Preformulation studies of <scp>l</scp>-glutathione: physicochemical properties, degradation kinetics, and <i>in vitro</i> cytotoxicity investigations

Liu, Mengyang; Sharma, Manisha; Yin, Naibo; Gailani, Murad Al; Sreebhavan, Sree; Wen, Jingyuan

doi:10.1080/03639045.2020.1752708

Cited by 10 publications

(7 citation statements)

References 28 publications

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“…The cytotoxicity of bLf and bLf-loaded unmodified, chitosan-, and pectin-modified SLPs towards Caco-2 cells was examined using the MTT assay for the assessment of cell viability [ 39 , 40 ]. Briefly, 10 4 cells/cm 2 per well were sub-cultured into 96-well plates.…”

Section: Methodsmentioning

confidence: 99%

“…The assessment of cell viability was accomplished through the MTT assay, which gauged the enzymatic conversion of yellow tetrazolium MTT to a purple formazan compound. The measurement occurred at a wavelength of 570 nm using a SpectraMax Plus 384 spectrophotometer from Molecular Devices, USA [ 39 , 40 ]. The percentage of cellular activity was computed using the formula: cell activity (%) = (Aexp − Aneg)/(Acon − Aneg) × 100%, where Aexp represents the absorbance value of the experimental group at 570 nm, Aneg signifies the absorbance value of the blank group at 690 nm, and Acon corresponds to the absorbance value of the control group at 570 nm.…”

Section: Methodsmentioning

confidence: 99%

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Enhanced Cellular Uptake and Transport of Bovine Lactoferrin Using Pectin- and Chitosan-Modified Solid Lipid Nanoparticles

Yao,

Bunt,

Liu

et al. 2023

Pharmaceutics

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Aim: The aim of this project is to use pectin- and chitosan-modified solid lipid nanoparticles for bovine lactoferrin to enhance its cellular uptake and transport. Methods: Solid lipid particles containing bovine lactoferrin (bLf) were formulated through the solvent evaporation technique, incorporating stearic acid along with either chitosan or pectin modification. bLf cellular uptake and transport were evaluated in vitro using the human adenocarcinoma cell line Caco-2 cell model. Results and Discussion: The bLf-loaded SLPs showed no significant effect on cytotoxicity and did not induce apoptosis within the eight-hour investigation. The use of confocal laser scanning microscopy confirmed that bLf follows the receptor-mediated endocytosis, whereas the primary mechanism for the cellular uptake of SLPs was endocytosis. The bLf-loaded SLPs had significantly more cellular uptake compared to bLf alone, and it was observed that this impact varied based on the time, temperature, and concentration. Verapamil and EDTA were determined to raise the apparent permeability coefficients (App) of bLf and bLf-loaded SLPs. Conclusion: This occurred because they hindered efflux by interacting with P-glycoproteins and had a penetration-enhancing influence. These findings propose the possibility of an additional absorption mechanism for SLPs, potentially involving active transportation facilitated by the P-glycoprotein transporter in Caco-2 cells. These results suggest that SLPs have the potential to be applied as effective carriers to improve the oral bioavailability of proteins and peptides.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Enhanced Cellular Uptake and Transport of Bovine Lactoferrin Using Pectin- and Chitosan-Modified Solid Lipid Nanoparticles

Yao,

Bunt,

Liu

et al. 2023

Pharmaceutics

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“…The preformulation scientist has a great deal of control over the medication-toexcipient ratio employed in these studies. The following conclusions are made from the drug-excipient compatibility studies [9].…”

Section: Drug-excipients Compatibilitymentioning

confidence: 99%

“…Hence, the preformulation studies are the optimum available tool for API and drug product development. It comprises a set of physicochemical parameters and biopharmaceutical principles to design and develop appropriate drug delivery systems [8,9]. Therefore, the experimental confirmation of the interaction of drug molecule and excipients are well studied at the preformulation level hence it gives an idea about their interaction and adduct formulation results in intelligent selection of drug molecules and excipients.…”

Section: Introductionmentioning

confidence: 99%

Preformulation Studies: A Versatile Tool in Formulation Design

Ahirwar¹,

Shukla²

2023

Drug Formulation Design

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The physicochemical properties of pharmacological molecules have a tremendous effect on safety and efficacy. Poor physicochemical properties can often make it hard to set up a reliable structure-activity relationship (SAR) with no prominent efficacy in preclinical and clinical models. This can lead to more variability in capability and higher drug development costs in the entire development process, and in the worst case, even to stop the clinical trials in the later period. Understanding the basic physicochemical properties makes it possible to separate and untangle investigational observations hence poor molecular properties can be changed or fixed during the design phase. This makes it more likely that the molecule will make it through the long and difficult development process. The decline in innovator pharmacotherapeutics number registrations decline each year and the industry is under even more pressure than in the past to speed up the drug development process. This reduces the length of time required for development and introduces innovative pharmaceutical products. To do this, it is imperative to proceed with an organised approach and act appropriately the first time. The current chapter aims to focus on the important physicochemical properties of the selected molecule, along with how those properties are evaluated and implicated in both discovery enablement and final dosage form development.

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“…Glutathione (GSH) is a tripeptide containing the amino acids glutamic acid, cysteine and glycine [1]. Endogenous GSH is a potent antioxidant involved in many basic biological processes, including protein and DNA synthesis, cell proliferation, and oxidation/reduction signaling [2].…”

Section: Introductionmentioning

confidence: 99%

Oral delivery of glutathione: antioxidant function, barriers and strategies

Wei

Thakur

Liu

et al. 2022

Acta Materia Medica

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Glutathione (GSH) is a tripeptide with potent antioxidant activity, which is involved in numerous basic biological processes and has been used for interventions in various degenerative diseases. However, oral delivery of GSH remains challenging, similarly to that of other protein and peptide drugs, because the physicochemical barriers in the gastrointestinal (GI) tract lead to low oral bioavailability. Although several approaches have been explored to improve delivery, such as co-administration with penetration enhancers and enzymatic inhibitors, or encapsulation into nanoparticles, microemulsions and liposomes, appropriate formulations with clinical therapeutic effects remain to be developed. This review discusses approaches explored to developing an oral GSH delivery system that could provide protection against proteolytic degradation in the GI tract and enhance molecular absorption across the epithelial membrane. This system may be beneficial for the design and development of an oral formulation of GSH in the future.

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Preformulation studies of l-glutathione: physicochemical properties, degradation kinetics, and in vitro cytotoxicity investigations

Cited by 10 publications

References 28 publications

Enhanced Cellular Uptake and Transport of Bovine Lactoferrin Using Pectin- and Chitosan-Modified Solid Lipid Nanoparticles

Enhanced Cellular Uptake and Transport of Bovine Lactoferrin Using Pectin- and Chitosan-Modified Solid Lipid Nanoparticles

Preformulation Studies: A Versatile Tool in Formulation Design

Oral delivery of glutathione: antioxidant function, barriers and strategies

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