Solid self-emulsifying nitrendipine pellets: preparation and in vitro/in vivo evaluation.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Poorly soluble drugs like nitrendipine (NTD) often exhibit low oral bioavailability.
• Solid self-emulsifying (SE) drug delivery systems offer potential to improve solubility and absorption.
• Developing stable and scalable solid SE formulations remains a challenge.

Purpose of the Study:

• To develop and evaluate novel solid SE pellets of nitrendipine (NTD).
• To assess the performance of these pellets compared to liquid SEDDS and conventional tablets.
• To investigate the suitability of the extrusion/spheronization technique for large-scale production.

Main Methods:

• Preparation of liquid self-emulsifying drug delivery systems (SEDDS) with NTD.
• Solidification of liquid SEDDS into pellets using extrusion/spheronization with adsorbents and excipients.
• Characterization of SE pellet size, shape, and self-emulsification properties.
• In vitro drug release studies and in vivo oral bioavailability assessment in beagle dogs.

Main Results:

• Uniform SE pellets (800-1000 microm) were successfully prepared.
• SE pellets demonstrated comparable droplet size distribution to liquid SEDDS.
• In vitro release from SE pellets exceeded 80% within 30 min, significantly higher than conventional tablets (35%).
• Oral bioavailability (AUC) of NTD from SE pellets was 1.6-fold greater than conventional tablets and similar to liquid SEDDS.

Conclusions:

• Extrusion/spheronization is a viable method for large-scale production of solid SE pellets from liquid SEDDS.
• The developed SE pellets enhance NTD oral absorption, achieving bioavailability close to liquid SEDDS.
• Solid SE pellets offer improved formulation stability, reduced drug leakage, and precipitation compared to liquid formulations.