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. 2014:2014:363404.
doi: 10.1155/2014/363404. Epub 2014 May 21.

Enhanced oral bioavailability of efavirenz by solid lipid nanoparticles: in vitro drug release and pharmacokinetics studies

Praveen Kumar Gaur  1 , Shikha Mishra  2 , Meenakshi Bajpai  1 , Anushika Mishra  1
Affiliations

Enhanced oral bioavailability of efavirenz by solid lipid nanoparticles: in vitro drug release and pharmacokinetics studies

Praveen Kumar Gaur et al. Biomed Res Int. 2014.

Abstract

Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6-98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).

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Figures

Figure 1
Figure 1
Drug excipients interaction studies by infrared spectra.
Figure 2
Figure 2
SEM images for ESLN-3.
Figure 3
Figure 3
Size distribution (ESLN-3).
Figure 4
Figure 4
Zeta potential distribution (ESLN-3).
Figure 5
Figure 5
In vitro drug release from SLN, ES, and EMF.
Figure 6
Figure 6
Plasma drug concentration time profiles.
See this image and copyright information in PMC

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References

    1. Sahoo SK, Labhasetwar V, editors. Nanoparticles Interface: An Important Determinant in nanoparticle-Mediated Drug/Gene Delivery. Nanoparticle Technology for Drug Delivery. New York, NY, USA: Taylor & Francis; 2006.
    1. Falzarano MS, Passarelli C, Bassi E. Biodistribution and molecular studies on orally administered nanoparticle-AON complexes encapsulated with alginate aiming at inducing dystrophin rescue in mdx mice. BioMed Research International. 2013;2013:13 pages.527418 - PMC - PubMed
    1. Gaur P, Purohit S, Mishra S. Solid lipid nanoparticles of guggul lipid as drug carrier for transdermal drug delivery. BioMed Research International. 2013;2013:10 pages.750690 - PMC - PubMed
    1. Gaur PK, Mishra S, Aeri V. Formulation and evaluation of guggul lipid nanovesicles for transdermal delivery of aceclofenac. The Scientific World Journal. 2014;2014:10 pages.534210 - PMC - PubMed
    1. Vyas SP, Khar RK, editors. Nanoparticles. Targeted and Controlled Drug Delivery—Novel Carrier Systems. New Delhi, India: CBS; 2002.

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