Self-assembled di- and tripeptide gels for the passive entrapment and pH-responsive, sustained release of an antidiabetic drug, glimepiride

Halder, Moumita; Bhatia, Yatin; Singh, Yashveer

doi:10.1039/d2bm00344a

Cited by 14 publications

(12 citation statements)

References 61 publications

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“…Binding of conjugates with ThT was measured by fluorescence spectra using a reported method. 61 An aqueous solution of ThT (50 μM) was prepared and filtered through a 0.2 μm syringe filter. To 100 μL of each sample (gels), 900 μL of the ThT solution was added and incubated for 6 h in the dark at room temperature.…”

Section: Discussionmentioning

confidence: 99%

“…The peptides were synthesized and conjugated with NSAIDs (naproxen and indomethacin) employing the standard 9-fluorenylmethoxycarbonyl (Fmoc)-based SPPS method using a Rink amide AM resin as a solid support. 61 Fmoc-protected amino acids (3 equiv) were coupled to the resin using a mixture of HATU (2.85 equiv) and DIEA (5.7 equiv) in anhydrous DMF for 4 h. After each coupling reaction, the Fmoc group was removed by mixing the resin with 20% piperidine in DMF for 50 min at room temperature. Each step was followed by washing the resin with DMF and DCM three times to remove unreacted reagents.…”

Section: Discussionmentioning

confidence: 99%

“…The scavenging capacity against the ABTS radicals was assessed according to the method mentioned earlier. 61 A stock solution of ABTS •+ was prepared by mixing 7 mM ABTS solution with 2.45 mM of potassium persulfate solution in PBS (pH 7.4) and kept overnight in the dark to generate radicals. The radical solution was diluted with PBS of pH 7.4, and the absorbance was adjusted to 0.8 at 734 nm.…”

Section: Discussionmentioning

confidence: 99%

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Supramolecular, Nanostructured Assembly of Antioxidant and Antibacterial Peptides Conjugated to Naproxen and Indomethacin for the Selective Inhibition of COX-2, Biofilm, and Inflammation in Chronic Wounds

2023

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Chronic wounds are a major healthcare challenge around the world. The presence of bacterial biofilms, accumulation of reactive oxygen species (ROS), and persistent inflammation have been identified as rate-limiting steps in chronic wound healing. Anti-inflammatory drugs, like naproxen (Npx) and indomethacin (Ind), show poor selectivity for the COX-2 enzyme, which plays a key role in producing inflammatory responses. To address these challenges, we have developed conjugates of Npx and Ind with peptides possessing antibacterial, antibiofilm, and antioxidant properties along with enhanced selectivity for the COX-2 enzyme. We have synthesized and characterized peptide conjugates Npx-YYk, Npx-YYr, Ind-YYk, and Ind-YYr, which were self-assembled into supramolecular gels. As envisaged, the conjugates and gels showed high proteolytic stability and selectivity toward the COX-2 enzyme and potent antibacterial activities (>95% within 12 h) against Gram-positive bacteria Staphylococcus aureus, implicated in wound-related infections, eradication of biofilm (∼80%), and radical scavenging (>90%) properties. Cell culture studies with mouse fibroblast cells (L929) and macrophage-like cells (RAW 264.7) showed that gels were cell proliferative in nature (120% viability), which resulted in faster and more efficient scratch healing. Treatment with gels led to a significant decrease in proinflammatory cytokine (TNF-α and IL-6) expressions and an increase in anti-inflammatory gene (IL-10) expression. The gels developed in this work show great promise as a topical agent for chronic wounds or as a coating for medical devices to prevent medical-device-associated infections.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Supramolecular, Nanostructured Assembly of Antioxidant and Antibacterial Peptides Conjugated to Naproxen and Indomethacin for the Selective Inhibition of COX-2, Biofilm, and Inflammation in Chronic Wounds

2023

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“…The ABTS solution was added to each sample and incubated in dark for 1 h. The suspension was centrifuged, and the absorbance of the collected supernatant was recorded using a UV–vis spectrophotometer. The percent antioxidant activity was calculated using the following equation, and ascorbic acid (1%) was taken as a positive control: % A ntioxidant activity = true[ A normalc − A normals A normalc true] × 100 where A c indicates the absorbance of the control, and A s represents the absorbance of the sample.…”

Section: Methodsmentioning

confidence: 99%

Thiol-Functionalized, Antioxidant, and Osteogenic Mesoporous Silica Nanoparticles for Osteoporosis

Rasool,

Negi,

Singh

2023

ACS Biomater. Sci. Eng.

