BN Hari

K Dhevendaran

N Narayanan

Springer - Publisher Connector

POSTER PRESENTATION Open Access
Development of Efavirenz nanoparticle for
enhanced efficiency of anti-retroviral therapy
against HIV and AIDS
BN Vedha Hari1*, K Dhevendaran1, N Narayanan2
From First International Science Symposium on HIV and Infectious Diseases (HIV SCIENCE 2012)
Chennai, India. 20-22 January 2012
Background
The FDA approved drug Efavirenz is a Non-Nucleoside
Reverse Transcriptase Inhibitor (NNRTI) successful first
line drug of choice in Highly Active Anti-Retroviral
Therapy (HAART) for treatment of HIV and AIDS. It is
poorly water soluble drug (10 g/ml) with 40-45% of
bioavailability and administered as high doses 600-800
mg/day. Increase in solubility can enhance bioavailabil-
ity; providing reduction of dose, resistance and harmful
side effects.
Methods
Efavirenz nanoparticles are developed using methacry-
late polymers (Eudragit E100) by emulsion solvent eva-
poration method (1:0.5, 1:1, 1:2 and 2:1 ratios) and the
in-vitro evaluations such as particle size, morphology,
solubility changes, drug release, compatibility and cyto-
toxicity tests are carried out.
Results
The particle size of 99-200 nm with narrow size distri-
bution and surface charge (-52 V) shows high stability.
The formulation with entrapment efficiency (75-90%)
shows higher drug release profile 95-100% within 1 hour
compared to 23%-58% of pure drug in water, 0.1N HCl
and phosphate buffer pH 7.4 media. The DSC, TG-DSC,
powder XRD and SEM morphology results reveal that
there is solid transition from crystalline structure to
amorphous state, which supports the solubility enhance-
ment. The FT-IR gives the compatibility results for drug
with other excipients. The Efavirenz nanoparticles
subjected for in-vitro cytotoxicity and cell uptake studies
using monocytes / macrophages (THP-1) proved better
uptake (Flocytometry and Confocal microscope) of
nanoparticles than free drug.
Conclusion
The solubility enhancement due to nanosizing helps in
hastening the drug release and also increasing cell
uptake, which helps in attaining high bioavailability with
low dose of Efavirenz.
Author details
1Department of Pharmacy, School of Chemical and Bio-Technology, SASTRA
University, Thanjavur-613 401, Tamil Nadu, India. 2Department of
Pharmaceutics, Madras Medical College, Chennai-600001, Tamil Nadu, India.
Published: 4 May 2012
doi:10.1186/1471-2334-12-S1-P7
Cite this article as: Hari et al.: Development of Efavirenz nanoparticle for
enhanced efficiency of anti-retroviral therapy against HIV and AIDS.
BMC Infectious Diseases 2012 12(Suppl 1):P7.
Submit your next manuscript to BioMed Central
and take full advantage of: 
• Convenient online submission
• Thorough peer review
• No space constraints or color figure charges
• Immediate publication on acceptance
• Inclusion in PubMed, CAS, Scopus and Google Scholar
• Research which is freely available for redistribution
Submit your manuscript at 
www.biomedcentral.com/submit
* Correspondence: vedhahari@scbt.sastra.edu
1Department of Pharmacy, School of Chemical and Bio-Technology, SASTRA
University, Thanjavur-613 401, Tamil Nadu, India
Full list of author information is available at the end of the article
Hari et al. BMC Infectious Diseases 2012, 12(Suppl 1):P7
http://www.biomedcentral.com/1471-2334/12/S1/P7
© 2012 Hari et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons
Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in
any medium, provided the original work is properly cited.


Development of Efavirenz nanoparticle for enhanced efficiency of anti-retroviral therapy against HIV and AIDS

file:///data/remote/core/dit/data/Springer-OA/pdf/bea/aHR0cDovL2xpbmsuc3ByaW5nZXIuY29tLzEwLjExODYvMTQ3MS0yMzM0LTEyLVMxLVA3LnBkZg==.pdf

Development of Efavirenz nanoparticle for enhanced efficiency of anti-retroviral therapy against HIV and AIDS

Abstract

Similar works

Full text

Available Versions

Springer - Publisher Connector

Springer - Publisher Connector