Synthesis of lactobionic acid based bola-amphiphiles and its application as nano-carrier for curcumin delivery to cancer cell cultures in-vitro

• Published in: International journal of pharmaceutics 2020-11, Vol.590, p.119897-119897, Article 119897
• Main Authors: Habib, Shahida Muhammad, Jawad-ur-Rehman, Maharjan, Rukesh, Kanwal, Tasmina, Althagafi, Ismail I., Saifullah, Salim, Ullah, Shafi, Simjee, Shabana Usman, Shah, Muhammad Raza
• Format: Article
• Language: English
• Subjects: Anticancer activity; Bola-amphiphile; Cellular uptake; Curcumin; Lactobionic acid; Nano-vesicles
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2020.119897

[Display omitted] •Lactobionic acid bola-amphiphiles with varying liphophilicity.•Bola-amphiphiles spontaneously aggregated into nano-vesicles.•Vesicles encapsulated curcumin and released it in a controlled manner.•The anti-cancer activity of curcumin is enhanced.•Cellular uptake of curcumin is also increased. Curcumin is highly effective against various types of cancers; however, its low aqueous solubility, high metabolism and non-specificity hinder its efficacy. This study reports the synthesis of three lactobionic acid containing bola-amphiphiles and their investigation for curcumin nano-vesicular delivery into cancer cells. Synthesized bola-amphiphiles were capable of forming nano-vesicles and curcumin loading in a lipophilicity dependent manner. Bola-amphiphile with higher lipophilicity (C12) caused 89.55 ± 5.52% drug encapsulation in its spherical shape nano-vesicles (195.90 ± 0.83 nm). Bola-amphiphile resulting increased curcumin encapsulation with minimum vesicles size was further investigated for cellular uptake and in-vitro anticancer activity. Anticancer activity of curcumin significantly increased against the tested cancer cells upon loading in bola-amphiphile nano-vesicles. Furthermore, nano-vesicular drug delivery of curcumin enhanced its cellular uptake even at the lowest concentration of 1.25 µg/mL.It is concluded that the synthesized bola-amphiphile based nano-vesicles can efficiently deliver curcumin to the tested cancer cells and needs to be tested for established anticancer drugs against different cancer cell lines for effective treatment of cancer.