Department of Pharmaceutical Engineering, Faculty of Engineering Technology, University Malaysia Pahang, Gambang 26300, Malaysia; Centre of Excellence for Advanced Research in Fluid Flow (CARIFF), University Malaysia Pahang, Gambang 26300, Malaysia; Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM), Kuantan 25200, Malaysia.
Department of Pharmaceutical Sciences & Technology, Maharaja Ranjit Singh Punjab Technical University (MRSPTU), Bathinda 151001, India; Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM), Kuantan 25200, Malaysia.
Int J Pharm. 2018 May 5;542(1-2):36-46. doi: 10.1016/j.ijpharm.2018.02.044. Epub 2018 Feb 28.
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method. The prepared systems were characterised by high resolution transmission electron microscopy (HRTEM), force emission electron microscopy (FESEM), atomic force microscopy (AFM), X-ray diffraction (XRD) and P NMR study. All these advanced characterization study established that the ethosome formulation was well defined by its size, shape and its bilayer formation. Transdermal flux of the optimized ethosome formulation was 22.14 ± 0.83 µg/ml/cm which was 21 times higher when compared to the conventional liposomes. Confocal microscopy study revealed an enhanced permeation of coumarin-6 dye loaded ethosomes to much deeper layers of skin when compared with conventional liposomes. The gel was found to be pseudoplastic with elastic behaviour. In-vivo studies on rats showed a higher bioavailability of RXL (157% times) for ethosomal formulation when compared with the oral formulation. In conclusion, RXL loaded ethosomal formulation via transdermal route showed superior drug delivery properties as compared to oral formulation.
盐酸雷洛昔芬属于选择性雌激素受体调节剂（SERM）类药物，用于乳腺癌的治疗。雷洛昔芬的主要问题是其生物利用度差，仅有 2%。本工作的主要目的是制备盐酸雷洛昔芬经皮给药的透皮贴剂，并与药物的口服制剂进行比较。通过旋转蒸发法制备了 5 种不同乙醇浓度的透皮贴剂和一种传统脂质体制剂。通过高分辨率透射电子显微镜（HRTEM）、力发射电子显微镜（FESEM）、原子力显微镜（AFM）、X 射线衍射（XRD）和 P NMR 研究对制备的系统进行了表征。所有这些先进的表征研究都表明，透皮贴剂的大小、形状和双层结构使其具有明确的定义。优化后的透皮贴剂的透皮通量为 22.14 ± 0.83 µg/ml/cm，是传统脂质体的 21 倍。共聚焦显微镜研究表明，与传统脂质体相比，香豆素-6 染料负载的透皮贴剂能够更深入地渗透皮肤。该凝胶具有假塑性和弹性行为。在大鼠体内研究中，与口服制剂相比，透皮贴剂的雷洛昔芬生物利用度提高了 157%。总之，与口服制剂相比，经皮给药的盐酸雷洛昔芬透皮贴剂具有更好的药物传递性能。
