Development and physicochemical characterization of nanostructured lipid carriers for entrapment of vitamin D3 prepared at different lipid ratios
DOI:
https://doi.org/10.46542/pe.2024.243.204210Keywords:
Miglyol, Monostearin, NLC, Physicochemical characteristic, Vitamin D3Abstract
Background: Vitamin D3 plays a role in immunity, especially in the body's regulation of the inflammatory response. The limitations of vitamin D3 are poor bioavailability and water-insoluble. Nanostructured Lipid Carriers (NLC) can increase the solubility of water-insoluble active ingredients.
Objective: To develop NLC as a delivery agent of vitamin D3 for topical application.
Method: NLC was created using a high-shear homogenisation method with various lipid ratios. NLC uses solid lipids (Monostearin) and liquid lipids (Miglyol 812) with variations in the ratios of F1 (7:3), F2 (8:2) and F3 (9:1). NLC is expected to be able to protect the active ingredients in the lipid matrix so that the stability of the active ingredients increases. Characterisation was performed in organoleptic, pH, particle size, viscosity, zeta potential, and entrapment efficiency.
Result: Vitamin D3 NLC system had good characteristics: pH suitable for topical use, particle size < 600nm, PI < 0.5, Zeta potential -26.80 to -33.76. F1 resulted in the highest entrapment efficiency of 82.18%.
Conclusion: Vitamin D3 NLC systems with different lipid concentration ratios affect the physical and chemical characteristics. Increasing the liquid lipid content in the Vit D3 NLC system can reduce particle size and viscosity and increase entrapment efficiency.
References
Almeida Moreira Leal, L. K., Lima, L. A., Alexandre de Aquino, P. E., Costa de Sousa, J. A., Jataí Gadelha, C. V., Felício Calou, I. B., Pereira Lopes, M. J., Viana Lima, F. A., Tavares Neves, K. R., Matos de Andrade, G., & Socorro de Barros Viana, G. (2020). Vitamin D (VD3) antioxidative and anti-inflammatory activities: Peripheral and central effects. European Journal of Pharmacology, 879. https://doi.org/10.1016/j.ejphar.2020.173099
Annisa. (2016). Pengembangan sistem Nanostructured Lipid Carriers (NLC) meloxicam dengan lipid monostearin dan miglyol 808 menggunakan metode emulsifikasi. Journal Of Tropical Pharmacy And Chemistry, 3(3), 156–169. https://doi.org/10.25026/jtpc.v3i3.102
Apostolou, M., Assi, S., Fatokun, A. A., & Khan, I. (2021). The effects of solid and liquid lipids on the physicochemical properties of nanostructured lipid carriers. Journal of Pharmaceutical Sciences, 110(8), 2859–2872. https://doi.org/10.1016/j.xphs.2021.04.012v
Barrea, L., Savanelli, M. C., Di Somma, C., Napolitano, M., Megna, M., Colao, A., & Savastano, S. (2017). Vitamin D and its role in psoriasis: An overview of the dermatologist and nutritionist. Reviews in Endocrine and Metabolic Disorders, 18(2), 195–205. https://doi.org/10.1007/s11154-017-9411-6
Beloqui, A., Solinís, M. Á., Rodríguez-Gascón, A., Almeida, A. J., & Préat, V. (2016). Nanostructured lipid carriers: Promising drug delivery systems for future clinics. Nanomedicine: Nanotechnology, Biology, and Medicine, 12(1), 143–161. https://doi.org/10.1016/j.nano.2015.09.004
Bubshait, D. A., Al-Dakheel, D. A., & Alanii, F. M. (2018). Topical vitamin D3: A randomized controlled trial (RCT). Clinical Nutrition ESPEN, 27, 16–19. https://doi.org/10.1016/j.clnesp.2018.05.009
Chauhan, I., Yasir, M., Verma, M., & Singh, A. P. (2020). Nanostructured lipid carriers: A groundbreaking approach for transdermal drug delivery. Advanced Pharmaceutical Bulletin, 10(2), 150–165. https://doi.org/10.34172/apb.2020.021v
Danaei, M., Dehghankhold, M., Ataei, S., Hasanzadeh Davarani, F., Javanmard, R., Dokhani, A., Khorasani, S., & Mozafari, M. R. (2018). Impact of particle size and polydispersity index on the clinical applications of lipidic nanocarrier systems. Pharmaceutics, 10(2). https://doi.org/10.3390/pharmaceutics10020057
