Rheological and physicochemical characterization of alpha-tocopherol loaded lipid nanoparticles in thermoresponsive gel for topical application
DOI:
https://doi.org/10.11113/mjfas.v13n3.596Keywords:
rheology, thermoresponsive gel, lipid nanoparticles, topical applicationAbstract
Features of a thermoresponsive gel is advantageous in topical application. Lipid nanoparticles is incorporated as a carrier for hydrophobic active ingredient which is not stable in the aqueous gel system. In this work, a thermoresponsive gel mixture consists of carboxymethyl cellulose (CMC) and iota-carrageenan (ι-C) was prepared. Nanostructured lipid carriers (NLC) made of fatty acids and lecithin was incorporated into the gel formulation as a carrier for alpha-tocopherol. Temperature effect on rheological behavior of the prepared gel mixture was investigated. The NLC was evaluated for its mean particle size, zeta potential, morphology, encapsulation efficiency and in vitro drug release. Physicochemical characterization showed that alpha-tocopherol loaded NLC being stored at 4 ˚C was stable for 1 month and encapsulation efficiency of alpha-tocopherol was more than 90 % for all formulations due to its hydrophobicity to stay in the lipid matrix. In vitro release studies proved that NLC was able to provide slow release of loaded alpha-tocopherol. On the other hand, the phase transition from gel-like to liquid-like of the formulated gel mixture was proven to be activated by temperature changes. The rheological gelling point of the gel mixture was represented by the crossover point of storage modulus, G’ and loss modulus, G’’ which was obtained in the vicinity of body temperature 37 ˚C. This property is useful in topical application for its better spreadability on skin upon usage and hence better penetration for the alpha-tocopherol loaded NLC across skin barrier. Prolong release of alpha-tocopherol with enhanced stability is favored as alpha-tocopherol is commonly known for its potent antioxidant activities. These results suggested that gel mixture of CMC and ι-C is a good candidate to be developed as a thermoresponsive gel while lipid nanoparticles is a promising carrier system for alpha-tocopherol in topical use.
References
Guimarães, K. L., Inês Ré, M. 2011. Lipid nanoparticles as carriers for cosmetic ingredients: The first (SLN) and the second generation (NLC). In Beck, R., Guterres, S., Pohlmann, A. (Eds.). Nanocosmetics and Nanomedicines: New approaches for skin care. (pp.101-122) Berlin Heidelberg: Springer-Verlag.
Chieng, Y. Y., Chen, S. B. 2010. Rheological study of hydrophobically modified hydroxyethyl cellulose and phospholipid vesicles. Journal of Colloid and Interface Science 349, 236-245.
Dingler, A., Blum, R. P., Niehus, H., Muller, R. H., Gohla, S. 1999. Solid lipid nanoparticles (SLNTM/LipopearlsTM) a pharmaceutical and cosmetic carrier for the application of Vitamin E in dermal products. Journal of Microencapsulation 16, 6, 751-767.
Friberg, S. E. 1990. Micelles, microemulsions, liquid crystals and the structure of stratum corneum lipids. Journal of the Society of Cosmetic Chemists 41, 3, 155-171.
Grana, A., Limpach, A., Chauhan, H. 2013. Formulation considerations and applications of solid lipid nanoparticles. Retrieved from American Pharmaceutical Review website: http://www.americanpharmaceutical review.com/Featured-Articles/131176- Formulation- Considerations- and- Applications-of-Solid-Lipid-Nanoparticles/
Han, F., Li, S., Yin, R., Liu, H., Xu, L. 2008. Effect of surfactants on the formation and characterization of a new type of colloidal drug delivery system: Nanostructured lipid carriers. Colloids and Surfaces A: Physicochemical and Engineering Aspects 315, 1-3, 210-216.
Islam, M. T., Rodriguez-Hornedo, N., Ciotti, S., Ackermann, C. 2004. Rheological characterization of topical carbomer gels neutralized to different pH. Pharmaceutical Research 21, 7, 1192-1199.
Jenning, V., Schӓfer-Korting, M., Gohla, S. 2000. Vitamin A-loaded solid lipid nanoparticles for topical use: drug release properties. Journal of Controlled Release 66, 2-3, 115-126.
Müller, R. H., Jacobs, C., Kayser, O. 2001. Nanosuspensions as particulate drug formulations in therapy: Rationale for development and what we can expect for the future. Advanced Drug Delivery Reviews 47, 1, 3-19.
Nishinari, K. 2009. Some thoughts on the definition of a gel. In Tokita, M. and Nishinari, K. (Eds.). Gels: Structures, Properties, and Functions: Fundamentals and Applications, pp. 87-94. Berlin, Heidelberg: Springer.
Podda, M., Grundmann-Kollmann, M. 2001. Low molecular weight antioxidants and their role in skin ageing. Clinical and Experimental Dermatology 26, 7, 578-582.
Rizvi, S., Raza, S. T., Ahmed, F., Ahmad, A., Abbas, S., Mahdi, F. 2014. The role of Vitamin E in human health and some diseases. Sultan Qaboos University Medical Journal 14, 2, e157-e165.
Sharipova, A. A., Aidarova, S. B., Grigoriev, D., Mutalieva, B., Madibekova, G., Tleuova, A., Miller, R. 2016. Polymer-surfactant complexes for microencapsulation of vitamin E and its release. Journal f Colloids and Surfaces B: Biointerfaces 137, 1, 152-157.
Shylaja, P. A., Mathew, M. M. 2016. Preparation and characterization of alpha tocopherol loaded solid lipid nanoparticles by hot homogenization method. International Journal of Pharmacy & Pharmaceutical Research. Human Journals 7, 1, 437-448.
Tan, H. W., Misran, M. 2014. Effect of chitosan-modified fatty acid liposomes on the rheological properties of the carbohydrate-based gel. Applied Rheology 24, 34839.
Üner, M., Yener, G. 2007. Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. International Journal of Nanomedicine 2, 3, 289-300.
Woo, J. O., Misran, M., Lee, P. F., Tan, L. P. 2014. Development of a controlled release of salicylic acid loaded stearic acid-oleic acid nanoparticles in cream for topical delivery. The Scientific World Journal 2014, 1-7. http://dx.doi.org/10.1155/2014/205703
Yenilmez, E., Baasaran, E., Yazan, Y. 2011. Release characteristics of vitamin E incorporated chitosan microspheres and in vitro-in vivo evaluation for topical application. Carbohydrate Polymers 84, 2, 807-811.
