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Updated: Jun 23, 2026
08:18
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
Extended release felodipine self-nanoemulsifying system
Pradeep R Patil1, Shailesh V Biradar, Anant R Paradkar
1Department of Pharmaceutics, Poona College of Pharmacy, Erandwane, Bharati Vidyapeeth University, Pune, 411 038, Maharashtra State, India.
AAPS Pharmscitech
|May 6, 2009
Summary
This study developed a novel self-nanoemulsifying system (SNES) for felodipine (FLD) to enhance solubility and achieve extended drug release. The optimized formulation demonstrated improved drug delivery for lipophilic compounds.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Lipophilic drugs like felodipine (FLD) often exhibit poor solubility, limiting their therapeutic efficacy.
- Developing advanced drug delivery systems is crucial for improving the bioavailability and pharmacokinetic profiles of poorly soluble compounds.
Purpose of the Study:
- To formulate and characterize a self-nanoemulsifying system (SNES) for the model lipophilic drug, felodipine (FLD).
- To develop an extended-release formulation by incorporating gelling and coating strategies to control FLD release.
Main Methods:
- Formulation of SNES using Miglyol 840, Cremophor EL, and Capmul MCM.
- Characterization of SNES for turbidity, droplet size, and in vitro drug release.
- Induction of gelling with Aerosil 200 (A200) and encapsulation within a Gelucire 43/01 (GEL) coat with Caprol PGE-860 (CAP) as a release enhancer.
- Evaluation of formulation variables using a 3(2) factorial design and rheological studies.
Main Results:
- Optimized SNES (3.5:1.0:1.0 oil:surfactant:co-surfactant) showed good emulsification, a median droplet size of 421 nm, and rapid FLD release (>90% in 15 min).
- Gelling with A200 enhanced microstructure elasticity, while the GEL/CAP coat extended FLD release.
- Factorial analysis revealed CAP promotes release via channel formation, A200 retards release via gelling, and their interaction governs extended release.
Conclusions:
- The developed gelled SNES encased within a hydrophobic coat provides an effective strategy for extended release of lipophilic drugs.
- This formulation holds potential for improving the therapeutic management of conditions requiring sustained drug delivery, such as hypertension.
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