Journal: Nature Communications

Article Title: Circadian fluctuation of soluble CD26 dictates the impact of the timing of cord blood transplantation on acute graft-versus-host disease

doi: 10.1038/s41467-026-68958-4

Figure Lengend Snippet: a Experimental design. Three doses of Sitagliptin (30 mg/kg, DPPIV inhibitor) or an equal volume of PBS were intraperitoneally given to ZT5 mice before human cord blood-derived mononuclear cells (CBMCs) infusions. b Representative images of PBS-treated (top) and Sitagliptin-treated (bottom) ZT5 recipients showing phenotypic differences on day 21 after CBT. c – e aGVHD scores ( c , P = 0.003), survival rates ( d , P = 0.030) and body weights ( e , P = 0.624) of recipients posttransplantation ( n = 8 mice for the control group; n = 5 for the Sitagliptin group). f , g Histopathologic analysis of liver, lung, spleen and colon sections on day 21 after CBT. Representative H&E-stained images ( f ) and quantification results ( g ) ( n = 24-30 images from 4-6 mice per group) Two-sided unpaired t-tests were used for comparisons. The exact P values were: P < 0.001 for liver, lung, and spleen; P = 0.850 for colon. h – k The infiltration of CD4 + T cells and CD8 + T cells in liver, lung, spleen and colon sections on day 21 after transplantation. Representative immunohistochemistry images and quantification results of staining with anti-human CD4 ( h , i ) or CD8 ( j , k ) polyclonal antibodies ( n = 3 mice per group; 24 fields of view were analyzed per organ). For CD4⁺ T cell infiltration, statistical comparisons yielded P < 0.001 for liver and lung, P = 0.002 for spleen, and P = 0.285 for colon; For CD8⁺ T cell infiltration, statistical comparisons yielded P < 0.001 for liver, lung and spleen, and P > 0.999 for colon. AOD, average optical density. Scale bars, 100 μm. The data are presented as the means ± SEMs and were analyzed by unpaired t tests followed by Bonferroni-Dunn correction ( g , i and k ), two-way ANOVA followed by the Bonferroni post hoc correction ( c and e ), and the log-rank test ( d ). Source data are provided as a Source Data file.

Article Snippet: To inhibit DPPIV activity in ZT5 recipient mice, the animals were intraperitoneally injected with 30 mg/kg of Sitagliptin phosphate monohydrate (S4002, Selleck) or an equal volume of PBS as indicated.

Techniques: Derivative Assay, Control, Staining, Transplantation Assay, Immunohistochemistry

Journal: Nature Communications

Article Title: Circadian fluctuation of soluble CD26 dictates the impact of the timing of cord blood transplantation on acute graft-versus-host disease

doi: 10.1038/s41467-026-68958-4

Figure Lengend Snippet: PBMCs from healthy donors were cultured with PHA-L (control group), PHA-L plus CD26/DPPIV (sCD26 group), or PHA-L plus Sitagliptin (DPPIV inhibitor, DPPIVi group) for 72 h. a Experimental design. PBMCs from healthy donors were cultured with PHA-L (control group), PHA-L plus CD26/DPPIV (sCD26 group), or PHA-L plus Sitagliptin (DPPIV inhibitor, DPPIVi group) for 72 h. b , c Representative plots (left) and quantified percentages (right) of CD86 + ( b ) and CD80 + ( c ) CD14 + cells after 72 h of PBMCs coculture in different groups (pooled data from 8 healthy donors across four independent experiments). d – i Representative plots (left) and quantified percentages (right) of Ki-67 + , IFNγ + , and CD38 + cells among CD4 + T cells ( d , f , h ) and CD8 + T cells ( e , g , i ) after 72 h of PBMCs coculture in different groups (pooled data from 6 healthy donors across three independent experiments).The data are presented as the means ± SEMs and were analyzed by one-way ANOVA with the Bonferroni correction for multiple comparisons ( b – i ). All P values are two-sided and reported as exact values unless <0.001. Source data are provided as a Source Data file.

Article Snippet: To inhibit DPPIV activity in ZT5 recipient mice, the animals were intraperitoneally injected with 30 mg/kg of Sitagliptin phosphate monohydrate (S4002, Selleck) or an equal volume of PBS as indicated.

