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Formulation and Characterization of CCD-based Optimized Geraniol-loaded Antidiabetic Niosomes
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DOI：10.2174/0113892002382359251122043509.png)
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Abstract
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Introduction: Type 2 Diabetes (T2D) presents a significant global health challenge, characterized by persistent hyperglycemia and insulin resistance, with effective long-term glycemic control remaining a critical unmet need. Geraniol, a naturally occurring monoterpene alcohol, holds promising antidiabetic potential but is limited by poor water solubility, which restricts its therapeutic application. This study focuses on the formulation and CCD-based optimization of geraniol-loaded niosomes. Additionally, to assess its antidiabetic effect, blood glucose levels were evaluated. Method: Geraniol-loaded niosomes were formulated using the thin-film hydration technique. A central composite design was generated using Design Expert software to evaluate the impact of Span 40 and cholesterol concentrations on dependent variables such as particle size and encapsulation efficiency. A streptozotocin-induced diabetic model was used to assess the in vivo antidiabetic effect of the geraniolloaded niosomes. Result: Using the thin-film hydration technique and CCD optimization, the niosomes demonstrated favorable characteristics, including an average particle size of 287.7 nm, an entrapment efficiency of 80.13%, and a zeta potential of-25.46 mV. Geraniol-loaded niosomes produced a notable hypoglycemic effect, reducing blood glucose levels from 275 +/- 0.28 mg/dL to 150 +/- 0.20 mg/dL by day 21. Although slightly less potent than metformin (117 +/- 0.93 mg/dL), the formulation showed significantly better efficacy than both the diabetic control and plain geraniol solution groups. Discussion: Pharmacokinetic analysis revealed that the AUC, AUMC, and MRT of the geraniol-loaded niosomal formulation were approximately 1.5-, 4-, and 3-fold higher, respectively, compared to plain geraniol. These findings indicate that niosomal formulations improve bioavailability while providing sustained and prolonged drug release. Conclusion: Overall, these results highlight the potential of geraniol-loaded niosomes as an innovative and effective strategy for managing T2D, supporting further clinical research to explore their therapeutic application in addressing this global health challenge.
Keywords:
Type 2 diabetes mellitus
geraniol
niosomes
antidiabetic potential
thin film hydration technique
Nanocarrier drug delivery
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