Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note
This study aimed to develop and evaluate nicotine--stearic acid conjugate-loaded solid lipid nanoparticles (NSA-SLNs) for transdermal delivery in nicotine replacement therapy (NRT). Nicotine conjugation to stearic acid prior to SLN formulation greatly increased drug loading. SLNs loaded with a nicot...
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| Format: | Article |
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MDPI AG
2023-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/4/1043 |
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| author | Jwala Renukuntla Samuel Peterson-Sockwell Bradley A. Clark Nipunika H. Godage Emanuela Gionfriddo Pradeep Kumar Bolla Sai H. S. Boddu |
| author_facet | Jwala Renukuntla Samuel Peterson-Sockwell Bradley A. Clark Nipunika H. Godage Emanuela Gionfriddo Pradeep Kumar Bolla Sai H. S. Boddu |
| author_sort | Jwala Renukuntla |
| collection | DOAJ |
| description | This study aimed to develop and evaluate nicotine--stearic acid conjugate-loaded solid lipid nanoparticles (NSA-SLNs) for transdermal delivery in nicotine replacement therapy (NRT). Nicotine conjugation to stearic acid prior to SLN formulation greatly increased drug loading. SLNs loaded with a nicotine–stearic acid conjugate were characterized for size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, and morphology. Pilot in vivo testing was carried out in New Zealand Albino rabbits. The size, PDI, and ZP of nicotine–stearic acid conjugate-loaded SLNs were 113.5 ± 0.91 nm, 0.211 ± 0.01, and −48.1 ± 5.75 mV, respectively. The entrapment efficiency of nicotine–stearic acid conjugate in SLNs was 46.45 ± 1.53%. TEM images revealed that optimized nicotine–stearic acid conjugate-loaded SLNs were uniform and roughly spherical in shape. Nicotine–stearic acid conjugate-loaded SLNs showed enhanced and sustained drug levels for up to 96 h in rabbits when compared with the control nicotine formulation in 2% HPMC gel. To conclude, the reported NSA-SLNs could be further explored as an alternative for treating smoking cessation. |
| first_indexed | 2024-03-11T04:37:58Z |
| format | Article |
| id | doaj.art-1bc3e55d29a64ecf9c3292db9ca988fb |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:37:58Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-1bc3e55d29a64ecf9c3292db9ca988fb2023-11-17T20:51:54ZengMDPI AGPharmaceutics1999-49232023-03-01154104310.3390/pharmaceutics15041043Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical NoteJwala Renukuntla0Samuel Peterson-Sockwell1Bradley A. Clark2Nipunika H. Godage3Emanuela Gionfriddo4Pradeep Kumar Bolla5Sai H. S. Boddu6School of Pharmacy, The University of Texas at El Paso, 1101 N Campbell St., El Paso, TX 79902, USADepartment of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High Point University, High Point, NC 27240, USADepartment of Basic Pharmaceutical Sciences, Fred Wilson School of Pharmacy, High Point University, High Point, NC 27240, USADepartment of Chemistry and Biochemistry, School of Green Chemistry and Engineering, College of Natural Sciences and Mathematics, University of Toledo, Toledo, OH 43606, USADepartment of Chemistry and Biochemistry, School of Green Chemistry and Engineering, College of Natural Sciences and Mathematics, University of Toledo, Toledo, OH 43606, USASchool of Pharmacy, The University of Texas at El Paso, 1101 N Campbell St., El Paso, TX 79902, USACollege of Pharmacy and Health Sciences, Ajman University, Ajman P.O. Box 346, United Arab EmiratesThis study aimed to develop and evaluate nicotine--stearic acid conjugate-loaded solid lipid nanoparticles (NSA-SLNs) for transdermal delivery in nicotine replacement therapy (NRT). Nicotine conjugation to stearic acid prior to SLN formulation greatly increased drug loading. SLNs loaded with a nicotine–stearic acid conjugate were characterized for size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, and morphology. Pilot in vivo testing was carried out in New Zealand Albino rabbits. The size, PDI, and ZP of nicotine–stearic acid conjugate-loaded SLNs were 113.5 ± 0.91 nm, 0.211 ± 0.01, and −48.1 ± 5.75 mV, respectively. The entrapment efficiency of nicotine–stearic acid conjugate in SLNs was 46.45 ± 1.53%. TEM images revealed that optimized nicotine–stearic acid conjugate-loaded SLNs were uniform and roughly spherical in shape. Nicotine–stearic acid conjugate-loaded SLNs showed enhanced and sustained drug levels for up to 96 h in rabbits when compared with the control nicotine formulation in 2% HPMC gel. To conclude, the reported NSA-SLNs could be further explored as an alternative for treating smoking cessation.https://www.mdpi.com/1999-4923/15/4/1043nicotinestearic acidsolid lipid nanoparticlesgeltransdermal permeationsmoking cessation |
| spellingShingle | Jwala Renukuntla Samuel Peterson-Sockwell Bradley A. Clark Nipunika H. Godage Emanuela Gionfriddo Pradeep Kumar Bolla Sai H. S. Boddu Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note Pharmaceutics nicotine stearic acid solid lipid nanoparticles gel transdermal permeation smoking cessation |
| title | Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note |
| title_full | Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note |
| title_fullStr | Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note |
| title_full_unstemmed | Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note |
| title_short | Design and Preclinical Evaluation of Nicotine–Stearic Acid Conjugate-Loaded Solid Lipid Nanoparticles for Transdermal Delivery: A Technical Note |
| title_sort | design and preclinical evaluation of nicotine stearic acid conjugate loaded solid lipid nanoparticles for transdermal delivery a technical note |
| topic | nicotine stearic acid solid lipid nanoparticles gel transdermal permeation smoking cessation |
| url | https://www.mdpi.com/1999-4923/15/4/1043 |
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