Abstract
Intravenous administration of Taxotere® (a commercial form of docetaxel, DTX) leads to many problems such as hypersensitivity, hemolysis, cutaneous allergy, and patient refusal due to its prolonged injection. The oral absorption of DTX is very low due to its hydrophobic nature. The purpose of this study was to prepare and carry out an in vitro evaluation of DTX-loaded nanomicelles for oral administration in order to increase the oral delivery of DTX. Studied formulations were prepared with the two surfactants Tween 20 and Tween 80 and were characterized for their particle size, zeta potential, stability, encapsulation efficiency, stability studies in gastric fluid and intestinal fluid, toxicity studies in C26 colon carcinoma cell line, and cellular uptake. The prepared nanomicelles with particle size of around 14 nm and encapsulation efficiency of 99% were stable in gastric fluid and intestinal fluid for at least 6 h and IC50 decreased significantly after 72 h exposure compared to that of Taxotere®. Nanomicelles increased the water solubility of DTX more than 1500 times (10 mg/mL in nanomicelles compared to 6 µg/mL in water). Results of this study reveal that the new formulation of DTX could be used for the oral delivery of DTX and merits further investigation.
Highlights
Docetaxel (DTX) is an antineoplastic compound from the anthranilates group [1]. It can be prepared through the semi-synthesis of taxol which is extracted from the European yew tree [2,3,4,5,6,7,8,9]
The results in this study demonstrated that nanoparticles were stable in the gastrointestinal tract and could protect loaded DTX against media pH, enzymatic dissolution, and drug efflux pumps [40]
Nanomicelles increased the water solubility of DTX more than 1500 times
Summary
Docetaxel (DTX) is an antineoplastic compound from the anthranilates group [1]. It can be prepared through the semi-synthesis of taxol which is extracted from the European yew tree [2,3,4,5,6,7,8,9].DTX has a wide range of antitumor ability. Docetaxel (DTX) is an antineoplastic compound from the anthranilates group [1]. It can be prepared through the semi-synthesis of taxol which is extracted from the European yew tree [2,3,4,5,6,7,8,9]. DTX has a wide range of antitumor ability It is used as a treatment for acute leukemia, Hodgkin and non-Hodgkin lymphoma, colorectal, breast, stomach, lung, and prostate cancers, as well as solid tumors [2,3,4,5,6,7,8,9,10,11]. The low hydrosolubility and high toxicity of this drug result in decreasing bioavailability and decreasing efficacy [2,15,16]
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