Surface modified nanoliposome formulations provide sustained release for 5-FU and increase cytotoxicity on A431 cell line


Yaman U., Aslan M., ÖZTÜRK Ş., ULUBAYRAM K., EROĞLU İ.

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, vol.25, no.10, pp.1192-1203, 2020 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 25 Issue: 10
  • Publication Date: 2020
  • Doi Number: 10.1080/10837450.2020.1803910
  • Journal Name: PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Business Source Elite, Business Source Premier, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, MEDLINE
  • Page Numbers: pp.1192-1203
  • Keywords: Malignant melanoma, nanoliposome, 5-Fluorouracil, poly-L-lysine, intra-tumoral injection, IN-VITRO, TOPICAL DELIVERY, 5-FLUOROURACIL, LIPOSOMES, COMPLEXES, THERAPY, SYSTEMS, ACID, SKIN
  • Hacettepe University Affiliated: Yes

Abstract

Malignant melanoma is a type of skin cancer with high risk of metastasis. 5-Fluorouracil is commonly used for treatment of skin cancer, however its penetration through the skin is found to be insufficient in some cases. Therefore, we optimized its pharmacokinetics by fabricating 5- Fluorouracil-loaded nanoliposome formulations modified with Poly-L-lysine coating. 5-Fluorouracil-loaded nanoliposome formulations were prepared using dipalmitoylphosphatidylcholine, dicethylphosphate and cholesterol having encapsulation efficiency of 45 +/- 9.61%. The particle size, zeta potential, polydispersity index and encapsulation rate of the prepared formulation was found to be 237.9 +/- 0.986 nm, 41.4 +/- 1.060 mV, 0.233 +/- 0.019 and 88.2 +/- 7.85%, respectively. Surface characterization, molecular structure and thermal property illumination of the formulations were performed alongside stability studies. TheIn-vitrorelease of 5-FU from Lipo-FU6 and PLL-1 formulations was investigated by dialysis membrane method. Within the first 12 hours, the percentage release of 5-FU from Lipo-FU6 and PLL-1 formulations was observed to be 47.17% and 20.84%, respectively. Moreover, the cytotoxicity study on A431 epidermal carcinoma cell lines has revealed that 5-FU-loaded formulations were toxic to cells unlike the 5-FU free formulations. In conclusion, PLL coated nanoliposome formulations showed a potential to be an effective option for further combined drug/gene therapy applications.