Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement
Abstract Background Ritonavir is an anti-retroviral protease inhibitor to treat HIV, AIDS infections. Methods The RN-SLNs were prepared by using hot homogenization followed ultrasonication method and optimized by using a two-factor, three-level central composte design (CCD). The independent variable...
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| Format: | Article |
| Language: | English |
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Springer
2025-01-01
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| Series: | Discover Applied Sciences |
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| Online Access: | https://doi.org/10.1007/s42452-024-06322-1 |
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| author | Ananda Kumar Chettupalli Sarad Pawar Naik Bukke Shaik Abdul Rahaman Aziz Unnisa Madhumitha Adepu Marati Kavitha Molakpogu Ravindra Babu Bayapa Reddy Narapureddy Hope Onohuean |
| author_facet | Ananda Kumar Chettupalli Sarad Pawar Naik Bukke Shaik Abdul Rahaman Aziz Unnisa Madhumitha Adepu Marati Kavitha Molakpogu Ravindra Babu Bayapa Reddy Narapureddy Hope Onohuean |
| author_sort | Ananda Kumar Chettupalli |
| collection | DOAJ |
| description | Abstract Background Ritonavir is an anti-retroviral protease inhibitor to treat HIV, AIDS infections. Methods The RN-SLNs were prepared by using hot homogenization followed ultrasonication method and optimized by using a two-factor, three-level central composte design (CCD). The independent variables were selected as phospholipids (X1) and type of surfactants (X2), whereas the dependent variables were chosen as percent entrapment efficiency (%EE) (Y1), size of the particle (Y2), and percent cumulative drug release (Y3). Further, the formulated R-SLNs were characterized and in vitro drug release studies were performed. The optimized R-SLNs were subjected to in vivo pharmacokinetic studies. Results The solid lipid soya leccithin showed the maximum solubility of RN (103.34 mg/g) compared to stearic acid (81.44 mg/g), glyceryl monostearate (67.21 mg/g), Gelucire 39/1 (44.22 mg/g), and Compritol 888 ATO (31.23 mg/g). Further, the surfactant blend (Tween 80: Poloxamer 188 (8:2)) showed the maximum entrapment efficiency and was the most suitable surfactant. The optimized RN-SLN formulation showed a particle size of 265.06 ± 5.12 nm, % EE of 86.2 ± 3.16 and cumulative drug release of 94.8 ± 0.16%. In addition, in-vitro drug release studies confirmed a biphasic release pattern, and followed Higuchi’s model. The in vivo pharmacokinetic studies showed an increase in bioavailability by 4.3 folds as compared to marketed formulation. Conclusions The optimized RN-SLNs significantly enhanced the solubility and bioavailability of RN. The results of the present study can become a promising platform for the enhancement of oral bioavailability by novel nano carriers. Graphical abstract |
| format | Article |
| id | doaj-art-a0dc57ea20894210bbf10c41238d4ec6 |
| institution | Kabale University |
| issn | 3004-9261 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Springer |
| record_format | Article |
| series | Discover Applied Sciences |
| spelling | doaj-art-a0dc57ea20894210bbf10c41238d4ec62025-01-12T12:35:12ZengSpringerDiscover Applied Sciences3004-92612025-01-017111810.1007/s42452-024-06322-1Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancementAnanda Kumar Chettupalli0Sarad Pawar Naik Bukke1Shaik Abdul Rahaman2Aziz Unnisa3Madhumitha Adepu4Marati Kavitha5Molakpogu Ravindra Babu6Bayapa Reddy Narapureddy7Hope Onohuean8Department of Pharmaceutical Sciences, School of Pharmacy, Galgotias UniversityDepartment of Pharmaceutics and Pharmaceutical Technology, Kampala International UniversityDepartment of Pharmaceutical Sciences, School of Pharmacy, Galgotias UniversityDepartment of Pharmaceutical Chemistry, College of Pharmacy, University of HailDepartment of Pharmaceutical Sciences, School of Pharmacy, Anurag UniversityDepartment of Pharmacology, Raja Bahadur Venkata Rama Reddy (RBVRR) Women’s College of PharmacyDepartment of Pharmaceutical Sciences, School of Pharmacy, Galgotias UniversityDepartment of Public Health, College of Applied Medical Sciences, King Khalid UniversityBiopharmaceutic Unit, Department of Pharmacology and Toxicology, Kampala International University, Western CampusAbstract Background Ritonavir is an anti-retroviral protease inhibitor to treat HIV, AIDS infections. Methods The RN-SLNs were prepared by using hot homogenization followed ultrasonication method and optimized by using a two-factor, three-level central composte design (CCD). The independent variables were selected as phospholipids (X1) and type of surfactants (X2), whereas the dependent variables were chosen as percent entrapment efficiency (%EE) (Y1), size of the particle (Y2), and percent cumulative drug release (Y3). Further, the formulated R-SLNs were characterized and in vitro drug release studies were performed. The optimized R-SLNs were subjected to in vivo pharmacokinetic studies. Results The solid lipid soya leccithin showed the maximum solubility of RN (103.34 mg/g) compared to stearic acid (81.44 mg/g), glyceryl monostearate (67.21 mg/g), Gelucire 39/1 (44.22 mg/g), and Compritol 888 ATO (31.23 mg/g). Further, the surfactant blend (Tween 80: Poloxamer 188 (8:2)) showed the maximum entrapment efficiency and was the most suitable surfactant. The optimized RN-SLN formulation showed a particle size of 265.06 ± 5.12 nm, % EE of 86.2 ± 3.16 and cumulative drug release of 94.8 ± 0.16%. In addition, in-vitro drug release studies confirmed a biphasic release pattern, and followed Higuchi’s model. The in vivo pharmacokinetic studies showed an increase in bioavailability by 4.3 folds as compared to marketed formulation. Conclusions The optimized RN-SLNs significantly enhanced the solubility and bioavailability of RN. The results of the present study can become a promising platform for the enhancement of oral bioavailability by novel nano carriers. Graphical abstracthttps://doi.org/10.1007/s42452-024-06322-1RitonavirSolid-lipid nanoparticlesAbsorptionBioavailabilityDrug-delivery |
| spellingShingle | Ananda Kumar Chettupalli Sarad Pawar Naik Bukke Shaik Abdul Rahaman Aziz Unnisa Madhumitha Adepu Marati Kavitha Molakpogu Ravindra Babu Bayapa Reddy Narapureddy Hope Onohuean Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement Discover Applied Sciences Ritonavir Solid-lipid nanoparticles Absorption Bioavailability Drug-delivery |
| title | Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| title_full | Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| title_fullStr | Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| title_full_unstemmed | Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| title_short | Ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| title_sort | ritonavir loaded solid lipid nanoparticles for oral drug delivery and bioavailability enhancement |
| topic | Ritonavir Solid-lipid nanoparticles Absorption Bioavailability Drug-delivery |
| url | https://doi.org/10.1007/s42452-024-06322-1 |
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