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Development of self-assembled nanocarriers to enhance antitumor efficacy of docetaxel trihydrate in MDA-MB-231 cell line

Rarokar, Nilesh R., Khedekar, Pramod B., Bharne, Ashish P., Umekar, Milind J.
International journal of biological macromolecules 2019 v.125 pp. 1056-1068
Fourier transform infrared spectroscopy, cell lines, cytotoxicity, drugs, guidelines, homogenization, nanocarriers, particle size, scanning electron microscopy, storage conditions, toxicity testing, viability, zeta potential
Self-assembled nanocarriers (SANs) as a novel colloidal controlled delivery for docetaxel trihydrate (DTX) were engineered by high-pressure homogenization method to overcome the several clinical problems. Drug-excipient compatibility was studied using DSC and FTIR spectroscopy. The fabricated SANs was characterized by particle size, zeta potential, and SEM. QbD based central composite design of experiment was employed for formula optimization. The cell viability of DTX-hydroalcoholic solution (DTX-HA) and DTX-loaded SANs has been determined in MDA-MB-231 cell line by MTT assay. The stability study of selected SANs formulations were carried out at various storage conditions as per ICH guidelines. The summary of results obtained shows high drug content with higher entrapment efficiency (91.23 ± 3.41% w/w) of DTX-loaded SANs. It shows diffusion controlled release of DTX over the period of 12 h which is higher than DTX-HA solution, releases the DTX within 4 h. The MTT assay expressed lower cellular viability and improved cell inhibition leads to increase cytotoxicity of formulations towards cells. The stability study reveals stability of DTX-loaded SANs formulations at various storage conditions over a period of three months. The strong experimental evidence confirms the SANs as an effective approach to formulate the controlled delivery system of antineoplastics with improved stability.