Intestinal membrane transporter-mediated approaches to improve oral drug delivery

Pangeni, Rudra; Kang, Soim; Jha, Saurav Kumar; Subedi, Laxman; Park, Jin Woo

doi:10.1007/s40005-021-00515-1

Cited by 26 publications

(11 citation statements)

References 128 publications

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“…In addition, P407, an amphiphilic polymeric carrier in SD-F4, increased the interface wetting and micellar solubilization of drugs, promoting intestinal drug absorption. Furthermore, the polymeric carriers in SD-F4 may increase the mucosal permeability of the intestinal epithelium, contributing to improved drug absorption [ 30 , 31 , 32 ]. Chen et al [ 25 ] developed SMEDDS formulations using an isolated indirubin (single component) to improve oral bioavailability.…”

Section: Resultsmentioning

confidence: 99%

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

et al. 2022

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This study aimed to develop a solid dispersion (SD) of MT-102, a new anti-inflammatory agent, to improve its oral bioavailability. The ternary SD formulations of MT-102 (a poorly soluble extract of Isatis indigotica and Juglans mandshurica) were prepared using a solvent evaporation method with various drug/excipient ratios. Following that, the effectiveness of various SDs as an oral formulation of MT-102 was investigated using indirubin as a marker component. By forming SDs with hydrophilic polymers, the aqueous solubility of indirubin was significantly increased. SD-F4, containing drug, poloxamer 407 (P407), and povidone K30 (PVP K30) at a 1:2:2 weight ratio, exhibited the optimal dissolution profiles in the acidic to neutral pH range. Compared to pure MT-102 and a physical mixture, SD-F4 increased indirubin’s dissolution from MT-102 by approximately 9.86-fold and 2.21-fold, respectively. Additionally, SD-F4 caused the sticky extract to solidify, resulting in improved flowability and handling. As a result, compared to pure MT-102, the oral administration of SD-F4 significantly improved the systemic exposure of MT-102 in rats. Overall, the ternary SD formulation of MT-102 with a blended mixture of P407 and PVP K30 appeared to be effective at improving the dissolution and oral absorption of MT-102.

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Section: Resultsmentioning

confidence: 99%

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

et al. 2022

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“…By enhancing the permeability of phospholipid membranes, Tween 80 improves skin penetration for transdermal drug delivery [ 35 , 36 ]. Tween 80 is also known to improve the bioavailability of a drug after oral administration [ 37 , 38 , 39 , 40 ]. Tween 80 may modulate the intestinal membrane permeability leading to improved oral bioavailability [ 40 ].…”

Section: Resultsmentioning

confidence: 99%

“…Tween 80 may modulate the intestinal membrane permeability leading to improved oral bioavailability [ 40 ]. Studies have indicated that Tween 80 may inhibit efflux transporters such as P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP2), and breast cancer resistance protein (BCRP) and improve oral absorption [ 38 , 39 , 41 ]. The low oral bioavailability of nafamostat is likely due to its high polarity, which would limit gastrointestinal permeability.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis

Kim

et al. 2022

Molecules

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Nafamostat, a synthetic serine protease inhibitor, has been used for the treatment of inflammatory diseases such as pancreatitis. Recently, an increasing number of studies have shown the promising antiviral effects of nafamostat for the treatment of coronavirus disease-19 (COVID-19). This study aimed to develop a novel liquid chromatography–tandem mass spectrometry (LC-MS/MS) analysis and to characterize the pharmacokinetics of nafamostat in rats. Nafamostat in the rat plasma was extracted by solid phase extraction, and 13C6-nafamostat was used as an internal standard. The quantification limit of nafamostat in the rat plasma was 0.5 ng/mL. The LC-MS/MS method was fully validated and applied to characterize the pharmacokinetics of nafamostat in rats. Following intravenous injection (2 mg/kg), nafamostat in the plasma showed a multiexponential decline with an average elimination half-life (t1/2) of 1.39 h. Following oral administration of nafamostat solutions (20 mg/kg) in 10% dimethyl sulfoxide (DMSO) and in 10% DMSO with 10% Tween 80, nafamostat was rapidly absorbed, and the average oral bioavailability was 0.95% and 1.59%, respectively. The LC-MS/MS method and the pharmacokinetic information of nafamostat could be helpful for the further preclinical and clinical studies of nafamostat.

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“…Promising strategy is the functionalization of liposomes with surfactants, which allows for controlling the size, shape and charge characteristics of vesicular nanocarriers, improving drug loading, overcoming the biological barriers, etc. [29][30][31][32][33][34][35][36]. Key factors that should be considered upon the modification are the nature of surfactant head group, hydrophobicity and presence of unsaturated C-C bonds in alkyl chains, and lipid/surfactant ratio [29].…”

Section: Lipid Nanocarriers Modified With Amphiphilic Moleculesmentioning

confidence: 99%

Nanocarriers for Biomedicine: From Lipid Formulations to Inorganic and Hybrid Nanoparticles

Kashapov

Ibragimova

Pavlov

et al. 2021

IJMS

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Encapsulation of cargoes in nanocontainers is widely used in different fields to solve the problems of their solubility, homogeneity, stability, protection from unwanted chemical and biological destructive effects, and functional activity improvement. This approach is of special importance in biomedicine, since this makes it possible to reduce the limitations of drug delivery related to the toxicity and side effects of therapeutics, their low bioavailability and biocompatibility. This review highlights current progress in the use of lipid systems to deliver active substances to the human body. Various lipid compositions modified with amphiphilic open-chain and macrocyclic compounds, peptide molecules and alternative target ligands are discussed. Liposome modification also evolves by creating new hybrid structures consisting of organic and inorganic parts. Such nanohybrid platforms include cerasomes, which are considered as alternative nanocarriers allowing to reduce inherent limitations of lipid nanoparticles. Compositions based on mesoporous silica are beginning to acquire no less relevance due to their unique features, such as advanced porous properties, well-proven drug delivery efficiency and their versatility for creating highly efficient nanomaterials. The types of silica nanoparticles, their efficacy in biomedical applications and hybrid inorganic-polymer platforms are the subject of discussion in this review, with current challenges emphasized.

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Intestinal membrane transporter-mediated approaches to improve oral drug delivery

Cited by 26 publications

References 128 publications

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis

Nanocarriers for Biomedicine: From Lipid Formulations to Inorganic and Hybrid Nanoparticles

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