Department of Pharmaceutics, School of Pharmaceutical Sciences, Jiangnan University, 1800 Lihu Road, Wuxi 214122, Jiangsu, PR China; Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia 19623, Egypt.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Jiangnan University, 1800 Lihu Road, Wuxi 214122, Jiangsu, PR China.
Mater Sci Eng C Mater Biol Appl. 2019 Jun;99:1448-1458. doi: 10.1016/j.msec.2019.02.095. Epub 2019 Feb 25.
The topical delivery of chemotherapeutics is a promising approach for the management of skin disorders. However, diverse pharmaceutical strategies are essential to allow penetration of large quantities of drugs to tumor tissue. Herein, an attempt was made to investigate the use of Derma roller® microneedles in combination with doxorubicin HCl (DOX) and celecoxib (CEL) co-loaded liposomes as a potential therapeutic approach for the management of melanoma. DOX/CEL co-loaded liposomes/Gels were prepared and characterized. The results showed that microneedle pretreatment with liposomes gel increased DOX penetration into the skin approximately 2-fold compared with the passive delivery. Both CEL liposomes and DOX liposomes caused significant growth inhibition on B16 cells. Besides, DOX/CEL co-loaded liposome was found more cytotoxic than DOX/CEL solution and single drug loaded liposome. The transdermal delivery of DOX/CEL co-loaded liposome successfully inhibited subcutaneous melanoma in female BALB/nude mice, and the co-administration of DOX/CEL with liposomes was better and significantly enhanced the antitumor effect more than single-drug-loaded liposomes. Furthermore, Dermarollers treatment prior to gel application strongly improved the tumor inhibition rate. DOX/CEL co-loaded liposome delivery via microneedles is a promising strategy for skin tumor treatment with targeting inhibition efficiency and negligible side effects.
局部递送化疗药物是治疗皮肤疾病的一种很有前途的方法。然而，需要各种药物策略来允许大量药物渗透到肿瘤组织中。本文尝试研究了多柔比星盐酸盐（DOX）和塞来昔布（CEL）共载脂质体联合 Dermaroller®微针在治疗黑色素瘤中的应用。制备并表征了 DOX/CEL 共载脂质体/凝胶。结果表明，与被动给药相比，微针预处理脂质体凝胶可使 DOX 渗透到皮肤中的量增加约 2 倍。CEL 脂质体和 DOX 脂质体均能显著抑制 B16 细胞的生长。此外，与 DOX/CEL 溶液和单药载脂质体相比，DOX/CEL 共载脂质体的细胞毒性更大。DOX/CEL 共载脂质体的经皮给药成功抑制了雌性 BALB/nude 小鼠的皮下黑色素瘤，并且 DOX/CEL 与脂质体联合给药比单药载脂质体更能显著增强抗肿瘤作用。此外，在凝胶应用前进行 Dermarollers 处理强烈提高了肿瘤抑制率。通过微针递送 DOX/CEL 共载脂质体是一种具有靶向抑制效率和可忽略的副作用的皮肤肿瘤治疗的有前途的策略。
