Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir
The influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for th...
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| Format: | Article |
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International Pharmaceutical Excipients Council
2017-09-01
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| Series: | Journal of Excipients and Food Chemicals |
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| Online Access: | https://jefc.scholasticahq.com/article/2579-influence-of-carrier-polymer-type-and-drug-carrier-ratio-in-the-development-of-amorphous-dispersions-for-solubility-and-permeability-enhancement-of-ritonavir |
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| author | Vivek S. Dave Nishikant A. Raut Deepak Gupta Suprit D. Saoji Pradip W. Dhore |
| author_facet | Vivek S. Dave Nishikant A. Raut Deepak Gupta Suprit D. Saoji Pradip W. Dhore |
| author_sort | Vivek S. Dave |
| collection | DOAJ |
| description | The influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for their physical-chemical properties. The dissolution and permeability assessments of the functionality of the SDs were carried out. The preliminary functional stability of these formulations was assessed at accelerated storage conditions for a period of six months. Ritonavir: Eudragit® L100-55 (RE, 1:3) SD showed a 36-fold higher ritonavir solubility compared to pure ritonavir. Similarly, ritonavir: Kolliphor® P188 (RP, 1:2) SD exhibited a 49-fold higher ritonavir solubility compared to pure ritonavir. Ritonavir dissolution from RE formulations increased with increasing ratios of Eudragit® L100-55, up to a ritonavir: carrier ratio of 1:3. The ritonavir dissolution from RP formulations was highest at ritonavir: Kolliphor® P188 ratio of 1:2. Dissolution efficiencies of these formulations were found to be in line with, and supported the dissolution results. The permeability of ritonavir across the biological membrane from the optimized formulations RE (1:3) and RP (1:2) were ~76 % and ~97 %, respectively; and were significantly higher compared to that of pure ritonavir (~20 %). A preliminary (six-month) stability study demonstrated the functional stability of prepared solid dispersions. The present study demonstrates that ritonavir solubility, dissolution, and permeability improvement can be achieved with a careful choice of the carrier polymer, and optimizing the amount of polymer in a SD formulation. |
| first_indexed | 2024-12-13T16:47:15Z |
| format | Article |
| id | doaj.art-2c72f1cab7ec47929250fce5d7ae851a |
| institution | Directory Open Access Journal |
| issn | 2150-2668 |
| language | English |
| last_indexed | 2024-12-13T16:47:15Z |
| publishDate | 2017-09-01 |
| publisher | International Pharmaceutical Excipients Council |
| record_format | Article |
| series | Journal of Excipients and Food Chemicals |
| spelling | doaj.art-2c72f1cab7ec47929250fce5d7ae851a2022-12-21T23:38:07ZengInternational Pharmaceutical Excipients CouncilJournal of Excipients and Food Chemicals2150-26682017-09-01837592Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of RitonavirVivek S. Dave0Nishikant A. Raut1Deepak Gupta2Suprit D. Saoji3Pradip W. Dhore4St. John Fisher College, Wegmans School of Pharmacy, Rochester, NY, USADepartment of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, IndiaLake Erie College of Osteopathic Medicine, School of Pharmacy, Bradenton, FL, USADepartment of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, IndiaDepartment of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, IndiaThe influence of the ratio of Eudragit® L100-55 or Kolliphor® P188 on the solubility, dissolution, and permeability of ritonavir was studied with a goal of preparing solid dispersions (SDs) of ritonavir. SDs were formulated using solvent evaporation or lyophilization techniques, and evaluated for their physical-chemical properties. The dissolution and permeability assessments of the functionality of the SDs were carried out. The preliminary functional stability of these formulations was assessed at accelerated storage conditions for a period of six months. Ritonavir: Eudragit® L100-55 (RE, 1:3) SD showed a 36-fold higher ritonavir solubility compared to pure ritonavir. Similarly, ritonavir: Kolliphor® P188 (RP, 1:2) SD exhibited a 49-fold higher ritonavir solubility compared to pure ritonavir. Ritonavir dissolution from RE formulations increased with increasing ratios of Eudragit® L100-55, up to a ritonavir: carrier ratio of 1:3. The ritonavir dissolution from RP formulations was highest at ritonavir: Kolliphor® P188 ratio of 1:2. Dissolution efficiencies of these formulations were found to be in line with, and supported the dissolution results. The permeability of ritonavir across the biological membrane from the optimized formulations RE (1:3) and RP (1:2) were ~76 % and ~97 %, respectively; and were significantly higher compared to that of pure ritonavir (~20 %). A preliminary (six-month) stability study demonstrated the functional stability of prepared solid dispersions. The present study demonstrates that ritonavir solubility, dissolution, and permeability improvement can be achieved with a careful choice of the carrier polymer, and optimizing the amount of polymer in a SD formulation.https://jefc.scholasticahq.com/article/2579-influence-of-carrier-polymer-type-and-drug-carrier-ratio-in-the-development-of-amorphous-dispersions-for-solubility-and-permeability-enhancement-of-ritonavirRitonavirsolid-dispersionsolubilitydissolutionpermeability |
| spellingShingle | Vivek S. Dave Nishikant A. Raut Deepak Gupta Suprit D. Saoji Pradip W. Dhore Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir Journal of Excipients and Food Chemicals Ritonavir solid-dispersion solubility dissolution permeability |
| title | Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir |
| title_full | Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir |
| title_fullStr | Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir |
| title_full_unstemmed | Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir |
| title_short | Influence of Carrier (Polymer) Type and Drug-Carrier Ratio in the Development of Amorphous Dispersions for Solubility and Permeability Enhancement of Ritonavir |
| title_sort | influence of carrier polymer type and drug carrier ratio in the development of amorphous dispersions for solubility and permeability enhancement of ritonavir |
| topic | Ritonavir solid-dispersion solubility dissolution permeability |
| url | https://jefc.scholasticahq.com/article/2579-influence-of-carrier-polymer-type-and-drug-carrier-ratio-in-the-development-of-amorphous-dispersions-for-solubility-and-permeability-enhancement-of-ritonavir |
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