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Solid Lipid Nanoparticles (SLNs) for Intracellular Targeting Applications
Published on: November 17, 2015
Lopinavir loaded solid lipid nanoparticles (SLN) for intestinal lymphatic targeting.
M R Aji Alex1, A J Chacko, S Jose
1Department of Pharmaceutical Sciences, Mahatma Gandhi University, Cheruvandoor Campus, Ettumanoor, Kerala, India.
Summary
Solid lipid nanoparticles (SLN) successfully encapsulated lopinavir, enhancing oral bioavailability and lymphatic targeting for Highly Active Anti-Retroviral Therapy (HAART). This formulation shows promising stability and extended shelf life.
Area of Science:
- Pharmaceutical Nanotechnology
- Drug Delivery Systems
- Pharmacokinetics
Background:
- Lopinavir exhibits poor oral bioavailability, limiting its efficacy in Highly Active Anti-Retroviral Therapy (HAART).
- Targeting intestinal lymphatic vessels is a strategy to improve the delivery of lipophilic drugs like lopinavir.
Purpose of the Study:
- To develop and characterize glyceryl behenate-based solid lipid nanoparticles (Lo-SLN) for enhanced oral delivery of lopinavir.
- To evaluate the lymphatic transport and bioavailability of lopinavir delivered via SLN.
Main Methods:
- Solid lipid nanoparticles (SLN) were prepared using hot homogenization and ultrasonication.
- Particle characterization involved DSC, WAXS, AFM, and particle size/PDI analysis.
- In vitro release studies, intestinal lymphatic transport assays, and pharmacokinetic evaluations were performed.
Main Results:
- Lo-SLN exhibited optimal particle size (230 nm) and surface charge (-27mV).
- Lymphatic secretion of lopinavir from SLN was 4.91-fold higher than conventional solution.
- AUC increased 2.13-fold, indicating significantly enhanced bioavailability.
Conclusions:
- Glyceryl behenate-based SLN effectively encapsulate lopinavir, improving lymphatic delivery and oral bioavailability.
- The developed Lo-SLN formulation demonstrates good stability with a shelf life of over 21 months.
- This nanocarrier system holds potential for improving HAART efficacy through enhanced drug delivery.
