Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables
Finasteride (FIN), a 5-α reductase enzyme inhibitor is mainly used orally for the treatment of androgenic alopecia and benign prostate hyperplasia. The present study was undertaken for systematic optimization and assessment of the designed nanostructured lipid carriers (NLC) to enhance follicular de...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-08-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844022014633 |
| _version_ | 1828745790362746880 |
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| author | Shweta Ramkar Preeti K. Suresh |
| author_facet | Shweta Ramkar Preeti K. Suresh |
| author_sort | Shweta Ramkar |
| collection | DOAJ |
| description | Finasteride (FIN), a 5-α reductase enzyme inhibitor is mainly used orally for the treatment of androgenic alopecia and benign prostate hyperplasia. The present study was undertaken for systematic optimization and assessment of the designed nanostructured lipid carriers (NLC) to enhance follicular delivery of FIN by topical administration. The NLCs were prepared by microemulsion method, by employing a 33 Box-Behnken design and subsequently confirmed by ANOVA analysis. Compritol ATO-888 and Fenugreek oil were selected as the solid lipid and liquid lipid respectively for the fabrication of NLCs. The formulations were characterized for particle size, zeta potential, entrapment efficiency, storage stability and in vitro drug release profile. Morphological profile of the NLCs nanocarriers was studied by transmission electron microscopy (TEM). The Fourier Transform Infrared Spectroscopy (FT-IR) spectrum and differential scanning calorimetry (DSC) thermogram demonstrated that FIN entrapment within NLCs was devoid of chemical interaction with the components. The prepared NLCs had satisfactory particle dimensions, zeta potential and entrapment efficiency. The numerical optimization process indicated the optimal NLC composition with 3 mg of SPC, 6 mg lipid and 5 mg of drug. NLCs loaded with FIN had acceptable particle size at 379.8 nm, zeta potential of −37.1 mV and an entrapment efficiency of 84%. Transmission electron microscopy indicated the spherical morphology. In vitro release profile indicated a fast initial release and subsequently a prolonged release of FIN from the carrier for 24 h. The release kinetics data displayed a Higuchi diffusion release model with the best match R2 value (0.848). Short-term stability tests conducted over 4 weeks at 6° and 25 °C demonstrated that the formulation could retain their initial properties during the test period. |
| first_indexed | 2024-04-14T04:11:04Z |
| format | Article |
| id | doaj.art-c2e08407040b4105a62029f88521f8f4 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-04-14T04:11:04Z |
| publishDate | 2022-08-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-c2e08407040b4105a62029f88521f8f42022-12-22T02:13:11ZengElsevierHeliyon2405-84402022-08-0188e10175Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variablesShweta Ramkar0Preeti K. Suresh1University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, IndiaCorresponding author.; University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, 492010, IndiaFinasteride (FIN), a 5-α reductase enzyme inhibitor is mainly used orally for the treatment of androgenic alopecia and benign prostate hyperplasia. The present study was undertaken for systematic optimization and assessment of the designed nanostructured lipid carriers (NLC) to enhance follicular delivery of FIN by topical administration. The NLCs were prepared by microemulsion method, by employing a 33 Box-Behnken design and subsequently confirmed by ANOVA analysis. Compritol ATO-888 and Fenugreek oil were selected as the solid lipid and liquid lipid respectively for the fabrication of NLCs. The formulations were characterized for particle size, zeta potential, entrapment efficiency, storage stability and in vitro drug release profile. Morphological profile of the NLCs nanocarriers was studied by transmission electron microscopy (TEM). The Fourier Transform Infrared Spectroscopy (FT-IR) spectrum and differential scanning calorimetry (DSC) thermogram demonstrated that FIN entrapment within NLCs was devoid of chemical interaction with the components. The prepared NLCs had satisfactory particle dimensions, zeta potential and entrapment efficiency. The numerical optimization process indicated the optimal NLC composition with 3 mg of SPC, 6 mg lipid and 5 mg of drug. NLCs loaded with FIN had acceptable particle size at 379.8 nm, zeta potential of −37.1 mV and an entrapment efficiency of 84%. Transmission electron microscopy indicated the spherical morphology. In vitro release profile indicated a fast initial release and subsequently a prolonged release of FIN from the carrier for 24 h. The release kinetics data displayed a Higuchi diffusion release model with the best match R2 value (0.848). Short-term stability tests conducted over 4 weeks at 6° and 25 °C demonstrated that the formulation could retain their initial properties during the test period.http://www.sciencedirect.com/science/article/pii/S2405844022014633Quality-by-designResponse surface methodologyNanomedicineLipidic carriersFollicularTransfollicular |
| spellingShingle | Shweta Ramkar Preeti K. Suresh Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables Heliyon Quality-by-design Response surface methodology Nanomedicine Lipidic carriers Follicular Transfollicular |
| title | Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables |
| title_full | Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables |
| title_fullStr | Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables |
| title_full_unstemmed | Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables |
| title_short | Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables |
| title_sort | finasteride loaded nano lipidic carriers for follicular drug delivery preformulation screening and box behnken experimental design for optimization of variables |
| topic | Quality-by-design Response surface methodology Nanomedicine Lipidic carriers Follicular Transfollicular |
| url | http://www.sciencedirect.com/science/article/pii/S2405844022014633 |
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