Demirbilek, M., Laçin Türkoglu, N., Aktürk, S., & Akça, C. (2017). VitD3-loaded solid lipid nanoparticles: stability, cytotoxicity and cytokine levels. Journal of Microencapsulation, 34(5), 454–462. https://doi.org/10.1080/02652048.2017.1345995v
Elmowafy, M., & Al-Sanea, M. M. (2021). Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies. Saudi Pharmaceutical Journal, 29(9), 999–1012. https://doi.org/10.1016/j.jsps.2021.07.015
Farooq, S. U., Kumar, D. S., & Shahid, A. A. (2019). Formulation and Evaluation of Vitamin D 3 ( Cholecalciferol ) Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility. International Journal of Pharmacie and Biological Sciences, 9(3), 587–598. http://www.ijpbs.comorwww.ijpbsonline.com
Garg, N. K., Tandel, N., Bhadada, S. K., & Tyagi, R. K. (2021). Nanostructured lipid carrier–Mediated transdermal delivery of aceclofenac hydrogel present an effective therapeutic approach for inflammatory diseases. Frontiers in Pharmacology, 12(September), 1–18. https://doi.org/10.3389/fphar.2021.713616
Khater, D., Nsairat, H., Odeh, F., Saleh, M., Jaber, A., Alshaer, W., Al Bawab, A., & Mubarak, M. S. (2021). Design, preparation, and characterization of effective dermal and transdermal lipid nanoparticles: A review. Cosmetics, 8(2), 1–43. https://doi.org/10.3390/cosmetics8020039v
Listiyana, A., Mutiah, R., Suyadinata, A., & Salsabilla, F. R. (2020). Pengembangan sistem Nanostructured Lipid Carrier (NLC) daun Chrysanthemum cinerariifolium (Trev.) vis dengan variasi konsentrasi lipid. Journal of Islamic Medicine, 4(2), 86–97. https://doi.org/10.18860/jim.v4i2.9787
Madni, A., Ekwal, M., Ahmad, S., Din, I., Hussain, Z., Ranjha, N. M., Khan, M. I., Akhlaq, M., Mahmood, M. A., & Zafar, H. (2015). Ftir drug-polymer interactions studies of Perindopril erbumine. Journal of the Chemical Society of Pakistan, 36(6), 1064–1070.
Pardeike, J., Hommoss, A., & Müller, R. H. (2009). Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. International Journal of Pharmaceutics, 366(1–2), 170–184. https://doi.org/10.1016/j.ijpharm.2008.10.003
Park, C. Y. (2019). Vitamin D in the prevention and treatment of osteoarthritis: From clinical interventions to cellular evidence. Nutrients, 11(2). https://doi.org/10.3390/nu11020243
Seo, T. R., Lee, I., Chun, Y. G., Park, D. J., Lee, S. H., & Kim, B. K. (2019). Improved stability of polyglycerol polyricinoleate-substituted nanostructured lipid carrier cholecalciferol emulsions with different carrier oils. Journal of Food Science, 84(4), 782–791. https://doi.org/10.1111/1750-3841.14423
Sianipar, E. A., & Jap, A. (2023). Anti-inflammatory activity of Eucheuma denticulatum from Warambadi coast: In-vivo study model of carrageenan-induced paw oedema. Pharmacy Education, 23(2), 216–222. https://doi.org/10.46542/pe.2023.232.216222v
Souto, E. B., Baldim, I., Oliveira, W. P., Rao, R., Yadav, N., Gama, F. M., & Mahant, S. (2020). Expert opinion on drug delivery SLN and NLC for topical , dermal , and transdermal drug delivery. Expert Opinion on Drug Delivery, 00(00), 1–21. https://doi.org/10.1080/17425247.2020.1727883
Tamjidi, F., Shahedi, M., Varshosaz, J., & Nasirpour, A. (2013). Nanostructured Lipid Carriers (NLC): A potential delivery system for bioactive food molecules. In Innovative Food Science and Emerging Technologies (Vol. 19). Elsevier B.V. https://doi.org/10.1016/j.ifset.2013.03.002
Vieira, E. F., & Souza, S. (2022). Formulation strategies for improving the stability and bioavailability of vitamin D-fortified beverages: A review. Foods, 11(6), 1–20. https://doi.org/10.3390/foods11060847v
Wat, H., & Dytoc, M. (2014). Off-label uses of topical vitamin D in dermatology: A systematic review. Journal of Cutaneous Medicine and Surgery, 18(2), 91–108. https://doi.org/10.2310/7750.2013.13109