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Efavirenz–eudragit E-100 nanoparticle-loaded aerosol foam for sustained release: in-vitro and ex-vivo evaluation

  • B. N. Vedha Hari EMAIL logo , N. Narayanan and K. Dhevedaran
Published/Copyright: December 12, 2014
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Chemical Papers
From the journal Chemical Papers Volume 69 Issue 2

Abstract

The control of HIV infection using antiretroviral agents, especially through targeted delivery, has attracted extensive attention in the last decade. Recently, the vaginal route of administration has become the one most recommended for HIV infections during pregnancy. Efavirenz is a non-nucleoside reverse transcriptase inhibitor anti-HIV drug and its prolonged half-life helps achieve long-term preexposure prophylaxis of HIV-1 infections; it is used as a first-line drug in the treatment using combination therapy. Nanotechnology has received attention as a major area of research into drug delivery in recent years. The aerosol foam formulation is packed under pressure and contains therapeutically active ingredients that are released as foam on the activation of an appropriate valve system. The objective of this study was to develop an aerosol foam formulation of efavirenz nanoparticles for vaginal drug delivery. The nanoparticles were prepared using the emulsion solvent evaporation method and converted into an aerosol foam formulation with the addition of 0.1 mass % of sodium lauryl sulphate as a foaming agent and pressurised with 1,1,1,2-tetrafluroethane. The nanoparticles containing the formulation and aerosol foam formulation were individually characterised by applying various tests such as particle size, zeta potential, pH, viscosity, drug content, entrapment efficiency, drug release studies and release kinetics. The compatibility of the materials was evaluated using FT-IR, polymorphic changes by TGA-DSC and also the morphological properties using SEM study. Foam density, bubble size and collapse time were evaluated in the aerosol-foam formulation; in addition, the drug content and release studies were compared with nanoparticle formulation. The results revealed that the nanoparticle-containing formulation and aerosol formulations were stable and the foam emerged as grade one with fine bubbles and became coarser over time.

Keywords: AIDS; nanotechnology; drug; aerosol; efavirenz; eudragit

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Received: 2014-4-10
Revised: 2014-6-23
Accepted: 2014-6-30
Published Online: 2014-12-12
Published in Print: 2015-2-1

© 2015 Institute of Chemistry, Slovak Academy of Sciences

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https://doi.org/10.1515/chempap-2015-0005
Keywords for this article
AIDS; nanotechnology; drug; aerosol; efavirenz; eudragit

Articles in the same Issue

  1. Selection and design of ionic liquids as solvents in extractive distillation and extraction processes
  2. Analytical procedure for steroid profiling valid for Athlete Biological Passport
  3. Fabrication of paper-based analytical device by silanisation of filter cellulose using alkyltrimethoxysilane coupled with UV radiation
  4. Synthesis, characterisation and photocatalytic activity of Ag+- and Sn2+-substituted KSbTeO6
  5. Dysprosium pertraction through facilitated supported liquid membrane using D2EHPA as carrier
  6. Volatile compounds composition and antioxidant activity of bee pollen collected in Lithuania
  7. Self-penetrating and interpenetrating 3D metal–organic frameworks constructed from 4-(4-carboxyphenoxy)-phthalic acid and N-donor auxiliary ligands
  8. Preparation of ceramic γ-Al2O3–TiO2 nanofiltration membranes for desalination
  9. Promoting effect of group VI metals on Ni/MgO for catalytic growth of carbon nanotubes by ethylene chemical vapour deposition
  10. Microwave-assisted solvent-free synthesis and luminescence properties of 2-substituted-4,5-di(2-furyl)-1H-imidazoles
  11. Synthesis of potential inhibitors of glycosyltransferases representing UDP-GlcNAc
  12. Development of transition state analogue inhibitors for N-acetylglycosyltransferases bearing D-psicoor D-tagatofuranose scaffolds
  13. Efavirenz–eudragit E-100 nanoparticle-loaded aerosol foam for sustained release: in-vitro and ex-vivo evaluation
  14. Photochromic and molecular switching behaviour of Schiff base-containing pyrazolone ring
  15. Improvements to CO2 headspace biodegradability test
  16. Synthesis of corn rootworm pheromones from commercial diols
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