[논문]미녹시딜과 다이아미노피리미딘옥사이드 성분을 함유하는 니오좀 제형의 물성 및 피부투과

김보경; 김원형; 윤경섭

doi:10.15230/scsk.2023.49.2.127

미녹시딜과 다이아미노피리미딘옥사이드 성분을 함유하는 니오좀 제형의 물성 및 피부투과
Physical Properties and Skin Penetration of Niosome Formulations Containing Minoxidil and Diaminopyrimidine Oxide 원문보기

大韓化粧品學會誌 = Journal of the society of cosmetic scientists of Korea, v.49 no.2, 2023년, pp.127 - 139

김보경 (제주대학교 화학.코스메틱스학과) , 김원형 (제주대학교 화학.코스메틱스학과) , 윤경섭 (제주대학교 화학.코스메틱스학과)

초록
AI-Helper

본 연구에서는 의약품 원료로 잘 알려진 minoxidil과 화장품 원료인 diaminopyrimidine oxide (DAO) 활성성분으로 사용하여 니오좀(niosome)의 물성평가와 더불어 인공피부에 대한 경피투과율을 비교하였다. 나노입자의 니오좀을 제조하기 위해 고압유화(high pressure homogenization) 방법을 이용하였으며 제타사이저(zetasizer)로 물성평가를 진행하였다. 활성성분을 포함한 니오좀의 입자크기는 HLB에 따라 평균 99 ~ 123 nm, 제타전위(zeta potential)는 -60 ~ -81 mV의 범위로 측정되었다. DSC (differential scanning colorimetry)를 통해 결정성 성분인 minoxidil이 니오좀 내에 무결정 상태로 균일하게 용해되어 있음을 확인하였다. 경피투과량을 확인 및 비교하기 위해 in vitro Franz diffusion cell 방법으로 측정하였으며, 니오좀 제형이 대조군인겔 제형보다 minoxidil의 경우 3.4배, DAO의 경우 11.1배 높은 투과율을 보였다. 또한 minoxidil과 DAO 니오좀의 경피투과 비교 시 유사한 경향을 보였으며, 상대적으로 DAO의 투과량이 많았다. HLB 값을 달리한 니오좀 제형을 Cryo-TEM을 이용하여 형상을 관찰하였으며, 모두 소포체가 형성되었으며 SUV (small unilamella vesicle)와 LUV (large unilamella vesicle)의 중간 형태임을 확인하였다. 본 연구를 통하여 탈모에 효과적인 약물인 minoxidil과 화장품 원료인 DAO 성분을 니오좀 제형에 캡슐화시킴으로써 효과적으로 피부에의 전달을 기대할 수 있다.

Abstract ▼ AI-Helper

In this study, minoxidil, which is well known as a pharmaceutical raw material, and diaminopyrimidine oxide (DAO), which is a cosmetic raw material, were used as active ingredients to evaluate the physical properties of niosomes and compare the skin penetrations of artificial skin. To prepare niosomes of the size of nanoparticles, a high pressure homogenization method was used, and physical properties were evaluated with a zetasizer. The particle size of the noisome including the active ingredient was measured to be 99 to 123 nm according to HLB, and the zeta potential was measured in the range of -60 to -81 mV. Through DSC (differential scanning colorimetry), it was confirmed that minoxidil, a crystalline component, was uniformly dissolved in an amorphous state in niosomes. In order to confirm and compare skin penetration, it was measured by the in vitro Franz diffusion cell method, and the niosome formulation showed 3.4 times higher penetration for minoxidil and 11.1 times higher penetration for DAO than the control gel formulation. In addition, when comparing the skin penetration of minoxidil niosome and DAO niosome, a similar trend was shown, and the penetration amount of DAO was relatively high. The shapes of the niosome formulations with different HLB values were observed using Cryo-TEM, and it was confirmed that vesicles were formed in all of them and that they were intermediate between SUV (small unilamella vesicle) and LUV (large unilamella vesicle). Through this study, minoxidil, an effective drug for hair loss, and DAO, a cosmetic raw material, can be effectively delivered to the skin by encapsulating them in a noisome formulation.

주제어

표/그림 (19)

그림 Figure 1. Chemical structures of minoxidil (A) and diaminopyrimidine oxide (B).
표 Table 1. Preparation of Active Ingredient Base
표 Table 2. Preparation of Niosome According to HLB
표 Table 3. Preparation of Niosome According to the Presence or Absence of PCP and increased PG Content
표 Table 4. Preparation of DAO Containing Niosome
표 Table 5. Preparation of Control by Gel Formulation (non niosome)
표 Table 6. Condition for HPLC Analysis of MXD and DAO
그림 Figure 2. Particle size data over time at 25 ℃ and different HLB values. The results were expressed as the mean ± SD (N = 3), * p < 0.05, ** p < 0.01 compared with each 1 d data.
그림 Figure 4. Particle size data over time at 25 ℃ and different HLB values with or without potassium cetyl phosphate. The results were expressed as the mean ± SD (N = 3), * p < 0.05, ** p < 0.01 compared with each 1 d data.
그림 Figure 3. Zeta potential data over time at 25 ℃ and different HLB values. The results were expressed as the mean ± SD (N = 3), * p < 0.05, ** p < 0.01 compared with each 1 d data.
그림 Figure 5. Zeta potential data over time at 25 ℃ and different HLB values with or without potassium cetyl phosphate. The results were expressed as the mean ± SD (N = 3), *p < 0.05, **p < 0.01 compared with each 1 d data.
그림 Figure 6. Particle size data over time at 25 ℃. The results were expressed as the mean ± SD (N = 3), * p < 0.05, ** p < 0.01 compared with each 1 d data.
그림 Figure 7. Zeta potential data over time at 25 ℃. The results were expressed as the mean ± SD (N = 3), * p < 0.05, ** p < 0.01 compared with each 1 d data.
그림 Figure 8. Microscopy image at 25 ℃ and different HLB values. MN #2-1 (niosome without MXD), MN #2-2 ~ MN #2-8 (niosomes with MXD); scale bar 20 μm.
그림 Figure 9. Microscopy image at 25 ℃ and different HLB values. MN #3-1 ~ MN #3-4 (niosome with potassium cetyl phosphate), MN #3-5 ~ MN #3-8 (niosomes without potassium cetyl phosphate); scale bar 20 μm.
그림 Figure 10. DSC chart of niosome without MXD (A), niosome with MXD (MN #3-7) (B), and MXD (C).
그림 Figure 11. DSC chart of niosome without DAO (A), niosome with DAO (DN #4-1) (B), and DAO (C).
그림 Figure 12. Cumulative skin penetration amounts of niosome with MXD (MN #3-7) and control (MG #5-1), niosome with DAO (DN #4-1) and control (DG #5-2). The results were expressed as the mean ± SD (N = 3).
그림 Figure 13. Cryo-TEM images of MN #3-1 (HLB 4. 7) a nd MN #3-4 (HLB 14.9).

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