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A study found that co-crystal berberine-ibuprofen (BJ) improves obesity.

Scientists found a co-crystal berberine-ibuprofen(BJ) improves obesity with dynamic solubility and good bioavailability.

Berberine (BBR), a natural alkaloid compound, is most commonly used as a supplement for diabetes, high cholesterol or other fat levels in the blood, and high blood pressure. And people in China commonly use it as an OTC drug to treat gastrointestinal tract infections.

Multiple publications have highlighted the ability of co-crystals and polymorphs of active pharmaceutical ingredients (APIs) to change their physicochemical properties without affecting their biological activity.

The new publication of the BJ was released on the website Nature recently, based on studies in vivo and vitro, which evaluated that the co-crystal berberine may improve obesity and related metabolic diseases by targeting TBK1 and IKK.

▶Compared to berberine, BJ has higher bioavailability and dynamic solubility.

In vitro, BJ has higher solubility in biological fluids than BBR, including gastric fluid (SGF), fasted state simulated intestinal fluid -V1 (FaSSIF-V1), and fed state simulated Intestinal fluid-V(FeSSIF-V1) and other buffers.(see as Fig2 on the right)

Meanwhile, after the same dose of BBR was administered to rats, the peak time of BJ was extended to 3.8 h, and the peak concentration was approximately 1.8 times that of BBR. The results showed that BJ increased BBR oral absorption and significantly increased BBR bioavailability.

co-crystal berberine-ibuprofen shows better solubility and higher bioavailability

▶Co-crystal berberine reduces bodyweight and increases energy expenditure in db/db mice.

The researchers used db/db mice to assess the effects of BJ on metabolism in vivo for 5 weeks and found that the effect of the BJ treatment on body weight was significantly enhanced, compared with the same dose of BBR: The average body weight gain in the BJ (75 mg/kg)-treated group was 9.4±2.7 g, 5.2±0.9 g in the BJ (150 mg/kg)-treated group, and 7.6 ±0.8 g in the BBR (150 mg/kg)-treated group.

What’s more, the food intake of the groups did not significantly differ, but the energy expenditure of the mice led to the weight loss. The results of the vivo study show that both BJ and BBR treatments reduced weight and increased energy consumption in db/db mice, but treatment with 150 mg/kg BJ outperformed BBR (150 mg/kg) and BJ (75 mg/kg). Weight loss was not related to food intake in this study, as observed in the experiment, which should be good news for foodies who want to stay fit and enjoy food at the same time.

▶In db/db mice, BJ improves obesity by improving lipid metabolism.

According to the assessments, both BBR and BJ have lower fat depots weight, decreasing serum levels of CHO1, TG2,FFA3, LDL-C 4and increased HDL-C5 and DAPN6. The differences in the BJ (150 mg/kg) treatment group were striking. Furthermore, when compared to BBR (150 mg/kg), BJ (150 mg/kg) treatment had a significant effect on lipid metabolism-related gene expression.

▶BJ improves blood sugar metabolism and decreases adipose tissue inflammation in db/db mice.

All the findings and data of the glucose tolerance test and insulin tolerance test of the mice groups indicate that all BBR and BJ treatments improved blood glucose levels, with the BJ (150 mg/kg) treatment having the greatest effect.

In addition, BJ (150 mg/kg) significantly reduced fasting serum insulin levels in db/db mice after 35 days of treatment.

▶BJ reduces IKK and TBK1 expression and activity in db/db mice eWAT.

▶In 3T3-L1 adipocytes, BJ reduces obesity by inhibiting lipid accumulation and inflammation. Furthermore, BJ regulates 3T3-L1 adipocytes by targeting TBK1 and IKK.

This publication on co-crystal berberine goes further than the past publications by the studies of in vivo and vitro, and evaluates more about the bioavailability and the pharmacokinetics for obesity improvement.

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    1, Total cholesterol
    2, Total triglycerides
    3, Free fatty acid
    4, Low-density lipoprotein cholesterol
    5, High-density lipoprotein cholesterol
    6, Adiponectin