2017, Number 1
Design of a parenteral formulation for prolonged risperidone release based on an in situ gelification system
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ABSTRACTIntroduction: Parenteral administration systems based on in situ gelifying liquid formulations forming semi-solid implants for sustained drug release after injection, are very attractive for a number of reasons. Their application is less invasive and painful in comparison with solid implants, for the latter require local anesthesia and a minor surgical procedure. On the other hand, sustained systemic release of the drug may be achieved for prolonged periods.
Objective: Prepare a formulation for prolonged release of risperidone based on polymeric microparticles formed in situ. The system consists in an emulsion composed of a solution of a biodegradable polymer containing the drug (phase A) and an external oily stage (phase B). Microglobules in phase A solidify at the injection site, and the drug is released by the polymeric microparticles in a controlled manner.
Methods: The system used consisted in two syringes coupled by a connector to prepare the phase A emulsion in phase B. The phase B components evaluated were peanut, sesame and cottonseed oils. The polymer solvent used was N-Methyl-2- pyrrolidone. Two biodegradable polymers were tested as components of phase A: poly(D, L-lactide and poly(D, L-lactide-co-glycolide, to compare their influence on the release profile of risperidone.
Results: No important differences were found in the release profiles of risperidone when different oils were used in the oily phase. In the system prepared with poly(D, L-lactide), risperidone release is smaller after the first ten days of the assay, due to its greater hydrophobic nature and slower degradation rate in comparison with the poly(D, L-lactide-co-glycolide) system. With poly(D, L-lactide-co-glycolide) and peanut oil, a system was achieved which provided controlled release for 60 days.
Conclusions: Results show that this is a promising system for the development of a formulation for prolonged controlled release of risperidone.
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An T, Choi J, Kim A, Lee J, Ho N, Yoonjin P, et al. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process. International Journal of Pharmaceutics. 2016 [citado 3 de junio de 2016]. Disponible en: http://dx.doi.org/10.1016/j.ijpharm.2016.02.023