Ruksiriwanich Warintorn, Sirithunyalug Jakkapan, Khantham Chiranan, Leksomboon Krot, Jantrawut Pensak
Pharmaceutical and Natural Products Research and Development Unit, Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Sci Pharm. 2018 Sep 1;86(3):E33. doi: 10.3390/scipharm86030033.
This study aimed to encapsulate seed oil (CPSO) in 2-hydroxypropyl-β-cyclodextrin (HPβCD) cavities and investigate their biological activity, physicochemical stability, and skin penetration by vertical Franz diffusion cells of the CPSO-HPβCD inclusion complex formulations. For biological activity studies-including 2,2-diphenyl-1-picryhydrazyl radical (DPPH) scavenging, metal ion chelating, and inhibition of lipid and tyrosinase inhibition activities-the CPSO-HPβCD inclusion complex exhibited lower inhibition activity than free CPSO. CPSO-HPβCD dispersion, serum, and gel formulations were prepared. All formulations containing the CPSO-HPβCD inclusion complex showed no significant changes in physical characteristics after three months' storage. The percentages of oleic acid remaining in all formulations were over 80% of the initial amount during a three-month stability study. For the skin-penetration study, compared to other formulations, the CPSO-HPβCD serum formulation exhibited the highest cumulative amount of oleic acid in the whole skin and flux through receptor fluid, after six hours, of 32.75 ± 1.25 µg/cm² and 1.02 ± 0.15 µg/cm²/h, respectively. The CPSO-HPβCD serum formulation also showed the proper viscosity. Hence, the CPSO-HPβCD inclusion complex will be beneficial for the further development of cosmeceutical products.
本研究旨在将种子油（CPSO）包封于2-羟丙基-β-环糊精（HPβCD）的空腔中，并通过CPSO-HPβCD包合物制剂的垂直Franz扩散池研究其生物活性、物理化学稳定性和皮肤渗透性。对于生物活性研究，包括2,2-二苯基-1-苦基肼自由基（DPPH）清除、金属离子螯合以及脂质和酪氨酸酶抑制活性的抑制，CPSO-HPβCD包合物表现出比游离CPSO更低的抑制活性。制备了CPSO-HPβCD分散体、血清和凝胶制剂。所有含有CPSO-HPβCD包合物的制剂在储存三个月后物理特性均无显著变化。在为期三个月的稳定性研究中，所有制剂中油酸残留百分比均超过初始量的80%。对于皮肤渗透研究，与其他制剂相比，CPSO-HPβCD血清制剂在全皮中油酸的累积量最高，六小时后通过受体液的通量分别为32.75±1.25μg/cm²和1.02±0.15μg/cm²/h。CPSO-HPβCD血清制剂还显示出合适的粘度。因此，CPSO-HPβCD包合物将有利于药妆产品的进一步开发。
