Cancer is the leading cause of death worldwide. Capecitabine (CP) shows severe side effects because of early metabolism in stomach that affects the normal cells and organs, particularly liver and stomach. In this scope, we report the biocompatible, nontoxic polymeric thin films loaded with anti-cancer drug, CP for target specific, sublingual delivery of CP. Chitosan (CS) and polyvinyl alcohol (PVA) were used as biodegradable polymers alongwith glutaraldehyde (GLA) cross linker. CP-loaded thin films (TFCP1–TFCP5) were fabricated by solvent casting method. The results of Fourier transform infrared spectroscopy confirmed the presence of CP and polymers (CS and PVA) with GLA which binds through hydrogen bonding, and compatibility of drug with different excipients. Thermogravemetric analysis showed that the thin films are highly stable while differential scanning calorimeter thermograms confirmed the complete miscibility/entrapment of CP within PVA/CS thin film matrix. X-ray diffraction patterns revealed the molecular ineractions between CP and polymer matrix. High degree of swelling index of thin films at pH 7.4 was observed in comparison to pH 5.5. CP release studies in acetate (pH 5.5) and phosphate buffer (pH 7.4) showed that the thin films swell and result in drug diffusion faster in phosphate buffer through diffusion governed by Higuchi’s model. Cytotoxicity results displayed that CPTFs killed MCF-7 and T47D (human breast adenocarcinoma) cells more effectively as compared to CP alone. The results of adhesion assay also showed that the PVA and CS both are safe and biocompatible. TFCP1 and TFCP3 thin films efficiently induced the apoptosis as compared to CP alone. The improved ability of TFCP1 and TFCP3 to induce cytotoxicity in MCF-7 cells reflects the potential of these thin films for targeted drug delivery. The CPTFs were stable for 4 months at 4 C/60% 2%RH and 25 C/70% 2%RH. In conclusion, the thin film formulations showed target specific controlled and burst release properties and thus could prove to be effective for human breast cancer treatment.

癌症是全世界死亡的主要原因。卡培他滨（CP）由于胃中的早期代谢影响正常细胞和器官，特别是肝脏和胃而表现出严重的副作用。在此范围内，我们报告了负载有抗癌药物 CP 的生物相容性、无毒聚合物薄膜，用于目标特异性舌下递送 CP。壳聚糖（CS）和聚乙烯醇（PVA）与戊二醛（GLA）交联剂一起用作可生物降解聚合物。负载CP的薄膜（TFCP1-TFCP5）是通过溶剂浇铸法制备的。傅里叶变换红外光谱的结果证实了CP和聚合物（CS和PVA）与GLA通过氢键结合的存在，以及药物与不同赋形剂的相容性。热重分析表明薄膜高度稳定，而差示扫描量热仪热分析图证实了 CP 在 PVA/CS 薄膜基质中完全混溶/包埋。X 射线衍射图揭示了 CP 和聚合物基质之间的分子相互作用。与 pH 5.5 相比，pH 7.4 时薄膜的溶胀指数较高。在醋酸盐 (pH 5.5) 和磷酸盐缓冲液 (pH 7.4) 中的 CP 释放研究表明，薄膜会膨胀，并通过 Higuchi 模型控制的扩散，导致药物在磷酸盐缓冲液中扩散得更快。细胞毒性结果显示，与单独使用 CP 相比，CPTF 更能有效地杀死 MCF-7 和 T47D（人乳腺癌）细胞。粘附试验的结果还表明PVA和CS都是安全且具有生物相容性的。与单独的 CP 相比，TFCP1 和 TFCP3 薄膜有效诱导细胞凋亡。TFCP1 和 TFCP3 在 MCF-7 细胞中诱导细胞毒性的能力提高，反映了这些薄膜用于靶向药物递送的潜力。CPTF 在 4 C/60% 2%RH 和 25 C/70% 2%RH 条件下可稳定稳定 4 个月。总之，薄膜制剂表现出目标特异性的控制和突释特性，因此可以证明对人类乳腺癌治疗有效。