Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers: Data analysis and modelling

被引:43
作者
Siafaka, Panoraia I. [1 ]
Barmpalexis, Panagiotis [1 ]
Lazaridou, Maria [1 ]
Papageorgiou, George Z. [2 ]
Koutris, Efthimios [3 ]
Karavas, Evangelos [3 ]
Kostoglou, Margaritis [4 ]
Bikiaris, Dimitrios N. [1 ]
机构
[1] Aristotle Univ Thessaloniki, Dept Chem, Lab Polymer Chem & Technol, Thessaloniki 54124, Macedonia, Greece
[2] Univ Ioannina, Dept Chem, GR-45110 Ioannina, Greece
[3] Pharmathen SA, Pharmaceut Ind, Athens 15351, Attiki, Greece
[4] Aristotle Univ Thessaloniki, Dept Chem, Lab Inorgan Chem Technol, Thessaloniki 54124, Macedonia, Greece
关键词
Poly(epsilon-caprolactone); Poly(propylene glutarate); Blends; Risperidone drug; Controlled release; Modelling; BIOPHARMACEUTICS CLASSIFICATION-SYSTEM; TRANSDERMAL PATCHES; SUCCINATE) BLENDS; SOLID DISPERSION; DESIGN; BEHAVIOR; SCHIZOPHRENIA; NANOPARTICLES; MISCIBILITY; MECHANISMS;
D O I
10.1016/j.ejpb.2015.06.027
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In the present study a series of biodegradable and biocompatible poly(epsilon-caprolactone)/poly(propylene glutarate) (PCL/PPGlu) polymer blends were investigated as controlled release carriers of Rispericlone drug (RISP), appropriate for transdermal drug delivery. The PCL/PPGlu carriers were prepared in different weight ratios. Miscibility studies of blends were evaluated through differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Hydrolysis studies were performed at 37 degrees C using a phosphate buffered saline solution. The prepared blends have been used for the preparation of RISP patches via solvent evaporation method, containing 5, 10 and 15 wt% RISP. These formulations were characterized using FT-IR spectroscopy, DSC and WAXD in order to evaluate interactions taking place between polymer matrix and drug, as well as the dispersion and the physical state of the drug inside the polymer matrix. In vitro drug release studies were performed using as dissolution medium phosphate buffered saline simulating body fluids. It was found that in all cases controlled release formulations were obtained, while the RISP release varies due to the properties of the used polymer blend and the different levels of drug loading. Artificial Neural Networks (ANNs) were used for dissolution behaviour modelling showing increased correlation efficacy compared to Multi-Linear-Regression (MLR). (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:473 / 484
页数:12
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