Abstract
The purpose of this investigation was to prepare and evaluate the colon-specific microspheres of Paclitaxel for the treatment of colon cancer. Core microspheres of alginate were prepared by the modified emulsification method in liquid paraffin and by cross-linking with calcium chloride. The core microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach and small intestine. The microspheres were characterized by shape, size, surface morphology, size distribution, incorporation efficiency, and in vitro drug release studies. The outer surfaces of the core and coated microspheres, which were spherical in shape, were rough and smooth, respectively. The size of the core microspheres ranged from 20 to 52 µm, and the size of the coated microspheres ranged from 107 to 178 µm. The core microspheres sustained the drug release for 10 hours. The release studies of coated microspheres were performed in a pH progression medium mimicking the conditions of the gastrointestinal tract. Release was sustained for up to 20 hours in formulations with core microspheres to a Eudragit S-100 coat ratio of 1:7, and there were no changes in the size, shape, drug content, differential scanning calorimetry thermogram, and in vitro drug release after storage at 40°C/75% relative humidity for 6 months.
Highlights
Colorectal cancer is a very common malignancy in industrialized nations and a major cause of mortality and morbidity
The core microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach and small intestine
Release was sustained for up to 20 hours in formulations with core microspheres to a Eudragit S-100 coat ratio of 1:7, and there were no changes in the size, shape, drug content, differential scanning calorimetry thermogram, and in vitro drug release after storage at 40°C/75% relative humidity for 6 months
Summary
Colorectal cancer is a very common malignancy in industrialized nations and a major cause of mortality and morbidity. It blocks the G-2 M phase of the cell cycle of proliferating cell[4] and stabilizes tubulin polymer formation by promoting microtubule assembly.[5] Paclitaxel is a very potent anticancer agent, but its efficacy is limited because of low solubility and oral bioavailability.[6] Some cancer cells have a high level of efflux pump, P-glycoprotein (Pgp), which results in removal of Paclitaxel from the cell during their transport through the cell.[7] Paclitaxel is administered by IV infusion, and to enhance its solubility, cremphor EL is used as a solvent This solvent causes severe hypersensitivity reactions and cytotoxicity and has shown incompatibility with polyvinyl chloride (PVC), commonly used in IV dosage forms.[8] Even though Paclitaxel is a highly effective anticancer agent, it cannot differentiate between cancer and normal cells, resulting in major toxicity to normal tissues. To minimize the cytotoxicity and adverse side effects associated with Paclitaxel, a targeted drug delivery system needs to be developed for colon cancer
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