Curso de Farmácia, Centro de Ciências da Saúde, Universidade Federal de Santa Maria (UFSM), Av. Roraima, 1000, 97105-900 Santa Maria, RS, Brazil.
J Biomed Nanotechnol. 2010 Jun;6(3):214-23. doi: 10.1166/jbn.2010.1120.
Tretinoin-loaded conventional nanocapsules have showed a significant protection of this drug against UVC radiation. However, this formulation presents a limited stability on storage. We hypothesized that the association of tretinoin to lipid-core nanocapsules could increase the physicochemical stability of such formulations, focusing on the development of a reliable nanomedicine for parenteral administration. However, this advantage should still be accompanied by the known photoprotective effect of conventional polymeric nanocapsules against the exposure of tretinoin to UV radiation. Results showed that tretinoin-loaded lipid-core nanocapsules improved the physicochemical stability of formulations under storage, without changing their ability to protect tretinoin either against UVA or UVC radiation. In addition, the effect of nanoencapsulation on the antiproliferative and differentiation properties of tretinoin was studied on human myeloid leukemia cells (HL60 cells) showing that tretinoin-loaded lipid-core nanocapsules presents a longer antitumor efficiency compared to the free tretinoin. These results allow us to propose the current formulation (tretinoin-loaded lipid-core nanocapsules) as a promising parenteral nanomedicine for the treatment of acute promyelocytic leukaemia.
载有维 A 酸的常规纳米胶囊已显示出对这种药物对抗 UVC 辐射的显著保护作用。然而，这种制剂在储存时稳定性有限。我们假设维 A 酸与脂质核纳米胶囊的结合可以增加这些制剂的物理化学稳定性，专注于开发一种可靠的用于注射给药的纳米药物。然而，这种优势仍应伴随着常规聚合物纳米胶囊对维 A 酸暴露于紫外线辐射的已知光保护作用。结果表明，载有维 A 酸的脂质核纳米胶囊改善了制剂在储存过程中的物理化学稳定性，同时不改变其保护维 A 酸免受 UVA 或 UVC 辐射的能力。此外，纳米包封对维 A 酸的抗增殖和分化特性的影响在人髓样白血病细胞 (HL60 细胞) 上进行了研究，结果表明，与游离维 A 酸相比，载有维 A 酸的脂质核纳米胶囊具有更长的抗肿瘤效果。这些结果使我们能够提出当前的制剂（载有维 A 酸的脂质核纳米胶囊）作为一种有前途的治疗急性早幼粒细胞白血病的注射用纳米药物。
