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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Self-emulsifying bifendate pellets: preparation, characterization and oral bioavailability in rats
Yanyu Xiao1, Shan Wang, Yinan Chen
1Department of Pharmacy, China Pharmaceutical University, Nanjing, PR China.
Drug Development and Industrial Pharmacy
|May 29, 2012
Summary
A novel self-emulsifying pellet (SEP) enhances the oral bioavailability of bifendate (DDB), a poorly soluble drug. This formulation uses extrusion/spheronization, offering a promising approach for improving drug delivery.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Biopharmaceutics
Background:
- Bifendate (DDB) exhibits poor water solubility, limiting its oral bioavailability.
- Traditional DDB pills show low in vitro release and limited absorption.
- Developing advanced drug delivery systems is crucial for improving the efficacy of poorly soluble drugs.
Purpose of the Study:
- To develop a self-emulsifying pellet (SEP) to enhance the oral bioavailability of bifendate (DDB).
- To investigate the potential of extrusion/spheronization technology in creating stable SEPs.
- To compare the in vitro and in vivo performance of the SEP with conventional DDB pills.
Main Methods:
- Formulation of a liquid self-emulsifying drug delivery system (SEDDS) using specific oil, surfactant, and co-surfactant ratios.
- Development of SEPs via extrusion/spheronization using the reconstituted emulsion and solid adsorbents.
- Characterization of SEP properties, including size, shape, and droplet size of the released emulsion.
- Evaluation of in vitro drug release in 0.1N HCl.
- Assessment of DDB pharmacokinetics (AUC) after oral administration in rats.
Main Results:
- Optimized liquid SEDDS and subsequent SEPs demonstrated comparable nano-droplet sizes.
- SEPs showed significantly enhanced in vitro DDB release compared to DDB pills.
- Oral administration of SEPs in rats resulted in a 2.36-fold increase in DDB AUC compared to DDB pills.
- The bioavailability enhancement with SEPs was comparable to the liquid SEDDS formulation.
Conclusions:
- Extrusion/spheronization is an effective technique for preparing self-emulsifying pellets.
- The developed SEP formulation significantly improves the oral bioavailability of bifendate (DDB).
- This SEP approach represents a promising strategy for enhancing the delivery of poorly water-soluble drugs.
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