PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery
Aceclofenac is a non-steroidal anti-inflammatory drug with poor aqueous solubility and a short half-life resulting in low bioavailability. Aceclofenac-loaded solid lipid microparticles based solidified reverse micellar solution (SLMs-SRMS) for oral drug delivery was investigated to improve the bioav...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-04-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844022005357 |
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| author | Calister E. Ugwu Jude N. Oraeluno Kingsley C. Eze Caleb O. Ezenma Anthony O. Nwankwo |
| author_facet | Calister E. Ugwu Jude N. Oraeluno Kingsley C. Eze Caleb O. Ezenma Anthony O. Nwankwo |
| author_sort | Calister E. Ugwu |
| collection | DOAJ |
| description | Aceclofenac is a non-steroidal anti-inflammatory drug with poor aqueous solubility and a short half-life resulting in low bioavailability. Aceclofenac-loaded solid lipid microparticles based solidified reverse micellar solution (SLMs-SRMS) for oral drug delivery was investigated to improve the bioavailability and control drug release. Hot homogenization method was adopted to prepare the SLMs using a homolipid irvingia fat and Phospholipon® 90H with or without propylene glycol 6000 (PEGylation) in different ratios and characterized in vitro. The in vivo anti-inflammatory activity of the drug was determined on mice inflamed with carrageenan as phlogistic agent. Results showed that the morphology and particle sizes of the SLMs were spherical and smooth and ranged between 5.24 ± 0.01–97.44 ± 0.18 μm. EE % ranged between 67 - 81 %. A significant (p < 0.05) viscosity of 490 mPasec-1 was obtained. FTIR spectra indicated compatibility amongst the constituents. DSC showed a broad peak which depicted an imperfect matrix resulting in a deformation of crystal arrangement creating many spaces for drug entrapment. Delayed drug release was observed in almost all the formulations in SIF (pH, 6.8). Anti-inflammatory activity showed a significant inhibitory effect (p < 0.05, up to 90 %). Hence, the aceclofenac-loaded SLMs-SRMS showed desirable characteristics and could be used for controlled delivery of aceclofenac and thus alternative to conventional aceclofenac oral formulation. |
| first_indexed | 2024-12-11T10:45:11Z |
| format | Article |
| id | doaj.art-b4c3c8404f5042a7b9d6f1715fba85f2 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-12-11T10:45:11Z |
| publishDate | 2022-04-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-b4c3c8404f5042a7b9d6f1715fba85f22022-12-22T01:10:30ZengElsevierHeliyon2405-84402022-04-0184e09247PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug deliveryCalister E. Ugwu0Jude N. Oraeluno1Kingsley C. Eze2Caleb O. Ezenma3Anthony O. Nwankwo4Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, Nigeria; Corresponding author.Department of Pharmaceutics and Pharmaceutical Technology, Niger Delta University Wilberforce Island Amassoma, Bayelsa State, NigeriaDepartment of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, NigeriaDepartment of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, NigeriaDepartment of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, NigeriaAceclofenac is a non-steroidal anti-inflammatory drug with poor aqueous solubility and a short half-life resulting in low bioavailability. Aceclofenac-loaded solid lipid microparticles based solidified reverse micellar solution (SLMs-SRMS) for oral drug delivery was investigated to improve the bioavailability and control drug release. Hot homogenization method was adopted to prepare the SLMs using a homolipid irvingia fat and Phospholipon® 90H with or without propylene glycol 6000 (PEGylation) in different ratios and characterized in vitro. The in vivo anti-inflammatory activity of the drug was determined on mice inflamed with carrageenan as phlogistic agent. Results showed that the morphology and particle sizes of the SLMs were spherical and smooth and ranged between 5.24 ± 0.01–97.44 ± 0.18 μm. EE % ranged between 67 - 81 %. A significant (p < 0.05) viscosity of 490 mPasec-1 was obtained. FTIR spectra indicated compatibility amongst the constituents. DSC showed a broad peak which depicted an imperfect matrix resulting in a deformation of crystal arrangement creating many spaces for drug entrapment. Delayed drug release was observed in almost all the formulations in SIF (pH, 6.8). Anti-inflammatory activity showed a significant inhibitory effect (p < 0.05, up to 90 %). Hence, the aceclofenac-loaded SLMs-SRMS showed desirable characteristics and could be used for controlled delivery of aceclofenac and thus alternative to conventional aceclofenac oral formulation.http://www.sciencedirect.com/science/article/pii/S2405844022005357AceclofenacIrvingia fatHomolipidAnti-inflammatoryLipid matrixSLMs-SMRS |
| spellingShingle | Calister E. Ugwu Jude N. Oraeluno Kingsley C. Eze Caleb O. Ezenma Anthony O. Nwankwo PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery Heliyon Aceclofenac Irvingia fat Homolipid Anti-inflammatory Lipid matrix SLMs-SMRS |
| title | PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery |
| title_full | PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery |
| title_fullStr | PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery |
| title_full_unstemmed | PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery |
| title_short | PEGylated aceclofenac solid lipid microparticles homolipid-based solidified reverse micellar solutions for drug delivery |
| title_sort | pegylated aceclofenac solid lipid microparticles homolipid based solidified reverse micellar solutions for drug delivery |
| topic | Aceclofenac Irvingia fat Homolipid Anti-inflammatory Lipid matrix SLMs-SMRS |
| url | http://www.sciencedirect.com/science/article/pii/S2405844022005357 |
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