Techniques: Cell Culture, Control

Journal: Nature Communications

Article Title: Circadian fluctuation of soluble CD26 dictates the impact of the timing of cord blood transplantation on acute graft-versus-host disease

doi: 10.1038/s41467-026-68958-4

Figure Lengend Snippet: a Experimental design. CellTrace TM Violet (CTV)-labeled human PBMCs were cocultured with irradiated allogeneic PBMCs in the presence of recombinant human sCD26/DPPIV protein (sCD26,1000 ng/ml) or Sitagliptin (200 μg/ml) for 96 h. b , c Representative plots (left) and quantified percentages (right) of cell proliferation in CD4⁺ ( b ) and CD8⁺ ( c ) T cells after 96 h of coculture. d , e Representative plots (left) and quantified percentages (right) of IFNγ production in CD4⁺ ( d ) and CD8⁺ ( e ) T cells after 96 h of coculture. f , g Representative plots (left) and quantified percentages (right) of CD38 expression in CD4⁺ ( f ) and CD8⁺ ( g ) T cells after 96 h of coculture. The data were pooled from three independent experiments. The data are presented as means ± SEMs. Statistical significance was determined by one-way ANOVA with Bonferroni correction ( b – g ). All P values are two-sided and reported as exact values unless <0.001. Source data are provided as a Source Data file.

Article Snippet: To inhibit DPPIV activity in ZT5 recipient mice, the animals were intraperitoneally injected with 30 mg/kg of Sitagliptin phosphate monohydrate (S4002, Selleck) or an equal volume of PBS as indicated.

Techniques: Labeling, Irradiation, Recombinant, Expressing

Journal: Scientific Reports

Article Title: Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells

doi: 10.1038/srep35633

Figure Lengend Snippet: The expression levels of 4 selected genes (metallothionein (Mt) 1, Mt2, S100a8, and S100a9) in the liver of vildagliptin (1000 mg/kg)-treated mice were measured by real-time RT-PCR analysis, and vildagliptin-induced fold changes were compared with those obtained from expression array analysis ( A ). The expression levels of Mt1, Mt2, S100a8, and S100a9 in the liver of sitagliptin (1000 mg/kg)-treated mice were also measured by real-time RT-PCR analysis ( B ). In the real-time RT-PCR analysis, expression was normalized with the expression of cyclophilin (CPH) and the expression level in the liver of control mice was defined as 1. Data represent the means ± S.D. of three independent experiments. ## P < 0.01, compared with the liver of control mice.

Article Snippet: Sitagliptin was obtained from LKT Laboratories (St. Paul, MN, USA).

Techniques: Expressing, Quantitative RT-PCR, Control

Journal: Scientific Reports

Article Title: Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells

doi: 10.1038/srep35633

Figure Lengend Snippet: HepG2 cells were treated with the indicated concentration (μM) of vildagliptin, M20.7, or sitagliptin for 24 h. The mRNA expression levels of S100A9 and TNF-α in HepG2 cells were measured by real-time RT-PCR analysis. Expression was normalized with the expression of GAPDH. Data represent the means ± S.D. of three independent experiments. *P < 0.05; **P < 0.01, compared with control (0.1% methanol).

Article Snippet: Sitagliptin was obtained from LKT Laboratories (St. Paul, MN, USA).

Techniques: Concentration Assay, Expressing, Quantitative RT-PCR, Control

Journal: Scientific Reports

Article Title: Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells

doi: 10.1038/srep35633

Figure Lengend Snippet: ( A ) HL-60 cells were treated with the indicated concentration (μM) of vildagliptin, M20.7, sitagliptin, or LPS for 24 h. The mRNA expression levels of S100A9 and TNF-α in HL-60 cells were measured by real-time RT-PCR analysis. Expression was normalized with the expression of GAPDH. ( B–E ) HL-60 cells were treated with the indicated concentration (μM) of vildagliptin, M20.7, sitagliptin, or LPS for 48 h. The release of S100A8/A9 complex ( B , D ) and TNF-α ( C , E ) in the culturing medium was measured by ELISA. LPS (10 μg/mL) was used as a positive control. Data represent the means ± S.D. of three independent experiments. *P < 0.05; **P < 0.01, compared with control (0.1% methanol). # P < 0.05, compared with 100 μM sitagliptin. Sita 100, sitagliptin 100 μM; Vilda 100 + Sita 100, vildagliptin 100 μM + sitagliptin 100 μM.