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Osteoporosis is a chronic bone disorder characterized by decreased bone mass, leading to brittle bones and fractures. Oxidative stress has been identified as the most profound trigger for the initiation and progression of osteoporosis. Current treatment strategies do not induce new bone formation and fail to address a high level of reactive oxygen species (ROS). Mesoporous silica nanoparticles (MSNs) have been explored in bone tissue regeneration owing to their inherent osteogenic property, but they lack antioxidant and cell adhesion properties, required in such applications. We have developed thiolated, bioactive mesoporous silica nanoparticles (MSN-SH) to address this challenge. MSNs were fabricated using the Stober method, and 11% of the surface was functionalized post-synthesis with thiol groups using MPTMS to obtain MSN-SH. The particle size measured by the dynamic light scattering technique was found to be around 300 nm. The surface morphology was investigated using HR-TEM, and their physical and chemical properties were characterized using various spectroscopic techniques. They exhibited more than 90% antioxidant activity, neutralized ROS formed in cells, and provided protection against ROSinduced cell damage. The cell viability assay in murine osteoblast precursor cells (MC3T3) showed that MSN-SH is cell-proliferative in nature with 140% cell viability. Osteogenic potential was evaluated by measuring the ALP activities, calcium deposition, and gene expression levels of osteogenic markers, such as RUNX2, ALP, OCN, and OPN, and results revealed that MSN-SH increases calcium deposition and induces osteogenesis through upregulation of osteogenic genes and markers without the involvement of any osteogenic supplements. Besides promoting osteogenesis, MSN-SH was found to inhibit osteoclastogenesis. The nanomaterial was found to be regenerative in nature, and it stimulated migration of osteoblast cells and caused a complete wound closure within 48 h. We were able to achieve a multifunctional nanomaterial by simply modifying the surface. MSNs have been explored for bone tissue engineering/osteoporosis as a composite system incorporating metals, like gold and cerium, or as a nanocarrier loaded with growth factors or active drugs. This study offers a simple and economical method to enhance the existing properties of MSNs and impart new activities by a single-step surface modification. It can be concluded that MSN-SH holds promise as a complementary and alternate treatment for osteoporosis along with the standardized therapy.

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“…S5 †). 16,17 As the pressing duration increased, the fluorescence intensity of FITC increased from 50 to 180, indicating that PRNV could gradually release drugs under appropriate external pressure (Fig. 3l).…”

Section: Biomaterials Science Papermentioning

confidence: 96%

A painless and flexible bi-directional blood glucose-regulating system inspired by an inverter air conditioner

et al. 2022

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Self-assembled di- and tripeptide gels for the passive entrapment and pH-responsive, sustained release of an antidiabetic drug, glimepiride

Abstract: Diabetes is a global epidemic that poses a severe challenge to public health. The characteristic features of this disease are hyperglycemia and deterioration of the function of pancreatic β-cells, which...

Cited by 14 publications

References 61 publications

Supramolecular, Nanostructured Assembly of Antioxidant and Antibacterial Peptides Conjugated to Naproxen and Indomethacin for the Selective Inhibition of COX-2, Biofilm, and Inflammation in Chronic Wounds

Supramolecular, Nanostructured Assembly of Antioxidant and Antibacterial Peptides Conjugated to Naproxen and Indomethacin for the Selective Inhibition of COX-2, Biofilm, and Inflammation in Chronic Wounds

Thiol-Functionalized, Antioxidant, and Osteogenic Mesoporous Silica Nanoparticles for Osteoporosis

A painless and flexible bi-directional blood glucose-regulating system inspired by an inverter air conditioner

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