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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Locally Acting Budesonide-Loaded Solid Self-Microemulsifying Drug Delivery Systems (SMEDDS) for Distal Ulcerative
Hany S M Ali1,2, Ahmed F Hanafy3, Rawan Bafail1
1Department of Pharmaceutics and Pharmaceutical Industries, College of Pharmacy, Taibah University, Madinah, Al-Madinah Al-Munawwarah, Saudi Arabia.
Solid self-microemulsifying drug delivery systems (SMEDDS) effectively delivered budesonide (BUD) for ulcerative colitis. These novel BUD-SMEDDS formulations showed superior efficacy in managing colitis in animal models.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Gastroenterology
Background:
- Budesonide (BUD) exhibits poor water solubility and low oral bioavailability, classifying it as a BCS class II medication.
- Ulcerative colitis (UC) requires effective local drug delivery for distal colon management.
Purpose of the Study:
- To develop innovative solid self-microemulsifying drug delivery systems (BUD-SMEDDS) for enhanced local delivery of budesonide.
- To evaluate the in vitro characteristics and in vivo efficacy of BUD-SMEDDS for treating ulcerative colitis.
Main Methods:
- Self-microemulsifying drug delivery system (SMEDDS) components (Capryol™ 90, Tween 80, Transcutol HP) were optimized using Box-Behnken design.
- Solid rectal formulations were prepared using optimized SMEDDS in Lutrol® bases.
- In vitro characterization and in vivo efficacy in a rat colitis model were assessed.
Main Results:
- Optimized BUD-SMEDDS achieved small globule size (33 ± 2.9 nm), low PDI (0.29 ± 0.03), and rapid self-emulsification time (25 ± 2.5 s).
- Formulations exhibited good physical properties, mucoadhesion, and controlled drug release.
- Significant clinical and histopathological improvements were observed in treated animals.
Conclusions:
- Solid SMEDDS demonstrated superior capability as budesonide carriers for managing distal colitis.
- The developed BUD-SMEDDS offer a promising approach for localized ulcerative colitis treatment.
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