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Updated: Aug 20, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Biocompatible phospholipid-based mixed micelles for posaconazole ocular delivery: Development, characterization, and
Mahraz Osouli1, Erfan Abdollahizad1, Sonia Alavi1
1Department of Pharmaceutics and Nanotechnology, School of Pharmacy, 556492Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Abstract:
Current study intended to prepare and evaluate phospholipid-based, mixed micelles (MMs) to improve the ocular delivery of posaconazole (POS), a broad-spectrum antifungal drug. For this, MMs based on egg phosphatidylcholine (EPC), as the main component, in combination with various bile salts (sodium cholate (NaC), sodium deoxycholate (NaDC), sodium taurocholate (NaTC)) or non-ionic surfactants (Pluronic® F-127, Pluronic® F-68, Tween 80, Labrasol® ALF, and d-a-tocopheryl polyethylene glycol 1000 succinate (TPGS)) were prepared. Particle size, polydispersity index, zeta potential and entrapment efficiency were evaluated to optimize the composition and preparation method of the MMs. Finally, morphology, stability, in vitro release pattern, and in vitro antifungal activity of the optimized formulation were investigated. Among the prepared MMs, vesicles composed of EPC: TPGS with a molar ratio of 70:30, prepared by the thin-film hydration method, showed more appropriate features. Among the prepared MMs, vesicles composed of EPC: TPGS with a molar ratio of 70:30 showed more appropriate features, including an entrapment efficiency (EE) greater than 80%, spherical shape morphology, an average particle size of about 58 nm, desirable stability over a month, slow-release without a noticeable initial burst, and a significantly higher in vitro antifungal activity in comparison with the drug suspension. Therefore, this formulation was selected as the optimal MMs and could be considered as a promising carrier for topical ocular delivery of POS.
Insights
Researchers developed phospholipid-based mixed micelles (MMs) for improved ocular delivery of the antifungal posaconazole (POS). The optimal formulation, egg phosphatidylcholine: d-a-tocopheryl polyethylene glycol 1000 succinate (EPC:TPGS) mixed micelles, demonstrated enhanced antifungal activity and stability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Ophthalmology
Background:
- Posaconazole (POS) is a broad-spectrum antifungal agent with limited ocular bioavailability.
- Developing effective ocular drug delivery systems is crucial for treating fungal eye infections.
Purpose of the Study:
- To prepare and evaluate phospholipid-based mixed micelles (MMs) for enhanced ocular delivery of posaconazole (POS).
- To optimize the composition and preparation method of MMs for improved drug entrapment and stability.
Main Methods:
- Mixed micelles (MMs) were formulated using egg phosphatidylcholine (EPC) with various surfactants (bile salts and non-ionic surfactants).
- Formulations were characterized by particle size, polydispersity index, zeta potential, and entrapment efficiency.
- Optimized MMs were evaluated for morphology, stability, in vitro release, and antifungal activity.
Main Results:
- The optimal formulation consisted of EPC: d-a-tocopheryl polyethylene glycol 1000 succinate (TPGS) at a 70:30 molar ratio, prepared via thin-film hydration.
- This formulation exhibited high entrapment efficiency (>80%), spherical morphology, particle size of ~58 nm, and good stability.
- Optimized MMs showed sustained drug release and significantly enhanced in vitro antifungal activity compared to POS suspension.
Conclusions:
- Phospholipid-based EPC:TPGS mixed micelles are a promising carrier for topical ocular delivery of posaconazole.
- This formulation offers improved bioavailability and efficacy for treating ocular fungal infections.
