Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug
In the present work, Risperidone microparticles from poly(lactic acid)/poly(hexylene succinate) (PLA-b-PHSu) block copolymers in different ratios, 95/05, 90/10 and 80/20 <i>w</i>/<i>w</i>, were examined as long-acting injectable formulations. Nuclear magnetic resonance (NMR)...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-09-01
|
| Series: | Polymers |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2073-4360/14/19/4111 |
| _version_ | 1797477345018249216 |
|---|---|
| author | Iouliana Chrysafi Stavroula Nanaki Alexandra Zamboulis Margaritis Kostoglou Eleni Pavlidou Dimitrios N. Bikiaris |
| author_facet | Iouliana Chrysafi Stavroula Nanaki Alexandra Zamboulis Margaritis Kostoglou Eleni Pavlidou Dimitrios N. Bikiaris |
| author_sort | Iouliana Chrysafi |
| collection | DOAJ |
| description | In the present work, Risperidone microparticles from poly(lactic acid)/poly(hexylene succinate) (PLA-b-PHSu) block copolymers in different ratios, 95/05, 90/10 and 80/20 <i>w</i>/<i>w</i>, were examined as long-acting injectable formulations. Nuclear magnetic resonance (NMR) was used to verify the successful synthesis of copolymers. Enzymatic hydrolysis showed an increase in weight loss as the content of PHSu increased, while the cytotoxicity studies confirmed the biocompatibility of the copolymers. The polyesters were further used to encapsulate Risperidone by spray drying. The drug-loaded microparticles were studied by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and X-ray diffraction (XRD). SEM microphotographs confirmed that spherically shaped microparticles were prepared with sizes about 5–12 μm, while XRD and differential scanning calorimetry (DSC) studies evidenced that Risperidone was encapsulated in amorphous form. The drug loading and the entrapment efficiency of Risperidone were studied as well as the in vitro release from the prepared microparticles. As the content of PHSu increased, a higher release of Risperidone was observed, with PLA-b-PHSu 80/20 <i>w</i>/<i>w</i> succeeding to release 100% of RIS within 12 days. According to theoretical modeling, the kinetics of RIS release from PLA-b-PHSu microparticles is complex, governed by both diffusion and polymer erosion. |
| first_indexed | 2024-03-09T21:16:16Z |
| format | Article |
| id | doaj.art-c8171d8c93944bd59beb1ea7df4c8007 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T21:16:16Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-c8171d8c93944bd59beb1ea7df4c80072023-11-23T21:34:27ZengMDPI AGPolymers2073-43602022-09-011419411110.3390/polym14194111Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone DrugIouliana Chrysafi0Stavroula Nanaki1Alexandra Zamboulis2Margaritis Kostoglou3Eleni Pavlidou4Dimitrios N. Bikiaris5Laboratory of Advanced Materials and Devices, Department of Physics, Faculty of Sciences, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceLaboratory of Polymers Chemistry and Technology, Department of Chemistry, Faculty of Sciences, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceLaboratory of Polymers Chemistry and Technology, Department of Chemistry, Faculty of Sciences, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceLaboratory of Chemical and Environmental Technology, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceLaboratory of Advanced Materials and Devices, Department of Physics, Faculty of Sciences, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceLaboratory of Polymers Chemistry and Technology, Department of Chemistry, Faculty of Sciences, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, GreeceIn the present work, Risperidone microparticles from poly(lactic acid)/poly(hexylene succinate) (PLA-b-PHSu) block copolymers in different ratios, 95/05, 90/10 and 80/20 <i>w</i>/<i>w</i>, were examined as long-acting injectable formulations. Nuclear magnetic resonance (NMR) was used to verify the successful synthesis of copolymers. Enzymatic hydrolysis showed an increase in weight loss as the content of PHSu increased, while the cytotoxicity studies confirmed the biocompatibility of the copolymers. The polyesters were further used to encapsulate Risperidone by spray drying. The drug-loaded microparticles were studied by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and X-ray diffraction (XRD). SEM microphotographs confirmed that spherically shaped microparticles were prepared with sizes about 5–12 μm, while XRD and differential scanning calorimetry (DSC) studies evidenced that Risperidone was encapsulated in amorphous form. The drug loading and the entrapment efficiency of Risperidone were studied as well as the in vitro release from the prepared microparticles. As the content of PHSu increased, a higher release of Risperidone was observed, with PLA-b-PHSu 80/20 <i>w</i>/<i>w</i> succeeding to release 100% of RIS within 12 days. According to theoretical modeling, the kinetics of RIS release from PLA-b-PHSu microparticles is complex, governed by both diffusion and polymer erosion.https://www.mdpi.com/2073-4360/14/19/4111poly(lactic acid)poly(hexylene succinate)Risperidonelong-acting injectabledrug deliveryenzymatic hydrolysis |
| spellingShingle | Iouliana Chrysafi Stavroula Nanaki Alexandra Zamboulis Margaritis Kostoglou Eleni Pavlidou Dimitrios N. Bikiaris Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug Polymers poly(lactic acid) poly(hexylene succinate) Risperidone long-acting injectable drug delivery enzymatic hydrolysis |
| title | Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug |
| title_full | Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug |
| title_fullStr | Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug |
| title_full_unstemmed | Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug |
| title_short | Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug |
| title_sort | poly lactic acid block copolymers with poly hexylene succinate as microparticles for long acting injectables of risperidone drug |
| topic | poly(lactic acid) poly(hexylene succinate) Risperidone long-acting injectable drug delivery enzymatic hydrolysis |
| url | https://www.mdpi.com/2073-4360/14/19/4111 |
| work_keys_str_mv | AT ioulianachrysafi polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug AT stavroulananaki polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug AT alexandrazamboulis polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug AT margaritiskostoglou polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug AT elenipavlidou polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug AT dimitriosnbikiaris polylacticacidblockcopolymerswithpolyhexylenesuccinateasmicroparticlesforlongactinginjectablesofrisperidonedrug |