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Development and Optimization of Mirabegron Solid Lipid Nanoparticles as an Oral Drug Delivery for Overactive Bladder
Prajakta Raut1, Makarand Gambhire1, Dhruvi Panchal1
1Department of Pharmaceutics, Sinhgad College of Pharmacy, Pune, India.
Background:
Mirabegron (MBN), a β-3 adrenergic agent, is used in the treatment of overactive bladder. MBN has alow water solubility, high first-pass metabolism, and low bioavailability, consequently having poor absorption in the gastrointestinal tract.
Objective:
The present study is intended to formulate Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400 to bypass hepatic first-pass metabolism and to improve its oral bioavailability.
Methods:
MBN-SLNs were developed using glyceryl monostearate by pre-emulsion-ultrasonication method, which was then optimized applying Box-Behnken Design. The optimized batch of MBN-SLN was selected for surface-modification with PEG-400 (MBN-PEG-SLN) and characterized by photon correlation spectroscopy, DSC, and XRD. Bioavailability studies were conducted in Wistar rats after oral administration of plain MBN dispersion, MBN-SLN, and MBN-PEG-SLN.
Results:
Stable MBN-SLNs and MBN-PEG-SLN of the optimized batch having a mean particle size of 162.7 nm and 149.9 nm; zeta potential of -39.1 mV and -30.9 mV; % entrapment of 89.90% and 90.12%, respectively, were developed. The results of the in vitro drug release studies demonstrated a significant slow release of MBN from MBN-SLN (69.38%) and MBN-PEG-SLN (61.33%) as compared to the dispersion of pure drug (92.10%). The relative bioavailability, as a result of the in vivo studies, of MBN from MBN-PEG-SLN increased by 2-fold, based on the Cmax values, in comparison with the plain MBN dispersion.
Conclusion:
Thus, the study established that the oral bioavailability of MBN could be improved by the administration of MBN-PEG-SLN. The obtained results indicate SLNs as a potential drug delivery system for improving the bioavailability of poorly bioavailable drugs such as MBN by abating the first-pass metabolism.
Insights
This study developed Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400 to enhance oral bioavailability. The MBN-PEG-SLN formulation successfully doubled the drug's bioavailability in rats by bypassing liver metabolism.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Mirabegron (MBN) is a β-3 adrenergic agent for overactive bladder.
- MBN exhibits poor oral absorption due to low water solubility and high first-pass metabolism.
- This limits its therapeutic efficacy and necessitates improved delivery strategies.
Purpose of the Study:
- To formulate Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400.
- To enhance oral bioavailability of Mirabegron by bypassing hepatic first-pass metabolism.
- To evaluate the potential of SLNs as a drug delivery system for poorly bioavailable drugs.
Main Methods:
- MBN-SLNs were prepared using glyceryl monostearate via pre-emulsion-ultrasonication and optimized with Box-Behnken Design.
- Optimized MBN-SLN were surface-modified with PEG-400 to create MBN-PEG-SLN.
- Characterization included particle size, zeta potential, entrapment efficiency, in vitro release, and in vivo bioavailability studies in Wistar rats.
Main Results:
- Stable MBN-SLNs and MBN-PEG-SLNs were successfully developed with controlled particle sizes and high entrapment efficiencies.
- In vitro studies showed sustained drug release from MBN-SLN and MBN-PEG-SLN compared to plain MBN dispersion.
- In vivo studies demonstrated a 2-fold increase in MBN bioavailability from MBN-PEG-SLN compared to plain MBN dispersion, based on Cmax.
Conclusions:
- The administration of MBN-PEG-SLN significantly improves the oral bioavailability of Mirabegron.
- Solid lipid nanoparticles (SLNs) represent a promising drug delivery system for enhancing the bioavailability of poorly absorbed drugs.
- PEGylation of SLNs further aids in overcoming pharmacokinetic limitations like first-pass metabolism.
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