Title:Nanostructured Lipid Carrier-Mediated Transdermal Delivery System of
Glibenclamide for Gestational Diabetes: Pharmacokinetic and
Pharmacodynamic Evaluation
Volume: 21
Issue: 10
Author(s): Ashwini M.*, Preethi Sudheer and Bharani S. Sogali
Affiliation:
- Department of Pharmaceutics, Nitte (Deemed to be University), NGSM Institute of Pharmaceutical Sciences, Mangaluru,
Karnataka 575018, India
Keywords:
Glibenclamide, gestational diabetes mellitus, nanostructured lipid carriers, hot homogenization with ultrasonication, melt dispersion technique.
Abstract:
Background: Gestational diabetes mellitus (GDM) poses significant risks during pregnancy
for both mother and fetus. Adherence to oral antidiabetic medications, like glibenclamide (GB),
can be challenging, necessitating novel drug delivery methods. Nanostructured lipid carriers (NLC)
offer a promising approach by efficiently permeating the skin due to their small size and lipid-based
composition.
Objective: This study aimed to develop and evaluate transdermal patches loaded with glibenclamide
NLCs to treat GDM.
Methods: Glibenclamide NLCs were prepared using hot homogenization with ultrasonication and
melt dispersion method. A central composite design was utilized to optimize the formulations. Transdermal
patches containing optimized NLCs were developed using HPMC K 100 and Eudragit L polymers.
The patches were evaluated for various parameters, and their pharmacokinetic and pharmacodynamic
studies were carried out to assess their safety and efficacy.
Results: Optimized NLCs efficiently permeated rat skin. Cell viability studies indicated the nontoxicity
of the formulations. NLC-loaded transdermal patches (F2 and F7) showed drug release of
1098 μg/cm2 and 1001.83 μg/cm2 in 24 h, with a 2.5-fold higher flux and permeation coefficient than
the GB patch. Pharmacokinetic analysis revealed Tmax of 8 and 10 h and Cmax of 7127 ng/ml and 7960
ng/ml for F2 and F7, respectively, ensuring sustained drug action. AUC0-α was 625681 ng/ml·h and
363625 ng/ml·h for F2 and F7, respectively, indicating improved bioavailability.
Conclusion: Transdermal patches incorporating NLCs hold promise for enhancing glibenclamide's
therapeutic efficacy in GDM treatment. Improved skin permeation, sustained drug release, and enhanced
bioavailability make NLC-based transdermal patches a potential alternative with better patient
compliance.
