Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach
The purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 3<sup>2</sup> factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substant...
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MDPI AG
2022-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/3/584 |
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| author | Afzal Haq Asif Prasanna Kumar Desu Rajasekhar Reddy Alavala Gudhanti Siva Naga Koteswara Rao Nagaraja Sreeharsha Girish Meravanige |
| author_facet | Afzal Haq Asif Prasanna Kumar Desu Rajasekhar Reddy Alavala Gudhanti Siva Naga Koteswara Rao Nagaraja Sreeharsha Girish Meravanige |
| author_sort | Afzal Haq Asif |
| collection | DOAJ |
| description | The purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 3<sup>2</sup> factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substantial first-pass metabolism resulting in a low (30%) bioavailability and a short elimination half-life. FLV-SLNPs were prepared using the nano-emulsion technique. For the optimization of the FLV-SLNPs, a total of nine formulations were prepared by varying two independent factors at three levels, using full factorial design. In this design, lipid (A) and surfactant (B) concentrations were chosen as independent factors, whereas entrapment efficiency (Y1) and in-vitro drug release (Y2) were selected as the dependent variables. Additionally, the prepared SLNPs were characterized for X-ray diffraction, Fourier transform-infrared spectroscopy, and differential scanning calorimetry. These studies revealed that there were no interactions between the drug and the selected excipients and the selected formulation components are compatible with the drug. Pharmacokinetic studies in rats confirmed significant improvement in AUC and MRT of SLNPs in comparison with the pure drug indicating the enhanced bioavailability of SLNPs. This study provides a proof-of-concept for the fact that SLNPs can be effectively developed via experimental factorial design, which requires relatively minimal experimentation. |
| first_indexed | 2024-03-09T12:59:13Z |
| format | Article |
| id | doaj.art-cbbaba77d62b4c83ad9b12a9ec9f8bb9 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T12:59:13Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-cbbaba77d62b4c83ad9b12a9ec9f8bb92023-11-30T21:57:00ZengMDPI AGPharmaceutics1999-49232022-03-0114358410.3390/pharmaceutics14030584Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design ApproachAfzal Haq Asif0Prasanna Kumar Desu1Rajasekhar Reddy Alavala2Gudhanti Siva Naga Koteswara Rao3Nagaraja Sreeharsha4Girish Meravanige5Department of Pharmacy Practice, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaCollege of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram 522502, IndiaShobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM’s NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai 400056, IndiaDepartment of Pharmacy, School of Medical and Allied Sciences, Galgotias University, Greater Noida 203201, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Biomedical Sciences, College of Medicine, King Faisal University, Al-Ahsa 31982, Saudi ArabiaThe purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 3<sup>2</sup> factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substantial first-pass metabolism resulting in a low (30%) bioavailability and a short elimination half-life. FLV-SLNPs were prepared using the nano-emulsion technique. For the optimization of the FLV-SLNPs, a total of nine formulations were prepared by varying two independent factors at three levels, using full factorial design. In this design, lipid (A) and surfactant (B) concentrations were chosen as independent factors, whereas entrapment efficiency (Y1) and in-vitro drug release (Y2) were selected as the dependent variables. Additionally, the prepared SLNPs were characterized for X-ray diffraction, Fourier transform-infrared spectroscopy, and differential scanning calorimetry. These studies revealed that there were no interactions between the drug and the selected excipients and the selected formulation components are compatible with the drug. Pharmacokinetic studies in rats confirmed significant improvement in AUC and MRT of SLNPs in comparison with the pure drug indicating the enhanced bioavailability of SLNPs. This study provides a proof-of-concept for the fact that SLNPs can be effectively developed via experimental factorial design, which requires relatively minimal experimentation.https://www.mdpi.com/1999-4923/14/3/584fluvastatin sodium3<sup>2</sup> factorial designparticle sizein vitro drug releasecontour plots |
| spellingShingle | Afzal Haq Asif Prasanna Kumar Desu Rajasekhar Reddy Alavala Gudhanti Siva Naga Koteswara Rao Nagaraja Sreeharsha Girish Meravanige Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach Pharmaceutics fluvastatin sodium 3<sup>2</sup> factorial design particle size in vitro drug release contour plots |
| title | Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach |
| title_full | Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach |
| title_fullStr | Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach |
| title_full_unstemmed | Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach |
| title_short | Development, Statistical Optimization and Characterization of Fluvastatin Loaded Solid Lipid Nanoparticles: A 3<sup>2</sup> Factorial Design Approach |
| title_sort | development statistical optimization and characterization of fluvastatin loaded solid lipid nanoparticles a 3 sup 2 sup factorial design approach |
| topic | fluvastatin sodium 3<sup>2</sup> factorial design particle size in vitro drug release contour plots |
| url | https://www.mdpi.com/1999-4923/14/3/584 |
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