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目的:制备携带氟尿嘧啶(5-FU)复乳的温度敏感凝胶,采用Caco-2细胞模型考察其转运吸收特性。方法:采用两步复乳法制备5-FU复乳,以泊洛沙姆407为温敏凝胶材料、海藻酸钠为生物粘附材料,制备携带5-FU复乳的温度敏感凝胶。建立跨Caco-2细胞转运模型,测定其跨生物膜转运、吸收率。结果:5-FU复乳温度敏感凝胶在室温下为固态,10℃条件下转变为自由流动的液态,其跨Caco-2细胞表观渗透系数Papp值为(1.47±0.11)×10-5(cm·s-1),细胞摄取率为(17.1±0.24)%,与5-FU水溶液相比,其跨膜转运率提高了约6倍(P<0.01),细胞摄取率提高了约3.9倍(P<0.01)。结论:5-FU复乳温度敏感凝胶结合了微乳剂与温度敏感凝胶剂的特点,既适用于直肠原位给药,又可增加药物于病灶部位的吸收效率,将为直肠癌的治疗提供新的有效途径治疗策略。
OBJECTIVE: To prepare temperature-sensitive gels containing fluorouracil (5-FU) complex emulsion and investigate its transport and absorption properties using Caco-2 cell model. Methods: The 5-FU multiple emulsion was prepared by two-step double-emulsion method. Poloxamer 407 was used as the thermosensitive gel and sodium alginate as the bioadhesive material to prepare the temperature-sensitive gel with 5-FU complex emulsion. Establishment of cross-Caco-2 cell transport model, measured transmembrane transport, absorption rate. Results: The 5-FU multiple emulsion temperature-sensitive gel was solid at room temperature and was transformed into a free-flowing liquid at 10 ℃. The Papp value of Caco-2 cells was (1.47 ± 0.11) × 10-5 (cm · s-1). The cell uptake rate was (17.1 ± 0.24)%. Compared with 5-FU aqueous solution, the transmembrane transport rate increased by about 6 folds (P <0.01) Times (P <0.01). Conclusion: 5-FU multiple emulsion temperature-sensitive gel combined with the characteristics of microemulsion and temperature-sensitive gel, both for rectal in situ administration, but also increase the absorption of drugs in the lesion site efficiency, will be the treatment of rectal cancer Provide a new effective approach to treatment strategies.