This study reports the development of a binary drug delivery system consisting of charged liposomes and an oppositely charged peptide–photosensitiser conjugate. Liposomes were prepared with phosphatidyl-l-serine as a negatively charged lipid. Calcein, a fluorophore marker, and doxorubicin, an anticancer drug, were used as model hydrophilic loads. The conjugate consisted of a positively charged arginine-rich peptide synthesised by solid-phase peptide synthesis, and a phthalocyanine derivative with characteristic absorption around 685 nm. Illumination of the binary system with far-red light of 12–15 mW/cm² intensity resulted in 5- to 15-fold increase in release of payloads from the liposomes. The mechanism of drug release was based on photosensitised oxidation of lipids destabilising the liposomal membrane. The cytotoxicity of the liposomes loaded with doxorubicin was tested on B16-F10 melanoma and Y79 retinoblastoma cells. The cytotoxicity of the illuminated binary system in melanoma cell line was significantly higher as compared to the system without illumination. The components of the binary system can be individually prepared and stored with greater storage stability. However, their combination will allow for substantial release of hydrophilic payload from the liposomes under externally applied light.

该研究报告了由带电脂质体和带相反电荷的肽-光敏剂偶联物组成的二元药物递送系统的开发。脂质体是用磷脂酰-1-丝氨酸作为带负电荷的脂质制备的。钙黄绿素（一种荧光团标记物）和阿霉素（一种抗癌药物）被用作模型亲水负载。该偶联物由通过固相肽合成合成的带正电荷的富含精氨酸的肽和在 685 nm 附近具有特征吸收的酞菁衍生物组成。用 12–15 mW/cm ^{2 的}远红光照明双星系统强度导致从脂质体释放的有效载荷增加 5 到 15 倍。药物释放的机制基于脂质的光敏氧化破坏脂质体膜的稳定性。在 B16-F10 黑色素瘤和 Y79 视网膜母细胞瘤细胞上测试了载有阿霉素的脂质体的细胞毒性。与没有光照的系统相比，光照二元系统在黑色素瘤细胞系中的细胞毒性显着更高。二元体系的组分可以单独制备和储存，具有更高的储存稳定性。然而，它们的组合将允许在外部施加的光下从脂质体中大量释放亲水性有效载荷。