Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions
Curcumin is one of the most promising natural therapeutics for use against Alzheimer’s disease. The major limitations of curcumin are its low oral bioavailability and difficulty in permeating the blood–brain barrier. Therefore, designing a delivery system of curcumin to overcome its limitations must...
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MDPI AG
2022-01-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/3/443 |
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| author | Rungsinee Phongpradist Wisanu Thongchai Kriangkrai Thongkorn Suree Lekawanvijit Chuda Chittasupho |
| author_facet | Rungsinee Phongpradist Wisanu Thongchai Kriangkrai Thongkorn Suree Lekawanvijit Chuda Chittasupho |
| author_sort | Rungsinee Phongpradist |
| collection | DOAJ |
| description | Curcumin is one of the most promising natural therapeutics for use against Alzheimer’s disease. The major limitations of curcumin are its low oral bioavailability and difficulty in permeating the blood–brain barrier. Therefore, designing a delivery system of curcumin to overcome its limitations must be employed. KLVFF, a peptide known as an amyloid blocker, was used in this study as a targeting moiety to develop a targeted drug delivery system. A prototype of transnasal KLVFF conjugated microemulsions containing curcumin (KLVFF-Cur-ME) for the nose-to-brain delivery was fabricated. The KLVFF-Cur-ME was developed by a titration method. A conjugation of KLVFF was performed through a carbodiimide reaction, and the conjugation efficiency was confirmed by FTIR and DSC technique. KLVFD-Cur-ME was characterized for the drug content, globule size, zeta potential, and pH. A transparent and homogeneous KLVFF-Cur-ME is achieved with a drug content of 80.25% and a globule size of 76.1 ± 2.5 nm. The pH of KLVFF-Cur-ME is 5.33 ± 0.02, indicating non-irritation to nasal tissues. KLVFD-Cur-ME does not show nasal ciliotoxicity. An ex vivo diffusion study revealed that KLVFF-Cur-ME partitions the porcine nasal mucosa through diffusion, following the Higuchi model. This investigation demonstrates the successful synthesis of a bifunctional KLVFF-Cur-ME as a novel prototype to deliver anti-A<i>β</i> aggregation via an intranasal administration. |
| first_indexed | 2024-03-09T23:17:02Z |
| format | Article |
| id | doaj.art-dfb08be069d14824b1d171bd5c71ff20 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T23:17:02Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-dfb08be069d14824b1d171bd5c71ff202023-11-23T17:33:54ZengMDPI AGPolymers2073-43602022-01-0114344310.3390/polym14030443Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional MicroemulsionsRungsinee Phongpradist0Wisanu Thongchai1Kriangkrai Thongkorn2Suree Lekawanvijit3Chuda Chittasupho4Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, ThailandChemistry Program, Faculty of Science and Technology, Pibulsongkram Rajabhat University, Phitsanuloke 65000, ThailandDepartment of Companion Animals and Wildlife Clinic, Faculty of Veterinary Medicine, Chiang Mai University, Chiang Mai 50100, ThailandDepartment of Pathology, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, ThailandDepartment of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, ThailandCurcumin is one of the most promising natural therapeutics for use against Alzheimer’s disease. The major limitations of curcumin are its low oral bioavailability and difficulty in permeating the blood–brain barrier. Therefore, designing a delivery system of curcumin to overcome its limitations must be employed. KLVFF, a peptide known as an amyloid blocker, was used in this study as a targeting moiety to develop a targeted drug delivery system. A prototype of transnasal KLVFF conjugated microemulsions containing curcumin (KLVFF-Cur-ME) for the nose-to-brain delivery was fabricated. The KLVFF-Cur-ME was developed by a titration method. A conjugation of KLVFF was performed through a carbodiimide reaction, and the conjugation efficiency was confirmed by FTIR and DSC technique. KLVFD-Cur-ME was characterized for the drug content, globule size, zeta potential, and pH. A transparent and homogeneous KLVFF-Cur-ME is achieved with a drug content of 80.25% and a globule size of 76.1 ± 2.5 nm. The pH of KLVFF-Cur-ME is 5.33 ± 0.02, indicating non-irritation to nasal tissues. KLVFD-Cur-ME does not show nasal ciliotoxicity. An ex vivo diffusion study revealed that KLVFF-Cur-ME partitions the porcine nasal mucosa through diffusion, following the Higuchi model. This investigation demonstrates the successful synthesis of a bifunctional KLVFF-Cur-ME as a novel prototype to deliver anti-A<i>β</i> aggregation via an intranasal administration.https://www.mdpi.com/2073-4360/14/3/443microemulsionsmodified Pluronictargetedsurface modificationKLVFFcurcumin |
| spellingShingle | Rungsinee Phongpradist Wisanu Thongchai Kriangkrai Thongkorn Suree Lekawanvijit Chuda Chittasupho Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions Polymers microemulsions modified Pluronic targeted surface modification KLVFF curcumin |
| title | Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions |
| title_full | Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions |
| title_fullStr | Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions |
| title_full_unstemmed | Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions |
| title_short | Surface Modification of Curcumin Microemulsions by Coupling of KLVFF Peptide: A Prototype for Targeted Bifunctional Microemulsions |
| title_sort | surface modification of curcumin microemulsions by coupling of klvff peptide a prototype for targeted bifunctional microemulsions |
| topic | microemulsions modified Pluronic targeted surface modification KLVFF curcumin |
| url | https://www.mdpi.com/2073-4360/14/3/443 |
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