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Development and Optimization of an Eplerenone-Loaded Liposomal In Situ Gel for Enhanced Intranasal Delivery
Juste Baranauskaite1, Ipek Ceken1, Asta Kubiliene2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Yeditepe University, 34755 Istanbul, Turkey.
This study developed an optimized intranasal Eplerenone (EPL) delivery system using liposomes in situ gel (Elip-GG). This novel formulation enhances sustained drug release in the nasal cavity, offering a promising alternative for hypertension treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Eplerenone (EPL) is a hydrophilic antihypertensive drug.
- Oral and parenteral delivery methods have limitations.
- Intranasal delivery offers potential for enhanced therapeutic outcomes.
Purpose of the Study:
- To develop and optimize an intranasal delivery system for Eplerenone (EPL).
- To incorporate EPL-loaded liposomes (Elip) into an in situ gellan gum gel (Elip-GG).
- To achieve prolonged nasal residence time and sustained drug release.
Main Methods:
- Liposomes (Elip) were prepared via thin-film hydration and optimized for encapsulation efficiency (EE), particle size (MPS), polydispersity index (PDI), and zeta potential (ZP).
- Elip was incorporated into a gellan gum (GG) in situ gel to form Elip-GG.
- Elip-GG was evaluated for pH, viscosity, rheology, mechanical properties, and in vitro release.
Main Results:
- Optimal Elip formulation achieved 86.3% EE, 86.56 nm MPS, 0.29 PDI, and -29.86 mV ZP.
- Elip-GG demonstrated sustained release, with over 93% cumulative drug release within 2.5 hours.
- The Elip-GG formulation significantly enhanced sustained intranasal release of Eplerenone.
Conclusions:
- The developed Elip-GG system is a promising intranasal delivery strategy for Eplerenone.
- This system offers an effective alternative to conventional oral and parenteral routes for hydrophilic antihypertensives.
- Further research may explore its clinical efficacy and safety profile.
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