Optimization of beta-carotene self-nanoemulsifying drug delivery system formula based on a low-energy method preparation and simplex lattice design
Abstract
Beta-carotene is an antioxidant compound that benefits health by boosting immunity and preventing chronic diseases. However, beta-carotene has low solubility (practically insoluble in water) and bioavailability, so it will produce a poor beneficial effect. An alternative candidate that may overcome this problem is a self-nanoemulsifying drug delivery system (SNEDDS). SNEDDS can enhance the oral bioavailability of poorly soluble active compounds by increasing the solubility and stability of active compounds in oil droplets. This study aims to develop beta-carotene SNEDDS by determining the optimum composition of SNEDDS. The low-energy method and simplex lattice design (SLD) were combined to determine the optimum formula. Based on the results, the solubility of beta-carotene in sesame oil, polysorbate 80, and PEG 400 as components of SNEEDS were 0.455 mg/mL, 1.538 mg/mL, and 0.667 mg/mL, respectively. The optimum formula of beta-carotene SNEDDS had a mixing ratio of sesame oil and surfactant mixture in 1:15.2 (v/v), emulsification time of 38.48 ± 0.70 seconds, the droplet size of 13.13 ± 0.50 nm, and size distribution (PdI) of 0.133 ± 0.06. The optimum formula of beta-carotene SNEDDS had good stability in the artificial gastric fluid after 4 hours of incubation. Moreover, the optimum beta-carotene SNEDDS formula had high stability during storage at room temperature and 40oC ± 2oC/75%RH±5%RH.
References
- [1] Rodriguez-Amaya DB. Food carotenoids: chemistry, biology, and technology. Wiley Blackwell, West Sussex, UK 2015.
- [2] Ashfaq M, Shah S, Rasul A, Hanif M, Khan HU, Khames, Abdelgawad MA, Ghoenim MM, Ali MY, Abourehab MA, Maheen S, Iqbal O, Abbas G, Sisi AM. Enhancement of the solubility and bioavailability of pitavastatin through a self-nanoemulsifying drug delivery system (SNEDDS). Pharmaceutics. 2022;14(3): 482. https://doi.org/10.3390/pharmaceutics14030482
- [3] Gibaud S and Attivi D. Microemulsions for oral administration and their therapeutic applications. Expert Opin Drug Deliv. 2012;9(8): 937-951. https://doi.org/10.1517/17425247.2012.694865
- [4] Mohd AB, Chella N, Sanka K, Shastri NR, Diwan PV. Improved anti-diabetic activity of glibenclamide using oral self-nanoemulsifying powder. J Microencapsul. 2015;32(1): 54-60. https://doi.org/10.3109/02652048.2014.944950
- [5] Zhang P, Liu Y, Feng N, dan Xu J. Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. Int J Pharmaceutics. 2008; 355(1-2): 269–276. https://doi.org/10.1016/j.ijpharm.2007.12.026
- [6] Ujilestari T, Martien R, Ariyadi B, Dono ND, Zuprizal. Self-nanoemulsifying drug delivery system (SNEDDS) of Amomum compactum essential oil: Design, formulation, and characterization. J App Pharm Sci. 2018; 8(6): 14-21. https://doi.org/10.1007/s13346-022-01193-8
- [7] Gupta A, Eral BH, Hatton TA, Doyle PS. Nanoemulsions: formation, properties, and applications. Soft Matter. 2016;12: 2826−2841. https://doi.org/10.1039/C5SM02958A
- [8] Balakumar K, Raghavan CV, Selvan NT, Prasad RH, and Abdu S. Self-nanoemulsifying drug delivery system (SNEDDS) of rosuvastatin calcium: Design, formulation, bioavailability, and pharmacokinetic evaluation. Coll Surf B Biointerfaces. 2013;112: 337-343. https://doi.org/10.1016/j.colsurfb.2013.08.025
- [9] Date AA, Desai N, Dixit R, and Nagarsenker M. Self-nanoemulsifying drug delivery systems: Formulation insights, applications, and advances. Nanomed. 2010; 5(10): 595-616. https://doi.org/10.2217/nnm.10.126
- [10] Patel MJ, Patel NM, Patel RB, Patel RP. Formulation and evaluation of self-microemulsifying drug delivery system of lovastatin. Asian J Pharm Sci. 2010;5: 266-267. https://doi.org/10.1016/j.ijpharm.2007.12.026
- [11] Huang YH, Zhang SH, Zhen RX, Xu XD, Zhen YS. Asiaticoside inducing apoptosis of tumor cells and enhancing antitumor activity of vincristine. Chinese J Cancer. 2004;23(12):1599-1604.
- [12] Jeevana JB, Sreelakshmi K. Design and evaluation of self-nanoemulsifying drug delivery system of flutamide. J Young Pharmacist. 2011; 3(1): 4-8. https://doi.org/10.4103/0975-1483.76413
- [13] Danov KD, Kralchevsky P, Ivanov IB. Encyclopedic Handbook of Emulsion Technology. Marcel Dekker, New York 2001.
Details
| Primary Language | English |
|---|---|
| Subjects | Pharmaceutical Delivery Technologies |
| Journal Section | Articles |
| Authors | |
| Publication Date | June 28, 2025 |
| Published in Issue | Year 2024 Volume: 28 Issue: 4 |