Journal of the Korean Applied Science and Technology (한국응용과학기술학회지)

The Korean Society of Applied Science and Technology (한국응용과학기술학회)
권호 표지
DOI QR코드

DOI QR Code

Study on Optimization and Skin Permeation of PIT Nanoemulsion Containing α-Bisabolol

α-Bisabolol을 함유한 PIT Nanoemulsion의 최적화 및 피부흡수연구

  • Kim, HuiJu (Department of Chemistry and Cosmetics, College of Natural Sciences Jeju National University) ;
  • Yoon, Kyung-Sup (Department of Chemistry and Cosmetics, College of Natural Sciences Jeju National University)
  • 김희주 (제주대학교 화학?코스메틱스학과,) ;
  • 윤경섭 (제주대학교 화학?코스메틱스학과,)
  • Received : 2020.11.18
  • Accepted : 2020.12.29
  • Published : 2020.12.31
Download PDF
⟨ Previous Next ⟩

Abstract

The skin is divided into three parts: the epidermis, the dermis, and the subcutaneous fat, and the stratum corneum, which is located at the top of the epidermis, acts as a barrier that prevents drug delivery. Nanoemulsions are known to be effective in transdermal delivery of drugs through intercellular lipids because of their unique small particle size. In this study, phase inversion temperature (PIT) nanoemulsion containing α-bisabolol was optimized using response surface methodology (RSM) for effective skin absorption of α-bisabolol. As a preliminary experiment, the 25-2 fractional factorial design method and the 23 full factorial design method were performed. Box-Behnken design was performed based on the results of the factorial design method. The content of surfactant (6.3~12.6%), co-surfactant (5.2~7.8%) and α-bisabolol (0.5~5.0%) were used as factors, and the dependent variable was the particle size of the nanoemulsion. PIT nanoemulsion optimization was performed according to the RSM results, and as a result, the optimal nanoemulsion formulation conditions were predicted to be 10.4% surfactant content, 6.3% co-surfactant content, and 5.0% α-bisabolol content. As a result of the skin absorption test, the final skin absorption rate of the PIT nanoemulsion was 35.11±1.01%, and the final skin absorption rate of the general emulsion as a control was 28.25±1.69%, confirming that the skin absorption rate of the PIT nanoemulsion was better.

피부는 표피, 진피, 피하지방의 세 부분으로 나누어져 있으며, 표피의 가장 윗부분에 존재하는 각질층은 약물의 피부 전달을 방해하는 장벽 역할을 한다. 나노에멀젼은 특유의 작은 입자크기 때문에 세포간 지질을 통과하여 약물의 피부전달에 효과적이라고 알려져 있다. 본 연구에서는 α-bisabolol의 효과적인 피부흡수를 위해 반응표면분석법(response surface methodology, RSM)을 이용하여 상반전온도(phase inversion temperature, PIT) 유화법으로 제조한 α-bisabolol을 함유한 나노에멀젼을 최적화하였다. 예비실험으로 25-2 일부요인배치법과 23 요인배치법이 수행되었다. 요인배치법의 결과를 바탕으로 계면활성제(6.3~12.6%), 보조계면활성제(5.2~7.8%) 및 α-bisabolol (0.5~5.0%) 함량을 인자로 하고 반응 변수를 나노에멀젼의 입자크기로 하는 Box-Behnken design을 수행하였다. RSM 결과에 따라 PIT 나노에멀젼 최적화를 수행하였고, 그 결과 최적의 나노에멀젼 처방 조건은 계면활성제 함량 10.4%, 보조계면활성제 함량 6.3%, α-bisabolol 함량 5.0%로 예측되었다. 피부흡수시험 결과 PIT 나노에멀젼의 최종 피부흡수율은 35.11±1.01%, 대조군인 일반에멀젼의 최종 피부흡수율은 28.25±1.69%로 PIT 나노에멀젼의 피부흡수율이 더 우수함을 확인하였다.

Keywords

Acknowledgement

본 연구는 산업통상자원부와 한국산업기술진흥원이 지원하는 광역협력권산업육성사업으로 수행된 연구결과입니다(과제번호 P0002186).