Article Snippet: Sitagliptin was obtained from LKT Laboratories (St. Paul, MN, USA).

Techniques: Concentration Assay, Expressing, Quantitative RT-PCR, Enzyme-linked Immunosorbent Assay, Positive Control, Control

Journal: Scientific Reports

Article Title: Vildagliptin and its metabolite M20.7 induce the expression of S100A8 and S100A9 in human hepatoma HepG2 and leukemia HL-60 cells

doi: 10.1038/srep35633

Figure Lengend Snippet: DPP-4 activity in HL-60 cells ( A ) and time-dependent changes of M20.7 concentration in the culturing medium of vildagliptin-treated HL-60 cells ( B ). ( A ) DPP-4 activity of S9 fraction of HL-60 cells was measured using a Gly-Pro-AMC as a substrate. Data represent the means ± S.D. of triplicate determinations. S9-active, active S9 fraction; S9-inactive, heat-inactivated S9 fraction (negative control); ND, not detectable. ( B ) HL-60 cells were treated with 100 μM vildagliptin with or without 100 μM sitagliptin for various durations. The M20.7 concentration in the culturing medium was measured by LC-MS/MS analysis. Data represent the means ± S.D. of three independent experiments. # P < 0.05; ## P < 0.01; ### P < 0.001, compared with vildagliptin and sitagliptin-treated HL-60 cells of each time point.

Article Snippet: Sitagliptin was obtained from LKT Laboratories (St. Paul, MN, USA).

Techniques: Activity Assay, Concentration Assay, Negative Control, Liquid Chromatography with Mass Spectroscopy

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Multiple comparisons of DEGs between groups. Summary table of the number of DEGs acquired for each comparison at distinct significance thresholds (green: db/db sitagliptin vs. db/+ control; red: db/db vehicle vs. db/+ control; blue: db/db sitagliptin vs. db/db vehicle) ( n = 10).

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Comparison, Control

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Comparison of retinal expression patterns between sitagliptin-treated and vehicle-treated db/db mice. ( A ) HeatMap for comparison of sitagliptin-treated db/db mice and vehicle-treated db/db mice with genes with an adjusted p -value of less than 0.05 and an absLogFC greater than 0.3 (20 genes). High and low row z-scores are represented in red and blue, respectively ( n = 10).

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Comparison, Expressing

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Most differentiated genes. ( A ) Table of top 10 genes more differentially expressed in the comparison between vehicle-treated and sitagliptin-treated mice. AveExpr is the average expression of the gene across all the arrays in log2 scale. t is a “moderated-t” statistic similar to the usual Student’s t statistic ( n = 10). ( B ) Volcano plot of db/db sitagliptin and db/db vehicle comparison. Genes are shown in purple when adjusted p -value was under 0.05, and absolute logarithmic fold change was above 0.3. Gene symbols are shown for the top 20 most significant genes ( n = 10).

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Comparison, Expressing

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Enrichment analysis of the transcriptome study between vehicle-treated db/db mice and db/db mice treated with sitagliptin using the GO Database (BP subcategory). ( A ) Table of top 10 enriched GO terms (BP) for the comparison “db/db sitagliptin vs. db/db vehicle”. ( B ) Network plot of the top five enriched GO term (BP) for “db/db sitagliptin vs. db/db vehicle”. ( C ) Dot plot of the top 15 enriched GO terms (BP) for the “db/db sitagliptin vs. db/db vehicle” comparison. Results were adjusted with a p -value less than 0.25 The results shown correspond to the top enriched terms with an adjusted p -value < 0.07.

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Comparison

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Enrichment analysis of the transcriptome comparison between vehicle-treated db/db mice and db/db mice treated with sitagliptin using the Reactome Pathway Database. ( A ) Table of the top 10 enriched pathways (Reactome Pathway Database) for the comparative study “db/db sitagliptin vs. db/db vehicle”. ( B ) Network plot of the top five enriched pathways for the comparison between db/db sitagliptin and db/db vehicle conditions (Reactome Pathway Database). ( C ) Dot plot of the top 15 enriched pathways (Reactome Pathway Database). The results shown correspond to the top enriched terms with an adjusted p -value < 0.05.

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Comparison

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Gene set enrichment analysis (GSEA). ( A – C ) Heatmaps of the most enriched neurotransmission-related pathways between vehicle-treated db/db mice and sitagliptin-treated db/db mice.

