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Preparation of New Risperidone Depot Microspheres Based on Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations.
J Pharm Sci 2018; 107(11):2891-2901JP

Abstract

Risperidone (RIS)-loaded microspheres based on poly(alkylene adipate)s derived from dicarboxylic acids and different aliphatic diols were prepared by the oil in water emulsion and solvent evaporation method. Specifically, 3 polyesters, namely poly(ethylene adipate), poly(propylene adipate), and poly(butylene adipate), were prepared with the aid of a 2-stage melt-polycondensation method and characterized by gel permeation chromatography, proton nuclear magnetic resonance (1H NMR), differential scanning calorimetry, and X-ray diffraction analysis. Results showed that the molecular weight of the polyesters increased as the diol molecular weight increased, while all polymers were of semi-crystalline nature and the melting temperature was varying from 49.1°C to 51.8°C and 65.9°C for poly(propylene adipate), poly(ethylene adipate), and poly(butylene adipate), respectively. The particle size of the RIS-loaded microspheres varied from 10 to 100 μm depending on the polyester type and the drug loading, while X-ray diffraction analysis revealed amorphous active pharmaceutical ingredient in the cases of high drug-loaded microspheres. In vitro drug release studies along with scanning electron microscopy images of microspheres after the completion of dissolution process showed that in all cases RIS release was controlled by the glass transition temperature of polyesters and physical state of active pharmaceutical ingredients via diffusion.

Authors+Show Affiliations

Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece.Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece.Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece.Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece. Electronic address: dbic@chem.auth.gr.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30096352

Citation

Nanaki, Stavroula, et al. "Preparation of New Risperidone Depot Microspheres Based On Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations." Journal of Pharmaceutical Sciences, vol. 107, no. 11, 2018, pp. 2891-2901.
Nanaki S, Barmpalexis P, Papakonstantinou Z, et al. Preparation of New Risperidone Depot Microspheres Based on Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations. J Pharm Sci. 2018;107(11):2891-2901.
Nanaki, S., Barmpalexis, P., Papakonstantinou, Z., Christodoulou, E., Kostoglou, M., & Bikiaris, D. N. (2018). Preparation of New Risperidone Depot Microspheres Based on Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations. Journal of Pharmaceutical Sciences, 107(11), pp. 2891-2901. doi:10.1016/j.xphs.2018.07.029.
Nanaki S, et al. Preparation of New Risperidone Depot Microspheres Based On Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations. J Pharm Sci. 2018;107(11):2891-2901. PubMed PMID: 30096352.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation of New Risperidone Depot Microspheres Based on Novel Biocompatible Poly(Alkylene Adipate) Polyesters as Long-Acting Injectable Formulations. AU - Nanaki,Stavroula, AU - Barmpalexis,Panagiotis, AU - Papakonstantinou,Zoi, AU - Christodoulou,Evi, AU - Kostoglou,Margaritis, AU - Bikiaris,Dimitrios N, Y1 - 2018/08/07/ PY - 2018/06/06/received PY - 2018/06/29/revised PY - 2018/07/31/accepted PY - 2018/8/11/pubmed PY - 2019/8/6/medline PY - 2018/8/11/entrez KW - controlled release KW - long-acting injectables KW - poly(butylene adipate) KW - poly(ethylene adipate) KW - poly(propylene adipate) KW - risperidone SP - 2891 EP - 2901 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 107 IS - 11 N2 - Risperidone (RIS)-loaded microspheres based on poly(alkylene adipate)s derived from dicarboxylic acids and different aliphatic diols were prepared by the oil in water emulsion and solvent evaporation method. Specifically, 3 polyesters, namely poly(ethylene adipate), poly(propylene adipate), and poly(butylene adipate), were prepared with the aid of a 2-stage melt-polycondensation method and characterized by gel permeation chromatography, proton nuclear magnetic resonance (1H NMR), differential scanning calorimetry, and X-ray diffraction analysis. Results showed that the molecular weight of the polyesters increased as the diol molecular weight increased, while all polymers were of semi-crystalline nature and the melting temperature was varying from 49.1°C to 51.8°C and 65.9°C for poly(propylene adipate), poly(ethylene adipate), and poly(butylene adipate), respectively. The particle size of the RIS-loaded microspheres varied from 10 to 100 μm depending on the polyester type and the drug loading, while X-ray diffraction analysis revealed amorphous active pharmaceutical ingredient in the cases of high drug-loaded microspheres. In vitro drug release studies along with scanning electron microscopy images of microspheres after the completion of dissolution process showed that in all cases RIS release was controlled by the glass transition temperature of polyesters and physical state of active pharmaceutical ingredients via diffusion. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/30096352/Preparation_of_New_Risperidone_Depot_Microspheres_Based_on_Novel_Biocompatible_Poly_Alkylene_Adipate__Polyesters_as_Long_Acting_Injectable_Formulations_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(18)30496-9 DB - PRIME DP - Unbound Medicine ER -