References

  1. S. B. Han, S. S. Kwon, Y. M. Jeong, B. J. Kong, E. R. Yu, S. N. Park, "Physical Characterizations and In vitro skin permeation of elastic liposomes for transdermal delivery of polygonum aviculare L. extract", Polymer (Korea), Vol.38 No.6, pp. 694-701, (2014). https://doi.org/10.7317/pk.2014.38.6.694
  2. S. K. Ahn, S. M. Hwang, E. H. Choi, W. S. Lee, "Morphologic characteristics of skin barrier and stratum corneum", The Journal of Skin Barrier Research, Vol.1, No.1, pp. 22-28, (1999).
  3. G. Y. Noh, J. Y. Suh, S. N. Park, "Ceramide-based nanostructured lipid carriers for transdermal delivery of isoliquiritigenin: Development, physico-chemical characterization, and in vitro skin permeation studies", Korean Journal of Chemical Engineering, Vol.34, No.2, pp. 400-406, (2017). https://doi.org/10.1007/s11814-016-0267-3
  4. S. P. Hong, "Bricks and mortar: Two compartment system", The Journal of Skin Barrier Research, Vol.12, No.1, pp. 35-40, (2010).
  5. Y. Chang, D. J. McClements, "Optimization of orange oil nanoemulsion formation by isothermal low-energy methods: influence of the oil phase, surfactant, and temperature", Journal of Agricultural and Food Chemistry, Vol.62, No.10, pp. 2306-2312, (2014). https://doi.org/10.1021/jf500160y
  6. Z. Jeirani, B. Mohamed Jan, B. Si Ali, I. Mohd Noor, S. Chun Hwa, W. Saphanuchart, "Prediction of phase-inversion temperature of a triglyceride microemulsion using design of experiments", Industrial and Engineering Chemistry Research, Vol.52, No.2, pp. 744-750, (2013). https://doi.org/10.1021/ie302180j
  7. J. Rao, D. J. McClements, "Stabilization of phase inversion temperature nanoemulsions by surfactant displacement", Journal of Agricultural and Food Chemistry, Vol.58, No.11, pp. 7059-7066, (2010). https://doi.org/10.1021/jf100990r
  8. P. huesiang, U. Siripatrawan, R. Sanguandeekul, L. McLandsborough, D. J. McClements, "Optimization of cinnamon oil nanoemulsions using phase inversion temperature method: Impact of oil phase composition and surfactant concentration", Journal of Colloid and Interface Science, Vol.514, No.5, pp. 208-216, (2018). https://doi.org/10.1016/j.jcis.2017.11.084
  9. R. Kadir, B. W. Barry, "α-Bisabolol, a possible safe penetration enhancer for dermal and transdermal therapeutics", International Journal of Pharmaceutics, Vol.70, No.1-2, pp. 87-94, (1991). https://doi.org/10.1016/0378-5173(91)90167-M
  10. N. F. M. Rocha, E. R. V. Rios, A. M. R. Carvalho, G. S. Cerqueira, A. de Araujo Lopes, L. K. A. M. Leal, M. L. Dias, D. P. de Sousa, F. C. F. de Sousa, "Anti-nociceptive and anti-inflammatory activities of (-)-α-Bisabolol in rodents", Naunyn-Schmiedeberg's Archives of Pharmacology, Vol.384, No.6, pp. 525-533, (2011). https://doi.org/10.1007/s00210-011-0679-x
  11. Y. B. Lim, S. H. Park, B. J. An, Y. I. Kim, "Practical design of experiments", Freeacademy, pp. 224-247, (2008).
  12. C. H. Sim, "Optimization of process variables for insulation coating of conductive particles by response surface methodology", Korean Chemical Engineering Research, Vol.54, No.1, pp. 44-51, (2016). https://doi.org/10.9713/kcer.2016.54.1.44
  13. I. M. Yang, G. T. Oh, C. B. Yu, I. G. Hwang, "Design and analysis of experiments", Minyoungsa, pp. 83-264, (2015).
  14. S. Kim, D. H. Kwon, D. H. Lim, G. S. Kim, C. Y. Kang, "In vitro dtudy of transdermal delivery system for caffein in slim patch type" Journal of Korean Pharmaceutical Sciences, Vol.36, No.2, pp. 97-102, (2006).
  15. L. Quanhong, F. Caili, "Application of response surface methodology for extraction optimization of germinant pumpkin seeds protein", Food Chemistry, Vol.92, No.4, pp. 701-706, (2005). https://doi.org/10.1016/j.foodchem.2004.08.042