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques:

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Sitagliptin-enhanced pathways related to synaptic transmission. ( A – C ) Most enriched terms involved in neurotransmission between sitagliptin-treated db/db mice and db/db mice treated with vehicle using the GO database (Biological Process (BP), Cellular Component (CC) and Molecular Function (MF) subcategories, respectively) ( p -value < 0.005). X-axis shows the enrichment score in each category. ( D ) Cluster related to synaptic transmission from the GO enrichment map of the top 60 enriched terms (BP) between db/db sitagliptin and db/db vehicle.

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Transmission Assay

Journal: International Journal of Molecular Sciences

Article Title: Transcriptomic Analysis Reveals That Retinal Neuromodulation Is a Relevant Mechanism in the Neuroprotective Effect of Sitagliptin in an Experimental Model of Diabetic Retinopathy

doi: 10.3390/ijms24010571

Figure Lengend Snippet: Study of gene expression. ( A ) RT-PCR analysis of genes related to synapse formation and neurotransmission at presynaptic level in db/db mice treated with vehicle (black bars) or sitagliptin eye drops (gray bars) and in non-diabetic mice (white bars) ( n = 4). * p < 0.05, ** p < 0.01, *** p < 0.001. ( B ) RT-PCR analysis of genes associated with neurotransmission at postsynaptic level in db/db mice treated with vehicle (black bars) or sitagliptin eye drops (gray bars) and in non-diabetic mice (white bars) ( n = 4). * p < 0.05, ** p < 0.01. ( C ) Gene interactions of studied genes (STRING ver. 11.5). The red cluster displays genes related to presynaptic proteins, the blue cluster displays those related to postsynaptic proteins and green cluster displays those related to proteins involved in synapse formation. Dashed lines represent interactions between genes from different clusters, while solid lines are the interactions of genes of the same cluster.

Article Snippet: At the age of 10 weeks, sitagliptin (sitagliptin phosphate monohydrate (Y0001812, Merck KGaA, Darmstadt, Germany)) eyedrops (10 mg/mL; n = 12) and vehicle (phosphate-buffered saline (PBS)) eyedrops ( n = 12) were randomly administered twice per day directly onto the superior corneal surface of each eye of diabetic mice with the aid of a micropipette (5 μL).

Techniques: Gene Expression, Reverse Transcription Polymerase Chain Reaction, Eye Drops

Journal: Nature

Article Title: Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance

doi: 10.1038/nature26138

Figure Lengend Snippet: a–d, Control, H-shDpp4- and sitagliptin-treated mice from those described in Extended Data Fig. 6c–h were analysed as follows. a, Plasma active GIP (1–42) and GLP1 (7–36). NS, not significant. b, CLS macrophages and Adgre1 mRNA in VAT, with representative images of F4/80-stained VAT. c, Il6, Mcp1, Tnfa and Il1b mRNA in VAT. d, Blood glucose after oral glucose (O-GTT), intraperitoneal glucose (IP-GTT), or intraperitoneal insulin (IP-ITT). Data are mean ± s.e.m., *P < 0.05 by one-way ANOVA.

Article Snippet: IRAK1–4 inhibitor I (A3505) and sitagliptin phosphate monohydrate (A4036) were from ApexBio.

Techniques: Staining

Journal: Vascular Health and Risk Management

Article Title: Sitagliptin/Simvastatin: a first combination tablet to treat type 2 diabetes and hypercholesterolemia – a review of its characteristics

doi: 10.2147/VHRM.S79198

Figure Lengend Snippet: Structural formula for sitagliptin.

Article Snippet: It was approved in October 2011 and is manufactured by MSD International GmbH for Merck and Co. Sitagliptin phosphate monohydrate is described chemically as 7-[(3 R )-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3- a ] pyrazine phosphate (1:1) monohydrate, with the structural formula shown in .

Techniques:

Journal: Vascular Health and Risk Management

Article Title: Sitagliptin/Simvastatin: a first combination tablet to treat type 2 diabetes and hypercholesterolemia – a review of its characteristics

doi: 10.2147/VHRM.S79198

Figure Lengend Snippet: Pharmacokinetics

Article Snippet: It was approved in October 2011 and is manufactured by MSD International GmbH for Merck and Co. Sitagliptin phosphate monohydrate is described chemically as 7-[(3 R )-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3- a ] pyrazine phosphate (1:1) monohydrate, with the structural formula shown in .

