Berberine-loaded liposomes for oral delivery: Preparation, physicochemical characterization and in-vivo evaluation in an endogenous hyperlipidemic animal model

Duong, Thuan Thi; Yen, Tran Thi Hai; Nguyen, Linh Tran; Nguyen, Thuy-Duong Thi; Nguyen, Thi-Quynh-Trang; Nghiem, Thi-Ha-Lien; Pham, Huyên; Raal, Ain; Heinämäki, Jyrki; Pham, Thi-Minh-Hue

doi:10.1016/j.ijpharm.2022.121525

Cited by 19 publications

(10 citation statements)

References 32 publications

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“…628% increment in oral bioavailability was obtained in comparison to plain drug. Moreover, reduction in low-density lipoprotein, total cholesterol, triglycerides and low-density lipoprotein cholesterol were in hyperlipidemic mice [39].…”

Section: Liposomesmentioning

confidence: 91%

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Desai¹,

Desai²,

Patel³

2023

Drug Formulation Design

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The drug administered by an oral route has to withstand a harsh environment of gastrointestinal media, absorb through intestinal epithelium and circumvent first-pass metabolism in liver before reaching portal blood circulation. Moreover, hydrophobic drug molecules offer challenges for formulation with respect to their solubility and hence bioavailability. Various approaches have been developed to overcome this barrier. One of them is the use of lipids in formulation. Incorporation of the drug in lipids can result in increased solubility, absorption and thereby enhanced bioavailability. Intestinal lymphatic route of absorption has also been explored for increasing bioavailability of hydrophobic drug moieties. In this chapter, we have discussed the pathway of lipid digestion in the human body as well as the mechanism of lipid particles upon oral administration. The various lipid formulations developed and the excipients used in the formulations have also been described. The importance of lipid chain length and the effect of food in increasing the bioavailability of drug is discussed. The lymphatic pathway of lipid carriers has also been discussed.

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Section: Liposomesmentioning

confidence: 91%

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Desai¹,

Desai²,

Patel³

2023

Drug Formulation Design

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“…28.629 ng/ml*h); (Choudhury et al, 2022). In rats, using berberineloaded liposomes at a dose of 100 mg/kg resulted in even 628% enhancement in the oral bioavailability compared to pure berberine (Duong et al, 2022). Paudel et al (2022), demonstrated that using berberine-loaded liquid crystalline nanoparticles instead of berberine alone could increase the therapeutic effectivity against human lung cancer cell line (A549) more than five times by increasing the poor bioavailability of berberine (Paudel et al, 2022).…”

Section: "Bioavailability and Anti-diabetic Effectsmentioning

confidence: 97%

“…Other in vivo and in vitro studies revealed that berberine‐loaded microparticles filled in‐house 3D printed hollow capsular (AUC value: 99.629 ng/ml*h) have higher oral bioavailability in comparison with the pristine berberine (AUC value: 28.629 ng/ml*h); (Choudhury et al, 2022). In rats, using berberine‐loaded liposomes at a dose of 100 mg/kg resulted in even 628% enhancement in the oral bioavailability compared to pure berberine (Duong et al, 2022).…”

Section: Pharmacokinetic Parametersmentioning

confidence: 99%

Pharmacokinetic of berberine, the main constituent of Berberis vulgaris L.: A comprehensive review

Khoshandam

Imenshahidi

Rahbardar

2022

Phytotherapy Research

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Barberry (Berberis vulgaris L.) is a medicinal plant and its main constituent is an isoquinoline alkaloid named berberine that has multiple pharmacological effects such as antioxidant, anti-microbial, antiinflammatory, anticancer, anti-diabetes, anti-dyslipidemia, and anti-obesity. However, it has restricted clinical uses due to its very poor solubility and bioavailability (less than 1%). It undergoes demethylenation, reduction, and cleavage of the dioxymethylene group in the first phase of metabolism. Its phase two reactions include glucuronidation, sulfation, and methylation. The liver is the main site for berberine distribution. Berberine could excrete in feces, urine, and bile.Fecal excretion of berberine (11-23%) is higher than urinary and biliary excretion routes. However, a major berberine metabolite is excreted in urine greater than in feces. Concomitant administration of berberine with other drugs such as metformin, cyclosporine A, digoxin, etc. may result in important interactions. Thus, in this review, we gathered and dissected any related animal and human research articles regarding the pharmacokinetic parameters of berberine including bioavailability, metabolism, distribution, excretion, and drug-drug interactions. Also, we discussed and gathered various animal and human studies regarding the developed products of berberine with better bioavailability and consequently, better therapeutic effects.

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“…Liposome BBR đã được bào chế thành công và đánh giá tác dụng giảm lipid máu nội sinh trên động vật thực nghiệm cho kết quả khả quan [28]. Vì vậy, trong nghiên cứu này, hệ mang dược chất liposome tiếp tục được nghiên cứu đánh giá làm giảm lipid máu trên mô hình chuột được gây tăng lipid máu ngoại sinh bằng chế độ ăn giàu cholesterol.…”

Section: Mở đầU *unclassified

In vivo Evaluation of Berberine-loaded Liposomes in the Exogenous Hyperlipidemia Animal Model

Thi Thuan,

Thi Quynh Trang,

Thuy Duong

et al. 2023

MPS

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Berberine (BBR) is an alkaloid presenting exogenous cholesterol lowering and anti-hyperlipidemia therapeutic effects in the literature. In this study, the exogenous lipid-lowering effects of oral BBR-loaded liposomes were investigated in rats compared with free BBR within four weeks. The BBR-loaded liposomes at the daily oral dose of 25 mg BBR/kg of body weight in rats reduced total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) by 22.34% (p>0.05), 43.93% (p<0.05), respectively. These values (TC and LDL-C) when rats were given BBR-loaded liposomes at the daily oral dose of 50 mg BBR/kg were 30.72% (p<0.05) and 42.77% (p<0.05) compared with those values of the untreated control group, respectively. Both doses of BBR-loaded liposomes have no signals in decreasing triglycerides. Keywords: Berberine, berberine-loaded liposomes, anti-hyperlipidemia, animal model.

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Berberine-loaded liposomes for oral delivery: Preparation, physicochemical characterization and in-vivo evaluation in an endogenous hyperlipidemic animal model

Cited by 19 publications

References 32 publications

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Lipid as a Vehicle/Carrier for Oral Drug Delivery

Pharmacokinetic of berberine, the main constituent of Berberis vulgaris L.: A comprehensive review

In vivo Evaluation of Berberine-loaded Liposomes in the Exogenous Hyperlipidemia Animal Model

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