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Didanosine-loaded chitosan microspheres optimized by surface-response methodology: a modified "Maximum Likelihood
Classius Ferreira da Silva1, Patrícia Severino2, Fernanda Martins3
1Departamento de Ciências Exatas e da Terra, Universidade Federal de São Paulo, Rua Arthur Riedel, 275, Diadema 09972-270, Brazil.
Summary
Chitosan microspheres successfully encapsulated didanosine (ddI), preserving its active form. Optimized conditions yielded a mucoadhesive formulation with high drug loading and sustained release in simulated enteric fluid.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Didanosine (ddI) is an antiviral drug susceptible to degradation in acidic environments.
- Developing stable and effective drug delivery systems for ddI is crucial for its therapeutic application.
- Chitosan offers mucoadhesive properties and biocompatibility, making it a suitable material for drug encapsulation.
Purpose of the Study:
- To develop and optimize didanosine-loaded chitosan microspheres.
- To ensure the stability of didanosine within the microspheres under physiological conditions.
- To create a mucoadhesive formulation for enhanced drug delivery.
Main Methods:
- Chitosan microspheres were prepared using ionotropic gelation with sodium tripolyphosphate (TPP) as a cross-linker.
- Magnesium hydroxide was incorporated to stabilize didanosine (ddI).
- Surface-response methodology and Maximum Likelihood Classification were employed for optimization of operational conditions.
Main Results:
- Optimized conditions (2% chitosan, 10% TPP) resulted in maximum ddI loading (1433 mg ddI/g chitosan).
- The developed microspheres exhibited an average diameter of 11.42 μm.
- A gradual release of ddI was observed over 2 hours in simulated enteric fluid.
Conclusions:
- The study successfully developed optimized didanosine-loaded chitosan microspheres.
- The formulation demonstrated high drug loading, mucoadhesion, and stability of ddI.
- The microspheres show potential for improved oral delivery of didanosine.
