고분자 마이셀을 이용한 레티놀 제형개발: 레티놀 안정성

양희선; 안주영; 김채진; 구태성; 이은희; 육순홍; 이재휘; 신병철; 조선행; Hee Seon Yang; Joo Young An; Chae Jin Kim; Tea-Sung Koo; Eun Hee Lee; Soon-Hong Yuk; Jae-Hwi Lee; Byung Cheol Shin; Seon-Hang Cho

Polymer(Korea), Vol.45, No.1, 79-88, January, 2021

DOI10.7317/pk.2021.45.1.79 Export Citation

고분자 마이셀을 이용한 레티놀 제형개발: 레티놀 안정성

Development of Retinol-loaded Polymeric Micelle: Stability of Retinol

양희선^{1, 2}, 안주영^{3, 2}, 김채진⁴, 구태성¹, 이은희³, 육순홍³, 이재휘⁴, 신병철², 조선행^{1, 2, †}

¹충남대학교 신약전문대학원 신약개발학과
²한국화학연구원 신약기반기술연구센터
³고려대학교 세종캠퍼스 일반대학원 약학과
⁴중앙대 약학대학 제약학과

Hee Seon Yang^{1, 2}, Joo Young An^{3, 2}, Chae Jin Kim⁴, Tea-Sung Koo¹, Eun Hee Lee³, Soon-Hong Yuk³, Jae-Hwi Lee⁴, Byung Cheol Shin², and Seon-Hang Cho^{1, 2, †}

¹Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon 34134, Korea
²Drug-based Technology Research Center, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea
³College of Pharmacy, Korea University Sejong Campus, Sejong 30019, Korea
⁴College of Pharmacy, Chung-Ang University, Seoul 06974, Korea

E-mail:

초록

레티놀은 빛, 열 및 산소에 대해 불안정하다는 특징이 있어 레티놀에 대한 안정화 기술이 계속해서 요구되고 있다. 이러한 추세에 따라 안정성이 개선된 레티놀 폴리머 마이셀 연구를 수행하게 되었다. 레티놀 조성에 산화방지제를 함량별 첨가하였고 입도 측정, 장기 및 가속 안정성, 피부투과 등 실험을 진행하였다. 입자 크기는 산화방지제 함량에 따라 차이를 나타내었다. 이 중 레티놀과 butylated hydroxyanisole(BHA) 비율이 1:1인 M3 조성은 80.83% 및 81.18%의 장기 및 가속안정성을 나타내었다. 이 제형을 대상으로 피부투과 실험을 진행하였을 때, 대조군으로 사용된 S 1보다 M3의 피부투과율(52.8%)이 더 크게 나타났다. 종합적으로 레티놀 안정성을 개선할 수 있는 산화방지제와 계면활성제의 적합한 비율을 확립하였다.

Retinol is unstable to the external environment and its properties can deteriorate. Therefore, new stabilization techniques for retinol are needed. According to this trend, a lot of research to improve the stability of retinol is ongoing. Antioxidants were added to the core part of the retinol polymeric micelle particle by content. After preparting the retinol micelle formulation with antioxidants by content, experiments such as particle size measurement, long-term and accelerated stability test, and skin permeation were performed. The micelle particle size depended on the antioxidant ratio. The retinol proportion of M3 composition with a ratio of retinol to butylated hydroxyanisole (BHA) of 1:1 did not show any change in both long-term stability test (80.83%) and accelerated stability test (81.18%). Skin permeation experiments were performed on this formulation. As a result, the skin permeability of M3 (52.8%) was greater than that of S1 used as a control. As a comprehensive result, retinol stability was improved by establishing an appropriate ratio of antioxidants and surfactants.

Keywords:polymeric micelle;antioxidant;retinol;stability;nanoparticle

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[9] Sinko PJ, Singh Y, Wolters Kluwer: China, pp.210 2011.

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[11] Lee SC, Lee KE, Kim JJ, Lim SH, J. Liposome Res., 15, 157 (2005)

[12] Lee CH, Kim DM, Byun SY, KSBB J., 26, 381 (2011)

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[26] Lanigan RS, Yamarik TA, Int. J. Toxicol., 21, 19 (2002)

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[28] Oh YK, Kim MY, Shin JY, Kim TW, Yun MO, Yang SJ, Choi SS, Jung WW, Kim JA, Choi HG, J. Pharm. Pharmacol., 58, 161 (2006)

[29] Makhmalzade BS, Chavoshy F, J. Adv. Pharm. Technol., 9, 2 (2018)

[30] Shaker DS, Ishak RAH, Ghoneim A, Elhuoni MA, Sci. Pharm., 87, 17 (2019)

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[32] Treiner C, CRC Press: Boca Raton, USA, vol. 55, pp 383 1995.

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[35] Bae M, Lim, J. Appl. Chem. Eng., 20, 15 (2009)

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