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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability
Hyuk Jun Cho1, Dong Won Lee, Nirmal Marasini
1College of Pharmacy, Yeungnam University, Gyungbuk, South Korea.
The Journal of Pharmacy and Pharmacology
|September 14, 2013
Summary
This study optimized a novel self-microemulsifying drug delivery system (SMEDDS) for telmisartan (TMS), significantly enhancing its solubility and bioavailability. The developed formulation demonstrated improved drug dissolution and absorption compared to plain TMS powder.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Telmisartan (TMS) exhibits poor water solubility, limiting its oral bioavailability.
- Self-microemulsifying drug delivery systems (SMEDDS) offer a promising strategy to enhance the solubility and absorption of lipophilic drugs.
Purpose of the Study:
- To develop and optimize a novel SMEDDS formulation for telmisartan (TMS).
- To enhance the water solubility and bioavailability of TMS using a Box-Behnken design (BBD) and desirability function.
Main Methods:
- A TMS-SMEDDS formulation was prepared using Peceol (oil), Labrasol (surfactant), and Transcutol (co-surfactant).
- A three-level Box-Behnken design (BBD) was employed to optimize the amounts of Peceol, Labrasol, and Transcutol.
- Response variables included droplet size, polydispersity index, and 15-minute drug dissolution percentage.
Main Results:
- Optimized formulation conditions were determined for Peceol (28.93 mg), Labrasol (80 mg), and Transcutol (28.08 mg).
- Predicted responses for the optimized formulation were droplet size (159.8 nm), polydispersity index (0.241), and dissolution (85.8%).
- The optimized TMS-SMEDDS formulation exhibited faster drug dissolution and higher bioavailability compared to TMS powder.
Conclusions:
- Response surface methodology utilizing BBD and desirability function is effective for optimizing SMEDDS formulations.
- The developed TMS-SMEDDS formulation successfully enhances telmisartan's solubility and bioavailability.
- This approach provides a robust method for understanding and optimizing SMEDDS variables for improved drug delivery.
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