Background <p>Diabetes mellitus is the main root of mortality worldwide and a major cause of death by 2030. As the global medical landscape shifts, diabetes presents a serious challenge to standard treatment methods. Orally administered insulin, used for treatment, has drawbacks including instability in the gastrointestinal system due to degrading enzymes and low absorption, resulting in comparatively poor uptake. Nanotechnology introduces remarkable possibilities for diabetes treatment through targeted and accurate drug delivery. Among various nanodosage forms, nanosponges and nanocrystals are considered the most appropriate strategy for diabetes care. The study intends to enhance the bioavailability of voglibose by encapsulating it in a voglibose nanosponges formulation (V-NSF) and a voglibose nanocrystals formulation (V-NCF). Design of experimentation was successfully carried out using the Box–Behnken design. The response parameters, essentially particle size, entrapment efficiency and PDI, have been speculated, followed by observed values using a particle size analyzer and entrapment efficiency methods. Various characterization parameters, such as in vitro drug release, FTIR, thermal analysis (DSC and XRD) and surface morphology (SEM), were used to analyze the results, accompanied by stability studies of the optimized formulation and in vivo studies performed using Sprague–Dawley rats.</p> Results <p>The particle size of V-NSF was 270.63 ± 5.9&#xa0;nm, and the PDI value was 0.165 ± 0.027. Entrapment efficiency was 78 ± 0.32%. In case of V-NCF, particle size was analyzed as 131 ± 0.31&#xa0;nm, PDI value of NCF was 0.140 ± 0.006, and entrapment efficiency was 74 ± 0.28%. All physical and chemical characterization parameters were confirmed by FTIR, SEM, DSC, XRD and in vitro release.</p> Conclusion <p>V-NSF and V-NCF exhibited confined size distribution, acceptable polydispersity index and greater value of entrapment efficiency. The pharmacodynamic studies showed that V-NSF elicits a remarkable antidiabetic effect compared to V-NCF, with moderate efficacy than voglibose itself. The data of optimized formulations can be useful for clinical implications and suggest that V-NSF and V-NCF could be effective in diabetic management.</p> Graphical abstract <p></p>

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In vitro characterization and in vivo antidiabetic studies of designed formulations: nanosponges and nanocrystals of voglibose

  • Preeti Aneja,
  • Rajender Guleria,
  • Dev Prakash Dahiya

摘要

Background

Diabetes mellitus is the main root of mortality worldwide and a major cause of death by 2030. As the global medical landscape shifts, diabetes presents a serious challenge to standard treatment methods. Orally administered insulin, used for treatment, has drawbacks including instability in the gastrointestinal system due to degrading enzymes and low absorption, resulting in comparatively poor uptake. Nanotechnology introduces remarkable possibilities for diabetes treatment through targeted and accurate drug delivery. Among various nanodosage forms, nanosponges and nanocrystals are considered the most appropriate strategy for diabetes care. The study intends to enhance the bioavailability of voglibose by encapsulating it in a voglibose nanosponges formulation (V-NSF) and a voglibose nanocrystals formulation (V-NCF). Design of experimentation was successfully carried out using the Box–Behnken design. The response parameters, essentially particle size, entrapment efficiency and PDI, have been speculated, followed by observed values using a particle size analyzer and entrapment efficiency methods. Various characterization parameters, such as in vitro drug release, FTIR, thermal analysis (DSC and XRD) and surface morphology (SEM), were used to analyze the results, accompanied by stability studies of the optimized formulation and in vivo studies performed using Sprague–Dawley rats.

Results

The particle size of V-NSF was 270.63 ± 5.9 nm, and the PDI value was 0.165 ± 0.027. Entrapment efficiency was 78 ± 0.32%. In case of V-NCF, particle size was analyzed as 131 ± 0.31 nm, PDI value of NCF was 0.140 ± 0.006, and entrapment efficiency was 74 ± 0.28%. All physical and chemical characterization parameters were confirmed by FTIR, SEM, DSC, XRD and in vitro release.

Conclusion

V-NSF and V-NCF exhibited confined size distribution, acceptable polydispersity index and greater value of entrapment efficiency. The pharmacodynamic studies showed that V-NSF elicits a remarkable antidiabetic effect compared to V-NCF, with moderate efficacy than voglibose itself. The data of optimized formulations can be useful for clinical implications and suggest that V-NSF and V-NCF could be effective in diabetic management.

Graphical abstract