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Published on: January 22, 2015
Surfactant-Free Chitosan/Cellulose Acetate Phthalate Nanoparticles: An Attempt to Solve the Needs of Captopril
Noelia Nieto González1, Guido Cerri2, Jesús Molpeceres3
1PhD Program in Chemical Science and Technology, Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
Insights
Researchers developed novel chitosan/cellulose nanoparticles for pediatric captopril delivery. These nanoparticles offer a stable, non-toxic liquid formulation for treating pediatric hypertension, heart failure, and diabetic nephropathy.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Pediatric Medicine
Background:
- The European Medicines Agency highlights the need for pediatric-specific medicinal products.
- Captopril formulations suitable for children are required for cardiovascular conditions.
Purpose of the Study:
- To develop a novel liquid nanoparticle formulation of captopril using chitosan and cellulose acetate phthalate.
- To create an age-appropriate drug delivery system for pediatric hypertension, heart failure, and diabetic nephropathy.
Main Methods:
- Nanoparticles (NP-C) were prepared via nanoprecipitation without surfactants.
- Various cellulose to chitosan ratios were evaluated for encapsulation efficiency.
- Physicochemical properties, stability, drug release, and cytotoxicity were assessed.
Main Results:
- A 1:3 chitosan concentration yielded high encapsulation efficiency (61.0 ± 6.5%).
- NP-C nanoparticles were spherical (427.1 ± 32.7 nm) with good stability for 28 days.
- Significant captopril release (70% in 2h) was observed, with no cytotoxicity on fibroblasts at relevant doses.
Conclusions:
- Chitosan/cellulose nanoparticles present a promising platform for pediatric captopril delivery.
- This formulation could be adapted for both solid and liquid dosage forms for pediatric use.
Abstract:
The Paediatric Committee of the European Medicines Agency encourages research into medicinal products for children, in particular, the development of an age-appropriate formulation of captopril is required in the cardiovascular therapeutic area. The aim of this study was the development of a liquid formulation using nanoparticles based only on chitosan and cellulose acetate phthalate containing captopril for the treatment of hypertension, heart failure and diabetic nephropathy in paediatric patients. Nanoparticles were prepared by a nanoprecipitation method/dropping technique without using surfactants, whose use can be associated with toxicity. A range of different cellulose to chitosan weight ratios were tested. A good encapsulation efficiency (61.0 ± 6.5%) was obtained when a high chitosan concentration was used (1:3 ratio); these nanoparticles (named NP-C) were spherical with a mean diameter of 427.1 ± 32.7 nm, 0.17 ± 0.09 PDI and +53.30 ± 0.95 mV zeta potential. NP-C dispersion remained stable for 28 days in terms of size and drug content and no captopril degradation was observed. NP-C dispersion released 70% of captopril after 2 h in pH 7.4 phosphate buffer and NP-C dispersion did not have a cytotoxicity effect on neonatal human fibroblasts except at the highest dose tested after 48 h. As a result, chitosan/cellulose nanoparticles could be considered a suitable platform for captopril delivery in paediatrics for preparing solid/liquid dosage forms.
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