Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability
Joint Authors
Omri, Abdelwahab
Misra, Ambikanandan
Gupta, Shweta
Kesarla, Rajesh
Chotai, Narendra
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-18, 18 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-01-23
Country of Publication
Egypt
No. of Pages
18
Main Subjects
Abstract EN
The nonnucleoside reverse transcriptase inhibitors, used for the treatment of HIV infections, are reported to have low bioavailability pertaining to high first-pass metabolism, high protein binding, and enzymatic metabolism.
They also show low permeability across blood brain barrier.
The CNS is reported to be the most important HIV reservoir site.
In the present study, solid lipid nanoparticles of efavirenz were prepared with the objective of providing increased permeability and protection of drug due to biocompatible lipidic content and nanoscale size and thus developing formulation having potential for enhanced bioavailability and brain targeting.
Solid lipid nanoparticles were prepared by high pressure homogenization technique using a systematic approach of design of experiments (DoE) and evaluated for particle size, polydispersity index, zeta potential, and entrapment efficiency.
Particles of average size 108.5 nm having PDI of 0.172 with 64.9% entrapment efficiency were produced.
Zeta potential was found to be −21.2 mV and the formulation was found stable.
The in-vivo pharmacokinetic studies revealed increased concentration of the drug in brain, as desired, when administered through intranasal route indicating its potential for an attempt towards complete eradication of HIV and cure of HIV-infected patients.
American Psychological Association (APA)
Gupta, Shweta& Kesarla, Rajesh& Chotai, Narendra& Misra, Ambikanandan& Omri, Abdelwahab. 2017. Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability. BioMed Research International،Vol. 2017, no. 2017, pp.1-18.
https://search.emarefa.net/detail/BIM-1137883
Modern Language Association (MLA)
Gupta, Shweta…[et al.]. Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability. BioMed Research International No. 2017 (2017), pp.1-18.
https://search.emarefa.net/detail/BIM-1137883
American Medical Association (AMA)
Gupta, Shweta& Kesarla, Rajesh& Chotai, Narendra& Misra, Ambikanandan& Omri, Abdelwahab. Systematic Approach for the Formulation and Optimization of Solid Lipid Nanoparticles of Efavirenz by High Pressure Homogenization Using Design of Experiments for Brain Targeting and Enhanced Bioavailability. BioMed Research International. 2017. Vol. 2017, no. 2017, pp.1-18.
https://search.emarefa.net/detail/BIM-1137883
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1137883