Abstract
Aims/Objective: To develop and estimate enteric-coated capsules containing mucoadhesive Microspheres of Capecitabine and Oxaliplatin to treat Colon cancer.
 Study Design: Box Behnken.
 Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2017 to 2021.
 Methodology: Capecitabine and Oxaliplatin are used as antineoplastic agents and can be delivered via the oral route of administration. For the estimation of drugs Analytical method has been developed by HPLC. Box Behnken design has been used to optimize Drug: polymer ratio (1:2), Inlet temperature 170ºC, and crosslinking agent with a 0.5 ml 1% Gluteraldehyde solution.
 The microspheres were successfully prepared by using the spray drying technique and evaluated.
 Results: The results of optimized Capecitabine microspheres were obtained as Particle size 87.91 µm ± 0.274,% yield 57.21± 1.5,% Mucoadhesion 57.21± 1.5,% entrapment efficiency 82.16± 0.725. The results of optimized Oxaliplatin microspheres were obtained as Particle size 99.88µm±0.034,% yield 56.0± 0.088,% Mucoadhesion 87.0± 0.80,% entrapment efficiency 82.61±0.085. The drug content of Capecitabine and Oxaliplatin in the filled capsule was 94.67% ±0.32 and 93.45%±0.712, respectively. % Drug release of Capecitabine and Oxaliplatin in Phosphate buffer pH 7.4 was found to be 94.83±0.22 and 96.94±0.11 respectively after 8 hrs. Stability study at 400C±20C / 75 ± 5 % RH revealed that there was no significant change in disintegration time, drug content and % CDR during 6 months. So, prepared formulation was stable during stability study. MTT assay has been performed on the formulation of Capecitabine and Oxaliplatin microspheres for assessing the % viability of both the drugs on the Caco-2 cell line.
 Conclusion: The present study confirmed that prepared mucoadhesive microspheres filled with enteric-coated capsules have an antitumor effect on colon cancer cells. The formulation induced high cell death within 48 hours, and less cell viability was obtained compared to API. Six months accelerated Stability study indicates that formulation is fairly stable at storage conditions.
Highlights
Cancer is a group of diseases involving abnormal cell growth to invade or spread to other parts of the body
Capecitabine is currently used as first-line therapy in patients with metastatic colorectal cancer [3]
The Endothermic peak of both drugs was observed in the Differential scanning Calorimetry (DSC) curve of the drug-polymer mixture at a specified temperature
Summary
Cancer is a group of diseases involving abnormal cell growth to invade or spread to other parts of the body. Benign tumours do not spread to other parts of the body [1]. Colon cancer is the cancer of the epithelial cells lining the colon. Colorectal cancer is mainly divided into different stages according to the invasiveness and metastatic ability of the tumour. Diagnosis of colorectal cancer can be made by sigmoidoscopy or by colonoscopy with biopsy confirmation of cancer tissue. Capecitabine is currently used as first-line therapy in patients with metastatic colorectal cancer [3]. Oxaliplatin is an anticancer ("antineoplastic" or "cytotoxic") chemotherapy drug. Oxaliplatin is used to treat colon or rectal cancer that has spread (metastasized); it is often given in combination with other anticancer drugs (fluorouracil and leucovorin) [4,5]
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
