SYNTHESIS AND CHARACTERIZATION OF ALPHA-TOCOPHEROL LOADED ALGINATE MICROPARTICLES
Abstract
Background. Microencapsulation technology can be used for protection of alpha-tocopherol from degradation in unfavorable environments and enhancement of bioavailability and shelf-life of vitamin E.
Methods. Four different formulations of alpha-tocopherol loaded calcium alginate microparticles were synthesized by external ionotropic gelation method. Vitamin E/sodium alginate ratio was 1:1 and 1:2. All microparticles were characterized by particles weight, size, swelling degree, vitamin E content, loading capacity and encapsulation efficiency.
Results. Spherical shaped microparticles with diameter of 500 to 1000 µm were obtained after drying process. The size and the swelling degree did not change significant in 0.1 M HCL, while it was increased in base conditions of phosphate buffer of pH 6.8 and 7.4. Encapsulated vitamin E content was similar in all formulations (0.30±0.010 - 0.60±0.021mg/mL). The loading capacities were in range between 10±0.11% and 20.45±0.22%, while encapsulation efficiency percentages were between 18.94±0.32 and 31.91±0.41.
Conclusion. All four formulations showed the expected behavior in different mediums, which simulated gastrointestinal fluids in vivo (0.1 M HCL, phosphate buffer pH 6.8 and pH 7.4): gastroresistance and increasing in size and swelling degree in intestinal fluids. The optimum conditions for alpha-tocopherol encapsulation with highest percentage of loading capacity and encapsulation efficacy were 1% sodium alginate, 2% calcium chloride and vitamin E/polymer ratio 1:1.
References
1. Singh J, Kaur K. & Kumar P. Optimizing microencapsulation of α-tocopherol with pectin and sodium alginate. J Food Sci Technol 2018; 55: 3625–31.
2. Ehterami A, Salehi M, Farzamfar S et al. Chitosan/alginate hydrogels containing Alpha-tocopherol for wound healing in rat model. Journal of Drug Delivery Science and Technology 2019; 51: 204–13.
3. Bansode SS, Banarjee SK, Gaikwad DD, Jadhav SL, Thorat RM. Microencapsulation: a review. Int J Pharm Sci Rev Res 2010; 1: 38–43.
4. Trojanowska A, Giamberini M, Tsibranska I et al. Microencapsulation in food chemistry. Journal of Membrane Science and Research 2017; 3: 265-071.
5. Abasalizadeh, F, Moghaddam, SV, Alizadeh E et al. Alginate-based hydrogels as drug delivery vehicles in cancer treatment and their applications in wound dressing and 3D bioprinting. J Biol Eng 2020; 14: 1-22.
6. Goh CH, Heng PW, Chan LW. Alginates as a useful natural polymer for microencapsulation and therapeutic applications. Carbohydr Polym 2012; 88: 1–12.
7. Hariyadi DM, Islam N. Current Status of Alginate in Drug Delivery. Adv Pharmacol Pharm Sci. 2020; 8886095.
8. Bhujbal SV, de Vos P, and Niclou SP. Drug and cell encapsulation: alternative delivery options for the treatment of malignant brain tumors. Advanced Drug Delivery Reviews 2014; 67-68: 142–53.
9. Gurruchaga H, Saenz del Burgo L, Ciriza J, Orive G, Hernandez RM, and Pedraz JL. Advances in cell encapsulation technology and its application in drug delivery. Expert Opinion on Drug Delivery 2015; 12(8): 1251–67.
10. Yoshida K and Onoe H. Functionalized core-shell hydrogel microsprings by anisotropic gelation with bevel-tip capillary. Scientific Reports 2017; 7(1): 1–9.
11. Jana S, Kumar Sen K, and Gandhi A. Alginate based nanocarriers for drug delivery applications. Current Pharmaceutical Design. 2016; 22(22): 3399–410.
12. Pestovsky YS and Martínez-Antonio A. The synthesis of alginate microparticles and nanoparticles. Drug Des Int Prop Int J 2019; 3(1): 293-327.
13. Čalija B, Cekić N, Savić S, Krajišnik D, Daniels R, Milić J. An Investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen. Arch Pharm Res 2011; 34(6): 919-29.
14. Nagamalleswari G, Krishna KS, Abhinandana P, Ramara N, Ravikumar M, Umashankar MS. Estimation of tocopherol (vit-e) content in different edible oils before and after heating. International Journal of Pharmaceutical Research 2019; 11(3): 75-8.
15. Čalija B, Milić J, Cekić N, Krajišnik D, Daniels R, Savić S. Chitosan oligosaccharide as prospective cross-linking agent for naproxen-loaded Ca-alginate microparticles with improved pH sensitivity. Drug Development and Industrial Pharmacy, 2013; 39(1): 77–88.
16. Hoad C, Rayment P, Cox E et al. Investigation of alginate beads for gastro-intestinal functionality, part 2: In vivo characterisation. Food Hydrocolloids 2009; 23(3): 833–39.
17. Gómez-Mascaraque L, Martínez-Sanz M, Hogan S, López-Rubio A, Brodkorb A. Nano- and microstructural evolution of alginate beads in simulated gastrointestinal fluids. Impact of M/G ratio, molecular weight and pH. Carbohydrate Polymers 2019; 223; 115-21.
18. Chuang JJ, Huang YY, Lo SH et al. Effects of pH on the shape of alginate particles and its release behavior. International Journal of Polymer Science 2017; 1: 1-9.
19. Strobel SA, Scher HB, Nitin N, and Jeoh T. In situ cross-linking of alginate during spray-drying to microencapsulate lipids in powder. Food Hydrocolloids 2016; 58: 141–9.
20. Somchue W, Sermsri W, Shiowatana J, Siripinyanond A. Encapsulation of a-tocopherol in protein-based delivery particles. Food Research International 2009; 42: 909–14.
21. Saez V, Souza IDL, Mansur CRE. Lipid nanoparticles (SLN & NLC) for delivery of vitamin E: a comprehensive review. Int J Cosmet Sci. 2018; 40(2): 103-16.