Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations.
Nanostructured lipid carriers (NLCs) loaded with lopinavir (LPV) were prepared by the high-shear homogenization method. The LPV-NLCs formulations were freeze-dried using trehalose as a cryoprotectant. In vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8...
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| Format: | Article |
| Language: | English |
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MDPI
2019
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| Online Access: | http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf |
| _version_ | 1848822101765521408 |
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| author | Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis |
| author_facet | Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis |
| author_sort | Khan, Arshad Ali |
| building | UMP Institutional Repository |
| collection | Online Access |
| description | Nanostructured lipid carriers (NLCs) loaded with lopinavir (LPV) were prepared by the high-shear homogenization method. The LPV-NLCs formulations were freeze-dried using trehalose as a cryoprotectant. In vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8) showed a burst release. The optimized freeze-dried formulation (LPV-NLC-7-Tres) had a particle size (PS), polydispersity index (PdI), zeta potential (ZP) and % entrapment efficiency (%EE) of 286.8 ± 1.3 nm, 0.413 ± 0.017, −48.6 ± 0.89 mV and 88.31 ± 2.04%, respectively. The optimized formulation observed by transmission and scanning electron microscopes showed a spherical shape. Differential scanning calorimetry study revealed the absence of chemical interaction between the drug and lipids. In vitro cellular uptake study using Caco-2 cell line showed a higher LPV uptake from LPV-NLC-7-Tres formulation compared to the free LPV-suspension. The 6-month stability study showed a minimum rise of ~40 nm in PS, while no significant changes in PdI, ZP and drug content of the LPV-NLC-7-Tres formulation stored at 5 °C ± 3 °C. The bioavailability of LPV following oral administration of LPV-NLC-7-Tres in male Wistar rats was found 6.98-fold higher than the LPV-suspension. In conclusion, the nanostructure lipid carriers are potential carriers for improving the oral bioavailability of lopinavir. |
| first_indexed | 2025-11-15T02:35:53Z |
| format | Article |
| id | ump-24708 |
| institution | Universiti Malaysia Pahang |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T02:35:53Z |
| publishDate | 2019 |
| publisher | MDPI |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | ump-247082019-06-10T03:27:51Z http://umpir.ump.edu.my/id/eprint/24708/ Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis QP Physiology Nanostructured lipid carriers (NLCs) loaded with lopinavir (LPV) were prepared by the high-shear homogenization method. The LPV-NLCs formulations were freeze-dried using trehalose as a cryoprotectant. In vitro release studies in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8) showed a burst release. The optimized freeze-dried formulation (LPV-NLC-7-Tres) had a particle size (PS), polydispersity index (PdI), zeta potential (ZP) and % entrapment efficiency (%EE) of 286.8 ± 1.3 nm, 0.413 ± 0.017, −48.6 ± 0.89 mV and 88.31 ± 2.04%, respectively. The optimized formulation observed by transmission and scanning electron microscopes showed a spherical shape. Differential scanning calorimetry study revealed the absence of chemical interaction between the drug and lipids. In vitro cellular uptake study using Caco-2 cell line showed a higher LPV uptake from LPV-NLC-7-Tres formulation compared to the free LPV-suspension. The 6-month stability study showed a minimum rise of ~40 nm in PS, while no significant changes in PdI, ZP and drug content of the LPV-NLC-7-Tres formulation stored at 5 °C ± 3 °C. The bioavailability of LPV following oral administration of LPV-NLC-7-Tres in male Wistar rats was found 6.98-fold higher than the LPV-suspension. In conclusion, the nanostructure lipid carriers are potential carriers for improving the oral bioavailability of lopinavir. MDPI 2019-02-25 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf Khan, Arshad Ali and Mudassir, Jahanzeb and Akhtar, Safia and Murugaiyah, Vikneswaran and Yusrida, Darwis (2019) Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. Pharmaceutics, 11 (2). pp. 1-19. ISSN 1999-4923. (Published) https://doi.org/10.3390/pharmaceutics11020097 https://doi.org/10.3390/pharmaceutics11020097 |
| spellingShingle | QP Physiology Khan, Arshad Ali Mudassir, Jahanzeb Akhtar, Safia Murugaiyah, Vikneswaran Yusrida, Darwis Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title | Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title_full | Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title_fullStr | Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title_full_unstemmed | Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title_short | Freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| title_sort | freeze-dried lopinavir-loaded nanostructured lipid carriers for enhanced cellular uptake and bioavailability: statistical optimization, in vitro and in vivo evaluations. |
| topic | QP Physiology |
| url | http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/ http://umpir.ump.edu.my/id/eprint/24708/1/Freeze-Dried%20Lopinavir-Loaded%20Nanostructured%20Lipid%20Carriers%20for%20Enhanced%20Cellular.pdf |