Bioavailability of berberine: challenges and solutions

Thomas, Anna; Kamble, Seema; Deshkar, Sanjeevani Shekhar; Kothapalli, Lata; Chitlange, Sohan S.

doi:10.26650/istanbuljpharm.2020.0056

Cited by 14 publications

(7 citation statements)

References 16 publications

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“…Several studies showed that berberine had low toxic effects on human beings. For example, a phase I clinical trial showed that berberine was safe at excessive doses [ 134 ]. Another study found that berberine showed low toxicity towards healthy cells [ 135 ].…”

Section: Safety Of Berberinementioning

confidence: 99%

Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

Xiong

Huang

et al. 2022

Molecules

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Cancer has been a serious public health problem. Berberine is a famous natural compound from medicinal herbs and shows many bioactivities, such as antioxidant, anti-inflammatory, antidiabetic, anti-obesity, and antimicrobial activities. In addition, berberine shows anticancer effects on a variety of cancers, such as breast, lung, gastric, liver, colorectal, ovarian, cervical, and prostate cancers. The underlying mechanisms of action include inhibiting cancer cell proliferation, suppressing metastasis, inducing apoptosis, activating autophagy, regulating gut microbiota, and improving the effects of anticancer drugs. This paper summarizes effectiveness and mechanisms of berberine on different cancers and highlights the mechanisms of action. In addition, the nanotechnologies to improve bioavailability of berberine are included. Moreover, the side effects of berberine are also discussed. This paper is helpful for the prevention and treatment of cancers using berberine.

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Section: Safety Of Berberinementioning

confidence: 99%

Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

Xiong

Huang

et al. 2022

Molecules

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“…The measurement of the bioavailability of any molecule is often calculated through its pharmacokinetic profile, which includes absorption, metabolism, biodistribution, and elimination (excretion). As Berberine is poorly absorbed and quickly eliminated from the body due to low bioavailability, high doses of Berberine need to be administered to achieve the therapeutic effects [ 52 ]. This reduction in bioavailability is further enhanced due to its binding with plasma proteins; eventually, only the fraction of unbounded Berberine is left to reach the target tissues [ 53 , 54 , 55 , 56 ].…”

Section: Berberinementioning

confidence: 99%

“…Similarly, dendrimers [ 140 ], nanogels [ 141 ], chitosan [ 142 ], and all other polymeric-based nanoparticle carriers were also shown to improve Berberine’s pharmacokinetics. Further, as discussed above, combining different anticancer therapies offers the advantages of using lower drug doses along with a better therapeutic outcome [ 52 ]. Other than the above-stated treatment options, utilizing the strong absorption in the blue wavelength region, Berberine can also be investigated as a potent chemo-photosensitizing agent against localized lung tumor mass.…”

Section: Limitations and Future Perspectivementioning

confidence: 99%

Multi-Target Potential of Berberine as an Antineoplastic and Antimetastatic Agent: A Special Focus on Lung Cancer Treatment

Achi

Sarbadhikary

George

et al. 2022

Cells

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Despite therapeutic advancements, lung cancer remains the principal cause of cancer mortality in a global scenario. The increased incidence of tumor reoccurrence and progression and the highly metastatic nature of lung cancer are of great concern and hence require the investigation of novel therapies and/or medications. Naturally occurring compounds from plants serve as important resources for novel drugs for cancer therapy. Amongst these phytochemicals, Berberine, an alkaloid, has been extensively explored as a potential natural anticancer therapeutic agent. Several studies have shown the effectiveness of Berberine in inhibiting cancer growth and progression mediated via several different mechanisms, which include cell cycle arrest, inducing cell death by apoptosis and autophagy, inhibiting cell proliferation and invasion, as well as regulating the expression of microRNA, telomerase activity, and the tumor microenvironment, which usually varies for different cancer types. In this review, we aim to provide a better understanding of molecular insights of Berberine and its various derivative-induced antiproliferative and antimetastatic effects against lung cancer. In conclusion, the Berberine imparts its anticancer efficacy against lung cancers via modulation of several signaling pathways involved in cancer cell viability and proliferation, as well as migration, invasion, and metastasis.

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“…Sinh khả dụng đường uống của berberin rất thấp (khoảng 5%) và được phân loại thuộc nhóm IV trong bảng phân loại BCS [8]. Do vậy, để cải thiện độ tan và tính thấm nhằm nâng cao sinh khả dụng của berberin một số dạng bào chế mới đã được triển khai như hệ nano mang thuốc, liposome, micell và phức hợp với phospholipid [9]. Trong nước, một số hệ có kích thước nano với berberin cũng đã được nghiên cứu như liposome, nano berberin [10][11][12].…”

Section: Mở đầU *unclassified

Preparation of Berberine Chloride Nanoparticles by Ball Milling Method

Anh¹,

Hung²,

Tuan³

et al. 2022

MPS

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Berberine is a quaternary benzylisoquinoline alkaloid that has been used for the local treatment of gastrointestinal tract diseases. Recently, several pharmacological effects of berberine have been reported, which include anti-hypertension, antitumor, anti-hypercholesterolemia, and neuroprotective effects. However, berberine has exhibited poor aqueous solubility and low oral bioavailability. To overcome these limitations, this study aims to develop and investigate nano berberine. Nano berberine fabricated by ball milling method is a simple process and easily applied in the production scale. The characterization of nano berberine was evaluated, including appearance, particle size, potential zeta, dissolution in vitro in a phosphate buffer media (pH 6.8), differential scanning calorimetry (DSC) analysis, fourier transformed infrared spectroscopy (FTIR), and X-ray diffraction analysis (XRD). Results from this study showed that spray-dried nano berberine powder was almost uniform in size, particle size average of 570.7 nm, and potential zeta of -28.6 mV. The dissolution in vitro study revealed that nano berberine was about 2 times more soluble than raw berberine for 60 minutes. No incompatibility between drug and excipients can be observed through FTIR and DSC analysis. XRD analysis suggested that raw berberine and nano berberine might exist in a crystal form. Thus, findings from this study indicate that the physicochemical properties of spray-dried nano berberine may increase the bioavailability of oral berberine.

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Bioavailability of berberine: challenges and solutions

Cited by 14 publications

References 16 publications

Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

Multi-Target Potential of Berberine as an Antineoplastic and Antimetastatic Agent: A Special Focus on Lung Cancer Treatment

Preparation of Berberine Chloride Nanoparticles by Ball Milling Method

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