Techniques: Clinical Proteomics

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Individual pharmacokinetic analysis of sitagliptin concentrations among the different ocular tissues. ( A – D ) Temporary profiles of sitagliptin concentrations in the aqueous humor ( A ), vitreous humor ( B ), iris/ciliary body ( C ), and retina/choroid ( D ) for each dose and eye. A total n of 21 rabbits (3 at each time of extraction) was used for each eye. Symbols illustrate the mean value of the 3 animals at each extraction time, while the error bars represent the standard deviation. The concentration and time axes are presented in a logarithmic base-2 scale format.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Extraction, Standard Deviation, Concentration Assay

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Average levels of sitagliptin over 24 h obtained for each eye and administered dose in the different eye matrices. Data are displayed as mean ± standard deviation (SD) in conjunction with the coefficient of variation (CV). Values under the quantification limit are represented as --. A total n of 21 rabbits (3 at each time of extraction) was used for each eye.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Standard Deviation, Extraction

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Comparison of sitagliptin pharmacokinetic profiles between the four eye matrices studied. ( A , B ) Sitagliptin measurements (ng/g tissue) in the four studied parts of the eye during the experimental course of rabbits treated with sitagliptin 10 mg/mL ( A ) or sitagliptin 5 mg/mL ( B ). The pharmacokinetic profile of the aqueous humor (green circles), vitreous humor (blue circles), iris/ciliary body (black circles), and retina/choroid (red circles). A total n of 21 rabbits (3 at each time of extraction) was used per experimental group. The symbols represent the mean of the 3 animals for each extraction time, while the error bars represent the standard deviation. The concentration and time axes are presented in a logarithmic base-2 scale format. The X axis (time) is presented in a logarithmic base-2 scale format. A statistical analysis was conducted to compare the different concentrations, with the time points displaying significant differences highlighted in the graph on the right (5 mg/mL). * p < 0.05, ** p < 0.01.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Comparison, Extraction, Standard Deviation, Concentration Assay

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Pharmacokinetic profile of sitagliptin bloodstream levels for both tested concentrations. ( A ) Blood sitagliptin measurements (ng/mL) during the experimental course of rabbits treated with sitagliptin 10 mg/mL (dark blue circles) or sitagliptin 5 mg/mL (light blue circles). A total n of 21 rabbits (3 at each time of extraction) was used per experimental group. The symbols represent the mean of the 3 animals for each extraction time, while the error bars represent the standard deviation (SD). The concentration and time axes are presented in a logarithmic base-2 scale format. ( B ) Table exhibiting sitagliptin bloodstream concentrations for both groups during the experimental course. Concentrations are expressed as the mean ± SD of 3 animals at each extraction time. n = 21; * p < 0.05, ** p < 0.01.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Extraction, Standard Deviation, Concentration Assay

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Pharmacokinetic parameters obtained after non-compartmental analysis of the mean sitagliptin levels quantified in the different eye matrices. C max , maximum concentration reached; T max , time at which C max is reached; AUC obs , area under the curve of the concentrations in each matrix from 0 to the last observed point; AUC ∞ , area under the curve of the concentrations in each matrix from 0 to infinity; AUC ∞ /Dose, dose-normalized AUC ∞ . Values under the quantification limit are represented as --. A total n of 21 rabbits (3 at each time of extraction) was used for each eye.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Concentration Assay, Extraction

Journal: Pharmaceuticals

Article Title: Ocular and Plasma Pharmacokinetics of Sitagliptin Eye Drops: Preclinical Data

doi: 10.3390/ph17121579

Figure Lengend Snippet: Scheme showing the transscleral route of sitagliptin eye drops’ absorption. After eye drops are applied and distributed across the tear film, the drug is absorbed through the conjunctiva and then penetrates the sclera via diffusion. Certain factors, such as molecular size and lipophilicity, influence this process, with smaller, lipophilic molecules penetrating more easily. Once through the sclera, the drug reaches the choroid and, subsequently, the retina, where it exerts therapeutic effects.

Article Snippet: One test group received a topical ocular administration of sitagliptin phosphate monohydrate (SMS Pharmaceuticals Ltd., Hyderabad, Telangana, India) concentrated to 10 mg/mL (1%), while in the other group sitagliptin was concentrated to 5 mg/mL (0.5%).

Techniques: Eye Drops, Diffusion-based Assay