Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir
Liquisolid pellets (LPs) prepared by extrusion-spheronization are promising delivery systems to improve the dissolution rate of poorly water-soluble drugs. However, developing LPs for high dose drugs (e.g. antiretroviral ritonavir, RTV) is a major challenge due to technical and quality constraints....
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| Format: | Article |
| Language: | English |
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Elsevier
2019-07-01
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| Series: | Saudi Pharmaceutical Journal |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016419300490 |
| _version_ | 1818424810040983552 |
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| author | Brenda De Espíndola André O'Reilly Beringhs Diva Sonaglio Hellen Karine Stulzer Marcos Antônio Segatto Silva Humberto Gomes Ferraz Bianca Ramos Pezzini |
| author_facet | Brenda De Espíndola André O'Reilly Beringhs Diva Sonaglio Hellen Karine Stulzer Marcos Antônio Segatto Silva Humberto Gomes Ferraz Bianca Ramos Pezzini |
| author_sort | Brenda De Espíndola |
| collection | DOAJ |
| description | Liquisolid pellets (LPs) prepared by extrusion-spheronization are promising delivery systems to improve the dissolution rate of poorly water-soluble drugs. However, developing LPs for high dose drugs (e.g. antiretroviral ritonavir, RTV) is a major challenge due to technical and quality constraints. In this study, formulations LP1 and LP2 were obtained (RTV 100 mg/unit dose) using microcrystalline cellulose (carrier), Kollidon® CL-SF (coating and disintegrating material) and high load (30%, w/w) of Kolliphor® EL or PEG 400 (non-volatile solvent). LP1 and LP2 had narrow size distribution, good morphological properties, and excellent flowability. The partial conversion of RTV polymorph I to the less soluble form II occurred during the preparation of the liquid medications. LP1 (containing Kolliphor® EL) achieved 82.64 ± 2.17% of drug dissolved in 30 min (Q30min), compared with 53.14 ± 0.6% and 42.42 ± 2.09% for LP2 (containing PEG 400) and Norvir® tablets, respectively. Also, LP1 promoted 1.9-fold/1.7-fold and 8.19-fold/8.29-fold increases in Q30min/DE60min (dissolution efficiency) as compared to neat RTV polymorphs I and II, respectively. Keywords: Liquisolid pellets, Kolliphor® EL, Kollidon® CL-SF, Dissolution rate, Ritonavir |
| first_indexed | 2024-12-14T14:03:57Z |
| format | Article |
| id | doaj.art-4601f6c2c6724093874551e22cd89e9d |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-12-14T14:03:57Z |
| publishDate | 2019-07-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-4601f6c2c6724093874551e22cd89e9d2022-12-21T22:58:38ZengElsevierSaudi Pharmaceutical Journal1319-01642019-07-01275702712Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavirBrenda De Espíndola0André O'Reilly Beringhs1Diva Sonaglio2Hellen Karine Stulzer3Marcos Antônio Segatto Silva4Humberto Gomes Ferraz5Bianca Ramos Pezzini6Department of Pharmaceutical Sciences, Federal University of Santa Catarina (UFSC), Florianópolis, BrazilDepartment of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut (UConn), Storrs, United StatesDepartment of Pharmaceutical Sciences, Federal University of Santa Catarina (UFSC), Florianópolis, BrazilDepartment of Pharmaceutical Sciences, Federal University of Santa Catarina (UFSC), Florianópolis, BrazilDepartment of Pharmaceutical Sciences, Federal University of Santa Catarina (UFSC), Florianópolis, BrazilFaculty of Pharmaceutical Sciences, University of São Paulo (USP), São Paulo, BrazilDepartment of Pharmaceutical Sciences, Federal University of Santa Catarina (UFSC), Florianópolis, Brazil; Corresponding author.Liquisolid pellets (LPs) prepared by extrusion-spheronization are promising delivery systems to improve the dissolution rate of poorly water-soluble drugs. However, developing LPs for high dose drugs (e.g. antiretroviral ritonavir, RTV) is a major challenge due to technical and quality constraints. In this study, formulations LP1 and LP2 were obtained (RTV 100 mg/unit dose) using microcrystalline cellulose (carrier), Kollidon® CL-SF (coating and disintegrating material) and high load (30%, w/w) of Kolliphor® EL or PEG 400 (non-volatile solvent). LP1 and LP2 had narrow size distribution, good morphological properties, and excellent flowability. The partial conversion of RTV polymorph I to the less soluble form II occurred during the preparation of the liquid medications. LP1 (containing Kolliphor® EL) achieved 82.64 ± 2.17% of drug dissolved in 30 min (Q30min), compared with 53.14 ± 0.6% and 42.42 ± 2.09% for LP2 (containing PEG 400) and Norvir® tablets, respectively. Also, LP1 promoted 1.9-fold/1.7-fold and 8.19-fold/8.29-fold increases in Q30min/DE60min (dissolution efficiency) as compared to neat RTV polymorphs I and II, respectively. Keywords: Liquisolid pellets, Kolliphor® EL, Kollidon® CL-SF, Dissolution rate, Ritonavirhttp://www.sciencedirect.com/science/article/pii/S1319016419300490 |
| spellingShingle | Brenda De Espíndola André O'Reilly Beringhs Diva Sonaglio Hellen Karine Stulzer Marcos Antônio Segatto Silva Humberto Gomes Ferraz Bianca Ramos Pezzini Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir Saudi Pharmaceutical Journal |
| title | Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| title_full | Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| title_fullStr | Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| title_full_unstemmed | Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| title_short | Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| title_sort | liquisolid pellets a pharmaceutical technology strategy to improve the dissolution rate of ritonavir |
| url | http://www.sciencedirect.com/science/article/pii/S1319016419300490 |
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