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Development and characterization of parenteral nanoemulsions containing thalidomide
F A Araújo1, R G Kelmann, B V Araújo
1Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, CEP 90.610-000, Porto Alegre, RS, Brazil.
Summary
This study developed stable nanoemulsions for intravenous thalidomide (THD) delivery. Optimized formulations showed consistent droplet size, drug content, and zeta potential, enabling potential therapeutic plasma concentrations with low doses.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery
Background:
- Thalidomide (THD) requires effective intravenous delivery systems for therapeutic applications.
- Nanoemulsions offer potential for improved drug solubility and bioavailability.
- Controlling drug crystallization within nanoemulsions is critical for stability.
Purpose of the Study:
- To develop and optimize stable nanoemulsions for intravenous thalidomide administration.
- To evaluate the impact of thalidomide concentration and polymorphic form on nanoemulsion stability.
- To assess the in vitro dissolution and pharmacokinetic potential of the optimized nanoemulsion.
Main Methods:
- Spontaneous emulsification method for nanoemulsion preparation.
- Optimization of thalidomide and polysorbate 80 concentrations.
- Characterization using dynamic light scattering, zeta potential measurements, and electron microscopy.
- Polymorph characterization via FTIR and XRD.
- In vitro dissolution testing using reverse dialysis sac technique.
Main Results:
- A stable nanoemulsion formulation with 0.01% THD and 0.5% polysorbate 80 was identified, maintaining properties over 60 days.
- Droplet size averaged ~200nm, drug content ~95%, and zeta potential ~-30mV.
- Drug crystallization in higher concentration nanoemulsions occurred in the alpha-polymorphic form, irrespective of the initial polymorph.
- In vitro dissolution showed rapid drug release, similar to an acetonitrile solution.
- Pharmacokinetic simulation indicated potential for therapeutic plasma concentrations with a 25mg dose.
Conclusions:
- Stable nanoemulsions for intravenous thalidomide delivery can be successfully developed.
- Formulation optimization is crucial to prevent drug crystallization and ensure long-term stability.
- The developed nanoemulsion demonstrates favorable in vitro release and potential for effective parenteral thalidomide therapy.
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