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Freeze-drying polymeric colloidal suspensions: nanocapsules, nanospheres and nanodispersion. A comparative study
Scheila R Schaffazick1, Adriana R Pohlmann, Teresa Dalla-Costa
1Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Summary
Freeze-drying polymeric nanoparticles loaded with diclofenac (a non-steroidal anti-inflammatory drug) preserved their integrity and drug content. These formulations demonstrated improved gastrointestinal tolerance compared to diclofenac salt solutions.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery Systems
Background:
- Polymeric nanoparticles offer potential for improved drug delivery.
- Freeze-drying is a common method for preserving nanoparticles but can cause structural damage.
- Understanding the impact of formulation components on nanoparticle stability during drying is crucial.
Purpose of the Study:
- To investigate the influence of lipophilic core and polymeric material on freeze-dried polymeric nanoparticles.
- To evaluate the drug content, morphology, and gastrointestinal tolerance of these nanoparticles.
- To assess the feasibility of freeze-drying nanocapsules without compromising integrity.
Main Methods:
- Nanoparticle preparation via nanoprecipitation using poly(epsilon-caprolactone) or Eudragit S90 with Miglyol 810 or benzyl benzoate.
- Freeze-drying of nanoparticle suspensions with colloidal silicon dioxide.
- Characterization using High-Performance Liquid Chromatography (HPLC) for drug content and Scanning Electron Microscopy (SEM) for morphology.
- In vivo evaluation of gastrointestinal mucosal toxicity in rats.
Main Results:
- Drug content ranged from 90.2% to 101.1% across different formulations.
- SEM revealed non-spherical microparticles with a homogeneous nanocovering.
- Most formulations showed lower gastrointestinal lesional indexes than diclofenac salt solution, except for benzyl benzoate-loaded ones.
- Freeze-drying did not cause drug leakage or structural damage to nanocapsules.
Conclusions:
- Freeze-drying is a viable method for preparing stable polymeric nanoparticle powders.
- Formulation composition significantly impacts nanoparticle characteristics and in vivo performance.
- Polymeric nanoparticles demonstrate potential for safer oral delivery of drugs like diclofenac.