Toward a better understanding of metabolic and pharmacokinetic characteristics of low-solubility, low-permeability natural medicines

Yang, Jie; Li, Kailing; He, Dongyi; Gu, Jie; Xu, Jingyu; Xie, Jiaxi; Zhang, Min; Liu, Yuying; Tan, Qunyou; Zhang, Jingqing

doi:10.1080/03602532.2020.1714646

Cited by 16 publications

(13 citation statements)

References 122 publications

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“…The local or topical administration of drugs in the skin or other membranes is an interesting alternative to the oral route, decreasing systemic side effects and avoiding firstpass metabolism [119]. Topical and transdermal drug administration may show advantages compared to oral administration, especially when a regional effect is expected due the possibility of drug application close to the action site, e.g., deeper skin layers, muscles, and blood vessels [120].…”

Section: Discussionmentioning

confidence: 99%

Inclusion Complexes of Non-Steroidal Anti-Inflammatory Drugs with Cyclodextrins: A Systematic Review

et al. 2021

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Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most widely used classes of medicines in the treatment of inflammation, fever, and pain. However, evidence has demonstrated that these drugs can induce significant toxicity. In the search for innovative strategies to overcome NSAID-related problems, the incorporation of drugs into cyclodextrins (CDs) has demonstrated promising results. This study aims to review the impact of cyclodextrin incorporation on the biopharmaceutical and pharmacological properties of non-steroidal anti-inflammatory drugs. A systematic search for papers published between 2010 and 2020 was carried out using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) protocol and the following search terms: “Complexation”; AND “Cyclodextrin”; AND “non-steroidal anti-inflammatory drug”. A total of 24 different NSAIDs, 12 types of CDs, and 60 distinct inclusion complexes were identified, with meloxicam and β-CD appearing in most studies. The results of the present review suggest that CDs are drug delivery systems capable of improving the pharmacological and biopharmaceutical properties of non-steroidal anti-inflammatory drugs.

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Section: Discussionmentioning

confidence: 99%

Inclusion Complexes of Non-Steroidal Anti-Inflammatory Drugs with Cyclodextrins: A Systematic Review

et al. 2021

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“…The D 0 value > 1 is the defining criterion of low solubility and log P ≤ 1.632 is the defining criterion of low permeability. 23 According to the solubility and permeability, the AvDs are classified into 3 groups (Figure 2). Among these drugs, 50% belong to BCS II with low solubility, 44% belong to BCS III with low permeability, 6% belong to BCS IV with low solubility and low permeability.…”

Section: Solubility Permeability and Structural Properties Of Avds Solubility And Permeability Limits Of Avdsmentioning

confidence: 99%

“…25 Solubility is a prerequisite to confirm drug absorption and clinical response for drugs given orally. 23 Permeability represents the speed and extent of oral drug diffusion through the mucus layer and then through the submucosa and epithelial cell barriers into the blood or lymphatic circulation. 26 Currently, numerous advanced pharmaceutical technologies have been applied to increase the solubility and permeability of AvDs, including adding auxiliary ingredients (such as latent solvents and penetration enhancers) and applying cutting-edge preparation methods (such as inclusion technology, solid dispersion technology and micronization technology and nanotechnology).…”

Section: Pharmaceutical Technology To Improve Solubility and Permeabilitymentioning

confidence: 99%

“…Phase II biotransformation (combination reaction) combines the polar groups produced by phase I with endogenous components in the body through covalent bonds. 23,44 The produced combination, possessing high polarity, is easy to dissolve in water and discharge from the body. Renal clearance is mainly controlled by membrane transport proteins and is an important elimination pathway for antiviral agents.…”

Section: Metabolic Enzyme Reaction and Metabolite Of Avdsmentioning

confidence: 99%

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Antiviral Drug Delivery System for Enhanced Bioactivity, Better Metabolism and Pharmacokinetic Characteristics

Chen¹,

Wang²,

Song³

et al. 2021

IJN

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Antiviral drugs (AvDs) are the primary resource in the global battle against viruses, including the recent fight against corona virus disease 2019 . Most AvDs require multiple medications, and their use frequently leads to drug resistance, since they have poor oral bioavailability and low efficacy due to their low solubility/low permeability. Characterizing the in vivo metabolism and pharmacokinetic characteristics of AvDs may help to solve the problems associated with AvDs and enhance their efficacy. In this review of AvDs, we systematically investigated their structure-based metabolic reactions and related enzymes, their cellular pharmacology, and the effects of metabolism on AvD pharmacodynamics and pharmacokinetics. We further assessed how delivery systems achieve better metabolism and pharmacology of AvDs. This review suggests that suitable nanosystems may help to achieve better pharmacological activity and pharmacokinetic behavior of AvDs by altering drug metabolism through the utilization of advanced nanotechnology and appropriate administration routes. Notably, such AvDs as ribavirin, remdesivir, favipiravir, chloroquine, lopinavir and ritonavir have been confirmed to bind to the severe acute respiratory syndrome-like coronavirus (SARS-CoV-2) receptor and thus may represent anti-COVID-19 treatments. Elucidating the metabolic and pharmacokinetic characteristics of AvDs may help pharmacologists to identify new formulations with high bioavailability and efficacy and help physicians to better treat virus-related diseases, including COVID-19.

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“…Natural medicines (NMs) are known for their high availability, clear efficacy, and low toxicity and economic cost ( Yang et al, 2020 ). Some NMs have been proven to have positive effects by regulating cerebral metabolism to ameliorate brain diseases.…”

Section: Introductionmentioning

confidence: 99%

Better Bioactivity, Cerebral Metabolism and Pharmacokinetics of Natural Medicine and Its Advanced Version

et al. 2022

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Currently, many people are afflicted by cerebral diseases that cause dysfunction in the brain and perturb normal daily life of people. Cerebral diseases are greatly affected by cerebral metabolism, including the anabolism and catabolism of neurotransmitters, hormones, neurotrophic molecules and other brain-specific chemicals. Natural medicines (NMs) have the advantages of low cost and low toxicity. NMs are potential treatments for cerebral diseases due to their ability to regulate cerebral metabolism. However, most NMs have low bioavailability due to their low solubility/permeability. The study is to summarize the better bioactivity, cerebral metabolism and pharmacokinetics of NMs and its advanced version. This study sums up research articles on the NMs to treat brain diseases. NMs affect cerebral metabolism and the related mechanisms are revealed. Nanotechnologies are applied to deliver NMs. Appropriate delivery systems (exosomes, nanoparticles, liposomes, lipid polymer hybrid nanoparticles, nanoemulsions, protein conjugation and nanosuspensions, etc.) provide better pharmacological and pharmacokinetic characteristics of NMs. The structure-based metabolic reactions and enzyme-modulated catalytic reactions related to advanced versions of NMs alter the pharmacological activities of NMs.

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Toward a better understanding of metabolic and pharmacokinetic characteristics of low-solubility, low-permeability natural medicines

Cited by 16 publications

References 122 publications

Inclusion Complexes of Non-Steroidal Anti-Inflammatory Drugs with Cyclodextrins: A Systematic Review

Inclusion Complexes of Non-Steroidal Anti-Inflammatory Drugs with Cyclodextrins: A Systematic Review

Antiviral Drug Delivery System for Enhanced Bioactivity, Better Metabolism and Pharmacokinetic Characteristics

Better Bioactivity, Cerebral Metabolism and Pharmacokinetics of Natural Medicine and Its Advanced Version

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