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Antineoplastic nano-lipobubbles for passively targeted ovarian cancer therapy

Frank, Derusha, Indermun, Sunaina, Govender, Mershen, Kumar, Pradeep, Choonara, Yahya E., du Toit, Lisa C., Pillay, Viness
Colloids and surfaces 2019 v.177 pp. 160-168
animal ovaries, cholesterol, coatings, colloids, cytotoxicity, drugs, epithelium, intravenous injection, neoplasm cells, ovarian neoplasms, patients, quality of life, therapeutics, zeta potential
The multivariate challenges associated with successful ovarian cancer therapy severely compromises the outcome of therapy and patient quality of life. Coated cholesterol (CHO) and distearoylphosphatidylethanolamine (DSPE) nano-lipobubbles (NLBs) loaded with silibinin and camptothecin were synthesized and evaluated as a possible intravenous delivery system for the treatment of ovarian cancer. Cytotoxicity analysis in addition to in vitro release, zeta potential and drug entrapment studies were conducted on the NLBs. Results of the cytotoxicity evaluation on A2780 epithelial ovarian cancer cells corroborated the benefits of the altered drug release characteristics achieved following polymeric coating. Cumulative cytotoxicity demonstrated by the NLBs 72 h post-treatment ranged between 85%–95%. Cellular internalization of the NLBs was swiftly achieved, with the extent of internalization exhibiting time-dependent characteristics. A size-dependent cellular internalization correlation between the NLB systems was also achieved. Evaluation of the prepared NLBs displayed favorable characteristics for the achievement of passive targeting and satisfactory drug incorporation for application in ovarian cancer treatment.