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Published on: May 22, 2017
Preparation and characterization of nitrendipine solid lipid nanoparticles
K Manjunath1, V Venkateswarlu, A Hussain
1NDDS Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India. manju_kop@yahoo.com
Die Pharmazie
|May 11, 2011
Summary
This study developed stable solid lipid nanoparticles (SLNs) for nitrendipine, significantly improving drug entrapment and stability. The novel SLN formulation enhances nitrendipine delivery, addressing its poor oral bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Nitrendipine, a dihydropyridine calcium channel blocker, exhibits poor oral bioavailability (10-20%) primarily due to first-pass metabolism.
- Effective drug delivery systems are crucial for enhancing the therapeutic efficacy of poorly bioavailable drugs like nitrendipine.
Purpose of the Study:
- To develop and characterize solid lipid nanoparticles (SLNs) for improved oral delivery of nitrendipine.
- To optimize SLN formulations and evaluate their physical stability, drug entrapment, and in vitro release profiles.
Main Methods:
- SLNs were prepared using hot homogenization and ultrasonication with various triglycerides, soy phosphatidylcholine, poloxamer 188, and charge modifiers.
- Particle size and zeta potential were determined using photon correlation spectroscopy (PCS).
- Drug-lipid interactions and physical state were analyzed by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD); in vitro release was assessed using a modified Franz diffusion cell.
Main Results:
- Stable nitrendipine-loaded SLNs with mean sizes ranging from 79 to 213 nm and zeta potentials from -38.2 to +34.6 mV were successfully developed.
- High drug entrapment efficiency (approximately 99%) was achieved, with SLNs demonstrating stability at 4°C and 25°C.
- DSC and PXRD indicated that nitrendipine exists in an amorphous state within the SLNs, and drug release followed Weibull distribution.
Conclusions:
- Solid lipid nanoparticles offer a promising platform for enhancing the oral delivery of nitrendipine by improving its bioavailability and stability.
- The amorphous dispersion of nitrendipine within SLNs and its release kinetics suggest potential for sustained drug delivery.
