Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz
Despite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efa...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-06-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/7/1318 |
| _version_ | 1827604632121114624 |
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| author | Grady K. Mukubwa Justin B. Safari Roderick B. Walker Rui W. M. Krause |
| author_facet | Grady K. Mukubwa Justin B. Safari Roderick B. Walker Rui W. M. Krause |
| author_sort | Grady K. Mukubwa |
| collection | DOAJ |
| description | Despite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efavirenz (EFV) as a drug model. EFV solubility was assessed in water, Labrafac Lipophile and medium chain triglycerides oil (MCT oil). EFV turned out to be more soluble in the two latter dissolving media (solubility > 250 mg/mL); hence, given its affordability, MCT oil was used for LNC formulation. LNC were prepared using a low-energy method named phase inversion, and following a design of experiments process. This one resulted in polynomial models that predicted LNC particle size, polydispersity index and zeta potential that were, respectively, around 50 nm, below 0.2 and below −33 mV, for the optimized formulations. Once synthesized, we were able to achieve an encapsulation efficacy of 87%. On the other hand, high EFV release from the LNC carrier was obtained in neutral medium as compared to acid milieu (pH 4) with, respectively, 42 and 27% EFV release within 74 h. Other characterization techniques were applied and further supported the successful encapsulation of EFV in LNCs in an amorphous form. Stability studies revealed that the developed LNC were quite stable over the period of 28 days. Ultimately, LNCs have been demonstrated to improve the biopharmaceutical properties of EFV and could therefore be used to fight against antiviral resistance. |
| first_indexed | 2024-03-09T06:04:54Z |
| format | Article |
| id | doaj.art-f6c078dacab74e76af51342387e4ce21 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T06:04:54Z |
| publishDate | 2022-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-f6c078dacab74e76af51342387e4ce212023-12-03T12:05:56ZengMDPI AGPharmaceutics1999-49232022-06-01147131810.3390/pharmaceutics14071318Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of EfavirenzGrady K. Mukubwa0Justin B. Safari1Roderick B. Walker2Rui W. M. Krause3Department of Chemistry, Faculty of Science, Rhodes University, P.O. Box 94, Grahamstown 6140, Eastern Cape, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, P.O. Box 94, Grahamstown 6140, Eastern Cape, South AfricaDepartment of Pharmaceutics, Faculty of Pharmacy, Rhodes University, P.O. Box 94, Grahamstown 6140, Eastern Cape, South AfricaDepartment of Chemistry, Faculty of Science, Rhodes University, P.O. Box 94, Grahamstown 6140, Eastern Cape, South AfricaDespite their incredible contribution to fighting viral infections, antiviral viral resistance is an increasing concern and often arises due to unfavorable physicochemical and biopharmaceutical properties. To address this kind of issue, lipid nanocapsules (LNC) are developed in this study, using efavirenz (EFV) as a drug model. EFV solubility was assessed in water, Labrafac Lipophile and medium chain triglycerides oil (MCT oil). EFV turned out to be more soluble in the two latter dissolving media (solubility > 250 mg/mL); hence, given its affordability, MCT oil was used for LNC formulation. LNC were prepared using a low-energy method named phase inversion, and following a design of experiments process. This one resulted in polynomial models that predicted LNC particle size, polydispersity index and zeta potential that were, respectively, around 50 nm, below 0.2 and below −33 mV, for the optimized formulations. Once synthesized, we were able to achieve an encapsulation efficacy of 87%. On the other hand, high EFV release from the LNC carrier was obtained in neutral medium as compared to acid milieu (pH 4) with, respectively, 42 and 27% EFV release within 74 h. Other characterization techniques were applied and further supported the successful encapsulation of EFV in LNCs in an amorphous form. Stability studies revealed that the developed LNC were quite stable over the period of 28 days. Ultimately, LNCs have been demonstrated to improve the biopharmaceutical properties of EFV and could therefore be used to fight against antiviral resistance.https://www.mdpi.com/1999-4923/14/7/1318viral resistancelipid nanocapsulesefavirenzdesign expert |
| spellingShingle | Grady K. Mukubwa Justin B. Safari Roderick B. Walker Rui W. M. Krause Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz Pharmaceutics viral resistance lipid nanocapsules efavirenz design expert |
| title | Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz |
| title_full | Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz |
| title_fullStr | Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz |
| title_full_unstemmed | Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz |
| title_short | Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz |
| title_sort | design manufacturing characterization and evaluation of lipid nanocapsules to enhance the biopharmaceutical properties of efavirenz |
| topic | viral resistance lipid nanocapsules efavirenz design expert |
| url | https://www.mdpi.com/1999-4923/14/7/1318 |
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