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Updated: May 20, 2026
10:33
Delivery of Therapeutic siRNA to the CNS Using Cationic and Anionic Liposomes
Published on: July 23, 2016
Enhanced delivery of lopinavir to the CNS using Compritol-based solid lipid nanoparticles
Aji Alex1, Willi Paul, A J Chacko
1Department of Pharmaceutical Sciences, Cheruvandoor Campus, Mahatma Gandhi University, Kottayam 686631, India.
Therapeutic Delivery
|July 27, 2012
Summary
Solid lipid nanoparticles enhance lopinavir delivery to the central nervous system (CNS). These nanoparticles show increased bioavailability and cerebrospinal fluid concentration in rats, overcoming poor CNS permeability.
Area of Science:
- Nanotechnology
- Pharmacology
- Drug Delivery
Background:
- Lopinavir, a protease inhibitor, has poor central nervous system (CNS) penetration due to biological barriers.
- Developing strategies to enhance CNS drug availability is crucial for treating neurological disorders.
Purpose of the Study:
- To develop and evaluate solid lipid nanoparticles (SLNs) for improved CNS delivery of lopinavir.
- To assess the pharmacokinetic profile and CNS bioavailability of lopinavir-loaded SLNs.
Main Methods:
- Formulation of compritol-based SLNs coated with poloxamer.
- In vivo pharmacokinetic studies in a rat model comparing SLNs with free drug suspension.
- Analysis of drug concentration in blood and cerebrospinal fluid (CSF).
Main Results:
- SLN formulations achieved a Cmax of 632.86 ng/ml and Tmax of 25 min.
- Demonstrated significantly increased bioavailability compared to free lopinavir suspension.
- Observed a notable increase in cerebrospinal fluid drug concentration.
Conclusions:
- Compritol-based SLNs effectively enhance lopinavir's CNS delivery.
- SLNs act as a drug reservoir, prolonging circulation and utilizing lymphatic absorption.
- The biocompatibility and targeting potential of these SLNs make them promising for CNS drug delivery.
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