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Glibenclamide Nanocrystals in a Biodegradable Chitosan Patch for Transdermal Delivery: Engineering, Formulation, and
Hany S M Ali1, Ahmed F Hanafy2
1Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawwarah, Saudi Arabia; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Journal of Pharmaceutical Sciences
|November 22, 2016
Summary
Engineered glibenclamide (GBD) nanocrystals offer improved transdermal delivery, enhancing blood glucose reduction and minimizing hypoglycemia compared to micro-sized GBD. This novel approach shows significant potential for diabetes management.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biotechnology
Background:
- Glibenclamide (GBD) is an effective antidiabetic drug, but its oral administration is associated with significant side effects.
- Transdermal drug delivery systems (TDDSs) offer a potential alternative route for GBD administration.
- Nanotechnology provides opportunities to improve drug solubility, bioavailability, and therapeutic efficacy.
Purpose of the Study:
- To engineer GBD nanocrystals for enhanced transdermal delivery.
- To fabricate and characterize nano- and micro-GBD loaded chitosan-based TDDSs.
- To evaluate the in vitro release, permeation, and in vivo efficacy of nano-GBD TDDSs compared to micro-GBD TDDSs.
Main Methods:
- Combined precipitation and homogenization techniques were used to produce GBD nanocrystals.
- Differential scanning calorimetry and X-ray analyses confirmed GBD crystallinity.
- In vitro release and permeation studies across rat skin were conducted.
- In vivo studies assessed the efficacy in reducing blood glucose levels in hyperglycemic animal models.
Main Results:
- GBD nanocrystals (D50 = 429 nm) were successfully fabricated while maintaining crystallinity.
- Nano-GBD TDDSs exhibited significantly higher drug release (85% vs 61%) and permeation (498 μg/cm² vs 362 μg/cm²) compared to micro-GBD TDDSs within 24 hours.
- In vivo studies demonstrated superior efficacy of nano-GBD in reducing blood glucose levels and maintaining therapeutic concentrations for longer periods (24 hours) with minimized hypoglycemia.
- An enhancement factor of 1.7 was observed for nano-GBD permeation.
Conclusions:
- The developed GBD nanocrystal-based TDDS offers a promising strategy for improved transdermal delivery of glibenclamide.
- Nanocarrier formulation significantly enhances GBD release, permeation, and in vivo glycemic control.
- This approach holds potential for a safer and more effective GBD therapy, mitigating risks associated with oral administration.
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