The European Medicine Agency has approved canagliflozin (CGF) drug to improve glycemic control in patients with type II diabetes. Our study aimed to enhance the solubility and pharmacokinetics of canagliflozin. Since crystalline canagliflozin is insoluble in water, its absolute bioavailability is less than 65%. Gelucire 50/13 was used as a lipid-based drug carrier to create solid dispersions of canagliflozin. SEM, PXRD, and DSC analysis all pointed to canagliflozin as having a crystal structure. Fusion and solvent evaporation methods were used to prepare the solid dispersions. In solid dispersions, the medication was found to be amorphized according to SEM, DSC, and PXRD studies. The water solubility of canagliflozin increased significantly by 11-23 fold using the solvent evaporation approach and by 12-25 fold using the fusion method. The pharmacokinetic parameters are improved at higher concentrations of gelucire. With pure canagliflozin, the AUC values climbed over 4 h (t) to 23440 µgh/mL, while with GDF 1:7, they grew to 52217. Gelucire 50/13 is an excellent option as a biomaterial carrier for drug delivery systems that use solid dispersion because it enhances biological membrane penetration. By dispersing the canagliflozin and gelucire, bioavailability may be enhanced by the fusion process that achieves molecular binding.

Download full-text PDF

Source
http://dx.doi.org/10.1080/10837450.2024.2436184DOI Listing

Publication Analysis

Top Keywords

solid dispersions
12
canagliflozin
8
gelucire 50/13
8
solvent evaporation
8
transforming canagliflozin
4
canagliflozin solubility
4
solubility lipidic
4
lipidic carrier
4
carrier pharmacokinetic
4
pharmacokinetic study
4

Similar Publications

Single-molecule resolution of the conformation of polymers and dendrimers with solid-state nanopores.

Talanta

January 2025

Chongqing Institute of Green and Intelligent Technology, Chinese Academy of Sciences & Chongqing School, University of Chinese Academy of Science, Chongqing, 400714, PR China. Electronic address:

Polymers and dendrimers are macromolecules, possessing unique and intriguing characteristics, that are widely applied in self-assembled functional materials, green catalysis, drug delivery and sensing devices. Traditional approaches for the structural characterization of polymers and dendrimers involve DLS, GPC, NMR, IR and TG, which provide their physiochemical features and ensemble information, whereas their unimolecular conformation and dispersion also are key features allowing to understand their transporting profile in confined ionic nanochannels. This work demonstrates the nanopore approach for the determination of charged homopolymers, neutral block copolymer and dendrimers under distinct bias potentials and pH conditions.

View Article and Find Full Text PDF

Metastasis of alveolar soft part sarcoma (ASPS) to the adrenal gland is infrequent, with only eight patients reported in the literature. Here we present an ASPS in an adolescent girl presented as a hypervascular adrenal incidentaloma along with a review of the available literature. This study aims to serve as a reference to aid in the pre-operative radiological and histopathological diagnosis of this rare entity.

View Article and Find Full Text PDF

Uptake and Transpiration of Solid and Hollow SiO Nanoparticles by Terrestrial Plant (Apium Graveolens var. secalinum).

Chemosphere

January 2025

Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China; Division of Environment and Sustainability, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China; HKUST Shenzhen-Hong Kong Collaborative Innovation Research Institute, Futian, Shenzhen, Guangdong Province, China. Electronic address:

Recent studies have raised concerns about the potential toxicity of amorphous silica (SiO) nanoparticles (NPs). This investigation explores the uptake, transport, and transpiration of silica NPs in Apium graveolens var. secalinum.

View Article and Find Full Text PDF

Determination of five alternaria toxins in peppermint by dispersive solid-phase extraction coupled with ultra-high performance liquid chromatography-tandem mass spectrometry based on MOF-808-TFA.

Food Chem

January 2025

School of Chemistry and Chemical Engineering, Nanchang University, Nanchang 330031, People's Republic of China; State Key Laboratory of Food Science and Resources, Nanchang University, Nanchang 330031, People's Republic of China. Electronic address:

An efficient and rapid ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MSMS) method was developed for simultaneous determination of 5 alternaria toxins (ATs) in edible and medicinal plant - peppermint using MOF-808-trifluoroacetic acid (MOF-808-TFA) as the adsorbent. Characterization methods such as scanning electron microscopy (SEM), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS) and N adsorption-desorption demonstrated that the synthesized MOF-808-TFA had a regular ortho-octahedral configuration and high specific surface area. Under the optimal conditions, the 5 ATs showed good linearity (R ≥ 0.

View Article and Find Full Text PDF

Melt electrowriting of amorphous solid dispersions: Influence of drug and plasticizer on rheology and printing performance.

Int J Pharm

January 2025

Soft Matter Chemistry, Department of Chemistry, and Helsinki Institute of Sustainability Science, Faculty of Science, University of Helsinki, PB55 00014 Helsinki, Finland. Electronic address:

Drug loaded microfiber scaffolds have potential for sublingual drug delivery due to their fast dissolution time and tunable porosity. Such microfiber scaffolds can be prepared by melt electrowriting (MEW), wherein a polymer melt is electrostatically drawn out of a syringe onto a computer controlled moving collector. The fabrication of such scaffolds via MEW has previously been shown for a polymer with a glass transition temperature (T) just above room temperature, making handling challenging.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!