Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies
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...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
Hindawi Limited
2014-01-01
|
Series: | BioMed Research International |
Online Access: | http://dx.doi.org/10.1155/2014/363404 |
id |
doaj-3bba3c2232104bd7b3f42bfcc01083bd |
---|---|
record_format |
Article |
spelling |
doaj-3bba3c2232104bd7b3f42bfcc01083bd2020-11-24T23:19:48ZengHindawi LimitedBioMed Research International2314-61332314-61412014-01-01201410.1155/2014/363404363404Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics StudiesPraveen Kumar Gaur0Shikha Mishra1Meenakshi Bajpai2Anushika Mishra3Department of Pharmaceutics, I.T.S. Paramedical College (Pharmacy), Muradnagar, Ghaziabad 201206, IndiaDepartment of Pharmacognosy & Phytochemistry, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmaceutics, I.T.S. Paramedical College (Pharmacy), Muradnagar, Ghaziabad 201206, IndiaDepartment of Pharmaceutics, I.T.S. Paramedical College (Pharmacy), Muradnagar, Ghaziabad 201206, IndiaSolid 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 (Cmax) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).http://dx.doi.org/10.1155/2014/363404 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Praveen Kumar Gaur Shikha Mishra Meenakshi Bajpai Anushika Mishra |
spellingShingle |
Praveen Kumar Gaur Shikha Mishra Meenakshi Bajpai Anushika Mishra Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies BioMed Research International |
author_facet |
Praveen Kumar Gaur Shikha Mishra Meenakshi Bajpai Anushika Mishra |
author_sort |
Praveen Kumar Gaur |
title |
Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies |
title_short |
Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies |
title_full |
Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies |
title_fullStr |
Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies |
title_full_unstemmed |
Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies |
title_sort |
enhanced oral bioavailability of efavirenz by solid lipid nanoparticles: in vitro drug release and pharmacokinetics studies |
publisher |
Hindawi Limited |
series |
BioMed Research International |
issn |
2314-6133 2314-6141 |
publishDate |
2014-01-01 |
description |
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 (Cmax) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES). |
url |
http://dx.doi.org/10.1155/2014/363404 |
work_keys_str_mv |
AT praveenkumargaur enhancedoralbioavailabilityofefavirenzbysolidlipidnanoparticlesinvitrodrugreleaseandpharmacokineticsstudies AT shikhamishra enhancedoralbioavailabilityofefavirenzbysolidlipidnanoparticlesinvitrodrugreleaseandpharmacokineticsstudies AT meenakshibajpai enhancedoralbioavailabilityofefavirenzbysolidlipidnanoparticlesinvitrodrugreleaseandpharmacokineticsstudies AT anushikamishra enhancedoralbioavailabilityofefavirenzbysolidlipidnanoparticlesinvitrodrugreleaseandpharmacokineticsstudies |
_version_ |
1725576804687675392 |