Etoposide delivery: mPEG-PCL based copolymeric micelles assessed by various in-vitro anti-cancer activity

Abstract

Discerning the complexity of metastasis during primary tumour, Polymeric micelles has the potential to improve the tumour treatment with chemotherapy and known to that the amphiphilic block co polymer yields self - assemble polymeric micelles in aqueous milieu. The present study was engineered and opti mized etoposide loaded polymeric micelles with mPEG/PCL di block copolymer thereby improving the dispersibility, prolonging the cellular   uptake and enhance the bioavailability. Micelles were characterized by particle size, drug loading capacity, CMC and Surface density. The stealth miceller formulation were evaluated with various in-vitro cell line studies using highly metastatic B16F10 cell lines and compared with unmodified etoposide loaded micelles. The average particle size of etoposide-mPEG-PCL was approximately 72 nm and the polydispersity index was in the range between 1.2 and 1.3. The encapsulation efficiency of the etoposide was in the range between 82.78 and 92.06 % and the maximum drug loading capacity of 5.89 %. The resultant micelles demonstrated ~15 fold higher cellular uptake and After 24 h incubation period, the calculated IC50 values of micellar formulations were up to 25 to 50 times higher as compared with unmodified etoposide. These findings illustrating that the engineered polymeric micell es may be a promising approach for the efficient treatment of tumour metastasis.