Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine

Zhang, Liang

doi:10.1080/10717544.2019.1660732

Cited by 113 publications

(58 citation statements)

References 94 publications

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“…It has a variety of biological functions and is widely used in various clinical fields. The ingredient can relieve coronary heart disease angina pectoris, provide adjuvant treatment for myocardial [1,2] and cerebral infarction, and promote the recovery of neurological functions [3][4][5]. However, Pur is a BCS IV drug with low oral bioavailability [6].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

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Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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“…CYP3A4 is the most abundant cytochrome P450 presented in human hepatocytes and intestinal enterocytes [45,46]. PME contains at least 17 phytoestrogenic substances [1]; drugdrug interaction can occur via bioenhancement or efflux transporter activity [47] as mentioned earlier. Thus, multiple oral dosing of PUE and PME caused the 3-to 5-fold lower clearance rate and longer T 1/2 .…”

Section: Discussionmentioning

confidence: 99%

Comparative Pharmacokinetics of Puerarin Alone and in Pueraria mirifica Extract in Female Cynomolgus Monkeys

et al. 2020

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Pueraria mirifica is an endemic Thai plant that has been used for rejuvenation and in the relief of various aging diseases. Puerarin is one of the major isoflavones found in this plant and shows several pharmacological activities in relation to the Thai traditional use of P. mirifica. Therefore, comparative pharmacokinetics of pure puerarin alone and that in a P. mirifica extract in cynomolgus monkeys were conducted in order to investigate the pharmacokinetic profiles of the 2 preparations. To this end, puerarin and P. mirifica extract, at an equivalent dose of 10 mg/kg of puerarin, were orally dosed to adult female monkeys for 7 consecutive days. A single intravenous injection of puerarin at a dose of 1 mg/kg was also peformed. Serial blood samples and excreta were collected from 0 – 24 h and 0 – 48 h after dosing. Determination of the puerarin levels and its metabolites in biological samples was conducted by liquid chromatography tandem mass spectrometry. Plasma levels of aspartate aminotransferase, alanine aminotransferase, and creatinine fluctuated in the normal range, with no abnormal physical signs in the animal. The absolute oral bioavailability of puerarin was approximately 1% in both preparations. Accumulation of puerarin was found after oral dosing for 7 consecutive days in both groups. Major metabolites of puerarin found in monkeys were hydroxylation and deglycosylation products. A negligible amount of unchanged puerarin was detected in urine and feces. Pharmacokinetic profiles obtained from this study could help to design the prescribed remedy of puerarin and P. mirifica extract phytopharmaceutical products for human use.

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“…Ohwi [12]. Puerarin has a wide range of pharmacological properties and is used to treat cardiovascular and cerebrovascular diseases, Alzheimer's disease, osteonecrosis, Parkinson's disease, diabetes and diabetic complications, endometriosis and cancer [13].…”

Section: Paragraphmentioning

confidence: 99%

The Protective Effect of Dietary Administration of Puerarin on Canine Osteoarthritis Model With Anterior Cruciate Ligament Transected

Wen

Song

et al. 2020

Preprint

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BackgroundLameness caused by osteoarthritis (OA) is one of the main causes of disability in elderly dogs. Non-steroidal anti-inflammatory drugs (NSAIDs) are important tools in the treatment of canine OA. In recent years, due to the many side effects of NSAIDs, patients cannot tolerate or do not want to take the risk of NSAIDs. People are becoming more and more interested in new treatments for canine OA, and so-called nutritional supplements have emerged. Puerarin has a wide range of pharmacological activities and is often used as a clinical prescription drug and dietary supplement in China. However, the effect of puerarin on canine OA has not been evaluated. Therefore, the purpose of this study is to evaluate the anti-inflammatory and anti-cartilage degradation effects of puerarin in a canine OA model induced by anterior cruciate ligament transection (ACLT), and to detect the serum inflammatory factor interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor α (TNF-α) levels and cartilage degradation biomarker C-terminal telopeptides of collagen type II (CTX-II), cartilage oligomeric matrix protein (COMP) and chondroitin sulfate 846 epitope (CS 846) levels in serum and synovial fluid at different periods of puerarin administration. ResultsEight weeks after the administration, the veterinarian performed clinical and imaging evaluations to comprehensively evaluate the protective effect of puerarin on canine OA. Daily oral administration of 20 mg/kg puerarin can significantly inhibit the expression of IL-1β, IL-6 and TNF-α in serum within 8 weeks (P < 0.05), and its anti-inflammatory effect is similar to oral celecoxib (negative control group). Puerarin has a certain protective effect on articular cartilage and can reduce the level of biomarkers CTX-II, COMP and CS 846 in serum and synovial fluid in the early stage of OA (P < 0.05). In addition, the clinical scores and radiographs scores were significantly reduced after 8 weeks of puerarin treatment (P < 0.05). ConclusionsCanine OA cartilage may be mediated through anti-inflammatory, anti-metabolism and anabolic effects, and strongly down-regulate the inflammatory factors IL-1β, IL-6 and TNF-α and cartilage degradation biomarkers CTX-II, COMP and CS 846 are related, providing a good alternative therapy for OA.

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Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine

Cited by 113 publications

References 94 publications

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Comparative Pharmacokinetics of Puerarin Alone and in Pueraria mirifica Extract in Female Cynomolgus Monkeys

The Protective Effect of Dietary Administration of Puerarin on Canine Osteoarthritis Model With Anterior Cruciate Ligament Transected

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