: 500 μg methylated bovine serum albumin (mBSA), 0.
1 mL saline and 0.
1 mL Freund’s complete adjuvant
.

mBSA: 500 μg methylated bovine serum albumin (mBSA), 0.
1 mL saline and 0.
1 mL Freund’s complete adjuvant
.

mBSA:

Pluronic : 127-Pluronic

Pluronic : 127-Pluronic Pluronic

intervention group 1 : 127-Pluronic−HCQ-MTX nanomicelles (2 mg / K and 1 mg / Kg, respectively);

intervention group 1 : 127-Pluronic−HCQ-MTX nanomicelles (2 mg / K and 1 mg / Kg, respectively); intervention group 1

intervention group 2: 127-Pluronic−HCQ-MTX nanomicelles (1 mg / K and 0.
5 mg / Kg, respectively).

intervention group 2: 127-Pluronic−HCQ-MTX nanomicelles (1 mg / K and 0.
5 mg / Kg, respectively).
intervention group 2:

Experimental results

Experimental results Experimental results

• In vitro drug release experiment:

In vitro drug release experiment:

In vitro drug release test: In vitro drug release test:

• Osteoclastogenesis experiment

Osteoclastogenesis experiment

Osteoclast production experiment Osteoclast production experiment

Expose monocytes in human peripheral blood to nanomicelles formed by the combination of two different concentrations of methotrexate and hydroxychloroquine (127-Pluronic-HCQ-MTX nanomicelles), 20 ug/mL HCQ and 074 ng/mL MTX and 70 ug/mL HCQ and 2.
6 ng/mL MTX
.

Four dilutions of nanomicelles (1:10, 1:100, 1:1000, and 1:2000) were tested in order to study a more effective concentration for RA treatment

Expose monocytes in human peripheral blood to nanomicelles formed by the combination of two different concentrations of methotrexate and hydroxychloroquine (127-Pluronic-HCQ-MTX nanomicelles), 20 ug/mL HCQ and 074 ng/mL MTX and 70 ug/mL HCQ and 2.

The results showed that the inhibition rate of MRP1 was 40-50%, proving that nanomicelles can improve the accumulation of drugs in cells

HCQ and MTX combined treatment of RA, compared with the current traditional way of administration, the lower dose of nanomicelle administration shows a better anti-inflammatory effect, and can be less drug-resistant
.

Original source: Tais Monteiro Magne, Edward Helal-Neto, Luana Barbosa Correa, et al.
Rheumatoid arthritis treatment using hydroxychloroquine and methotrexate co-loaded nanomicelles: In vivo results, Colloids and Surfaces B: Biointerfaces,
Volume 206,2021,111952,https ://doi.
org/10.
1016/j.
colsurfb.
2021.
111952.

Original source: Tais Monteiro Magne, Edward Helal-Neto, Luana Barbosa Correa, et al.
Rheumatoid arthritis treatment using hydroxychloroquine and methotrexate co-loaded nanomicelles: In vivo results, Colloids and Surfaces B: Biointerfaces, et al.

Volume 206,2021, 111952, https://doi.
org/10.
1016/j.
colsurfb.
2021.
111952.
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